Unit -2

Drugs acting on autonomic nervous system

The autonomic nervous system (ANS) is a division of the peripheral nervous system responsible for regulating
involuntary physiological processes. It controls functions such as heart rate, blood pressure, digestion, respiration,
and body temperature, often without conscious effort.

ACETYLCHOLINE

Acetylcholine (ACh) is a crucial neurotransmitter in both the central and peripheral nervous systems, involved in
various physiological and neurological functions. It plays a key role in communication between neurons and other
target cells, such as muscles or glands.

PHARMACOLOGICAL ACTION

• Heart:
o Acts on muscarinic (M2) receptors in the heart.
o Decreases heart rate (negative chronotropic effect).
o Reduces the force of contraction,
• Blood Vessels:
o Causes vasodilation by stimulating muscarinic (M3) receptors on endothelial cells, leading to the
release of nitric oxide (NO).

2. Actions on the Respiratory System

• Stimulates muscarinic receptors (M3) in the bronchial smooth muscle, causing bronchoconstriction.
• Increases secretion of mucus from the respiratory tract glands.
3. Actions on the Gastrointestinal System

• Enhances gastrointestinal motility and peristalsis by acting on M3 receptors in the smooth muscle of the GI
tract.
• Stimulates secretion of digestive enzymes and gastric acid by activating M3 receptors in the glands.

4. Actions on the Urinary System

• Promotes contraction of the bladder muscle.

• Relaxes the internal urethral muscle, facilitating urination.

5. Actions on the Eye

• Causes miosis (pupil constriction) by stimulating M3 receptors on the sphincter pupillae muscle.

6. Actions on Exocrine Glands

• Increases secretion from glands such as salivary, lacrimal, sweat, and digestive glands by stimulating M3
receptors.

7. Actions on the Neuromuscular Junction

• to muscle contraction in skeletal muscles.

8. Actions in the Central Nervous System (CNS)

• Modulates functions like attention, learning, and memory.

ACH receptors( cholinergic receptor)

Receptor Type Subtype Location Function

Nicotinic Acetylcholine Neuromuscular junction (skeletal Mediates muscle contraction by
Muscle-Type (Nm)
Receptors (nAChRs) muscles) depolarizing muscle fibers.
- Transmits signals in autonomic
ganglia.
Autonomic ganglia, adrenal
Neuronal-Type (Nn) - Stimulates adrenal release of
medulla, CNS
catecholamines (e.g., epinephrine).

- Enhances cognitive function.(

Muscarinic Acetylcholine CNS, gastric glands, autonomic
M1 (Neuronal) memory ,learning )
Receptors (mAChRs) ganglia
- Stimulates gastric acid secretion.
- Decreases heart rate (negative
chronotropy).
M2 (Cardiac) Heart (especially atria)
- Slows AV node conduction
(negative dromotropy).
- Causes bronchoconstriction and
Smooth muscle (e.g., bronchi,
M3 (Glandular/Smooth increases glandular secretions.
bladder, GI tract), exocrine glands,
Muscle) - Promotes miosis (pupil constriction)
eyes
and accommodation.
Modulates dopamine release and
other neural activities.
M4 CNS

Plays a role in dopamine regulation

M5 CNS, peripheral blood vessel and vasodilation
 ADRENERGIC
RECEPTORS

Alpha (α) Receptors

- Blood vessels (vascular smooth muscle)
- Causes vasoconstriction (increases blood pressure).
α1 - Bladder sphincter
- Contracts bladder sphincter (urinary retention).
- Prostate
- Presynaptic nerve terminals - Inhibits norepinephrine release (negative feedback).
α2
- CNS (brainstem) - Reduces sympathetic outflow.
Beta (β) Receptors
- Increases heart rate (positive chronotropy).
- Heart (myocardium, SA/AV nodes)
β1 - Enhances cardiac contractility (positive inotropy).
- Kidneys (juxtaglomerular cells)
- Stimulates renin release.
- Smooth muscle (bronchi, blood vessels,
- Causes bronchodilation.
GI tract)
β2 - Relaxes uterine smooth muscle.
- Uterus
- Stimulates glycogenolysis in liver.
- Liver

- Promotes lipolysis (fat breakdown).

- Adipose tissue
β3 - Relaxes the bladder detrusor muscle (increases bladder
- Bladder detrusor muscle
capacity).
 CHOLINERGIC DRUGS ( Parasympathomimetics)
Cholinergics are a class of drugs or agents that mimic or enhance the effects of acetylcholine (ACh), a key
neurotransmitter in the nervous system. These agents act on cholinergic receptors (nicotinic and
muscarinic) to produce their effects.

Pilocarpine

Mechanism of Action (MOA): Pilocarpine is a muscarinic cholinergic agonist that primarily stimulates M3
muscarinic receptors in the smooth muscle and exocrine glands. This stimulation results in the following:
o Increased secretion from salivary and sweat glands (used in treating dry mouth conditions).
o Constriction of the pupil (miosis) and increased aqueous humor outflow in the eye (used in
treating glaucoma).
Indications:

1. Glaucoma: Pilocarpine is used in the treatment of open-angle glaucoma and angle-closure glaucoma to
reduce intraocular pressure (IOP). It does this by promoting drainage of the aqueous humor through the
trabecular meshwork.
2. Xerostomia (dry mouth): Pilocarpine is used to treat dry mouth, often in conditions such as Sjögren's
syndrome or after radiation therapy to the head and neck.
3. Dry Eye Syndrome: It may be used off-label to promote tear production.

Adverse Effects: Common adverse effects are related to the muscarinic activation:

• Ocular Effects:
o Miosis (pupil constriction) which may cause difficulty seeing in low light (night blindness).
o Blurred vision due to pupil constriction.
• Systemic Effects:
o Sweating (due to stimulation of sweat glands).
o Salivation (due to increased salivary secretion).
o Bradycardia (slow heart rate).
o Hypotension (low blood pressure).
o Gastrointestinal distress such as nausea, vomiting, diarrhea.
o Headache and dizziness.
o Cholinergic crisis if overdosed (symptoms include excessive salivation, sweating, and difficulty
breathing).

Contraindications: Pilocarpine should not be used in the following conditions:

1. Hypersensitivity to pilocarpine or any component of the formulation.

2. Asthma or Chronic Obstructive Pulmonary Disease (COPD): Due to potential bronchoconstriction.
 3. Severe cardiovascular disease, including bradycardia and arrhythmias, since pilocarpine can further
decrease heart rate.
4. Retinal disease: Patients with conditions like retinal detachment may experience worsened symptoms due
to miosis.
5. Uveitis (inflammation of the uveal tract in the eye) due to risk of increasing inflammation.

Dose and Dosage Form:

• For Glaucoma: Pilocarpine eye drops (most common form): Initial dose: 1–2 drops in the affected eye(s)
2–4 times daily.
▪ Maintenance dose: The dose may be adjusted based on intraocular pressure response, with
typical dosing 2–4 times per day.
o Note: Pilocarpine 1%, 2%, 4% solutions are available.
• For Xerostomia (Dry Mouth):
o Pilocarpine tablets:
▪ Initial dose: 5 mg orally 3 times a day.
▪ Maintenance dose: May be increased based on therapeutic response up to 10 mg three times
daily.
▪ Max dose: 30 mg/day.

Dosage Forms:

1. Eye Drops: Available in concentrations such as 1%, 2%, 4% for ocular indications (glaucoma).
2. Oral Tablets: Typically available in 5 mg tablets for dry mouth treatment.
ANTICHOLINERGIC DRUGS(parasympatholytics)

Anticholinergic drugs are substances that inhibit the action of acetylcholine (ACh) at cholinergic receptors in the
body. These drugs block or antagonize the effects of acetylcholine, particularly at the muscarinic receptors (M1–
M5), which are part of the parasympathetic nervous system.

Classification
1.Atropine
• Mechanism of Action:
• Atropine is a competitive antagonist of acetylcholine at muscarinic receptors( blocks the action of Ach). It
blocks parasympathetic activity, leading to increased heart rate, bronchodilation, and reduced secretion of
glands such as salivary and bronchial glands.
• Indications:
• Bradycardia (slow heart rate)
• Organophosphate poisoning (by counteracting muscarinic effects)
• Pre-anesthetic medication to reduce secretions
• Asystole (in some emergency protocols)
• Dose:
• Bradycardia: 1 mg IV, can repeat every 3-5 minutes, up to 3 mg total.
• Organophosphate poisoning: 2-5 mg IV, repeated every 20-30 minutes.
• Pre-anesthetic: 0.4-0.6 mg IM or IV.
• Dosage Form:
• Injectable solution (IV)
• Oral tablets (rarely used)
• Adverse Effects:
• Dry mouth
• Blurred vision
• Tachycardia
• Urinary retention
• Constipation
• Confusion (especially in elderly patients)
• Contraindications:
• Narrow-angle glaucoma
 • Tachycardia
• Myasthenia gravis (unless given for a specific purpose)
• Prostatic hypertrophy (due to risk of urinary retention)

2.Hyoscine

• Mechanism of Action:

• Hyoscine is a muscarinic receptor antagonist that blocks the effects of acetylcholine. It primarily acts on the
CNS to reduce motion sickness and nausea and on the peripheral nervous system to reduce glandular
secretions.

• Indications:

• Motion sickness
• Nausea and vomiting (especially related to surgery or chemotherapy)
• Preoperative sedation (as an adjunct to anesthesia)

• Dose:

• Motion sickness: 0.3-0.6 mg orally every 6-8 hours or as a patch (transdermal) with 1.5 mg applied every 72
hours.
• Nausea/Vomiting: 0.3-0.6 mg IV or IM every 4-6 hours.

• Dosage Form:

• Oral tablets
• Transdermal patch
• Injectable solution
• Adverse Effects:

• Drowsiness, Blurred vision

• Dry mouth,Urinary retention
• Constipation
• Confusion (especially in the elderly)

• Contraindications:

• Glaucoma
• Prostatic hypertrophy
• Myasthenia gravis

3.Pralidoxime

• Mechanism of Action:
• Organophosphates inhibit acetylcholinesterase, leading to excessive acetylcholine buildup and
overstimulation of muscarinic and nicotinic receptors, which results in symptoms of poisoning. Pralidoxime
restores the enzyme’s function and breaks the bond between the organophosphate and
acetylcholinesterase, thus reversing the toxic effects of organophosphates.
• Indications:
o Organophosphate poisoning (in combination with atropine)
o It is often used in combination with atropine, which helps control the muscarinic effects like
bradycardia and excessive secretions.
• Dose:
o For organophosphate poisoning: Initial dose is 1-2 g IV, repeated as necessary based on clinical
response, often every 2-6 hours.
• Dosage Form:
o Injectable solution (IV)
 • Adverse Effects:
o Tachycardia
o Hypertension
o Muscle stiffness
o Dizziness
o Nausea and vomiting
• Contraindications:
o None generally when used for organophosphate poisoning, but caution in patients with renal or
hepatic dysfunction.

4. Ipratropium Bromide

• Mechanism of Action:
o Ipratropium is an anticholinergic drug that blocks acetylcholine at muscarinic receptors in the smooth
muscles of the bronchi, leading to bronchodilation without significant systemic effects.
• Indications:
o Chronic obstructive pulmonary disease (COPD)
o Asthma (as an adjunct to beta-agonists)
o Acute bronchospasm (in some emergency situations)
• Dose:
o COPD/Asthma: 18 mcg per inhalation, typically 2 inhalations 4 times daily (up to 12 inhalations per
day).
o Acute bronchospasm: 0.5 mg via nebulizer every 20 minutes for up to 3 hours.
• Dosage Form:
o Inhalation aerosol (metered-dose inhaler), Nebulizer solution
• Adverse Effects:
o Dry mouth
o Throat irritation
o Cough, Blurred vision (if sprayed in eyes)
 • Contraindications:
o Hypersensitivity to ipratropium or atropine
o Acute narrow-angle glaucoma (if inadvertently inhaled into the eyes)
o Prostatic hypertrophy (due to risk of urinary retention)

4.ipratropium bromide

• Mechanism of Action:
• Ipratropium is an anticholinergic drug that blocks acetylcholine at muscarinic receptors in the smooth
muscles of the bronchi, leading to bronchodilation without significant systemic effects.
• Indications:
• Chronic obstructive pulmonary disease (COPD)
• Asthma (as an adjunct to beta-agonists)
• Acute bronchospasm (in some emergency situations)
• Dose:
• COPD/Asthma: 18 mcg per inhalation, typically 2 inhalations 4 times daily (up to 12 inhalations per day).
• Acute bronchospasm: 0.5 mg via nebulizer every 20 minutes for up to 3 hours.
• Dosage Form:
• Inhalation aerosol (metered-dose inhaler)
• Nebulizer solution
• Adverse Effects:
• Dry mouth
• Throat irritation
• Cough
• Blurred vision (if sprayed in eyes)
• Contraindications:
• Hypersensitivity to ipratropium or atropine
• Acute narrow-angle glaucoma , Prostatic hypertrophy (due to risk of urinary retention)
ADRENERGICS(sympathomimetics)

Adrenergic drugs (also known as sympathomimetics) are medications that mimic the effects of the
sympathetic nervous system, primarily by stimulating adrenergic receptors. These receptors are divided
into two main categories: alpha (α) and beta (β) receptors. Adrenergic drugs are used in various clinical
settings to manage conditions like low blood pressure, asthma, and heart failure.
1. Adrenaline (Epinephrine)

• Mechanism of Action:
o Adrenaline is a sympathomimetic drug that stimulates both alpha (α) and beta (β) adrenergic
receptors.
▪ Alpha-1 receptors: Causes vasoconstriction, leading to increased blood pressure.
▪ Beta-1 receptors: Increases heart rate (positive chronotropy) and contractility (positive
inotropy), improving cardiac output.
▪ Beta-2 receptors: Causes bronchodilation, and vasodilation in skeletal muscles.
o Overall, epinephrine increases blood pressure, improves myocardial perfusion, relieves
bronchoconstriction, and supports circulation.
• Uses:
o Anaphylaxis: First-line treatment to reverse the effects of severe allergic reactions.
o Cardiac arrest: Used in advanced cardiac life support (ACLS) to restore circulation and stimulate the
heart.
o Asthma and COPD exacerbations: Used for bronchodilation during acute asthma attacks or
bronchospasm.
o Hypotension and shock: Used in shock states (e.g., septic shock, anaphylactic shock) to support
blood pressure and improve circulation.
• Contraindications:
o Hypersensitivity to epinephrine.
o Narrow-angle glaucoma (can increase intraocular pressure).
o Shock due to non-cardiac causes (e.g., hypovolemic shock may not respond well to epinephrine).
o Cardiovascular conditions: Caution in patients with arrhythmias, coronary artery disease, or
hyperthyroidism.
• Adverse Effects:
o Cardiovascular: Tachycardia, hypertension, arrhythmias, palpitations.
o CNS: Anxiety, tremors, headache, restlessness.
o Metabolic: Hyperglycemia (due to beta-2 activation).
 o Respiratory: Paradoxical bronchospasm in sensitive patients.
o Others: Tissue necrosis (if injected extravasally).
• Dose and Dosage Form:
o Anaphylaxis: 0.3-0.5 mg intramuscularly (IM) for adults (0.01 mg/kg for children).
o Cardiac arrest: 1 mg intravenously (IV) every 3-5 minutes during resuscitation.
o Asthma/COPD: Nebulized 2.5 mg (adult) or 0.05 mg/kg (children).
o Shock: IV infusion, starting at 0.01-0.5 mcg/kg/min, titrated based on response.
o Dosage Form: Injectable (IM, IV), auto-injector (for anaphylaxis), nebulizer solution.

2.Noradrenaline

• Mechanism of Action:
o Noradrenaline primarily stimulates alpha-1 adrenergic receptors to cause vasoconstriction,
leading to an increase in systemic vascular resistance and blood pressure.
o It has mild stimulation of beta-1 receptors, increasing heart rate and contractility but not as
significantly as epinephrine.
• Uses:
o Septic shock: First-line agent for raising blood pressure in septic shock.
o Hypotension: For patients with significant hypotension unresponsive to other agents.
o Cardiogenic shock: To increase systemic vascular resistance and improve perfusion.
• Contraindications:
o Hypersensitivity to norepinephrine.
o Patients with hypotension due to blood loss or hypovolemia (prior fluid resuscitation is
recommended before use).
o Peripheral vascular disease: Risk of ischemia with vasoconstriction.
 • Adverse Effects:
o Cardiovascular: Tachycardia, hypertension, arrhythmias, decreased blood flow to extremities,
myocardial ischemia.
o Metabolic: Hyperglycemia.
o Extravasation: Can cause severe tissue necrosis at the injection site due to vasoconstriction.
o CNS: Anxiety, headache, restlessness.
• Dose and Dosage Form:
o Shock: IV infusion, typically starting at 0.01-0.5 mcg/kg/min, titrated to achieve target blood
pressure.
o Dosage Form: IV infusion (in a diluted solution).

3.Dobutamine

• Mechanism of Action:

• Dobutamine is a beta-1 adrenergic agonist that primarily stimulates beta-1 receptors in the heart,
increasing heart rate (chronotropy), contractility (inotropy), and cardiac output.
• It also has weak beta-2 and alpha-1 effects, which may lead to mild vasodilation and reduced systemic
vascular resistance.
• Unlike epinephrine, dobutamine has minimal effect on beta-2 receptors, so it does not cause significant
bronchodilation.

• Uses:

• Heart failure: Short-term management of acute heart failure or decompensated heart failure to increase
cardiac output.
• Cardiogenic shock: To improve myocardial contractility and maintain blood pressure.
• Cardiac stress testing: To stimulate the heart in patients who cannot undergo exercise stress testing.
• Contraindications:

• Hypersensitivity to dobutamine or any component of the formulation.

• Tachyarrhythmias: Caution in patients with pre-existing arrhythmias due to the risk of exacerbation.
• Idiopathic hypertrophic subaortic stenosis (IHSS): May worsen obstruction due to increased contractility.

• Adverse Effects:

• Cardiovascular: Tachycardia, arrhythmias (especially supraventricular arrhythmias), increased myocardial

oxygen demand.
• Metabolic: Mild hypertension (due to alpha-1 stimulation), hyperglycemia.
• CNS: Headache, anxiety, tremors.
• Gastrointestinal: Nausea, vomiting.

• Dose and Dosage Form:

• Heart failure/CV shock: IV infusion, typically starting at 2.5-5 mcg/kg/min, titrated based on clinical
response.
• Cardiac stress testing: 5-10 mcg/kg/min IV infusion.
• Dosage Form: IV infusion (requires dilution).

Antiadrenergics(sympatholytics)
Antiadrenergic drugs (also called adrenergic antagonists or sympatholytics) are medications that block the
effects of the adrenergic system, which is activated by adrenergic (sympathetic) neurotransmitters like
norepinephrine (noradrenaline) and epinephrine. These drugs inhibit the action of adrenergic receptors
(alpha and beta receptors), leading to various therapeutic effects.
 1.Phentolamine
• Mechanism of Action:
• Phentolamine is a non-selective alpha-adrenergic antagonist that blocks both alpha-1 and alpha-2
adrenergic receptors.
• Alpha-1 blockade leads to vasodilation, reducing blood pressure.
• Alpha-2 blockade increases the release of norepinephrine, which can also contribute to tachycardia.
• Indications:
• Pheochromocytoma: Management of hypertensive crises in patients with pheochromocytoma (tumor of the
adrenal gland that secretes catecholamines).
• Management of erectile dysfunction (in combination with other therapies).
• Preoperative preparation for surgery in pheochromocytoma patients.
• Contraindications:
• Hypersensitivity to phentolamine.
• Coronary artery disease: Risk of exacerbating ischemia due to vasodilation.
• History of myocardial infarction.
• Adverse Effects:

• Cardiovascular: Tachycardia, arrhythmias, hypotension, reflex tachycardia.

• CNS: Headache, dizziness, anxiety.
• GI: Nausea, vomiting, abdominal pain.
• Others: Nasal congestion, flushing.

• Dose and Dosage Form:

• Hypertensive crisis (pheochromocytoma): 5-10 mg IV, repeat as necessary.

• Erectile dysfunction: 1-2.5 mg intramuscularly.
• Dosage Form: Injectable solution for IV administration.

2.Tamsulosin

• Mechanism of Action:

• Tamsulosin is a selective alpha-1 adrenergic antagonist that primarily blocks the alpha-1A receptors
found in the prostate, bladder neck, and urethra.
• This causes smooth muscle relaxation in the lower urinary tract, improving urine flow and reducing
symptoms of benign prostatic hyperplasia (BPH).

• Indications:

• Benign prostatic hyperplasia (BPH): Symptom relief of urinary retention and difficulty urinating due to
BPH.
• Off-label use: Kidney stones (to facilitate passage of stones by relaxing the ureter).
• Contraindications:
• Hypersensitivity to tamsulosin.
• Severe hepatic impairment (due to altered metabolism of the drug).
• Severe renal impairment (caution in dose adjustment).
• Adverse Effects:
• Cardiovascular: Orthostatic hypotension, dizziness, syncope (especially during the first dose).
• CNS: Headache, dizziness, fatigue.
• Gastrointestinal: Nausea, retrograde ejaculation (common but not harmful).
• Other: Rhinitis, sleep disturbances.
• Dose and Dosage Form:
• BPH: 0.4 mg orally once daily (after a meal), can be increased to 0.8 mg if necessary.
• Dosage Form: Oral capsule (typically 0.4 mg or 0.8 mg).

3.Prazocin
• Mechanism of Action:

• Prazosin is a selective alpha-1 adrenergic antagonist. It works by blocking alpha-1 receptors on vascular
smooth muscle, leading to vasodilation, reduction of systemic vascular resistance, and lower blood
pressure.

• Indications:

• Hypertension: As an antihypertensive agent (often used in combination with other drugs).

• Benign Prostatic Hyperplasia (BPH): Symptom relief from urinary retention.
• Post-traumatic stress disorder (PTSD): psychiatric disorder that can occur in people who have experienced or witnessed a
traumatic event such as natural disasters, serious accidents, war/combat, or personal)
• Contraindications:

• Hypersensitivity to prazosin.
• Severe hypotension or orthostatic hypotension (risk of syncope).
• Renal failure (caution required).

• Adverse Effects:

• Cardiovascular: Orthostatic hypotension (first-dose effect), dizziness, tachycardia.

• CNS: Drowsiness, fatigue, headache, vivid dreams.
• GI: Nausea, vomiting.
• Other: Fluid retention (in some patients).

• Dose and Dosage Form:

• Hypertension: 1 mg orally twice or three times a day, gradually increased to 6-15 mg/day.
• BPH: 1-5 mg orally twice daily.
• PTSD nightmares: 1-2 mg at bedtime.
• Dosage Form: Oral tablet (1 mg, 2 mg, 5 mg).

o Erectile dysfunction: 1-2.5 mg intramuscularly.

o Dosage Form: Injectable solution for IV administration
o

4. Timolol

• Mechanism of Action:
o Timolol is a non-selective beta-adrenergic antagonist (beta-blocker) that blocks both beta-1 and beta-2 adrenergic
receptors. This results in reduced heart rate, decreased myocardial contractility, and reduced intraocular
pressure.
o It does not have intrinsic sympathomimetic activity and is used to lower blood pressure and treat glaucoma.
• Indications:
o Hypertension: To reduce blood pressure.
o Glaucoma: As eye drops to reduce intraocular pressure in open-angle glaucoma or ocular hypertension.
o Angina pectoris and arrhythmias (especially atrial fibrillation and supraventricular tachycardia).
• Contraindications:
o Asthma or COPD (due to beta-2 receptor blockade causing bronchoconstriction).
o Severe bradycardia, heart block, or cardiogenic shock.
o Hypersensitivity to timolol or other beta-blockers.
o Pregnancy (use with caution in the second and third trimesters).
• Adverse Effects:
o Cardiovascular: Bradycardia, hypotension, heart block.
o Respiratory: Bronchospasm (due to beta-2 blockade).
o CNS: Fatigue, dizziness, depression, sleep disturbances.
o Other: Sexual dysfunction, cold extremities, dry eyes (if used topically).
• Dose and Dosage Form:
o Hypertension: 5-10 mg orally once daily, up to 20-40 mg daily.
o Angina: 10-30 mg orally twice daily.
o Glaucoma: 1 drop of Timolol ophthalmic solution (0.25% or 0.5%) in the affected eye(s) once or twice daily.
o Dosage Form: Oral tablets (5 mg, 10 mg), ophthalmic solution (0.25%, 0.5%).
 UNIT-3
Drug Acting on Peripheral Nervous system
The Peripheral Nervous System (PNS) is a crucial part of the nervous system that lies outside the brain and
spinal cord. It connects the central nervous system (CNS) to limbs and organs. The PNS plays an essential
role in communication between the body and the CNS, carrying sensory information to the brain and
conveying motor instructions to muscles and glands.

Skeletal muscle relaxants

Skeletal muscle relaxants are a class of drugs used to relieve muscle spasms, spasticity, and associated
pain or discomfort. These medications work by affecting the nervous system or directly acting on the
muscle fibers. They are commonly used in conditions like musculoskeletal disorders, spinal cord injuries,
multiple sclerosis, cerebral palsy, and acute muscle strains.
1.Tizanidine
Tizanidine

Mechanism of Action
• Tizanidine works by stimulating alpha-2 adrenergic receptors in the brain and spinal cord, particularly in the presynaptic
motor neurons. This results in the inhibition of the release of excitatory neurotransmitters, which leads to decreased
muscle tone and spasticity.
• It decreases the frequency and intensity of muscle spasms, making it useful in conditions with spasticity (such as multiple
sclerosis or spinal cord injuries).
Indications
• Spasticity: Especially in conditions such as multiple sclerosis, spinal cord injury, and cerebral palsy.
• Muscle spasm: For symptomatic relief of acute muscle spasms related to musculoskeletal conditions.
Contraindications

• Hypersensitivity to tizanidine.
• Severe hepatic impairment: Tizanidine is metabolized by the liver, and liver dysfunction can increase its concentration and
risk of toxicity.
• Concomitant use with fluvoxamine: Fluvoxamine inhibits tizanidine metabolism and can cause significant increases in
tizanidine levels.
• Pregnancy and breastfeeding: Safety during pregnancy has not been established (Category C).

Adverse Effects

• Sedation: Tizanidine can cause drowsiness or fatigue, especially when treatment is initiated or when doses are increased.
• Hypotension: A common side effect, as tizanidine can lower blood pressure, especially in the first few hours after dosing.
• Dry mouth: Due to its action on adrenergic receptors.
• Dizziness and lightheadedness: Particularly when standing up quickly.
• Liver toxicity: Elevated liver enzymes or hepatotoxicity can occur, so liver function tests should be monitored.
• Weakness and muscle hypotonia: Excessive muscle relaxation leading to weakness may occur.
• Bradycardia: Lower heart rate due to alpha-2 agonist activity.

Dose and Dosage Form

• Initial Dose: 2 mg orally 3 times a day.
• Maximum Dose: 36 mg per day (given in divided doses). The dose can be gradually increased based on patient tolerance and
therapeutic response.
• Dosage Form: Oral tablet, capsule.

2.Chlorzoxazone
Mechanism of Action

• The exact mechanism of action of chlorzoxazone is not completely understood. However, it is believed to work by acting
centrally within the spinal cord and brain, suppressing the neural activity responsible for muscle spasms. This leads to
muscle relaxation.
• Unlike other muscle relaxants, it does not act directly on the muscle but rather on the CNS pathways controlling motor output.
Indications

• Muscle spasm: Chlorzoxazone is used to relieve discomfort and pain caused by acute musculoskeletal conditions and muscle
spasms.
• Musculoskeletal pain: For conditions like strains, sprains, and back pain.

Contraindications

• Hypersensitivity to chlorzoxazone or any component of the formulation.

• Severe liver dysfunction: Chlorzoxazone is metabolized by the liver, and its use is contraindicated in patients with liver
diseases (e.g., cirrhosis).
• Pregnancy: Category C, meaning it should only be used if the potential benefits outweigh the risks.
• Breastfeeding: Chlorzoxazone is excreted in breast milk and should be avoided or used cautiously during breastfeeding.

Adverse Effects

• Drowsiness: A common effect due to its CNS depressant action.

• Dizziness and lightheadedness: Can cause difficulty with balance or coordination.
• Liver toxicity: Elevated liver enzymes, and rare cases of hepatitis or jaundice have been reported, so liver function should be
monitored.
• Gastrointestinal disturbances: Nausea and vomiting may occur.
• Skin rash: A rare side effect but should be monitored.
• Hypotension: Dizziness or lightheadedness, especially when standing up too quickly.

Dose and Dosage Form

• Dose: 250 mg to 750 mg orally 3 to 4 times per day.

• Maximum Dose: Up to 3,000 mg per day (depending on patient response).
• Dosage Form: Oral tablet.
Local anesthetics
Local anesthetics are medications used to induce temporary loss of sensation in a specific area of the body without affecting consciousness.
They work by blocking the transmission of nerve impulses, typically in the peripheral nervous system (PNS), to prevent pain sensation in the
targeted region.

1.lignocaine
Mechanism of Action:
• Lidocaine works by blocking voltage-gated sodium channels on the neuronal cell membrane. This blockage prevents the
transmission of pain signal from the affected nerves to the brain, leading to anesthesia.
• It blocks both sensory and motor nerve fibers, with sensory fibers being more sensitive to the drug.
Indications:
• Local anesthesia: For minor surgical procedures, dental procedures, and diagnostic interventions.
• Nerve blocks: To provide regional anesthesia, for example, in limb surgeries.
• Topical anesthesia: For conditions like sunburn, sore throat, and skin irritation.
• Antiarrhythmic: Used in ventricular arrhythmias, especially after myocardial infarction, due to its ability to stabilize the
cardiac cell membrane.
• Post-operative pain management: Used as an adjunct for pain relief after surgeries.
Contraindications:

• Hypersensitivity to lidocaine or any other components of the formulation.

• Severe heart block or Arrhythmias (if used for antiarrhythmic purposes, should be used with caution).
• Severe liver disease: As lidocaine is metabolized in the liver, impaired liver function can increase the risk of systemic toxicity.
• Porphyria: A metabolic disorder that can be worsened by lidocaine.
• Pregnancy and lactation: Use cautiously, especially in the first trimester (Category B), but it is generally considered safe
when needed.

Adverse Effects:

• CNS toxicity: Early symptoms include tinnitus, dizziness, numbness of the tongue, and seizures in severe cases.
• Cardiovascular effects: Hypotension, bradycardia, and arrhythmias.
• Local reactions: Mild redness, swelling, or itching at the injection site.
• Allergic reactions: Rare but possible, including rash, urticaria, or angioedema.
• Methemoglobinemia (rare, but more common with higher doses or prolonged use).
• Toxicity: In case of overdose, symptoms can include CNS depression, respiratory depression, and cardiac arrest.

Dose and Dosage Form:

• Dose:
o For local anesthesia: 1-5% solution depending on the procedure and patient condition.
o For nerve blocks: 3-5 mg/kg (max dose of 300 mg).
o For ventricular arrhythmias: Initial IV dose: 50-100 mg bolus, then infusion at 1-4 mg/min.
• Dosage Form:
o Injectable solution (1%, 2%, 4% solutions for local anesthesia).
o Topical gel, cream, or spray (5%).
o Oral solution (for throat numbing or as a local anesthetic in mouth conditions).
o Patch (e.g., lidocaine patches for localized pain relief)
2.Bupivacaine
Mechanism of Action:SAME

• Bupivacaine is a long-acting amide-type local anesthetic that works similarly to lidocaine by blocking voltage-gated
sodium channels on nerve cells. However, bupivacaine binds more strongly to sodium channels, producing a longer duration
of action compared to lidocaine.
• It has a higher affinity for motor neurons, leading to longer-lasting motor block compared to sensory block, which can be
useful for certain types of surgeries (e.g., labor and delivery).

Indications:

• Local anesthesia: For major surgeries, such as orthopedic procedures, abdominal surgery, or dental procedures.
• Regional anesthesia: Used in epidural anesthesia, spinal anesthesia, and nerve blocks.
• Labor and delivery: As an epidural anesthetic for pain relief during childbirth.
• Post-operative pain management: For extended pain relief after surgeries.

Contraindications:

• Hypersensitivity to bupivacaine or any of the components of the formulation.

• Severe heart block: Due to the risk of cardiac toxicity.
• Severe liver disease: As bupivacaine is metabolized in the liver, impaired liver function can lead to toxic accumulation.
• Pregnancy and lactation: Caution is required, though bupivacaine is commonly used in labor for epidurals (Category C).
• Pediatric patients: Use with caution in infants and small children, as they are more susceptible to the toxic effects of local
anesthetics.

Adverse Effects:

• CNS toxicity: Symptoms like seizures, drowsiness, tinnitus, dizziness, and visual disturbances.
• Cardiovascular toxicity: Hypotension, bradycardia, arrhythmias, and in severe cases cardiac arrest.
• to muscle weakness.
• Local reactions: Redness, swelling, or pain at the injection site.
• Allergic reactions: Rash, urticaria, and anaphylaxis (though rare)..
Dose and Dosage Form:

• Dose:
o For local anesthesia: 0.25%-0.5% solution for infiltration, up to 175 mg maximum dose.
o For epidural anesthesia: 0.25%-0.5% solution at 10-15 mL (maximum dose 225 mg).
o For spinal anesthesia: 0.5% solution, up to 3-5 mL.
• Dosage Form:
o Injectable solution (0.25%, 0.5%, 0.75%, 1%).
o Epidural and spinal injections (1-2% for regional blocks).
o Infusion solutions for longer-term management of pain.
 UNIT-4
Drug acting on CNS

General Anesthesia
General anesthesia is a controlled and reversible state characterized by the following effects:

* Loss of consciousness
* Loss of sensation (analgesia)
* Amnesia (no memory of the procedure)
* Skeletal muscle relaxation
* Suppression of reflexes

These effects enable surgical or diagnostic procedures to be performed without pain or awareness.

Stages of General Anesthesia

As the dose or concentration of the anesthetic increases in the body (particularly in the brain), the patient progresses
through the four stages of anesthesia:

* Stage I: Analgesia (Induction Stage)

* Patient remains conscious but drowsy
* Experiences pain relief (analgesia)
* Reflexes are intact
* Respiration is normal
* Suitable for minor procedures

* Stage II: Excitement (Delirium Stage)

* Patient becomes unconscious but may exhibit: * Irregular breath* Involuntary movements
* Vomiting or laryngospasm
* Increased muscle tone. This stage is undesirable and hazardous, so it is swiftly overcome using rapid-acting agents.
* Stage III: Surgical Anesthesia
* Optimal stage for surgery
* Unconsciousness, muscle relaxation, loss of reflexes
* Regular, shallow breathing
* Further divided into four planes, from light to deep anesthesia
* Plane 1: Eyelid reflex absent
* Plane 2: Loss of laryngeal reflex
* Plane 3: Pupils dilated, no light reflex
* Plane 4: Intercostal muscle paralysis

* Stage IV: Medullary Paralysis ( Overdose Stage😊

* Extremely dangerous
* Severe depression of brainstem centers
* Cessation of respiration and circulation
* Can lead to death if not reversed immediately
* Requires immediate resuscitation
◦
Types of General Anesthesia:

1. Inhalational Anesthetics:
* Halothane
* Isoflurane
* Sevoflurane
* Desflurane
* Nitrous oxide (N₂O)

3. Intravenous Anesthetics:
* Thiopental (barbiturate)
* Propofol
* Etomidate
* Ketamine
* Midazolam (benzodiazepine)
1.Nitrous Oxide (N₂O):

Mechanism of Action:

* Nitrous oxide inhibits the N-methyl-D-aspartate (NMDA) subtype of glutamate receptors in the central nervous
system. By blocking these excitatory receptors, it reduces excitatory neurotransmission, contributing to analgesia
and sedation.
* Mild CNS depressant and analgesic effect

Indications:

* Supplementary inhalational anesthetic

* Used with other agents for balanced anesthesia
* Dental procedures, minor surgeries
* Analgesia in labor

Contraindications:

* Pneumothorax or air embolism (Accumulation of air in the pleural space between the lung and chest wall, causing
partial or complete lung collapse.)
* Severe COPD or respiratory obstruction
* Middle ear surgery
* Bowel obstruction (risk of gas expansion)

Adverse Effects:

* Diffusion hypoxia (temporary low oxygen level due to rapid diffusion of N₂O)
* Nausea, vomiting
Bone Marrow Suppression and Vitamin B12 Inactivation
 4. PRECAUTION:

- Avoid use in enclosed spaces (e.g., pneumothorax, bowel obstruction, middle ear surgery).
- Administer 100% oxygen after cessation of inhalation to prevent diffusion hypoxia.
- Prolonged use may lead to vitamin B12 deficiency; monitor in long-term use.

Dose and Dosage Form:

- Inhalational gas mixture of oxygen (commonly 30-70% N₂O with oxygen)

- Administered via mask or endotracheal tube
- Typically combined with other anesthetics for surgical anesthesia

2.Halothane
Mechanism of Action:
• Halothane increases the inhibitory effect of gamma-aminobutyric acid (GABA) at the GABA-A receptor.

• This leads to increased chloride ion influx into neurons → hyperpolarization → neuronal inhibition.

• Result: CNS depression, unconsciousness, muscle relaxation, and loss of reflexes.

Indications:

- Maintenance of general anesthesia

- Used in surgeries requiring controlled anesthesia

Contraindications:

- History of malignant hyperthermia (rapid temperature increase, severe muscle contraction)

- Severe liver disease (risk of halothane hepatitis)
- Sensitivity to halogenated anesthetics
Adverse Effects:

- Hepatotoxicity (halothane hepatitis)

- Malignant hyperthermia
- Hypotension and bradycardia
- Respiratory depression
- Arrhythmias

PRECAUTION:

- Avoid repeated use due to risk of halothane hepatitis.

- Screen for malignant hyperthermia susceptibility.
- Use with caution in patients with liver disease or cardiac arrhythmias.

Dose and Dosage Form:

• Dosage form: Volatile liquid for inhalation (via anesthesia vaporizer)

• Dose:
o Induction: 0.5% – 1% inhaled concentration
o Maintenance: 0.5% – 2% inhaled concentration

3.ketamine
Mechanism of Action:
- Ketamine acts as an NMDA(N-Methyl-D-Aspartate) receptor antagonist, blocking the excitatory neurotransmitter
glutamate.
- This action leads to CNS depression and dissociative anesthesia.
- Ketamine produces analgesia, amnesia, and sedation without causing complete loss of consciousness.
Indications:
- Induction and maintenance of anesthesia
- Analgesia in trauma or burn patients
- Sedation in procedures outside the operating room (OR)
- Pediatric anesthesia (due to minimal respiratory depression)

Contraindications:
- Patients with hypertension
- Severe cardiovascular disease
- Psychiatric disorders (may cause hallucinations or delirium)

Adverse Effects:
- Emergence reactions (hallucinations, vivid dreams)
- Increased salivation
- Increased blood pressure and heart rate
- Rarely, respiratory depression
- Nausea and vomiting

Precautions:
- Use cautiously in hypertensive or cardiac patients (increased blood pressure and heart rate)
- May cause emergence reactions (hallucinations, nightmares) - Premedicate with benzodiazepines

Dose and Dosage Form:

- IV/IM injection:
- IV induction dose: 1-2 mg/kg
- IM dose: 4-10 mg/kg
- Also available as oral or nasal preparations (less common)
- Given as a single bolus or infusion, depending on the need
SEDATIVES AND HYPNOTICS

• Sedatives:
Drugs that calm the patient, reduce anxiety, and produce relaxation without causing sleep (at low doses).

• Hypnotics:
Drugs that induce and maintain sleep (at higher doses) and are used in the treatment of insomnia.

Classification of Sedatives and Hypnotics

1. Benzodiazepines (BZDs)
• Examples: Diazepam, Alprazolam, Lorazepam, Clonazepam, Midazolam

2. Barbiturates
• Examples: Phenobarbitone, Thiopental, Amobarbital

3. Non-Benzodiazepine Hypnotics (Z-drugs)

• Examples: Zolpidem, Zaleplon, Eszopiclone

4. Others
• Antihistamines: Hydroxyzine, Diphenhydramine (used for mild sedation)
• Melatonin receptor agonists: Ramelteon
• Alpha-2 agonists: Dexmedetomidine (sedation)
• Alcohol and related compounds (used historically as sedatives)
1. Diazepam

• Mechanism of Action:( common)

• Enhances the effect of GABA (gamma-aminobutyric acid), (a calming chemical in the brain.)
• It increases the frequency at which chloride channels open → leads to hyperpolarization , which causes
relaxation, sleepiness, and less anxiety.

• Indications (Uses):
• Anxiety
• Muscle spasms
• Seizures (e.g., status epilepticus)
• Alcohol withdrawal symptoms
• Pre-surgery sedation
.
• Side Effects:
• Drowsiness
• Confusion
• Muscle weakness
• Dependence (if used for long time)
. Ataxia( loss on co-ordination)

• Contraindications (When not to use):

• Severe breathing problems
• Myasthenia gravis (a disease causing weak muscles)
• Severe liver disease

• Dose and Form:

• 2–10 mg orally, 2 to 4 times a day
• Forms: Tablet, oral solution, injection
2. Alprazolam

• Indications:
• Anxiety disorders
• Panic attacks

• Side Effects:
• Sleepiness
• Poor coordination
• Risk of dependence and withdrawal (especially if stopped suddenly)
. Fatigue
. dry mouth
.Drawsiness

• Contraindications:
• Narrow-angle glaucoma (a serious eye condition)
• Severe lung or liver problems

• Dose and Form:

• 0.25–0.5 mg orally, 2–3 times a day
• Forms: Tablets (regular and extended release), oral liquid

3. Lorazepam

• Indications:
• Anxiety
• Seizures (e.g., status epilepticus) • Sedation before surgery • Short-term treatment of insomnia

• Side Effects:

• Drowsiness
• Dizziness, Low blood pressure,• Breathing difficulty (at high doses), Ataxia
•Fatigue
• Contraindications:
• Severe liver damage
• Breathing problems like sleep apnea

• Dose and Form:

• 1–4 mg per day in divided doses
• Forms: Tablets, injection, oral solution

4. Clonazepam

• Indications:
• Seizure disorders (like absence or myoclonic seizures)
• Panic disorder ( anxiety)

• Side Effects:
• Tiredness
• Confusion
• Difficulty in coordination
• Depression (in some)
•Fatigue
•Drawsiness and dizziness

• Contraindications:
• Severe liver disease
• Sleep apnea(Sleep apnea is a sleep disorder characterized by repeated pauses in breathing during sleep.)
• History of drug abuse

• Dose and Form:

• Start with 0.5 mg twice a day, adjust as needed
• Forms: Tablets, orally disintegrating tablets (ODT)
⸻

5. Phenobarbitone (Phenobarbital)

• Mechanism of Action:
• Enhances GABA effect → keeps chloride channels open longer → cause hyperpolarization which leads to
strong CNS (brain) depression.

• Indications:
• Epilepsy (especially tonic-clonic seizures)
• Sedation
• Febrile seizures (in children)
•Pre- anaesthetic medication

• Side Effects:
• Sleepiness
• Slowed breathing
• Memory issues
• Risk of addiction
•Ataxia

• Contraindications:
• Porphyria (a rare blood disease)
• Severe breathing problems
• Liver disease

• Dose and Form:

• Usual: 60–100 mg/day in divided doses
• Forms: Tablets, syrup, injection
 Antiepileptic drug
Definition of Epilepsy

Epilepsy is a neurological disorder characterized by recurrent(repeatedly), unprovoked(without cause) seizures due to

abnormal, excessive electrical discharges in the brain.

Antiepileptic Drugs (AEDs)

Antiepileptic drugs are medications used to prevent or reduce the frequency and severity of seizures in patients with epilepsy

Classification of Antiepileptic Drugs (with Examples)

I. Sodium Channel Blockers
• Phenytoin
• Carbamazepine
• Lamotrigine
II. Calcium Channel Blockers
• Ethosuximide (used in absence seizures)
III. GABA Enhancers
• Phenobarbital
• Benzodiazepines (e.g., diazepam, clonazepam)
• Valproic acid
IV. Glutamate Inhibitors
• Topiramate
• Felbamate
V. Multiple Mechanisms
• Valproic acid
• Lamotrigine
• Levetiracetam
1.Carbamazepine

• Mechanism of Action (MOA): (common)

• Blocks voltage-gated sodium (Na⁺) channels in the neuronal membrane.
• Stabilizes the inactive state of sodium channels → prevents high-frequency repetitive firing of neurons.
• This reduces neuronal excitability and prevents seizure propagation.
• Indications:
o Partial seizures( starts in just one specific area of brain)
o Generalized tonic-clonic seizures( Affects whole brain)
o Trigeminal neuralgia (pain condition affecting trigeminal nerve which carry sensation from face to brain)
o Bipolar disorder (Extreme mood swings)
• Adverse Effects:
o Dizziness, ataxia
o Blurred vision
o Aplastic anemia
o Hyponatremia (SIADH)
o Rash (risk of Stevens-Johnson Syndrome)
• Contraindications:
o History of bone marrow depression
o Hypersensitivity to tricyclic drugs
• Dose and Dosage Form:
o Adults: 200–400 mg/day initially; maintenance: 800–1200 mg/day in divided doses
o Forms: Tablets, extended-release tablets, syrup, chewable tablets

2. Phenytoin

• Indications:
o Generalized tonic-clonic seizures
o Partial seizures
o Status epilepticus (IV form) ( seizure lasts more then 5 min) or person have back to back seizure .
 • Adverse Effects:
o Gum hyperplasia( Abnormal overgrowth of gum)
o Hirsutism(Excess hair growth in women)
o Ataxia ( loss of coordination)
o Megaloblastic anemia
o Osteomalacia (WEAk bone)
o Teratogenicity (fetal hydantoin syndrome)
• Contraindications:
• hypersensitivity
o Sinus bradycardia(TOO slow heart beat)
o SA block, AV block( electrical signal in heart are blocked)
o Pregnancy (category D)
• Dose and Dosage Form:
o Oral: 100 mg 2–3 times daily
o IV (loading for status epilepticus): 15–20 mg/kg slowly
o Forms: Tablets, capsules, oral suspension, injection

3. Valproic Acid / Valproate

• Mechanism of Action (MOA):

o Multiple actions:

• Enhances GABAergic inhibition:

• Inhibits GABA transaminase → prevents GABA breakdown → increases GABA levels in the brain.
• Result: Enhanced inhibitory neurotransmission → CNS depression → seizure control.

• Blocks voltage-gated sodium (Na⁺) channels:

• Blocks voltage-gated sodium (Na⁺) channels in the neuronal membrane.

• Stabilizes the inactive state of sodium channels → prevents high-frequency repetitive firing of neurons.
• This reduces neuronal excitability and prevents seizure propagation.
 Indications:

o Broad-spectrum AED:
▪ Absence seizures(loss of awareness but not jerking)
▪ Myoclonic seizures(sudden quick jerks)
▪ Tonic-clonic seizures
▪ Bipolar disorder
▪ Migraine prophylaxis
• Adverse Effects:
o GI upset (nausea, vomiting)
o Hepatotoxicity
o Pancreatitis
o Weight gain
o Hair loss
o Tremor
o Teratogenic (neural tube defects)
• Contraindications:
o Liver disease
o Pregnancy (category D/X)
o Urea cycle disorders
• Dose and Dosage Form:
o Initial: 10–15 mg/kg/day → maintenance: 30–60 mg/kg/day
o Forms: Tablets, syrup, injection, sprinkle capsules
 Antipsychotics and Antianxiety

Antipsychotics
Definition:

Antipsychotics are drugs used to manage psychotic disorders such as schizophrenia, delusional disorders, and bipolar disorder.
They primarily help in reducing hallucinations, delusions, thought disorders, and agitation(REStlessness,nervousness).

Schizophrenia -is a chronic mental disorder characterized by distorted thinking, perceptions, emotions, and behavior.

delusional disorders- A psychiatric condition where a person has one or more non-bizarre delusions (i.e., false but possible beliefs) for at
least 1 month, without other major symptoms of schizophrenia

bipolar disorder- excessive mood swings

Classification of Antipsychotics

1. Typical (First-Generation) Antipsychotics

• High potency: Haloperidol, Fluphenazine

• Low potency: Chlorpromazine, Thioridazine

2. Atypical (Second-Generation) Antipsychotics

• Examples: Risperidone, Olanzapine, Quetiapine, Clozapine, Aripiprazole, Ziprasidone

Antianxiety Drugs (Anxiolytics)

Definition:

Antianxiety drugs, or anxiolytics, are medications used to reduce excessive anxiety, tension, or fear without causing significant
sedation (at therapeutic doses).

Classification of Antianxiety Drugs

1. Benzodiazepines (BZDs)

Diazepam, Lorazepam, Alprazolam, Clonazepam, midazolam

2. Non-Benzodiazepine Anxiolytics

Buspirone

3. Antidepressants (used for chronic anxiety)

Fluoxetine, Sertraline, Escitalopram, Venlafaxine, Duloxetine

4. Others

• Beta-blockers (e.g., Propranolol) – for performance anxiety

• Antihistamines (e.g., Hydroxyzine) – short-term anxiety relief
• Atypical antipsychotics (low dose) – used off-label in some anxiety disorders
 1. Olanzapine
Mechanism of Action (MOA):

Olanzapine works by blocking several neurotransmitter receptors in the brain:

• Dopamine D₂ receptor antagonism → reduces positive symptoms of schizophrenia (hallucinations, delusions)

• Serotonin 5-HT₂A receptor antagonism → helps improve negative symptoms (social withdrawal, lack of motivation) and
reduces extrapyramidal side effects
• Also blocks:
o Histamine H₁ receptors → causes sedation and weight gain
o Muscarinic receptors (M1–M5) → causes dry mouth, constipation
o Alpha-1 adrenergic receptors → may cause orthostatic hypotension (dizziness on standing)

Uses:

• Schizophrenia
• Bipolar disorder
• Psychosis associated with dementia (Dementia is a chronic and progressive decline in brain function that affects:

• Memory
• Thinking
• Behavior
• Ability to perform daily activities

Adverse Effects:

• Weight gain
• Sedation (sleepiness)
• Hyperglycemia (high blood sugar)
• Dyslipidemia (abnormal cholesterol)
 • Extrapyramidal symptoms (EPS) – less common than typical antipsychotics
(EPS = abnormal movements like tremors, stiffness)
• Increase appitite
• Dry mouth

Contraindications:

• History of neuroleptic malignant syndrome (Neuroleptic Malignant Syndrome is a serious reaction that can happen when
someone takes certain psychiatric (mental health) medicines, especially antipsychotics (also called neuroleptics).
• Severe liver disease
• Caution in diabetic patients

Dose and Dosage Form:

• Oral tablets: 5–20 mg once daily

• Orally disintegrating tablets (ODT)
• IM injection for acute agitation

2. Haloperidol
MOA:

• Primarily blocks dopamine D₂ receptors in the mesolimbic pathway of the brain → controls positive symptoms of psychosis
(hallucinations, delusions)
• Strong D₂ blockade in the nigrostriatal pathway can lead to extrapyramidal side effects (EPS)
• Also blocks:

• Alpha-1 adrenergic receptors → hypotension

• Minimal anticholinergic or antihistamine activity compared to other drugs
Uses:

• Schizophrenia
• Acute psychosis
• Tourette’s syndrome (Tourette’s Syndrome is a neurological disorder that causes a person to make involuntary movements or sounds
called tics.)
• Agitation in elderly

Adverse Effects:

• Extrapyramidal symptoms (EPS)( EPS are movement-related side effects)

• Tardive dyskinesia (involuntary mouth/facial movements)
• Sedation
• QT prolongation (risk of abnormal heart rhythm)
• Headache

Contraindications:

• Parkinson’s disease
• CNS depression (e.g., coma)
• Cardiac arrhythmia

Dose and Dosage Form:

• Oral tablets: 0.5–10 mg/day

• IM/IV injection for acute episodes
• Depot injection (long-acting, monthly)
 3. Chlorpromazine
MOA
• Blocks dopamine D₂ receptors → treats positive psychotic symptoms

• Blocks histamine H₁ receptors → causes sedation and weight gain

• Blocks muscarinic cholinergic receptors → causes anticholinergic effects (dry mouth, blurred vision, constipation)

• Blocks alpha-1 adrenergic receptors → causes hypotension, dizziness

• Also has antiemetic (anti-vomiting) action due to dopamine blockade in the chemoreceptor trigger zone (CTZ)

Uses:

• Schizophrenia
• Mania(Mania is a state of abnormally elevated mood, energy, and activity levels that is uncontrolled and not normal happiness)
• Severe nausea/vomiting
• Intractable hiccups( HICCUPS FOR MORE THEN 48 HRS)

Adverse Effects:

• Sedation
• Hypotension (low blood pressure)
• Dry mouth, constipation (anticholinergic effects)
• Photosensitivity (skin reacts to sunlight)
• Drawsiness
• Weight gain
 Contraindications:

• Severe CNS depression

• Bone marrow suppression
• Glaucoma
• Liver disease

Dose and Dosage Form:

• Oral tablets: 25–100 mg 2–3 times/day

• Injection (IM/IV) for acute use
• Syrup

4. Chlordiazepoxide
MOA:

• Enhances the effect of GABA (gamma-aminobutyric acid), the main inhibitory neurotransmitter in the brain

• Binds to a specific site on the GABA-A receptor complex

• Increases the frequency of chloride (Cl⁻) channel opening

• Leads to:

• Hyperpolarization of the neuron (less likely to fire)

• CNS depression → results in sedation, anxiolysis (anxiety relief), muscle relaxation, and anticonvulsant effec

Uses:
• Anxiety disorders
• Alcohol withdrawal symptoms
• Preoperative sedation
• Muscle spasms

Adverse Effects:

• Drowsiness
• Confusion
• Ataxia (loss of coordination)
• Dependence and withdrawal symptoms on long-term use
• FATIGUE
• Blur vision
• headache

Contraindications:

• Severe respiratory depression

• Sleep apnea
• Myasthenia gravis (muscle weakness disorder)
• Severe liver disease

Dose and Dosage Form:

• Tablets/Capsules: 5–25 mg 1–4 times/day (depending on condition)

• Injection (IV/IM) in hospital settings
• Oral syrup

Antidepressants / mood stabilizers

Mood Stabilizers:

Mood stabilizers are a group of drugs used to treat and prevent mood fluctuations, particularly in bipolar disorder, by reducing the
severity and frequency of manic and depressive episodes.
They help stabilize mood over time and prevent relapse.

Classification of Mood Stabilizers::

1. Classical Mood Stabilizers (True Mood Stabilizers)
• Lithium
• Valproic acid (Valproate)
• Carbamazepine
2. Atypical Antipsychotics with Mood-Stabilizing Properties.
• Olanzapine
• Risperidone
• Quetiapine
• Aripiprazole
• Lurasidone
3. Anticonvulsants with Mood-Stabilizing Effects
• Lamotrigine (better for bipolar depression)
• Topiramate
• Oxcarbazepine
4. Others (Less Common / Investigational)
• Gabapentin (off-label, weak mood stabilizer)
• Levetiracetam (limited evidence)
Antidepressants

Antidepressants are a group of drugs used to treat depressive disorders and other psychiatric conditions (like anxiety, OCD, PTSD)
by increasing levels of neurotransmitters such as serotonin (5-HT), norepinephrine (NE), and sometimes dopamine (DA) in the
brain, thereby improving mood and emotional state.

Classification of Antidepressants::

1. Selective Serotonin Reuptake Inhibitors (SSRIs)

• Mechanism: Inhibit reuptake of serotonin (5-HT) → increased serotonin levels.
o Fluoxetine
o Sertraline
o Paroxetine
o Escitalopram
2. Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs)
o Venlafaxine
o Desvenlafaxine
o Duloxetine
3. Tricyclic Antidepressants (TCAs.
o Amitriptyline
o Imipramine
o Nortriptyline
o Clomipramine
4. Monoamine Oxidase Inhibitors (MAOIs)
o Phenelzine
o Tranylcypromine
o Selegiline
5. Atypical Antidepressants (Miscellaneous group)
o Bupropion (dopamine-norepinephrine reuptake inhibitor; used in smoking cessation)
o Mirtazapine (increases NE and 5-HT by blocking α2 receptors)
o Trazodone (5-HT modulator; also used for insomnia)
o Vilazodone and Vortioxetine (newer agents)
o
1. Fluoxetine

Mechanism of Action:

Fluoxetine is a Selective Serotonin Reuptake Inhibitor (SSRI) that works by blocking the serotonin transporter (SERT) on
presynaptic neurons(A synaptic neuron refers to a neuron involved in transmitting signals across a synapse, the junction between two nerve
cells (neuron)). This prevents reuptake of serotonin , leading to increased serotonin levels at the synapse. Over time, this enhances
serotonergic neurotransmission and improves mood and emotional regulation.

Indications:

• Major depressive disorder

• Obsessive-compulsive disorder (OCD)( unwanted, repetitive thoughts)
• Bulimia nervosa(Eats large amounts of food and Tries to get removeby vomiting, using laxatives, or fasting)
• Panic disorder
• Premenstrual dysphoric disorder(severe form of PMS (premenstrual syndrome).

Adverse Effects:

• Insomnia, headache, Sexual dysfunction

• GI upset (nausea, diarrhea)
• Weight changes
• Anxiety, agitation
• Risk of serotonin syndrome (especially with MAOIs)
• Increased suicidal thoughts in young adults, QT prolongation (rare)

Contraindications:

• Hypersensitivity
• Caution in seizure disorders
• Concomitant use with MAOIs
Dose:
• Depression: Start with 20 mg/day orally, max up to 80 mg/day
• OCD: 20–60 mg/day
Dosage Forms:
• Capsules (10 mg, 20 mg, 40 mg)
• Tablets
• Oral solution

2. Escitalopram
Mechanism of Action:
Same
Indications:
• Major depressive disorder
• Generalized anxiety disorder
Adverse Effects:
• Nausea, insomnia, fatigue
• Sexual dysfunction
• Increased sweating
• Headache, dizziness
• Suicidal ideation (young patients)
• QT prolongation
Contraindications:
• Concomitant use with MAOIs
• QT prolongation
• Hypersensitivity
Dose:
• Depression/Anxiety: 10 mg/day orally; max: 20 mg/day
Dosage Forms:
• Tablets (5 mg, 10 mg, 20 mg)
• Oral solution
3. Paroxetine
Mechanism of Action:
Same
Indications:
• Major depressive disorder
• OCD
• Panic disorder
• Social anxiety disorder
• PTSD
• Generalized anxiety disorder
Adverse Effects:
• Sedation, sexual dysfunction
• Weight gain
• GI upset
• Withdrawal symptoms (due to short half-life)
• Hyponatremia
• Increased risk of bleeding
• Teratogenic (Category D – cardiac defects)
Contraindications:
• Use with MAOIs, thioridazine, pimozide
• Pregnancy (if avoidable)
• Hypersensitivity
Dose:
• Depression: 20 mg/day orally, max up to 50 mg/day
• Panic disorder: Start 10 mg/day, titrate
Dosage Forms:
• Tablets (10, 20, 30, 40 mg)
• Controlled-release tablets
• Oral suspension
4. Amitriptyline

Mechanism of Action:

• Amitriptyline blocks the reuptake of two key neurotransmitters in the CNS:

• Serotonin (5-HT)
• Norepinephrine (NE)

• By inhibiting the serotonin transporter (SERT) and norepinephrine transporter (NET) on presynaptic neurons, it increases the
levels of these neurotransmitters in the synaptic cleft.

• This enhances serotonergic and noradrenergic neurotransmission, which helps improve mood and relieve depression.

Indications:

• Depression
• Neuropathic pain
• Migraine prophylaxis
• Insomnia
• Fibromyalgia(A chronic disorder characterized by widespread musculoskeletal pain, fatigue, sleep disturbances, and cognitive
difficulties (sometimes called “fibro fog”).

Adverse Effects:

• Sedation (H1 blockade)

• Dry mouth, constipation, urinary retention, blurred vision (anticholinergic)
• Orthostatic hypotension (α1 blockade)
• Cardiotoxicity: arrhythmias (QT prolongation)
• Weight gain
• Seizures
• Suicidal thoughts
Contraindications:

• Recent MI
• Arrhythmias
• Glaucoma
• Urinary retention
• Concurrent MAOIs

Dose:

• Depression: 25–50 mg/day at bedtime; may increase to 150–300 mg/day

Dosage Forms:

• Tablets (10, 25, 50, 75, 100 mg)

• Injection (rarely used)

5. Lithium Salts

• Class: Mood stabilizer

Mechanism of Action:

Lithium works by inhibiting enzymes involved in cellular signaling (like inositol monophosphatase and GSK-3β), which reduces
overactive brain signaling. This stabilizes mood, protects brain cells, and balances neurotransmitters like serotonin and dopamine,
helping to prevent mania and depression.

Indications:
• Bipolar disorder (manic episodes and maintenance)
• Augmentation in treatment-resistant depression(reatment-resistant depression (TRD) means depression that does not improve
adequately after trying standard antidepressant treatments.)
Adverse Effects:

• Tremor
• Polyuria, polydipsia (nephrogenic diabetes insipidus)
• Hypothyroidism
• Weight gain
• GI distress
• Acne
• Teratogenic (Ebstein’s anomaly)
• Narrow therapeutic index → lithium toxicity: confusion, seizures, coma

Contraindications:

• Renal impairment
• Dehydration
• Sodium depletion
• Pregnancy (Category D)
• Concomitant use with diuretics, NSAIDs (↑ lithium levels)

Dose:

• Initial: 300 mg 2–3 times/day

• Maintenance: 900–1200 mg/day
• Therapeutic level: 0.6–1.2 mEq/L (requires blood monitoring)

Dosage Forms:

• Tablets (lithium carbonate – 300 mg)

• Extended-release tablets
• Oral solution (lithium citrate)
 Management of migraine headache
A headache is defined as pain or discomfort in the head, scalp, or neck. It is a common condition that can vary in intensity,
location, and duration.

A migraine headache is a type of neurological disorder characterized by recurrent, intense, and pulsating pain(pain matches the
pulses), usually on one side of the head, and often accompanied by nausea, vomiting, and sensitivity to light and sound.

Drugs used to treat migraine headaches fall into two main categories:

1. Acute (Abortive) Treatments.

a. Analgesics and NSAIDs

• Examples: Ibuprofen, Naproxen, Aspirin, Acetaminophen

• Use: For mild to moderate migraines

b. Triptans (Selective 5-HT_1B/1D receptor agonists)

• Examples: Sumatriptan, Rizatriptan, Zolmitriptan, Naratriptan

• Use: First-line treatment for moderate to severe migraine attacks

c. Ergot Alkaloids

• Examples: Ergotamine, Dihydroergotamine (DHE)

• Use: Alternative to triptans, often used in severe or prolonged attacks

d. Antiemetics

• Examples: Metoclopramide, Prochlorperazine

• Use: To control nausea and vomiting associated with migraines
e. Ditans

• Example: Lasmiditan
• Use: New class for acute treatment; useful when triptans are contraindicated

f. Gepants (CGRP receptor antagonists)

• Examples: Ubrogepant, Rimegepant

• Use: Acute treatment with fewer cardiovascular side effects than triptans

1. Ergometrine (also known as Ergonovine)

Mechanism of Action (MOA):

• Serotonin Receptor Agonism: Ergometrine acts as a non-selective agonist (activator) at various serotonin (5-HT) receptors,
particularly 5-HT1B and 5-HT1D receptors.

• Vasoconstriction: Activation of 5-HT1B receptors on intracranial blood vessels(Intracranial blood vessels are the blood vessels
located within the skull that supply the brain with oxygen and nutrients and remove waste products) leads to vasoconstriction
(narrowing of blood vessels). Migraine headaches are believed to involve the dilation of cranial arteriesthe arteries that supply
blood to the brain ), so this vasoconstrictive effect helps to reduce the throbbing pain.
• Neurogenic Inhibition: Activation of 5-HT1D receptors on sensory nerve terminals inhibits the release of vasoactive
neuropeptides (like CGRP (Calcitonin gene related peptide ) that contribute to pain and inflammation during a migraine attack.

• Alpha-Adrenergic Receptor Agonism: Ergometrine also has agonist activity at alpha-adrenergic receptors. This contributes to its
vasoconstrictive effects, though its alpha-adrenoceptor blocking property seen at higher doses is less relevant to therapeutic use in
migraine.
Indications:

• Prevention and treatment of postpartum hemorrhage (PPH)(Excessive bleading following the delivery)
• Management of uterine atony(uterus fails to contract effectively)
• Management of migraine headache

Dose & Dosage Form:

• Dose:
o IM/IV: 200 micrograms (0.2 mg) after delivery of the anterior shoulder or placenta
o Oral: 0.2–0.4 mg every 6–12 hours if needed (max duration: 1 week)
• Dosage Forms:
o Tablets (e.g., 0.2 mg)
o Ampoules for IM/IV injection (e.g., 0.5 mg/mL)

Adverse Effects:

• Nausea and vomiting

• Hypertension
• Chest pain (coronary vasospasm)
• Peripheral vasoconstriction
• Seizures (rare)

Contraindications:

• Hypertension
• Preeclampsia or eclampsia(Preeclampsia is a pregnancy-specific hypertensive disorder that typically occurs after 20 weeks of
gestation)
• Ischemic heart disease
• Peripheral vascular disease
• Hepatic or renal impairment
• Pregnancy (before delivery, can cause uterine rupture)
2. Sumatriptan
Mechanism of Action (MOA): SAME

Sumatriptan activates serotonin (5-HT₁B and 5-HT₁D receptors) on cranial blood vessels and sensory nerves of the trigeminal
system.
→ This causes:

• Vasoconstriction of dilated cranial blood vessels

• Inhibition of pro-inflammatory neuropeptides like CGRP(Calcitonin gene related peptide)
• Reduction in migraine pain and associated symptoms

Indications:

• Acute treatment of migraine attacks (with or without aura)

• Acute treatment of cluster headaches(recurrent severe headache on one side of head typically around the eye)

Not for prevention of migraines.

Dose & Dosage Form:

• Oral: 50–100 mg as a single dose; may repeat once after 2 hours (max: 200 mg/day)
• Subcutaneous (SC): 6 mg SC injection; may repeat after 1 hour (max: 12 mg/day)
• Nasal Spray: 5–20 mg; may repeat after 2 hours (max: 40 mg/day)
• Dosage Forms:
o Tablets (25 mg, 50 mg, 100 mg)
o Prefilled injection pens (6 mg)
o Nasal spray (5 mg, 20 mg)
 Adverse Effects:

• Tingling or numbness
• Chest pressure or tightness (non-cardiac in most cases)
• Flushing
• Dizziness or fatigue
• Injection site reactions (SC)
• Rare: Coronary vasospasm, myocardial infarction (MI)

Contraindications:

• Ischemic heart disease or coronary artery disease

• History of stroke or TIA
• Uncontrolled hypertension
• Hemiplegic or basilar migraine
• Use of ergotamines or other triptans within 24 hours
• Severe hepatic impairment

Indication, side effect, contraindication and dose of

1. Levodopa

• Indication:
Used in the treatment of Parkinson’s disease and Parkinsonism. Helps reduce tremors, rigidity, and bradykinesia.
• Parkinson’s Disease is a chronic and progressive neurological disorder characterized by the gradual loss of dopamine-producing nerve
cells in the brain, leading to symptoms such as tremors, muscle stiffness, slow movement, and impaired balance and coordination.
 • Mechanism of Action (MOA):
Levodopa is a precursor of dopamine. It crosses the blood-brain barrier and is then converted to dopamine in the brain,
compensating for the dopamine deficiency seen in Parkinson's disease.
• Side Effects:
o Nausea and vomiting
o Orthostatic hypotension- low blood pressure that happens when a person stands up from a sitting or lying position.
o Dyskinesia (involuntary movements)
o Hallucinations, confusion
o Motor fluctuations (Motor fluctuations refer to variations in a patient's movement control during the day)
• Contraindications:
o Narrow-angle glaucoma
o History of melanoma(skin cancer)
o Concurrent use of non-selective MAO inhibitors (can cause hypertensive crisis)
• Dose:
Usually given with carbidopa.. Commonly used in combination form (Sinemet) with 25 mg carbidopa + 100 mg levodopa, 3
times daily.
• TAB,cap,susp

2. Carbidopa

• Indication:
Always used with levodopa in Parkinson’s disease to enhance its effectiveness.
• MOA:
Carbidopa inhibits peripheral dopa decarboxylase, reducing the breakdown of levodopa outside the brain. This increases the
amount of levodopa that reaches the brain and reduces peripheral side effects like nausea.
• Side Effects:
o Nausea
o Orthostatic hypotension
o Headache
o Dyskinesia(abnormal involuntary movement)
 • Contraindications:
o Hypersensitivity
o Caution with asthma, cardiac disease
• Dose:
Commonly used in combination form (Sinemet) with 25 mg carbidopa + 100 mg levodopa, 3 times daily.
• Tab,cap,susp

3. Morphine

• Indication:
Moderate to severe acute or chronic pain, including pain from myocardial infarction, cancer, or trauma.

Pre-anaesthetic medication

• MOA:
Morphine is a mu-opioid receptor agonist. It binds to opioid receptors in the CNS, inhibiting the transmission of pain signals.
• Side Effects:
o Respiratory depression
o Constipation
o Sedation
o Nausea and vomiting
o Tolerance and dependence
• Contraindications:
o Severe respiratory depression
o Acute asthma
o Head trauma (increased intracranial pressure)
o Paralytic ileus
• Dose:
o Oral: 10–30 mg every 4 hours- tab, cap,
o IV: 2.5–10 mg every 2–4 hours (titrated to pain)
4. Pethidine (Meperidine)

• Indication:
Used for moderate to severe pain, especially short-term (e.g., during labor). Pre anaesthetic medication.
• MOA:
It is also a mu-opioid receptor agonist, It binds to opioid receptors in the CNS, inhibiting the transmission of pain signals.
similar to morphine, but with a shorter duration and different metabolite profile.
• Side Effects:
o Dizziness
o Respiratory depression
o Tremors or seizures (with repeated use, due to buildup of normeperidine)
o Nausea
o Seizure
o sedation
• Contraindications:
o Severe renal or hepatic impairment
o Use with MAO inhibitors (risk of serotonin syndrome)
o Epilepsy (due to neurotoxic metabolite)
• Dose:
o IM/SC/IV: 50–150 mg every 3–4 hours as needed . oral- 25-100 mg every 4-6 hr.
o Should not be used long-term
o Tab ,oral susp,iv ,im

5. Amphetamine

• Indication:
o ADHD (Attention Deficit Hyperactivity Disorder)( ADHD is a neurodevelopmental disorder that affects children and
often continues into adulthood. It is characterized by inattention, hyperactivity, and/or impulsivity that interfere with daily
functioning or development.)
o Narcolepsy(Narcolepsy is a chronic neurological sleep disorder that affects the brain’s ability to regulate the sleep-wake cycle
• MOA:
Increases release of norepinephrine and dopamine in the brain, and also inhibits their reuptake, leading to increased
alertness and focus.
 • Side Effects:
o Insomnia
o Loss of appetite
o Weight loss
o Hypertension, tachycardia
o Anxiety, dependence
• Contraindications:
o Cardiovascular disease
o Glaucoma
o Hyperthyroidism
o History of drug abuse
o Concurrent use of MAO inhibitors
• Dose:
o ADHD: Start with 5 mg once or twice daily, may increase to 20–30 mg/day in divided doses. Extended-release forms
are available. Tab, cap

6. Naloxone
• Indication:
Emergency treatment of opioid overdose, reversing respiratory depression caused by opioids.
• MOA:
Naloxone is a competitive opioid antagonist at mu, kappa, and delta receptors. It displaces opioids from receptors and blocks
their effects.
• Side Effects:
o Acute opioid withdrawal (agitation, pain, tachycardia)
o Nausea, vomiting
o Seizures (rare)
• Contraindications:
o None absolute in emergency; use caution in opioid-dependent individuals (risk of severe withdrawal)
•
• Dose:
o IV/IM/SC: 0.4 to 2 mg every 2–3 minutes as needed (max 10 mg)
o Nasal spray: 4 mg, may repeat after 2–3 minutes
 UNIT-5
Drugs used in cardiovascular system
ANTIHYPERTENSIVES
Hypertension (High Blood Pressure): Hypertension is a chronic medical condition in which the blood pressure in the
arteries is consistently elevated. Blood pressure is the force exerted by circulating blood on the walls of the body's arteries, the major
blood vessels in the body.

• Normal blood pressure: Below 120/80 mmHg

Antihypertensive Drugs: Antihypertensive drugs are medications used to lower high blood pressure and reduce
the risk of complications like stroke, heart attack, and kidney failure.

Classification of Antihypertensive Drugs

1. Diuretics

• Thiazide diuretics – e.g., Hydrochlorothiazide, Chlorthalidone

• Loop diuretics – e.g., Furosemide, Bumetanide
• Potassium-sparing diuretics – e.g., Spironolactone, Amiloride
• Osmotic diuretics -eg mannitol
• Carbonic anhydrase inhibitor- Acetazolamide, mehazolamide.

2. Sympatholytic (Anti-adrenergic) Drugs

a. Beta-blockers
• e.g., Atenolol, Metoprolol, Propranolol

b. Alpha-blockers

• e.g., Prazosin, Doxazosin

c. Centrally acting agents

• e.g., Clonidine, Methyldopa

d. Ganglion blockers (rarely used today)

• e.g., Trimethaphan

3. Renin-Angiotensin-Aldosterone System (RAAS) Inhibitors

a. ACE inhibitors (Angiotensin-Converting Enzyme inhibitors)

• e.g., Lisinopril, Enalapril , captopril,Ramipril

b. ARBs (Angiotensin II Receptor Blockers)

• e.g., Losartan, Valsartan ,telmisartan

c. Direct renin inhibitors

• e.g., Aliskiren

4. Calcium Channel Blockers (CCBs)

• e.g., Amlodipine, Nifedipine, Verapamil, Diltiazem

5. Vasodilators

• e.g., Hydralazine, Minoxidil

6. Aldosterone Antagonists (Mineralocorticoid Receptor Antagonists)

• e.g., Spironolactone, Eplerenone

 DIURETICS

Diuretics are a class of medications that promote the excretion of equivalent amount salt (sodium) and water from the body
through the kidneys. They increase urine output and are primarily used to:

• Treat hypertension (high blood pressure)

• Manage edema (fluid retention) in heart failure, kidney disease, and liver disease
• Treat certain electrolyte disturbances and metabolic disorders

1. Hydrochlorothiazide (HCTZ)
➤ Mechanism of Action:
• Inhibits the Na⁺/Cl⁻ transportor in the distal convoluted tubule of the nephron.
• This decreases sodium and chloride reabsorption → water follows sodium → increased diuresis.
➤ Indications:
• Primary hypertension (especially in elderly and Black patients)
• Mild to moderate edema (from CHF, liver cirrhosis, nephrotic syndrome)
• Prevention of calcium kidney stones (↓ calcium excretion)
• Nephrogenic diabetes insipidus (Nephrogenic Diabetes Insipidus (NDI) is a rare disorder characterized by the kidneys' inability to
concentrate urine, leading to excessive urination )
➤ Adverse Effects:
• Hypokalemia (low potassium), Hyponatremia (low sodium), Hyperuricemia (can trigger gout)
• Hyperglycemia
• Hyperlipidemia (↑ LDL and triglycerides)
• Erectile dysfunction
• Photosensitivity and rash (rare)
➤ Contraindications:
• Sulfonamide allergy
• Severe renal impairment
• Electrolyte imbalances (e.g., hypokalemia)
• Pregnancy Category B (use with caution)
➤ Dose & Dosage Forms:
• Adult dose: 12.5–50 mg once daily (typically 25 mg)
• Dosage forms: Tablets (12.5 mg, 25 mg, 50 mg)

2. Furosemide

➤ Mechanism of Action:

• Inhibits the Na⁺/K⁺/2Cl⁻ transporter in the thick ascending limb of the loop of Henle.
• This inhibits reabsorption of sodium, chloride, and potassium → profound diuresis.
• Also increases calcium and magnesium excretion.

➤ Indications:

• Acute pulmonary edema

• Congestive heart failure
• Renal and hepatic edema
• Hypertension (in patients with fluid overload or resistant cases)
• Hypercalcemia

➤ Adverse Effects:

• Hypokalemia, hypocalcemia, hypomagnesemia, Dehydration, hypotension

• Ototoxicity (hearing loss, especially with high IV doses)
• Hyperuricemia (risk of gout), Metabolic alkalosis

➤ Contraindications:

• Anuria (no urine production)

• Severe electrolyte disturbances
• Sulfa allergy, Pregnancy Category C
➤ Dose & Dosage Forms:

• Oral: 20–80 mg daily in divided doses

• IV/IM: 20–40 mg slow IV, may repeat in 2 hours
• Max IV dose: 600 mg/day
• Forms: Tablets (20 mg, 40 mg, 80 mg); Injection

3. Spironolactone
➤ Mechanism of Action:

• Competitively blocks aldosterone receptors in the distal tubules and collecting ducts.
• Prevents aldosterone-induced Na⁺ reabsorption and K⁺ excretion.
• Promotes mild diuresis while retaining potassium.

➤ Indications:

• Heart failure (improves survival in reduced ejection fraction)

• Primary hyperaldosteronism (Conn's syndrome)
• Resistant hypertension
• Ascites(abnormal accumulation of fluid within the peritoneal cavity) due to liver cirrhosis
• Polycystic ovarian syndrome (PCOS)
• Hirsutism, acne (in women)

➤ Adverse Effects:

• Hyperkalemia
• Gynecomastia (breast development in men)
• Menstrual irregularities
• Impotence(inability of a male to achieve or maintain an erection of the penis adequate for sexual intercourse)
• GI disturbances
➤ Contraindications:

• Hyperkalemia
• Addison's disease
• Severe renal impairment (CrCl <30 mL/min)
• Pregnancy Category C

➤ Dose & Dosage Forms:

• Edema/Heart failure: 25–100 mg/day (single or divided doses)

• Hyperaldosteronism: up to 400 mg/day (short-term test)
• Forms: Tablets (25 mg, 50 mg, 100 mg)

4. Acetazolamide
➤ Mechanism of Action:

• Inhibits carbonic anhydrase enzyme in the proximal tubule

• Reduces conversion of carbonic acid into bicarbonate and ↓ reabsorption of bicarbonate and sodium
• Causes alkaline urine and mild diuresis

➤ Indications:
• Glaucoma (↓ aqueous humor production)
• Altitude sickness (prevents/treats symptoms)
• Metabolic alkalosis
• Epilepsy (adjunctive therapy)
• Periodic paralysis
➤ Adverse Effects:

• Metabolic acidosis
• Hypokalemia
• Renal stone formation
• Paresthesia (tingling in hands/feet)
• Drowsiness, confusion
• Sulfa-related allergic reactions

➤ Contraindications:

• Sulfa allergy
• Severe hepatic or renal dysfunction
• Adrenal insufficiency
• Metabolic acidosis

➤ Dose & Dosage Forms:

• Adult oral dose: 250–1000 mg/day (in divided doses)

• For altitude sickness: 125–250 mg twice daily
• Forms: Tablets (250 mg); IV injection (500 mg vial)

ACE Inhibitors
An ACE inhibitor (Angiotensin-Converting Enzyme inhibitor) is a type of medication used primarily to treat high blood pressure
(hypertension) and heart failure. It works by blocking the action of the enzyme that converts angiotensin I into angiotensin II.
 MOA(common)

CAPTOPRIL

Indications:
• Hypertension
• Congestive heart failure
• Diabetic nephropathy(Diabetic nephropathy is a chronic kidney disease (CKD) caused by long-term diabetes mellitus)
• Post-myocardial infarction
Contraindications:
• History of angioedema related to previous ACE inhibitor use
• Pregnancy
• Bilateral renal artery stenosis(Bilateral renal artery stenosis is the narrowing of both renal arteries)
• Hypersensitivity to captopril
Side Effects:

• Dry cough (common to all ACE inhibitors)

• Hyperkalemia
• Angioedema(Angioedema is a sudden, localized swelling of the skin, mucosa, or submucosal tissues, affecting the face, lips, tongue,
throat, and sometimes the GI tract or genitals.)
• Rash
• Neutropenia (Neutropenia refers to an abnormally low number of neutrophils)
• Taste disturbances (metallic or loss of taste)

Dose & Dosage Form:

• Initial dose: 25 mg 2-3 times/day

• Maintenance dose: 25–150 mg/day in 2-3 divided doses
• Dosage Form: Oral tablets

ENALAPRIL

Indications:

• Hypertension
• Congestive heart failure
• left ventricular dysfunction

Contraindications:

• Angioedema associated with previous ACE inhibitor therapy

• Pregnancy
• Severe renal impairment without close monitoring
• Hypersensitivity to enalapril or other ACE inhibitors
Side Effects:

• Dry cough
• Hyperkalemia
• Dizziness, hypotension
• Angioedema
• Elevated serum creatinine
• Fatigue

Dose & Dosage Form:

• Initial dose for hypertension: 5 mg once daily

• Maintenance dose: 10–40 mg/day in 1–2 divided doses
• Heart failure: Start at 2.5 mg and titrate
• Dosage Form: Oral tablets, oral solution (some formulations)

RAMIPRIL

Indications:

• Hypertension
• Heart failure post-myocardial infarction
• Prevention of cardiovascular events in high-risk patients
• Diabetic nephropathy (off-label)

Contraindications:

• Angioedema with previous ACE inhibitor use

• Pregnancy
• Bilateral renal artery stenosis
• Severe hypotension
Side Effects:
• Cough
• Hyperkalemia
• Angioedema
• Hypotension
• Headache, fatigue
• Elevated blood urea nitrogen/creatinine
Dose & Dosage Form:
• Hypertension: Start at 2.5 mg once daily, can be increased to 5–10 mg/day
• Heart failure post-MI: Start 2.5 mg BID, target 5 mg BID
• Dosage Form: Oral capsules, tablets

ARBs (Angiotensin II Receptor Blockers)

ARBs (Angiotensin II Receptor Blockers) are a class of medications that block the action of angiotensin II at its receptor (AT1
receptor), leading to vasodilation, reduced aldosterone secretion, and decreased blood pressure.

MOA(common)
 LOSARTAN
Uses (Indications):

• Hypertension
• Diabetic nephropathy (especially in Type 2 diabetes)
• Heart failure (when ACE inhibitors not tolerated)
• Stroke risk reduction (in hypertensive patients with LVH)

Contraindications:

• Pregnancy (especially 2nd and 3rd trimesters)

• Severe hepatic impairment
• Bilateral renal artery stenosis
• Hypersensitivity to losartan
• Hyperkalemia

Adverse Effects:

Common Serious
Dizziness Angioedema
Fatigue Hypotension
Hyperkalemia Acute kidney injury
Back pain Liver dysfunction (rare)
Nasal congestion Rhabdomyolysis (rare)
 Dose & Dosage Form:

Indication Initial Dose Max Dose

Hypertension 50 mg once daily 100 mg/day
Diabetic nephropathy 50 mg once daily 100 mg/day
Stroke prevention 50 mg once daily 100 mg/day
Dosage Form:
• Oral tablets: 25 mg, 50 mg, 100 m

TELMISARTAN
Uses (Indications):
• Hypertension
• Cardiovascular risk reduction (e.g., in high-risk patients similar to those in the HOPE trial)
• Heart failure (off-label when ACE inhibitors not tolerated)
• Diabetic nephropathy (off-label)
Contraindications:
• Pregnancy
• Bilateral renal artery stenosis
• Severe hepatic impairment
• Hypersensitivity to telmisartan
• Hyperkalemia

Adverse Effects:

Common Serious
Dizziness Angioedema
Back pain Hypotension
Diarrhea Hyperkalemia
Sinus pain Acute renal failure
Fatigue Liver enzyme elevation
Dose & Dosage Form:

Indication Initial Dose Max Dose

Hypertension 40 mg once daily 80 mg once daily
CV risk reduction 80 mg once daily —

Dosage Form:

• Oral tablets: 20 mg, 40 mg, 80 mg

Calcium channel blockers

A calcium channel blocker (CCB) is a class of medication that inhibits the movement of calcium ions (Ca²⁺)
through L-type calcium channels in the cardiac and smooth muscle cells of the heart and blood vessels.
 1. Nifedipine
Uses
• Hypertension (high blood pressure)
• Angina pectoris (chest pain due to heart ischemia)
• Raynaud’s phenomenon (Raynaud’s phenomenon is a condition characterized by episodic vasospasm (narrowing) of the small
arteries and arterioles, primarily in the fingers and toes, leading to color changes, numbness, and pain in response to cold or
emotional stress.)
• Certain types of pulmonary hypertension (Pulmonary hypertension is a condition characterized by elevated blood pressure in the
pulmonary arteries, the vessels that carry blood from the right side of the heart to the lungs.)
Dosage and Dosage Forms:
• Immediate-release tablets: 10 mg, 20 mg (often used for angina or acute hypertension)
• Extended-release tablets/capsules: 30 mg, 60 mg, 90 mg (preferred for chronic hypertension and angina)
• Typical adult dose:
o Hypertension: 30-60 mg once daily (extended-release)
o Angina: 10-20 mg three times daily (immediate-release)
Adverse Effects:
• Headache
• Flushing(Flushing is a sudden, temporary redness of the skin, usually over the face, neck, or upper chest)
• Peripheral edema (swelling of ankles/feet)
• Dizziness
• Palpitations/tachycardia (reflex increase in heart rate)
• Hypotension
• Gingival hyperplasia (gum overgrowth)
• Rare: severe hypotension, myocardial ischemia (if abrupt withdrawal)
Contraindications:
• Known hypersensitivity to nifedipine or other dihydropyridines
• Cardiogenic shock
• Unstable angina or acute myocardial infarction (caution with immediate-release form)
• Severe hypotension
2. Amlodipine
Uses:

• Hypertension
• Angina pectoris

Dosage and Dosage Forms:

• Tablets: 2.5 mg, 5 mg, 10 mg

• Usual starting dose for adults: 5 mg once daily
• Maintenance dose: 5-10 mg once daily
• Dose adjustment depending on blood pressure response.

Adverse Effects:

• Peripheral edema (most common)

• Flushing
• Palpitations
• Dizziness
• Fatigue
• Headache
• Nausea
• Rare: hypotension, hepatic enzyme elevation

Contraindications:

• Known hypersensitivity to amlodipine

• Severe hypotension
• Cardiogenic shock
 Beta Adrenergic blockers

A beta-adrenergic blocker is a class of medication that blocks the beta-adrenergic receptors in the body, particularly beta-1
and beta-2 receptors, which respond to the hormones epinephrine (adrenaline) and norepinephrine.

MOA common

1. Decrease cardiac output

• Beta blockers reduce heart rate (negative chronotropic effect) and force of contraction (negative inotropic effect) by
blocking beta-1 receptors in the heart.
• This leads to a reduced cardiac output, which lowers blood pressure.

2. Suppress renin release

• Beta-1 receptors are present on juxtaglomerular cells in the kidney.

• Blocking these receptors decreases renin secretion, reducing activation of the renin-angiotensin-aldosterone system
(RAAS).
• This causes less angiotensin II production, leading to vasodilation and decreased aldosterone-mediated sodium and water
retention, both of which reduce blood volume and pressure.

1. Propranolol
Uses:

• Hypertension
• Angina pectoris
• Arrhythmias (e.g., atrial fibrillation)
• Migraine prophylaxis
• Essential tremor
• Thyrotoxicosis (to control symptoms)
• Post-myocardial infarction (secondary prevention)
Dosage and Dosage Forms:

• Tablets: 10 mg, 40 mg, 80 mg

• Extended-release capsules: 60 mg, 80 mg, 120 mg, 160 mg
• Typical dose:
o Hypertension: 40 mg twice daily, may increase up to 320 mg/day
o Angina: 80-320 mg/day in divided doses
• Dose adjusted based on clinical response

Adverse Effects:

• Bradycardia
• Fatigue
• Hypotension
• Bronchospasm (due to β2 blockade)
• Cold extremities
• Depression
• Sleep disturbances (vivid dreams)
• Sexual dysfunction
• Hypoglycemia masking (in diabetics)
• Withdrawal symptoms if abruptly stopped

Contraindications:

• Asthma or reactive airway disease

• Severe bradycardia or heart block (second- or third-degree AV block)
• Cardiogenic shock
• Severe peripheral arterial disease
• Untreated heart failure
2. Atenolol
Uses:
• Hypertension
• Angina pectoris
• Post-myocardial infarction
• Certain arrhythmias
Dosage and Dosage Forms:

• Tablets: 25 mg, 50 mg, 100 mg

• Typical dose:
o Hypertension: 50-100 mg once daily
o Angina: 50-100 mg once daily
• Dose adjusted based on clinical response
•
Adverse Effects:
• Bradycardia
• Fatigue
• Hypotension
• Cold extremities
• Dizziness
• Depression (less common than propranolol)
• May mask hypoglycemia symptoms in diabetics
• Less bronchospasm risk than propranolol but still possible at higher doses
•
Contraindications:
• bradycardia(
• Heart block (2nd or 3rd degree)
• Cardiogenic shock
• Severe peripheral arterial disease
3. Metoprolol
Uses:
• Hypertension
• Angina pectoris
• Heart failure (metoprolol succinate)
• Post-myocardial infarction
• Certain arrhythmias
Dosage and Dosage Forms:
• Metoprolol tartrate (immediate-release) tablets: 25 mg, 50 mg, 100 mg
• Metoprolol succinate (extended-release) tablets: 25 mg, 50 mg, 100 mg, 200 mg
• Typical dose:
o Hypertension: 50-100 mg daily (up to 200 mg/day)
o Angina: 100-200 mg/day in divided doses
• Dose adjusted based on clinical response
Adverse Effects:
• Bradycardia
• Fatigue
• Hypotension
• Dizziness
• Depression
• Cold extremities
• Masking of hypoglycemia symptoms
• Rarely, worsening of heart failure if not properly managed
Contraindications:
• Severe bradycardia
• Heart block (2nd or 3rd degree)
• Cardiogenic shock
• Severe peripheral arterial disease
Antianginal drugs
Angina pectoris, often simply called angina, is a type of chest pain or discomfort that occurs when a part of the heart muscle doesn't
receive enough oxygen-rich blood. It's not a heart attack itself, but it's a common symptom of underlying heart disease, most
frequently coronary artery disease (CAD).
Antianginal Drugs:
Antianginal drugs are medications used to relieve or prevent angina pectoris by improving blood flow to the heart or
reducing the heart’s oxygen demand.

Classification of Antianginal Drugs

1. Nitrates
Nitroglycerin, Isosorbide dinitrate, Isosorbide mononitrate
2. Beta-Adrenergic Blockers
Propranolol, Atenolol, Metoprolol
3. Calcium Channel Blockers (Non-dihydropyridines)
Verapamil, Diltiazem

1.Nitroglycerin

1. Mechanism of Action (MOA):

Nitroglycerin is an organic nitrate that acts as a prodrug. It is converted to nitric oxide (NO) in the vascular smooth muscle, which:
• Activates guanylate cyclase enzyme.
• Which Increases cyclic GMP (cGMP) (Cyclic Guanosine Monophosphate)- cGMP is a secondary messenger molecule involved in
many cellular signaling
• Causes dephosphorylation of myosin light chains(Myosin is a motor protein involved in muscle contraction)
Dephosphorylation means removel of phosphate from myosin
• Leads to vascular smooth muscle relaxation (vasodilation)
Effects:

• Venodilation → ↓ Preload → ↓ Myocardial oxygen demand

• Coronary vasodilation → ↑ Myocardial oxygen supply (especially in vasospastic angina)
2. Indications:

• Angina pectoris (acute attack and prophylaxis)

• Heart failure (especially in acute decompensated cases)
• Hypertensive emergencies
• Myocardial infarction (as adjunct therapy)
• Perioperative hypertension

3. Adverse Effects:

• Headache (most common, due to cerebral vasodilation)

• Hypotension
• Dizziness
• tachycardia
• Flushing(Flushing is a sudden redness, warmth, or feeling of heat in the skin, usually noticeable on the face, neck, or
chest. It is caused by dilation of blood vessels (vasodilation) in the skin.)
• Nausea

4. Contraindications:

• Severe hypotension
• Hypovolemia
• Increased intracranial pressure (ICP)( refers to the pressure inside the skul)
• Severe anemia
• Use of phosphodiesterase-5 inhibitors (e.g., sildenafil, tadalafil) within 24–48 hours → risk of severe hypotension

5. Dose and Dosage Forms:

• Sublingual Tablets: Typically 0.3mg, 0.4mg, or 0.6mg. Placed under the tongue; can be repeated every 5 mins for up to 3
doses in 15 mins.
• Translingual Spray: 0.4mg/spray. Sprayed onto or under the tongue; similar dosing to sublingual tablets.
• Sublingual Powder: 0.4mg or 0.8mg per packet. Placed under the tongue; similar dosing to sublingual tablets.
• Long-acting (for chronic prevention):

• Transdermal Patch: Delivers 0.1mg/hr to 0.8mg/hr. Applied to skin once daily, with a 10-12 hour "nitrate-free" interval to
prevent tolerance.
• Transdermal Ointment: 2% strength. Applied to skin, usually 2-3 times daily, also requiring a nitrate-free interval.
• Oral Extended-Release Capsules/Tablets: 2.5mg, 6.5mg, or 9mg. Taken orally, typically 2-4 times daily, often with a drug-
free period.

Cardiac glycosides
Cardiac glycosides are a class of naturally occurring drugs used to increase the force of contraction of the heart
(positive inotropic effect).They are primarily used in the treatment of heart failure and certain types of arrhythmias
(especially atrial fibril

Digoxin
1. Mechanism of Action (MOA):

1. Inhibits Na⁺/K⁺-ATPase
2. ↑ Intracellular Na⁺
3. ↓ Activity of Na⁺/Ca²⁺ exchanger
4. ↑ Intracellular Ca²⁺
5. ↑ Ca²⁺ stored in sarcoplasmic reticulum
6. ↑ Myocardial contractility (positive inotropy)
2. Uses / Indications:
• Congestive Heart Failure (CHF)
• Atrial fibrillation (Atrial fibrillation is an irregular and often rapid heart rhythm (arrhythmia) that originates in the atria (upper
chambers of the heart).)
• Atrial flutter (Atrial flutter is a rapid but regular atrial rhythm)
 3. Adverse Effects:
GI Nausea, vomiting, anorexia
CNS Confusion, dizziness, visual disturbances (yellow vision, "halos")
Cardiac Arrhythmias (e.g., AV block, ventricular tachycardia, bradycardia)
Others Fatigue, weakness, gynecomastia (rare)

4. Contraindications:

• Ventricular fibrillation
• Hypokalemia (↑ risk of toxicity)
• Advanced AV block without pacemaker
• Renal failure (↓ clearance → ↑ toxicity)
• Acute myocardial infarction (caution)

5. Dose and Dosage Forms:

a. Tablets

• Strengths: 0.125 mg, 0.25 mg

b. Oral Solution / Elixir

• Concentration: 0.05 mg/mL (or 50 mcg/mL)

2. Parenteral (Injectable) Form

a. Intravenous (IV) Injection

• Concentration: 0.25 mg/mL-0.5mg/ml

DIGITALIZATION

Digitalization is the process of administering loading doses of digoxin to rapidly achieve therapeutic drug levels
in the body, especially in cases like atrial fibrillation or heart failure.

Steps in the Process of Digitalization:

1. Patient Evaluation
o Assess renal function, electrolyte levels (especially potassium and magnesium), and heart rate.
o digoxin hypersensitivity.
2. Calculate the Loading Dose
o Total digitalizing dose is typically 0.75 to 1.5 mg (adults), given in divided doses.
o Dose depends on age, weight, renal function, and clinical urgency.
3. Administer Digoxin in Divided Doses
o Example:
▪ 0.5 mg initially
▪ 0.25 mg after 6 hours
▪ 0.25 mg after another 6 hours
o Observe for clinical response and signs of toxicity.
4. Monitoring
o Watch for improvement in heart rate or rhythm.
o Monitor for signs of digoxin toxicity:
▪ Nausea, vomiting
▪ Visual disturbances (yellow vision)
▪ Bradycardia or arrhythmias
5. Maintenance Therapy
o Once therapeutic levels are reached, switch to a maintenance dose (e.g., 0.125–0.25 mg/day in adults).
o Monitor serum digoxin levels regularly.
 Digitalis Toxicity (Digoxin Toxicity)

Digitalis toxicity refers to the harmful effects caused by excessive levels of digoxin, a cardiac glycoside commonly used to treat heart
failure and atrial fibrillation.

Signs and Symptoms of Digitalis Toxicity:

1. Gastrointestinal (early signs):

• Nausea
• Vomiting
• Diarrhea
• Abdominal pain
2. Visual Disturbances (classic sign):
• Blurred vision
• Xanthopsia (yellow-green vision or "halos" around lights)
3. Neurological:
• Confusion
• Dizziness
• Weakness
• Fatigue
4. Cardiac (most dangerous):
• Bradycardia
• Heart blocks (especially AV block)
• Arrhythmias:

Lipid-Lowering Agents

Definition:

Lipid-lowering agents (also called antihyperlipidemic agents) are drugs used to reduce blood lipid levels, particularly cholesterol
and triglycerides, to prevent cardiovascular diseases such as atherosclerosis, heart attacks, and strokes.
CLASSIFICATION

1. HMG-CoA Reductase Inhibitors (Statins)

• Atorvastatin, Simvastatin, Rosuvastatin, Pravastatin, Lovastatin

2. Fibrates (Fibric Acid Derivatives)

• Fenofibrate, Gemfibrozil, Bezafibrate

3. Bile Acid Sequestrants (Resins)

• Cholestyramine, Colestipol, Colesevelam

5. Cholesterol Absorption Inhibitors

• Ezetimibe

1. Atorvastatin (Statin Class)

Mechanism of Action (MOA):
• Inhibits HMG-CoA reductase, which is involve in cholesterol biosynthesis. So, decrease in blood cholesterol.
• Increases LDL receptors on liver cells → ↑ LDL uptake by receptor. which leads to clearance of LDL → ↓ blood LDL

Uses:

• Hypercholesterolemia (high LDL)

• Mixed dyslipidemia (elevated levels of multiple lipid fractions in the blood)
• Cardiovascular risk reduction
 Dose and Dosage Form:

• Dose: 10–80 mg once daily, orally

• Forms: Tablets (10 mg, 20 mg, 40 mg, 80 mg)

Adverse Effects:

• Liver enzyme elevation (↑ ALT, AST)

• Headache
• GI upset (nausea, constipation)
• Rare: memory issues, new-onset diabetes
• • Myopathy: Muscle weakness or pain caused by muscle damage.
• • Rhabdomyolysis: Severe muscle breakdown releasing muscle contents into the blood, which can damage kidneys.

Contraindications:

• Active liver disease

• Pregnancy and lactation
• Hypersensitivity to atorvastatin

2. Fenofibrate (Fibrate Class)

Mechanism of Action (MOA):

• Fenofibrate is a fibrate class drug that works by activating Peroxisome Proliferator-Activated Receptor-alpha (PPAR-α), a
nuclear receptor.

• Activation of PPAR-α leads to:

• ↑ Lipoprotein lipase synthesis → increased breakdown of triglyceride-rich lipoproteins (like VLDL).

• ↑ Fatty acid oxidation in liver and muscle.
• ↓ production of apolipoprotein C-III (an inhibitor of lipoprotein lipase), enhancing triglyceride clearance.
• increases HDL cholesterol.(Beneficial bcz it remove excess cholesterol)

Uses:

• Hypertriglyceridemia
• Mixed dyslipidemia(Mixed dyslipidemia is a lipid disorder characterized by elevated levels of: LDL ,Triglycerides (TGs),Low
HDL cholesterol (good cholesterol)
• Prevention of pancreatitis due to very high triglycerides (>500 mg/dL)

Dose and Dosage Form:

• Dose: 145 mg once daily (or lower based on renal function)

• Forms: Tablets (54 mg, 67 mg, 145 mg) and capsules

Adverse Effects:

• GI discomfort (nausea, abdominal pain)

• Gall stones
• Myopathy
• Liver enzyme elevation

Contraindications:

• Severe renal or hepatic dysfunction

• Gallbladder disease
• Breastfeeding
• Known hypersensitivity
•
 Indication, Side effect, Contraindication and dose of
1. Labetalol

• MOA: Non-selective β-blocker + α1-blocker → ↓ HR and vasodilation → ↓ BP

• Indications: Hypertension, hypertensive emergencies, pregnancy-induced hypertension
• Side Effects: hypotension, bradycardia, dizziness, fatigue, bronchospasm
• Contraindications: Asthma, severe bradycardia, heart block
• Dose: Oral 100 mg BID (up to 2400 mg/day), IV 20 mg bolus
• Dosage Form: Tablets, Injectable solution (IV)

2. Prazosin

• MOA: Selective α1-adrenergic antagonist → vasodilation → ↓ peripheral resistance

• Indications: Hypertension, BPH(Benign Prostatic Hyperplasia)
• Side Effects: hypotension, dizziness, headache, nasal congestion,drowsiness,nausea
• Contraindications: Hypersensitivity
• Dose: Oral 1 mg BID, titrate up to 20 mg/day
• Dosage Form: Tablets

3. Phentolamine
• MOA: Non-selective α-blocker → vasodilation
• Indications: hypertensive crisis(A sudden, severe elevation in blood pressure), Prevention and treatment of extravasation of
vasoconstrictors(Extravasation vasoconstriction refers to the tissue damage caused when a vasoconstrictor drug leaks (extravasates)
from a blood vessel into surrounding tissues, leading to intense narrowing of blood vessels in that area.)
• Side Effects: Tachycardia, arrhythmias, hypotension,tachycardia,dizziness, headache
• Contraindications: CAD(coronary artery disease), MI
• Dose: IV 5 mg bolus, repeat as needed
• Dosage Form: Injectable solution (IV)
4. Methyldopa

• MOA: Central α2 agonist → ↓ sympathetic outflow → ↓ BP

• Indications: Hypertension (especially pregnancy)
• Side Effects: Sedation, dry mouth, hemolytic anemia, hepatotoxicity, Drawsiness
• Contraindications: Active liver disease
• Dose: Oral 250 mg 2-3 times/day, max 3 g/day
• Dosage Form: Tablets, Injection

5. Mannitol

• MOA: Osmotic diuretic → ↑ plasma osmolality → draws water from tissues → diuresis
• Indications: Cerebral edema, increased intraocular pressure, acute renal failure
• Side Effects: Electrolyte imbalance, dehydration,headache , nausea ,vomiting, pulmonary edema(ccumulation of excess fluid
in the lungs’ alveoli and interstitial spaces, leading to impaired gas exchange and difficulty breathing.)
• Contraindications: Anuria(Anuria is the failure of the kidneys to produce urine), severe dehydration, pulmonary edema,
• Dose: IV 0.25–2 g/kg over 30–60 min
• Dosage Form: Injectable solution (IV)

6. Vasopressin

• MOA: Vasopressin binds to V1 receptors causing vasoconstriction — this increases peripheral vascular resistance and raises blood
pressure.
• Vasopressin binds to V2 receptors in the kidneys, promoting insertion of aquaporin-2 channels into the collecting duct membrane,
which increases water reabsorption → concentrates urine and reduces urine volume.
• Indications: Diabetes insipidus(A condition characterized by excessive urination (polyuria) and intense thirst (polydipsia) due to
inability to concentrate urine.), vasodilatory shock, cardiac arrest
• Side Effects: Hypertension, bradycardia, arrhythmias, abdominal cramps,tremor
• Contraindications: CAD, chronic nephritis (caution)
• Dose: IV infusion 0.01–0.04 units/min (shock), IM/SC 0.4–4 units (DI)
• Dosage Form: Injectable solution

7. Aspirin
 • MOA: Irreversible COX-1 inhibitor → ↓ thromboxane A2 → ↓ platelet aggregation
• Indications: MI, stroke prevention, angina, anti-inflammatory, analgesic
• Side Effects: GI bleeding, gastric irritation, gastric ulcer, nausea, heartburn,bronchospasm, tinnitus,
• Contraindications: Peptic ulcer, bleeding disorders, children with viral illness
• Dose: 75–325 mg daily (cardioprotection), up to 650 mg every 4–6 h (analgesic)
• Dosage Form: Tablets, chewable tablets, enteric-coated tablets

8. Clopidogrel

• MOA: Clopidogrel is an antiplatelet agent that:

• Irreversibly inhibits the P2Y12 ADP receptor on platelet surfaces
• This prevents ADP-mediated activation of the glycoprotein IIb/IIIa complex
• Result: Inhibition of platelet aggregation, reducing clot formation
• Indications: Prevention of thrombotic events in CAD, stroke, PAD(pulmonary artery disease)
• Side Effects: Bleeding, GI upset, rash, diarrhea, rarely TTP(Thrombotic Thrombocytopenic Purpura )
• Contraindications: Active bleeding
• Dose: 75 mg once daily
• Dosage Form: Tablets

9. Heparin

• MOA: Activates antithrombin III → inhibits thrombin and factor Xa → anticoagulation

• Indications: Deep Vein Thrombosis (DVT) and Pulmonary Embolism (A blockage in one of the pulmonary arteries in the lungs), acute
coronary syndrome(A spectrum of conditions caused by sudden reduction of blood flow to the heart muscle due to coronary
artery blockage, leading to myocardial ischemia or infarction.), prophylaxis of thromboembolism
• Side Effects: Bleeding, osteoporosis (long-term), pain redness and swelling at inj site, hyperkelemia.
• Contraindications: Active bleeding, severe thrombocytopenia
• Dose: IV bolus 5,000 units, infusion 20,000–40,000 units/day; SC prophylaxis 5,000 units every 8–12 h
• Dosage Form: Injectable solution (IV, SC)
10. Warfarin

• MOA: Vitamin K antagonist → inhibits synthesis of clotting factors II, VII, IX, X

Indications:
1.Thrombosis
Formation of a blood clot (thrombus) inside a blood vessel, which obstructs blood flow.
2.Embolism
A travelling clot or debris (embolus) that moves through the bloodstream and blocks a vessel elsewhere..

3.Atrial Fibrillation (AF)

An irregular and often rapid heartbeat caused by chaotic electrical signals in the atria (upper chambers of the heart).

• Side Effects: Bleeding, skin necrosis, teratogenic effect.

• Contraindications: Pregnancy, active bleeding
• Dose: 2–10 mg daily, adjusted by INR (target 2–3)
• Dosage Form: Tablets

11. Vitamin K

• MOA: Cofactor for γ-carboxylation of clotting factors II, VII, IX, X → promotes clotting
• Indications: Warfarin overdose, vitamin K deficiency, hemorrhagic disease of newborn
• Side Effects: Hypersensitivity (rare), flushing (IV), taste changes , inj site reaction
• Contraindications: Hypersensitivity
• Dose: Oral 2.5–10 mg; IV slow 1–10 mg in emergencies
• Dosage Form: Oral tablets, Injectable solution
 UNIT-6
Drug acting on respiratory system
1. Cough
A cough is a protective reflex action that clears the airways of mucus, irritants, foreign particles, or microbes. It can be acute (short-
term) or chronic (long-term), and may be productive (with mucus) or dry (without mucus).

2. Demulcents
Demulcents are soothing agents, usually mucilaginous substances, that relieve irritation in the mucous membranes by forming a
protective film.
Example: Honey, glycerin, and syrup of licorice.

3. Expectorants
Expectorants are drugs that help clear mucus and secretions from the respiratory tract by increasing the volume or decreasing the
viscosity of bronchial secretions.
Example: Guaifenesin, ammonium chloride.

4. Antitussives
Antitussives are cough suppressants used to relieve dry, irritating coughs by acting on the cough center in the brain or local mucosal
receptors.
Example: Codeine, dextromethorphan.

5. Bronchodilators
Bronchodilators are medications that relax and widen the bronchial airways, making it easier to breathe. They are commonly used in
conditions like asthma and COPD. Example: Salbutamol, theophylline.

6. Asthma
Asthma is a chronic inflammatory disease of the airways characterized by reversible airflow obstruction, bronchospasm, and
symptoms like wheezing, shortness of breath, and coughing.

7. COPD (Chronic Obstructive Pulmonary Disease)

COPD is a progressive, non-reversible lung disease that causes airflow limitation due to chronic bronchitis. It is commonly caused by
long-term smoking or exposure to harmful particles.
Classifications
1.Expectorants

a) Secretomotor Expectorants (Stimulate respiratory secretions):

• Guaifenesin
• Potassium iodide
• Ammonium chloride
• Sodium citrate
b) Mucolytic Expectorants (Break mucus structure):
• Bromhexine
• Ambroxol
• Acetylcysteine
• Carbocisteine
•
2. Antitussives (Cough Suppressants)

A. Central Acting:
a) Narcotic (Opioid):
• Codeine
• Pholcodine
• Morphine (severe cases)
b) Non-narcotic (Non-opioid):
• Dextromethorphan
• Noscapine
• Butamirate
B. Peripheral Acting:
• Benzonatate
• Levodropropizine
• Menthol (local soothing)
 3. Drugs Used in Asthma and COPD

A. Bronchodilators
a) β2-Agonists:
• Short-acting (SABA): Salbutamol, Terbutaline
• Long-acting (LABA): Salmeterol, Formoterol
b) Anticholinergics:
• Short-acting: Ipratropium
• Long-acting: Tiotropium, Aclidinium
c) Methylxanthines:
• Theophylline
• Aminophylline
B. Anti-inflammatory Drugs
a) Corticosteroids:
• Inhaled: Beclomethasone, Budesonide, Fluticasone
• Oral: Prednisolone
b) Leukotriene receptor antagonists (LTRA):
• Montelukast
• Zafirlukast
c) Mast cell stabilizers: (Mainly for asthma)
• Cromolyn sodium
• Nedocromil
C. Biologics (Severe Asthma)
• Omalizumab (anti-IgE), Mepolizumab
• Mepolizumab (anti-IL-5)

4.Antihistaminics
Antihistaminics are drugs that block or inhibit the effects of histamine, a chemical involved in allergic reactions, inflammation,
gastric acid secretion, and neurotransmission. They are mainly classified based on the type of histamine receptor they act on.
A. H1 Antihistamines
➡ Block H1 receptors; used for allergy, motion sickness, cold, etc.
i. First-generation H1-antihistamines

(cause sedation, cross the blood-brain barrier)

• Diphenhydramine
• Chlorpheniramine
• Hydroxyzine
• Promethazine
• Dimenhydrinate
• Meclizine
• Clemastine
• ketotifen

ii. Second-generation H1-antihistamines

• Loratadine
• Cetirizine
• Levocetirizine
• Fexofenadine
• Desloratadine
• Mizolastine

B. H2 Antihistamines

➡ Block H2 receptors in the stomach; used to reduce gastric acid secretion.

• Ranitidine (withdrawn in many countries)

• Famotidine
• Cimetidine
• Nizatidine
5.nasal decongestants
Nasal decongestants are drugs used to relieve nasal congestion (blocked nose) by reducing swelling and inflammation of the nasal
mucosa, primarily through vasoconstriction.

They are commonly used in common cold, allergic rhinitis, sinusitis, and upper respiratory tract infections.

Classification

A. Topical Nasal Decongestants (Nasal Drops/Sprays)

• Oxymetazoline, Xylometazoline, Phenylephrine, Naphazoline, Tetrahydrozoline

B. Systemic Nasal Decongestants (Oral)➡ Work throughout the body; used when longer action or broader effect is needed.

• Pseudoephedrine, Phenylephrine, Ephedrine

Bronchodilators
1. Salbutamol (Albuterol) (CAMP-Cyclic adenosyl monophosphate)

• MOA:
• Adverse Effects: Tremors, tachycardia, headache, hypokalemia, nervousness.
 • Contraindications: Hypersensitivity to salbutamol, caution in cardiac arrhythmias,insomnia
• Uses: Acute asthma, bronchospasm, COPD (rescue inhaler).
• Dose & Dosage Forms:
o Inhalation: 100 mcg/puff MDI (1–2 puffs every 4–6 hrs)
o Nebulizer solution: 2.5 mg via nebulizer every 4–6 hrs
o Oral: 2–4 mg 3–4 times daily

2. Terbutaline

• MOA; same
• Adverse Effects: Tremor, nervousness, tachycardia, palpitations, nausea,headache
• Contraindications: Hypersensitivity; use caution in hyperthyroidism, diabetes, or cardiovascular disorders.
• Uses: Asthma, bronchospasm, COPD
• Dose & Dosage Forms:
o Oral: 2.5–5 mg three times daily
o Injection: 0.25 mg SC every 20 mins up to 3 doses
o Nebulizer: 2.5–5 mg every 4–6 hour

3. Salmeterol

• MOA: same
• Adverse Effects: Headache, dizziness, palpitations, paradoxical bronchospasm.( A paradoxical bronchospasm is an unexpected
and opposite reaction to a bronchodilator medication, where instead of relaxing the airway muscles and opening the airways, the drug
causes worsening bronchoconstriction leading to increased airway narrowing.)
• Contraindications: Monotherapy in acute asthma( Salmeterol + Fluticasone (e.g., Advair, Seretide), Salmeterol + Budesonide)
• hypersensitivity.
• Uses: Maintenance treatment of asthma, COPD, prevention of exercise-induced bronchospasm.
• Dose & Dosage Forms:
o Inhalation (DPI/MDI): 50 mcg twice daily
o Always used with inhaled corticosteroids in asthma
4. Theophylline

• MOA:1. theophylline→PDE(phosphodiesterase enzyme) inhibition → ↑ cAMP → bronchodilation

2.Theophylline→Adenosine receptor blockade → ↓ bronchoconstriction
• Adverse Effects: Nausea, vomiting, insomnia, arrhythmias, seizures , headache
• Contraindications: Hypersensitivity; caution in seizure disorders, cardiac arrhythmias, liver disease.
• Uses: Chronic asthma, COPD (less preferred now).
• Dose & Dosage Forms:
o Oral (sustained-release): 300–600 mg/day in divided doses
o IV: Loading dose 5 mg/kg, then maintenance dose adjusted to therapeutic levels (10–20 mcg/mL)

5. Ipratropium Bromide

• MOAipratropium bromide→ inhibits M3 receptors in bronchial smooth muscle → bronchodilation.

• Adverse Effects: Dry mouth, cough, dizziness, blurred vision (if sprayed in eyes)., Headache, nausea
• Contraindications: Hypersensitivity to ipratropium or atropine derivatives.
• Uses: COPD (main use), asthma (adjunct), rhinorrhea.
• Dose & Dosage Forms:
o Inhalation (MDI): 20 mcg/puff, 2 puffs 3–4 times daily
o Nebulizer: 250–500 mcg every 6–8 hours

Leukotriene Antagonist
Leukotriene antagonists are drugs that block leukotriene receptors (especially CysLT1), preventing the action of leukotrienes —
inflammatory mediators involved in conditions like asthma and allergic rhinitis.
1. Montelukast

Mechanism of Action (MOA)

Montelukast selectively blocks cysteinyl leukotriene receptor type 1 (CysLT1) in the lungs and bronchial tubes, reducing:
Bronchoconstriction, Inflammation, Edema, Mucus secretionThis action helps in asthma control and alleviates allergic rhinitis
symptoms.

4. Adverse Drug Reactions (ADR)

• Headache
• Abdominal pain
• Fatigue
• agitation, anxiety, depression, suicidal thoughts
• Elevated liver enzymes
5. Contraindications
• Hypersensitivity to Montelukast or any component of the formulation
• Caution in patients with psychiatric disorders

6. Indications

• Asthma (prophylaxis and chronic treatment)

• Exercise-induced bronchoconstriction
• Allergic rhinitis (seasonal/perennial)
• Aspirin-sensitive asthma

7. Dose and Dosage Form

Adults:: 10 mg once daily (usually in the evening)
Child:5mg once daily
Dosage Forms:
• Tablets: 10 mg
• Chewable tablets: 4 mg, 5 mg
• Oral granules: 4 mg per packet
Antitussives

1. CODEINE
Mechanism of Action:
• Codeine is a weak opioid agonist.
• It binds to mu-opioid receptors in the brain, reducing the cough reflex in the cough center of the medulla.
• It is also metabolized into morphine, contributing to its analgesic and sedative effects
Adverse Effects (ADR):
• Common:
o Drowsiness, Dizziness
o Constipation
o Nausea/vomiting
o Respiratory depression (especially in children)
o Dependence and tolerance
o Hypotension, Allergic reactions
Contraindications:
• Respiratory depression
• Acute asthma attacks
• Children <12 years (due to risk of respiratory depression)
• Known hypersensitivity to codeine
Indications:
• Dry (non-productive) cough
• Mild to moderate pain
• Diarrhea (less common use)
Dose and Dosage Form:
Adults:
• 10–20 mg orally every 4–6 hours (max 120 mg/day) for cough
Dosage Forms:
• Tablets: 15 mg, 30 mg, 60 mg
• Syrup (as a combination with guaifenesin or other agents)
• Capsules
 2. DEXTROMETHORPHAN
Mechanism of Action:

• Acts on the medullary cough center in the brainstem.

• Inhibits the cough reflex pathway, reducing the urge to cough.
• Non-opioid, but structurally related to codeine.
Adverse Effects (ADR):
• Common:
o Drowsiness
o Dizziness
o GI upset
o Euphoria (A feeling of intense happiness)
o Hallucinations(a person sees, hears, feels, smells, or tastes something that isn't actually there.)
o Dissociation (A state where a person feels detached from their body)
Contraindications:
• Concurrent use with MAO inhibitors or within 14 days of stopping them
• Known hypersensitivity
• Children <4 years (depends on national guidelines)
• Severe hepatic impairment (caution)
Indications:

• Dry (non-productive) cough

Dose and Dosage Form:

Adults:
• 10–20 mg every 4 hours or 30 mg every 6–8 hours
• Maximum: 120 mg/day
•
Dosage Forms:
• Syrups: 5 mg/5 mL, 10 mg/5 mL (often in combo with other agents)
• Capsules,Lozenges,Extended-release formulations
 3.Levodropropizine
MOA

• • Acts on peripheral sensory nerves (C-fibers) in the respiratory tract.

• • Inhibits sensory nerve activation and neurogenic inflammation, thereby suppressing the cough reflex.
• • No central action → minimal risk of sedation or dependence (unlike codeine or dextromethorphan).

Indications (Uses):

• Dry (non-productive) cough of various causes

• Allergic cough (e.g., allergic rhinitis or mild asthma-related cough)
• Cough due to respiratory tract infections (URTI, pharyngitis, laryngitis)
• Cough due to environmental irritants (dust, smoke, pollution)

Dose and Dosage Forms:

Adults: 60 mg orally 3 times daily (TID), preferably before meals
Children: 1 mg/kg body weight TID, max 3 doses per day
• Commonly available as:
o Syrup (30 mg/5 mL or 60 mg/5 mL)
o Drops (for infants) in specific pediatric concentrations

Adverse Drug Reactions (ADRs):

• Nausea, Vomiting, Diarrhea, Mild drowsiness (rare)

• Rash or skin allergy (rare), Dizziness,Palpitations or mild tachycardia (rare)

Contraindications:

• Hypersensitivity to levodropropizine or any component of the formulation

• Children <2 years old (due to immature metabolic function and airway control)
• Severe hepatic or renal impairment (caution advised)
 Antihistamines
1. Chlorpheniramine
Mechanism of Action (MOA):
• First-generation H₁ antihistamine
• Blocks H₁ receptors → prevents histamine-induced symptoms (e.g., sneezing, runny nose)
• Also has anticholinergic and mild sedative effects
Indications:
• Allergic rhinitis(nasal mucosa to allergens, causing sneezing, nasal congestion, runny nose, and itching.)
• Urticaria (hives)
• Common cold
• Allergic conjunctivitis
Adverse Effects (ADRs):
• Drowsiness, urinary retention
• Dry mouth, constipation, tachycardia
• Dizziness
• Blurred vision
Contraindications:
• Narrow-angle glaucoma
• Severe liver disease
• MAO inhibitor use within 14 days
• Hypersensitivity
Dose & Dosage Form:
• Adults: 4 mg every 4–6 hours (Max 24 mg/day)
• Forms: Tablets, syrup, injectable
•
2. Cetirizine
MOA:
• Second-generation H₁ antihistamine
• Selectively blocks peripheral H₁ receptors
• Produce antihistaminic action.
• Less sedating than first-generation
 Indications:
• Allergic rhinitis
• Urticaria
• Atopic dermatitis(Atopic dermatitis is a chronic, relapsing inflammatory skin condition characterized by itchy, dry, red,
and scaly patches)
• Allergic conjunctivitis.
ADRs:
• Mild drowsiness
• Headache
• Dry mouth
• Fatigue
• Dizziness , GI upset.
Contraindications:
• Severe renal impairment
• Hypersensitivity to cetirizine or hydroxyzine
Dose & Dosage Form:
• Adults: 10 mg once daily
• Children (2–5 yrs): 2.5–5 mg daily
• Forms: Tablets, syrup, chewable tablets

3. Levocetirizine (Active R-enantiomer of cetirizine)

MOA:
• Same as cetirizine, but more potent
• Higher receptor affinity and longer duration
Indications:
Same as cetrizine
ADRs:same
• Drowsiness (less than cetirizine)
• Dry mouth
• Headache
• Fatigue
• Dizziness , GI upset
Contraindications:same
• End-stage renal disease
• Hypersensitivity
Dose & Dosage Form:
• Adults: 5 mg once daily
• Children (6–11 yrs): 2.5–5 mg once daily
• Forms: Tablets, syrup

4. Fexofenadine
MOA:
Selectively blocks peripheral H₁ histamine receptors.
Prevents the actions of histamine, a chemical released during allergic reactions.
Reduces symptoms like sneezing, itching, runny nose, watery eyes, and hives.

Indications:
• Seasonal allergic rhinitis
• Chronic idiopathic urticaria
• Atopic dermatitis(Atopic dermatitis is a chronic, relapsing inflammatory skin condition characterized by itchy, dry, red,
and scaly patches)
• Allergic conjunctivitis.
ADRs:
• Headache, back pain, drawsiness
• Dizziness
• Nausea
• Fatigue (rare)
Contraindications:
• Hypersensitivity
• Avoid with fruit juices (reduce absorption)
Dose & Dosage Form:
• Adults: 120–180 mg once daily
• Children (6–11 yrs): 30 mg twice daily
• Forms: Tablets, suspension
 5. Promethazine
MOA:
Blocks H₁ histamine receptors → reduces allergy symptoms
Anticholinergic effect → dries secretions
Dopamine receptor antagonist → anti-nausea and antiemetic effect
CNS depressant → causes sedation

Indications:
• Allergy symptoms
• Nausea and vomiting
• Motion sickness
• Sedation (preoperative/postoperative)
• Cough and cold formulations
ADRs:
• Drowsiness
• Dry mouth
• Dizziness
• Confusion (especially in elderly)
• Respiratory depression (especially in children <2 yrs)
Contraindications:
• Children under 2 years (due to risk of fatal respiratory depression)
• Comatose patients (coma patient)
• Hypersensitivity
Dose & Dosage Form:
• Adults: 12.5–25 mg every 4–6 hours
• For nausea/sedation: 25–50 mg
• Forms: Tablets, syrup, injection, suppository
•
 6.ketotifen
Mechanism of Action (MOA):
• Blocks H₁-histamine receptors → reduces allergic symptoms
• Stabilizes mast cells → prevents release of histamine and other inflammatory mediators
• Has anti-inflammatory and mild bronchodilatory properties

Indications:
1. Allergic conjunctivitis (as eye drops)
2. Allergic rhinitis
3. Asthma prophylaxis (especially in children, oral form)
4. Chronic urticaria
5. Eczema and atopic dermatitis (adjunctive use)

Dose and Dosage Forms:

Oral (tablets/syrup):
• Adults and children: 1 mg twice daily (tablet or syrup)
• Children 6 months – 3 years: 0.05 mg/kg twice daily (syrup)
Ophthalmic (eye drops):mKetotifen fumarate 0.025%
• 1 drop in affected eye(s) twice daily

Adverse Drug Reactions (ADRs):

• Drowsiness or sedation (especially with oral forms)
• Dry mouth
• Weight gain (rare)
• Dizziness
• Irritability (in children)
• Eye irritation (with eye drops, rare)
Contraindications:
• Hypersensitivity to ketotifen or its components
• Caution in patients with epilepsy (may lower seizure threshold)
• Avoid in combination with CNS depressants (due to additive sedation)
Nasal decongestants

1. Phenylephrine
Mechanism of Action (MOA):
• Selective α₁-adrenergic receptor agonist
• Causes vasoconstriction of blood vessels in the nasal mucosa
• Reduces nasal congestion by shrinking swollen nasal tissues and decreasing mucus secretion
Adverse Effects:
o Nasal irritation, Sneezing
o Rebound congestion (Rebound congestion is the worsening of nasal congestion that occurs after prolonged use of
topical nasal decongestants,)
o Hypertension
o Headache
o Anxiety
o Palpitations
o bradycardia
Contraindications:
• Severe hypertension or coronary artery disease
• Closed-angle glaucoma
• Hyperthyroidism
• Monoamine oxidase inhibitor (MAOI) use within 14 days
Indications:
• Nasal congestion (e.g., cold, allergy, sinusitis)
• Hypotension (in IV form, used in anesthesia settings)
• Mydriasis induction (eye drops – rarely)
 Dose and Dosage Forms:
Nasal (topical):
• 0.25% to 1% solution: 2–3 sprays or drops in each nostril every 4 hours – nasal spray
Oral:
• 10 mg every 4 hours (max 60 mg/day)- oral tablet
Forms: nasal spray, tablet , eyedrop, iv( for hypotension)

2. Oxymetazoline
Mechanism of Action (MOA):
• Non-selective α-adrenergic agonist (mainly α₁, partial α₂)
• Causes vasoconstriction in the nasal mucosa → reduces swelling and congestion

Adverse Effects:
• Nasal dryness or irritation
• Sneezing
• Rebound congestion (rhinitis medicamentosa) if used >3–5 days
• Headache
• Rare systemic effects (e.g., high blood pressure, insomnia)
Contraindications:
• Children <6 years (unless pediatric-specific formulation)
• Narrow-angle glaucoma
• Severe hypertension or heart disease
• MAOI use (within 14 days)

Indications:
• Short-term relief of nasal congestion due to:
o Common cold
o Allergic rhinitis
o Sinusitis
 Dose and Dosage Forms:
Nasal (topical):
• 0.05% spray: 2–3 sprays in each nostril every 10–12 hours
• Max: 2 doses in 24 hours
• Use no longer than 3 consecutive days
Forms:
• Nasal spray (most common)
• Nasal drops
Indication, side effect,contraindication, dose and dosage form of :

corticosteroids
corticosteroids are a class of steroid hormones produced by the adrenal cortex (naturally) or synthesized (as medications).
They play key roles in inflammation, immune response, metabolism, and electrolyte balance.

Classification
1. Glucocorticoids
• Hydrocortisone (Cortisol)
• Prednisolone
• Methylprednisolone
• Dexamethasone
• Betamethasone,
• Mometasone
• Fluticasone
• Budesonide
2. Mineralocorticoids
• Aldosterone
• Fludrocortisone
1. Betamethasone

• Indications:
o Inflammatory and allergic conditions (eczema, dermatitis, psoriasis)
o Autoimmune diseases
o Severe asthma (systemic use)
o Skin disorders requiring potent corticosteroids
• Side Effects:
o Skin thinning (topical)
o Hyperglycemia
o Immunosuppression
o Acne, stretch marks
o Osteoporosis , hypertension, mood changes, delayed wound healing.
• Contraindications:
o Systemic fungal infections
o bacterial or viral skin infections
o Hypersensitivity
• Dose and Dosage Forms: 0.6–7.2 mg/day
o Forms: Cream , ointment, lotion, injectable, oral tablets

2. Mometasone
• Indications:
o Allergic rhinitis (nasal spray)
o Asthma (inhaler)
o Atopic dermatitis (topical)
• Side Effects:
o Nasal irritation, dryness, or bleeding (nasal spray)
o Oral thrush (inhaler)
o Headache
o Rare systemic effects with prolonged use
• Contraindications:
o Hypersensitivity
 o Active untreated infections in the area of use
o Recent nasal surgery or trauma (for nasal spray)
• Dose and Dosage Forms:
o Nasal spray: 2 sprays per nostril once daily (50 mcg/spray)
o Inhaler: 220–440 mcg twice daily (asthma)
o Topical cream/ointment: Apply once daily(0.1%)
o Forms: Nasal spray, inhaler, cream, ointment

3. Fluticasone
Indications:

o Asthma (inhaler)
o Allergic rhinitis (nasal spray)
o dermatitis (topical)
• Side Effects:
o Oral candidiasis (inhaler)
o Voice changes
o Nasal irritation or bleeding (nasal spray)
o Headache
o Possible adrenal suppression with high doses
• Contraindications:
o Hypersensitivity
o Acute bronchospasm (not for rescue therapy)
o Active untreated infections
• Dose and Dosage Forms:
o Inhaler: 100–500 mcg twice daily (asthma)
o Nasal spray: 1–2 sprays per nostril once daily (50–100 mcg/spray)
o Topical: Apply once or twice daily
o Forms: Inhaler, nasal spray, cream, ointment(0.05%)
4. Hydrocortisone
• Indications:
o Adrenal insufficiency (oral/systemic)
o Mild to moderate inflammatory skin conditions (topical)
o Allergic reactions
o Ulcerative colitis (rectal forms)
• Side Effects:
o Skin irritation (topical), thinning of skin
o Hypertension, delayed wound healing
o Muscle weakness
o Hyperglycemia
o Fluid retention
o Osteoporosis (long-term use)
• Contraindications:
o Systemic fungal infections
o Hypersensitivity
o Untreated bacterial or viral infections
• Dose and Dosage Forms:
o Oral: 20–240 mg/day depending on indication
o Topical: Apply 2–3 times daily
o Injectable: Dose varies(100-500mg)
o Forms: Oral tablets, topical creams/ointments(0.5%,1%), injectables, rectal preparations

5. Budesonide

• Indications:
o Asthma (inhaler), Allergic rhinitis (nasal spray)
o Inflammatory bowel disease (oral or rectal forms), COPD
• Side Effects:
o Oral thrush (inhaler), hypertension, Nasal irritation (nasal spray)
o Headache, muscle weakness, osteoporosis, Adrenal suppression with prolonged/high-dose use
•
 • Contraindications:
o Hypersensitivity, Acute bronchospasm (not rescue)
o Active infections
• Dose and Dosage Forms:
o Inhaler: 180–720 mcg twice daily (asthma)
o Nasal spray: 64–256 mcg daily (allergic rhinitis)
o Oral (enteric-coated): 3–9 mg/day (IBD)
o Forms: Inhaler, nasal spray, oral capsules

Biologics( omalizumab)- Drugs used in asthama

Mechanism of Action (MOA):

• Binds to free IgE antibody in the blood and interstitial fluid.
• Prevents IgE from attaching to mast cells and basophils.
• Inhibits release of allergic mediators (histamine, leukotrienes, cytokines).
• Reduces allergic inflammation and hypersensitivity responses.
Indications:
1. Moderate to severe persistent allergic asthma (in patients ≥6 years old):
2. Chronic spontaneous urticaria (≥12 years old):
o Not responding adequately to H₁-antihistamines
Dose and Dosage Form:
Form:
• Injection (subcutaneous)
• Available as pre-filled syringes or vials
Dosing:
• Administered subcutaneously every 2 to 4 weeks
• Common adult dose: 150 mg to 300 mg SC q2-4 weeks
• For urticaria: 150–300 mg SC every 4 weeks, independent of IgE levels
Adverse Effects (Side Effects):
• Injection site reactions (pain, swelling, redness)
• Headache
 • Fatigue
• Arthralgia
• Upper respiratory infections
• Anaphylaxis (rare but serious → monitor after injection)
• Fever, rash, eosinophilia
Contraindications:
• Hypersensitivity to omalizumab or any of its components
• Caution in patients with a history of anaphylaxis

Expectorant (Ammonium chloride)

Indications:
• Expectorant in productive coughs (helps loosen phlegm)
• Used in urinary alkalinization disorders (less common)
• Sometimes used to treat metabolic alkalosis (off-label)
• Occasionally as a systemic acidifying agent
Dose and Dosage Forms:
• Oral dose (Adults): 0.5 to 1 g three times daily (TID)
• Syrup and tablets
• Adverse Effects:
• Gastric irritation, nausea, vomiting
• Metabolic acidosis (if overdosed or in renal impairment)
• Electrolyte imbalance (rare)
• Hypersensitivity reactions (rare)
Contraindications:
• Metabolic acidosis
• Severe renal or hepatic disease
• Respiratory acidosis
• Hypertension or edema (due to ammonium ion effect)
 Unit -12
Nutritional supplements: Vitamins and Minerals
Vitamins:

Vitamins are organic compounds that are essential for normal physiological functions such as growth, reproduction, and maintenance
of health. They are required in small quantities and usually cannot be synthesized in sufficient amounts by the body, so they must be
obtained through diet.

Classification

A. Fat-Soluble Vitamins:
1. Vitamin A
2. Vitamin D
3. Vitamin E
4. Vitamin K
B. Water-Soluble Vitamins:
Vitamin C
Vitamin B:
1. B1 (Thiamine)
2. B2 (Riboflavin)
3. B3 (Niacin)
4. B5 (Pantothenic acid)
5. B6 (Pyridoxine)
6. B7 (Biotin)
7. B9 (Folic acid)
8. B12 (Cobalamin)

Vitamins – Sources, Deficiency Syndrome, and Therapeutic Use

Vitamin Sources Deficiency Syndrome Therapeutic Use

Carrots, liver, dairy, green

Vitamin A Night blindness, xerophthalmia Eye disorders, skin conditions
leafy vegetables
Sunlight, fish oil, fortified Rickets (children), osteomalacia
Vitamin D Bone disorders, osteoporosis
milk (adults)
Hemolytic anemia, neurological
Vitamin E Vegetable oils, nuts, seeds Antioxidant therapy, skin healing
symptoms

Green leafy vegetables, gut Bleeding disorders, delayed Promotes blood clotting, used with
Vitamin K
flora clotting anticoagulants
Citrus fruits, tomatoes, green Scurvy (bleeding gums, poor Boosts immunity, wound healing,
Vitamin C
vegetables wound healing) antioxidant
Vitamin B1 Beriberi, Wernicke's
Whole grains, pork, legumes Neurological disorders, alcoholism
(Thiamine) encephalopathy
Vitamin B2
Milk, eggs, green vegetables Cheilitis, glossitis, eye problems Skin disorders, migraines
(Riboflavin)
Pellagra (diarrhea, dermatitis,
Vitamin B3 (Niacin) Meat, legumes, peanuts Hyperlipidemia treatment
dementia)
Vitamin B5
Whole grains, meat, eggs Fatigue, irritability, numbness General metabolic support
(Pantothenic acid)
Vitamin B6
Bananas, meat, cereals Anemia, irritability, depression PMS, morning sickness, neuropathy
(Pyridoxine)
Vitamin B7 (Biotin) Eggs, nuts, seeds Hair loss, dermatitis Hair and nail growth
Vitamin B9 (Folic Leafy greens, citrus fruits, Megaloblastic anemia, neural tube
Pregnancy, anemia, cell growth
acid) legumes defects
Vitamin B12
Meat, eggs, dairy Pernicious anemia, neuropathy Anemia, neurological disorders
(Cobalamin)
 Xerophthalmia – Severe dryness of the eye that can lead to blindness, often due to Vitamin A deficiency.
Rickets – Softening and weakening of bones in children, usually due to Vitamin D deficiency.
Osteomalacia – Bone softening in adults, typically caused by a lack of Vitamin D.
Osteoporosis – A condition where bones become fragile and porous, increasing fracture risk.
Hemolytic anemia – A disorder where red blood cells are destroyed faster than they can be made.
Scurvy – A disease caused by Vitamin C deficiency, leading to bleeding gums, weakness, and poor wound
healing.
Beriberi – A nervous system disorder caused by Thiamine (B1) deficiency, affecting movement and heart
function.
Wernicke’s encephalopathy – A brain disorder from severe Thiamine deficiency, with confusion, poor
coordination, and eye issues.
Cheilitis – Inflammation and cracking of the lips, often from a deficiency in B vitamins.
Glossitis – Inflammation of the tongue, making it red, swollen, and painful.
Pellagra – A condition caused by Niacin (B3) deficiency, leading to diarrhea, dermatitis, and dementia.
Numbness – Loss of sensation, often due to nerve damage or vitamin B deficiency.
PMS (Premenstrual Syndrome) – A group of physical and emotional symptoms occurring before
menstruation.
Megaloblastic anemia – A type of anemia with abnormally large red blood cells, due to lack of folic acid or
B12.
Neural tube defects – Birth defects of the brain or spine, often preventable with adequate folic acid.
Pernicious anemia – A severe form of anemia caused by Vitamin B12 deficiency, often due to poor absorption.
Neuropathy – Damage or dysfunction of nerves causing pain, weakness, or numbness, especially in hands and
feet.
Minerals:

Minerals are inorganic elements essential for the normal functioning of the body. They play key roles in building strong bones and
teeth, nerve signaling, muscle contraction, and maintaining fluid balanc

Classification of Minerals:

1. Macrominerals (Major minerals):

These are needed by the body in amounts greater than 100 mg per day.

o Calcium (Ca)
o Phosphorus (P)
o Magnesium (Mg)
o Sodium (Na)
o Potassium (K)
o Chloride (Cl)
o Sulfur (S)

2. Microminerals (Trace elements):

These are needed in very small amounts (less than 100 mg per day).

o Iron (Fe)
o Zinc (Zn)
o Copper (Cu)
o Iodine (I)
o Fluoride (F)
o Selenium (Se)
o Manganese (Mn)
o Chromium (Cr)
o Molybdenum (Mo)
 Minerals:Sources, Deficiency Syndrome, and Therapeutic Use

Element Sources Deficiency Syndrome Therapeutic Uses

- Treatment of hypocalcemia
Milk, cheese, yogurt, green leafy - Osteoporosis prevention
Calcium (Ca) Osteoporosis, rickets, muscle cramps, tetany
vegetables, fortified cereals - Antacid
- Cardiac arrhythmias
- Electrolyte replenishment
Potassium Bananas, oranges, potatoes, spinach, Muscle weakness, arrhythmia, fatigue,
- Treatment of hypokalemia
(K) legumes, dairy products hypokalemia
- Control of arrhythmias
- Laxative
- Antacid
Magnesium Nuts, seeds, whole grains, leafy Muscle cramps, tremors, seizures, cardiac
- Treatment of
(Mg) greens, dairy products arrhythmias, hypomagnesemia
preeclampsia/eclampsia
- Cardiac protection
- Treatment of iron-deficiency
Red meat, liver, beans, spinach, Iron-deficiency anemia (fatigue, pallor, anemia
Iron (Fe)
fortified cereals weakness), poor immunity - Iron supplementation during
pregnancy
 UNIT-11
Vaccine, Antisera and Immunoglobulin

1. Vaccine
A vaccine is a biological preparation that provides active acquired immunity to a particular infectious disease by stimulating the
immune system to recognize and fight pathogens.
Importance:
• Prevents from infectious diseases (e.g., measles, polio).
• Helps in eradicating diseases (e.g., smallpox).
• Reduces disease transmission.
• Protects individuals and community (herd immunity).
•
Types of vaccine

1. Live Attenuated Vaccines

• Contain weakened (attenuated) live organisms that replicate in the body without causing disease.
• Induce strong, long-lasting immunity (both humoral and cellular).
• Examples: BCG, MMR (measles, mumps, rubella), Oral Polio Vaccine (OPV).
2. Inactivated (Killed) Vaccines
• Contain killed microorganisms that cannot replicate.
• Safe for immunocompromised persons but may require booster doses.
• Examples: Rabies vaccine, Hepatitis A vaccine, Inactivated Polio Vaccine (IPV).

3. Toxoid Vaccines
• Contain inactivated bacterial toxins (toxoids).
• Used to protect against diseases caused by bacterial toxins.
• Examples: Tetanus toxoid, Diphtheria toxoid.

4. Subunit Vaccines
• Contain only specific antigenic parts of the pathogen (e.g., proteins, sugars).
• Lower risk of side effects, but may need adjuvants or boosters.
• Examples: Hepatitis B vaccine, Human papillomavirus (HPV) vaccine.
 5. Conjugate Vaccines
• Combine a weak antigen with a strong antigen to improve immune response.
• Especially useful in infants and young children.
• Examples: Hib (Haemophilus influenzae type b) vaccine, Pneumococcal conjugate vaccine.

6. mRNA Vaccines
• Contain messenger RNA that instructs cells to produce an antigen (usually a viral protein).
• Fast to develop and very effective.
• Examples: Pfizer-BioNTech COVID-19 vaccine, Moderna COVID-19 vaccine.

7. DNA Vaccines (experimental/limited use)

• Contain DNA plasmids that encode for antigen proteins.
• Induce both antibody and T-cell responses.
• Example: ZyCoV-D (India’s COVID-19 DNA vaccine).

2.Antisera
Antisera are preparations containing preformed antibodies obtained from the blood serum of immunized humans or
animals. They provide passive immunity against specific toxins or pathogens.

Importance

3. Provides immediate protection by supplying ready-made antibodies.

4. Used in emergencies like snake bites, rabies, tetanus, and diphtheria.
5. Neutralizes toxins such as tetanus toxin and snake venom effectively.
6. Offers temporary (short-term) immunity until active immunity can develop.
7. Useful for non-immunized individuals exposed to infections.
8. Can be used when vaccines are contraindicated or unavailable.
9. Helps prevent disease progression after exposure.
10. Reduces the severity of infection by rapidly lowering toxin/pathogen levels.
 Types of Antisera

1. Monovalent Antisera

• Contains antibodies against a single specific antigen or toxin.

• Used for targeted passive immunity.
• Example: Anti-tetanus serum (ATS) – acts only against tetanus toxin.
•
2. Polyvalent Antisera
• Contains antibodies against multiple antigens or toxins.
• Provides broader protection in cases involving multiple pathogens or toxins.
• Example: Polyvalent snake venom antiserum – neutralizes venom from different snake species.

3. Human Antisera
• Prepared from the blood of immunized humans.
• Safer with low risk of allergic reactions.
• Example: Human rabies immune serum.

4. Animal (Heterologous) Antisera

• Prepared from animals (usually horses) immunized with the antigen.
• More widely available but may cause allergic reactions like serum sickness.
• Example: Equine anti-snake venom serum.

3.Immunoglobulin:
Immunoglobulin is a sterile, concentrated solution of antibodies (mainly IgG) prepared from the pooled plasma of healthy
human donors. It is used to provide passive immunity against various infections by neutralizing pathogens or their toxins.

Importance

1. Provides immediate passive immunity by supplying ready-made antibodies.

2. Protects high-risk individuals exposed to infections (e.g., hepatitis B, rabies).
3. Offers short-term protection when quick immunity is needed.
4. Used in immune deficiency disorders (e.g., primary immunodeficiency, agammaglobulinemia).
5. Reduces severity and complications of diseases when given early.
6. Used as post-exposure prophylaxis in diseases like tetanus, measles, and rabies.
7. Safer than animal-derived antisera, with a lower risk of hypersensitivity reactions.
8. Can be used in pregnant women and newborns for certain infections to prevent transmission.

Types of Immunoglobulins

1. IgG (Immunoglobulin G-gamma)

• Percentage in serum: ~75–80% (most abundant)
• Site in body: Found in blood, lymph, extracellular fluid; crosses the placenta

2. IgA (Immunoglobulin A-alpha)

• Percentage in serum: ~10–15%
• Site in body: Found in mucosal secretions such as saliva, tears, breast milk, intestinal and respiratory secretions

3. IgM (Immunoglobulin M-mu)

• Percentage in serum: ~5–10%
• Site in body: Found in blood and lymph

4. IgE (Immunoglobulin E-epsilon)

• Percentage in serum: <0.01% (very low)
• Site in body: Attached to mast cells and basophils in skin, lungs, and mucous membranes

5. IgD (Immunoglobulin D-delta)

• Percentage in serum: ~0.2–1%
• Site in body: Present on the surface of immature B lymphocytes
Type , Dose,Indication, Time of administration,Adverse effect of:
1. BCG Vaccine
• Type: Live attenuated vaccine derived from Mycobacterium bovis.
• Dose: 0.05 ml intradermal (newborns/infants), 0.1 ml for older children/adults.
• Indication: Prevents tuberculosis, especially severe forms such as miliary TB and tuberculous meningitis in
children.
• Time of Administration: Given at birth or within first few weeks of life.
• Adverse Effects: Local ulceration, formation of typical scar(small, round, slightly raised mark that
usually forms at the site of the BCG injection ), regional lymphadenitis(inflammation and swelling of
the lymph nodes that are located near the site of an infection or injection.)

2. DPT Vaccine (Diphtheria, Pertussis, Tetanus) Pertussis,- also known as whooping cough, is a highly
contagious respiratory disease caused by the bacterium Bordetella pertussis.
• Type: Combination vaccine containing diphtheria and tetanus toxoids plus whole-cell inactivated pertussis
bacteria.
• Dose: 0.5 ml intramuscular; primary series at 6, 10, and 14 weeks; boosters at 16-24 months and 5-6 years.
• Indication: Prevention of diphtheria, pertussis (whooping cough), and tetanus.
• Time of Administration: Starting at 6 weeks of age.
• Adverse Effects: Fever, swelling, redness, pain at injection site; rare severe allergic reactions.

3. OPV (Oral Polio Vaccine)

• Type: Live attenuated poliovirus vaccine.
• Dose: 2 drops orally per dose; multiple doses given at birth and during infancy per national immunization
schedule.
• Indication: Prevention of poliomyelitis.
• Time of Administration: At birth (zero dose) and subsequent doses at 6, 10, and 14 weeks.
• Adverse Effects: Rarely vaccine-associated paralytic poliomyelitis (inflammation of the spinal cord’s motor
neurons, leading to muscle weakness and paralysis.)
4. MR Vaccine (Measles, Rubella)
• Type: Live attenuated vaccine.
• Dose: 0.5 ml subcutaneous; two doses at 9 and 15 months of age.
• Indication: Prevention of measles and rubella infections.
• Time of Administration: First dose at 9 months, second at 15 months or as per local schedule.
• Adverse Effects: Mild fever, rash, lymphadenopathy, very rare allergic reactions.

5. TT Vaccine (Tetanus Toxoid)

• Type: Purified tetanus toxoid (inactivated toxin).
• Dose: 0.5 ml intramuscular; given in multiple doses (primary series and boosters).
• Indication: Prevention of tetanus, especially in pregnant women and for wound prophylaxis.
• Time of Administration: Immediately, Starting at 6 weeks; recommended during pregnancy at 16 and 26
weeks or as per schedule.
• Adverse Effects: Local pain, swelling, fever, rarely allergic reactions.

6. Hepatitis B Vaccine
• Type: Recombinant subunit vaccine containing hepatitis B surface antigen (HBsAg).
• Dose: 0.5 ml intramuscular; typically 3 doses at birth, 6 weeks, and 14 weeks.
• Indication: Prevention of hepatitis B infection and its chronic complications.
• Time of Administration: First dose at birth; subsequent doses as per schedule.
• Adverse Effects: Mild pain at injection site, low-grade fever.
•
7. JE Vaccine (Japanese Encephalitis)- Japanese Encephalitis (JE) is a viral brain infection caused by the Japanese
Encephalitis virus
• Type: Inactivated or live attenuated vaccine (varies by formulation).
• Dose: 0.5 ml intramuscular, two doses given 7-28 days apart.
• Indication: Prevention of Japanese encephalitis in endemic areas.
• Time of Administration: From 9 months of age, especially in high-risk regions.
• Adverse Effects: Fever, local reactions, rarely allergic reactions.
8. TCV (Typhoid Conjugate Vaccine)
• Type: Conjugate vaccine linking Vi polysaccharide to a protein carrier to enhance immune response.
• Dose: 0.5 ml intramuscular, single dose.
• Indication: Prevention of typhoid fever caused by Salmonella typhi.
• Time of Administration: From 6 months of age onwards.
• Adverse Effects: Local pain, swelling, mild fever.

9. Cholera Vaccine
• Type: Oral killed whole-cell vaccine, sometimes combined with B subunit toxin.
• Dose: Two doses orally, 1-6 weeks apart depending on formulation.
• Indication: Prevention of cholera in endemic areas or during outbreaks.
• Time of Administration: Prior to travel to endemic regions or during outbreaks.
• Adverse Effects: Mild gastrointestinal symptoms such as diarrhea and abdominal discomfort.

10. Antitetanic Serum (ATS)

• Type: Polyclonal antibodies from horse serum.
• Dose: 250-500 IU intramuscular or intravenous depending on wound severity.
• Indication: Passive immunization after tetanus-prone wounds in unimmunized or incompletely immunized
individuals.
• Time of Administration: As soon as possible after exposure.
• Adverse Effects: Risk of serum sickness(hypersensitivity after administration of serum), anaphylaxis; pre-
test sensitivity recommended.

11. Anti-Snake Venom Serum (ASV)

• Type: Polyclonal antibodies derived from immunized horses.
• Dose: Dose varies depending on snake species and severity; administered intravenously.
• Indication: Neutralization of venom in venomous snake bites.
• Time of Administration: Immediately after snakebite as early as possible.
• Adverse Effects: Anaphylactic reactions, serum sickness, local pain.
12. Anti-Rabies Serum (ARS)
• Type: Polyclonal antibody
• Dose: Calculated based on body weight (20 IU/kg for human rabies immunoglobulin); infiltrated around
wound and remaining dose IM.
• Indication: Post-exposure prophylaxis for rabies exposure before clinical disease develops.
• Time of Administration: At the same time as first dose of rabies vaccine after exposure.
• Adverse Effects: Local pain, rare allergic reactions.

13. Anti-D Immunoglobulin

• Type: Human IgG anti-D immunoglobulin.
• Dose: 300 mcg intramuscular at 28 weeks gestation and within 72 hours postpartum if baby is Rh-positive.
• Indication: Prevention of Rh sensitization (Rh factor (Rhesus factor) is a protein found on the surface of
red blood cells.) in Rh-negative mothers to avoid hemolytic disease of the newborn.
• Time of Administration: During pregnancy and after delivery as prophylaxis.
• Adverse Effects: Rare mild allergic reactions.

14. COVID-19 Vaccines

• Type: mRNA (Pfizer, Moderna), viral vector (Covishield, Janssen), inactivated (Covaxin), protein subunit
(Novavax).
• Dose: Usually 2 doses IM spaced 3-12 weeks apart, with boosters as recommended.
• Indication: Prevention of COVID-19 infection and severe disease.
• Time of Administration: Per national immunization schedules.
• Adverse Effects: Local pain, fever, fatigue, rare anaphylaxis or myocarditis (mRNA vaccines).
15. FIPV Vaccine ( Fractional-dose Inactivated Poliovirus Vaccine)

Type: Inactivated (killed) virus vaccine

Dose:0.1 mL Given intradermally (ID) — usually over the upper arm or forearm
Indication: Primary prevention of poliomyelitis
Time of Administration: First dose: At 6 weeks of age, Second dose: At 14 weeks of age
• Booster (full-dose IPV) may be given later, depending on national schedule
Adverse Effects
• Local reactions at injection site:
o Redness
o Swelling
o Pain
• Rarely:
o Fever
o Irritability
o Allergic reaction (very rare)

16. HPV Vaccine (Human Papillomavirus)

• Type: subunit vaccine.
• Dose: 0.5 ml IM; 2 doses (if started before age 15) or 3 doses (if started after 15).
• Indication: Prevention of cervical cancer and other HPV-related diseases.
• Time of Administration: Recommended at 9-14 years before onset of sexual activity.
• Adverse Effects: Pain at injection site, mild fever, dizziness, rare allergic reactions.
 Unit-10
NSAIDS (nonsteroidal anti-inflammatory drugs)
Pain:
Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage.
It is a protective mechanism that helps the body respond to injury or illness.

Pyrexia (Fever):
Pyrexia is an abnormal elevation of body temperature above the normal range (usually > 37.5°C or 99.5°F), often due to infection,
inflammation, or other disease processes.
It is a natural response of the body to fight pathogens.

Inflammation:
Inflammation is the body’s local protective response to injury, infection, or irritation.
It is characterized by:
• Redness
• Heat
• Swelling
• Pain
• Loss of function

Analgesics:
Analgesics are drugs that relieve pain without causing loss of consciousness.
Examples: Paracetamol, Ibuprofen, Morphine.

Antipyretics:
Antipyretics are drugs that reduce fever (pyrexia) by acting on the hypothalamic heat-regulating center.
Examples: Paracetamol, Ibuprofen, Aspirin.

NSAIDS-
NSAIDs, or Non-Steroidal Anti-Inflammatory Drugs, are a group of medications that reduce pain (analgesic effect), fever (antipyretic
effect), and inflammation (anti-inflammatory effect).
1. Based on Chemical Structure:
• Salicylates: aspirin
• Propionic acid derivatives: ibuprofen, naproxen, and ketoprofen, fenoprofen.
• Acetic acid derivatives: diclofenac, Aceclofenac, indomethacin, and ketorolac.
• Enolic acid derivatives: piroxicam and meloxicam.
• Fenamate (anthranilic acid derivatives): mefenamic acid and flufenamic acid.
• Selective COX-2 inhibitors: celecoxib and etoricoxib.
• Para aminophenol derivative: paracetamol, Phenacetin which has weak anti-inflammatory action

2. Based on COX Enzyme Selectivity:

• Non-selective COX inhibitors inhibit both COX-1 and COX-2 enzymes: aspirin, ibuprofen, and diclofenac.
• Preferential COX-2 inhibitors inhibit COX-2 more than COX-1: meloxicam and nimesulide, etodolac.
• Selective COX-2 inhibitors: celecoxib and etoricoxib, valdecoxib

MOA

NSAIDs inhibit cyclooxygenase enzymes (COX-1 and COX-2), which reduces production of prostaglandins—the chemicals
that cause pain, inflammation, and fever.
• COX-1 inhibition can cause stomach irritation and reduce platelet function.
• COX-2 inhibition mainly reduces inflammation and pain.

1. Aspirin (Acetylsalicylic Acid)

• MOA: Irreversibly inhibits COX-1 and COX-2 enzymes → decreases synthesis of prostaglandins and thromboxane A2 →
reduces pain, inflammation, fever, and platelet aggregation (antithrombotic effect).
• Indications & Types of Pain:
o Mild to moderate nociceptive pain (headache, toothache, musculoskeletal pain)
o Inflammatory pain (arthritis)
o Fever, inflammation
o Cardiovascular prophylaxis (not pain)
• Side Effects: Gastric irritation, peptic ulcers, GI bleeding, tinnitus (high doses), Reye’s syndrome in children(A rare but
serious condition causing acute encephalopathy (brain swelling) and fatty liver degeneration.), hypersensitivity (asthma
exacerbation), bronchospasm, tinnitus.
• Contraindications: Active peptic ulcer, bleeding disorders, children with viral infections, asthma.
• Dose:
o Analgesic/Antipyretic: 300–600 mg every 4–6 hours
o Cardioprotective: 75–150 mg once daily
• Dosage Forms: Tablets, chewable tablets, enteric-coated tablets, suppositories.

2. Paracetamol (Acetaminophen)
• MOA: Weak inhibition of COX enzymes, primarily Act on CNS → analgesic and antipyretic effects; minimal anti-
inflammatory action.
• Indications & Types of Pain:
o Mild to moderate nociceptive pain (headache, musculoskeletal pain, dental pain)
o Fever
o Not effective for inflammation
• Side Effects: Hepatotoxicity (especially in overdose), rash (rare), renal toxicity on high dose, thrombocytopenia
(rare),urticaria.
• Contraindications: Severe liver disease, chronic alcoholism.
• Dose: 500–1000 mg every 4–6 hours; max 4 g/day in adults.
• Dosage Forms: Tablets, syrups, injections, suppositories.

3. Ibuprofen
• MOA: Non-selective reversible inhibition of COX-1 and COX-2 → decreases prostaglandin synthesis.
• Indications & Types of Pain:
o Mild to moderate nociceptive pain (headache, dental pain, musculoskeletal pain)
o Inflammatory pain (arthritis- OA,RA)
o Dysmenorrhea (menstrual pain)
o Fever
• Side Effects: GI irritation, nausea, peptic ulcers, renal impairment, dizziness, bronchospasm, meningitis.
• Contraindications: Peptic ulcer disease, renal impairment, heart failure.
• Dose: 200–400 mg every 6–8 hours; max 1200–2400 mg/day.
• Dosage Forms: Tablets, suspensions, topical gels, capsules.
 4. Naproxen
• MOA: Non-selective COX inhibitor ( COX-1 and COX-2 )→ reduces prostaglandins involved in pain and inflammation.
• Indications & Types of Pain:
o Mild to moderate nociceptive pain(headache, dental pain, musculoskeletal pain)
o Inflammatory pain (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis)
o Dysmenorrhea
o Acute gout pain
• Side Effects: GI upset, headache, dizziness, fluid retention, GI bleeding, Photosensitivity, nausea.
• Contraindications: Peptic ulcer, renal or hepatic impairment.
• Dose: 250–500 mg twice daily; max 1000 mg/day.
• Dosage Forms: Tablets, suspensions.

5. Ketorolac
• MOA: Potent non-selective COX inhibitor (COX-1 and COX-2) → strong analgesic and anti-inflammatory effects.
• Indications & Types of Pain:
o Moderate to severe acute nociceptive pain (postoperative pain, trauma -injury pain)
o Ocular pain and inflammation.
o Not for chronic pain
• Side Effects: GI bleeding, ulcers, renal toxicity, headache, dizziness., inject time pain.
• Contraindications: Active peptic ulcer, renal failure, before or after major surgery.
• Dose: 10–30 mg IV/IM every 6–8 hours; max 5 days treatment.
• Dosage Forms: Tablets, injections, eye drops.

6. Indomethacin
• MOA: Non-selective COX inhibitor (COX-1 and COX-2 )→ reduces prostaglandin synthesis.
• Indications & Types of Pain:
o Moderate to severe inflammatory pain (gout attacks, rheumatoid arthritis)
o Ankylosing spondylitis(Ankylosing spondylitis (AS) is a chronic inflammatory disease that primarily affects the
spine and leading to pain and stiffness)
o Closure of patent ductus arteriosus (The ductus arteriosus is a normal fetal blood vessel that connects the
pulmonary artery to the aorta.)
• Side Effects: CNS effects (headache, dizziness, confusion), GI ulcers, fluid retention, abdominal pain, Nausea, fluid retention.
• Contraindications: Peptic ulcer, epilepsy, severe CNS disorders.
• Dose: 25–50 mg 2–3 times daily.
• Dosage Forms: Capsules, suppositories, injections.

7. Mefenamic Acid
• MOA: Reversibly inhibiting cyclooxygenase enzymes (COX-1 and COX-2). → decreases prostaglandins causing pain and
inflammation.
• Indications & Types of Pain:
o Mild to moderate nociceptive pain(postoperative pain, trauma -injury pain)
o Dysmenorrhea
o Dental pain
o Postoperative pain
• Side Effects: GI upset, dizziness, headache, rare cases of anemia, skin rash, Thrombocytopenia(rare)
• Contraindications: Peptic ulcer, renal/hepatic impairment.
• Dose: 500 mg initial dose, then 250 mg every 6 hours.
• Dosage Forms: Capsules, tablets.

8. Nimesulide
• MOA: Preferential COX-2 inhibitor → reduces prostaglandin synthesis mainly at sites of inflammation.
• Indications & Types of Pain:
o Mild to moderate inflammatory pain (osteoarthritis, musculoskeletal pain)
o Dysmenorrhea
o Acute pain conditions (Joint pain, low back pain, headache)
• Side Effects: Hepatotoxicity (monitor liver enzymes), GI upset, skin rash, Nausea, vomiting, abdominal pain, Diarrhea,
pruritic)
• Contraindications: Liver disease, children under 12 years, active peptic ulcer.
• Dose: 100 mg twice daily.
• Dosage Forms: Tablets, suspensions.
 9. Diclofenac
• MOA: Non-selective COX inhibitor((COX-1 and COX-2). ) → inhibits prostaglandin synthesis.
• Indications & Types of Pain:
o Mild to moderate nociceptive and inflammatory pain (arthritis, musculoskeletal disorders)
o Postoperative pain
o Acute gout pain
o Ankylosing spondylitis
o Dental pain
o Dysmenorrhea
• Side Effects: GI irritation, elevated liver enzymes, renal impairment, rash, peptic ulcer, bleeding,urticaria.
• Contraindications: Peptic ulcer, hepatic or renal impairment.
• Dose: 50 mg 2–3 times daily; max 150 mg/day.
• Dosage Forms: Tablets, injections, topical gels, eye drops.
10. Aceclofenac
• MOA: Derivative of diclofenac; inhibits COX enzymes((COX-1 and COX-2).), reduces prostaglandin production.
• Indications & Types of Pain:
o Mild to moderate inflammatory pain (osteoarthritis, rheumatoid arthritis, ankylosing spondylitis)
o Dental pain
o Acute gout attack
• Side Effects: GI discomfort, dizziness, rash (rare), headache, liver enzyme elevation
• Contraindications: Peptic ulcer, severe renal/hepatic impairment.
• Dose: 100 mg twice daily.
• Dosage Forms: Tablets.
11. Etoricoxib
• MOA: Selective COX-2 inhibitor → reduces prostaglandin production, inflammation with less GI irritation.
• Indications & Types of Pain:
o Chronic inflammatory pain (osteoarthritis, rheumatoid arthritis, ankylosing spondylitis)
o Acute gout pain
o Postoperative pain
• Side Effects: Hypertension, edema, increased cardiovascular risk, headache, dizziness, Dry mouth, elevated liver enzyme.
• Contraindications: History of cardiovascular disease, active GI bleeding, pregnancy.
• Dose: 60–120 mg once daily.
• Dosage Forms: Tablets.
 Gout is a type of inflammatory arthritis characterized by sudden, severe attacks of pain, redness, and
swelling in joints, often the big toe. It occurs due to the deposition of monosodium urate crystals in joints
and tissues, caused by elevated levels of uric acid in the blood (hyperuricemia).

Antigout Drugs:
Antigout drugs are medications used to treat or prevent gout attacks by either:
• Reducing inflammation during acute attacks.
• Lowering serum uric acid levels to prevent future attacks.

Classification of Antigout Drugs:

For Acute Gout Attacks:

• Colchicine
• Indomethacin
• Naproxen
• Ibuprofen
• Celecoxib
• Prednisone
• Methylprednisolone
For Chronic Gout:
• Allopurinol
• Febuxostat
• Probenecid
• Lesinurad
• Benzbromarone (Note: Not available in all regions, e.g., US)
• Pegloticase
• Rasburicase
1. Colchicine
Mechanism of Action (MOA):

• Colchicine binds to tubulin —( a protein that helps build microtubules in cells.)

• This prevents microtubule formation.
• Without microtubules, neutrophils can’t move properly or release inflammation chemicals.
• So, inflammation is reduced, and gout pain/swelling improves.

Indications:
• Acute gout attacks
• Prophylaxis of gout flares (A gout flare is a sudden onset of intense joint pain, redness, and swelling caused
by acute inflammation due to monosodium urate (MSU) crystals in the joint space.)
• Familial Mediterranean Fever (FMF) (Familial Mediterranean Fever (FMF) is a genetic autoinflammatory
disorder characterized by recurrent episodes of fever and serositis (inflammation of the linings of organs,
like the peritoneum, pleura, and joints).
Adverse Drug Reactions (ADR):
• GI toxicity (most common): nausea, vomiting, diarrhea, abdominal pain.
• Bone marrow suppression (rare): leukopenia, aplastic anemia
• Neuropathy and myopathy (Neuropathy-damage peripheral nerve)(myopathy- muscle weakness)
• Hepatotoxicity (rare)
Contraindications:
• Severe renal or hepatic impairment
• Concomitant use with strong CYP3A4 inhibitors (e.g., clarithromycin) in renal/hepatic impairment
• Blood dyscrasias(lood dyscrasia refers to any abnormal or pathological condition of the blood like-
anaemia)
• Pregnancy (use with caution)
 Dose:
• Acute Gout Attack:
Initial: 1.2 mg, then 0.6 mg after 1 hour (max: 1.8 mg/day)
Maintenance: 0.6 mg once or twice daily
Dosage Forms:
• Tablets: 0.6 mg
• Oral solution (some brands/countries)
2. Allopurinol
Mechanism of Action (MOA):

Indications:
• Chronic gout
• Hyperuricemia due to chemotherapy (tumor lysis syndrome)
• Kidney stones with uric acid component
• Recurrent uric acid nephropathy(Recurrent uric acid nephropathy refers to kidney damage caused by
repeated uric acid crystal deposition)
 Adverse Drug Reactions (ADR):
• Skin rash
• GI upset: nausea, diarrhea
• Hepatotoxicity
• Bone marrow suppression

Contraindications:
• Known hypersensitivity
• Asymptomatic hyperuricemia (Asymptomatic hyperuricemia means elevated serum uric acid levels
without any symptoms or sign)
• Caution in renal impairment – dose adjustment needed
Dose:
• Initial: 100 mg/day
• Increase gradually (by 100 mg/week) to 300–600 mg/day, depending on uric acid level and renal function.
• Max: 800 mg/day
• Dose adjust in renal impairment!
Dosage Forms:
• Tablets: 100 mg, 300 mg

3. Febuxostat
Mechanism of Action (MOA):
SAME AS ALLOPURINOL
Indications:
• Chronic hyperuricemia in patients with gout
• Use in patient’s intolerant to allopurinol
 Adverse Drug Reactions (ADR):
• Liver function abnormalities
• Rash
• Nausea
• Joint pain
• Cardiovascular risks
Contraindications:
• Severe hepatic impairment
• Ischemic heart disease or congestive heart failure (use caution)
• Hypersensitivity to febuxostat
Dose:
• Starting dose: 40 mg once daily
• May increase to 80 mg once daily if uric acid >6 mg/dL after 2 weeks
• No need to adjust dose in mild/moderate renal impairment
Dosage Forms:
• Tablets: 40 mg, 80 mg
 Unit -13
Locally acting drugs
1. Local Route
The local route of drug administration refers to the application of a drug directly to the site where the therapeutic
effect is desired, with minimal systemic absorption. It is mainly used for local action.
Example:
• Eye drops like Timolol for treating glaucoma
• Skin ointments like Hydrocortisone for eczema

2. Local Application
Local application is the direct application of a drug or substance to a specific area of the body (skin or mucous
membranes) to produce a local effect, often used for skin conditions or infections.
Example:
• Clotrimazole cream applied to treat athlete’s foot
• Povidone-iodine used as a wound disinfectant

3. Local Anaesthetics
Local anaesthetics are drugs that cause temporary loss of sensation or pain in a specific area by blocking nerve
conduction, without affecting consciousness.
Example:
• Lidocaine – used in dental procedures
• Bupivacaine – used in epidural anesthesia

4. Germicide
A germicide is a chemical substance that kills pathogenic microorganisms, including bacteria, viruses, and fungi.
It is used for disinfection and sterilization.
Example:
• Chlorhexidine – used for skin disinfection before surgery
5. Keratolytic Agents
Keratolytic agents are substances that soften, loosen, and help in the shedding of the outer layer of the skin
(stratum corneum). They are used to treat conditions with excessive skin thickening or scaling.
Example:
• Salicylic acid – used to treat acne, psoriasis, and warts

6. Soothing Agents
Soothing agents are substances that relieve irritation, inflammation, or itching of the skin or mucous membranes
by forming a protective barrier or cooling effect.
Example:
• Calamine lotion – used to relieve itching in chickenpox
• Aloe vera gel – used to soothe sunburns

7. Astringents
Astringents are substances that cause contraction of body tissues by protein precipitation, especially the skin,
helping to reduce bleeding, secretion, or swelling. They also tighten pores and have a drying effect.
Example:
• Alum – used as a styptic to stop bleeding from small cuts

8. Oxidizing Agents
Definition:
Oxidizing agents are chemical substances that release oxygen or cause oxidation of cellular components, which
helps in killing microbes and disinfecting wounds or surfaces.
Example:
• Hydrogen peroxide (3%) – used to clean wounds
• Potassium permanganate – used in dilute solution for infected eczema
9. Scabies
Scabies is a contagious skin condition caused by the infestation of the mite Sarcoptes scabiei, resulting in intense
itching, especially at night, and a rash.
Example (Treatment):
• Permethrin 5% cream – applied from neck to toes
• Ivermectin tablets – used orally in resistant cases

10. Pediculosis
Pediculosis is an infestation of lice (head lice, body lice, or pubic lice) on the human body, causing itching and
irritation.
Example (Treatment):
• Permethrin 1% lotion – applied to the scalp for head lice
• Malathion lotion – used when resistance to other agents occurs
1. Gentian Violet
• Indication:
Used as a topical antiseptic for treating fungal infections like oral thrush (Candida), athlete’s foot, and minor
cuts or abrasions. Also has mild antibacterial properties.
• Contraindication:
Hypersensitivity, infants under 4 weeks (due to toxicity concerns), mucosal application for prolonged
periods.
• Adverse Effects:
Skin and mucous membrane irritation, staining of skin, nails, and clothes, ulceration with repeated use,
rarely necrosis in mucosal tissue.
• Dose:
Apply directly to affected area once or twice daily.
• Dosage Form:
Topical solution (0.5% to 1%).
 2. Mercurochrome (Merbromin)
• Indication:
Mild antiseptic for minor cuts, scrapes(crapes are a type of superficial wound that occurs when the outer layers of
the skin (epidermis and part of the dermis) are rubbed or torn off due to friction against a rough surface.), and burns.
Acts as a bacteriostatic agent.
• Contraindication:
Mercury sensitivity, deep wounds, prolonged use (due to mercury accumulation), not recommended in
children.
• Adverse Effects:
Local irritation, dermatitis, hypersensitivity reactions, potential mercury toxicity with overuse.
• Dose:
Apply once or twice daily.
• Dosage Form:
2% aqueous or alcoholic solution.

3. Acriflavine
• Indication:
Antiseptic for wounds, ulcers, burns, and infected skin. Occasionally used in bladder irrigation.
• Contraindication:
Hypersensitivity, open mucosa, prolonged use.
• Adverse Effects:
Skin staining (yellow), irritation, allergic dermatitis.
• Dose:
Apply diluted solution once or twice daily.
• Dosage Form:
0.1–0.2% aqueous solution, ointment.
 4. Potassium Permanganate
• Indication:
Used in dermatology for fungal infections, weeping eczema(dermatitis), abscesses (An abscess is a
localized collection of pus within tissue), and ulcers. Acts as an oxidizing antiseptic and deodorizer.
• Contraindication:
Broken skin, mucous membranes, hypersensitivity, undiluted application.
• Adverse Effects:
Irritation, chemical burns if concentrated, brown staining of skin .
• Dose:
Dilute to 0.01% (1:10,000); used as soaks or compresses once or twice daily.
• Dosage Form:
Crystals or tablets (for dilution), solution.

5. Zinc Permanganate
• Indication:
Astringent and mild antiseptic. Used for skin conditions with exudation. (Exudation refers to the leakage of
fluid, cells, or cellular substances from blood vessels into surrounding tissues or on the surface of a
wound due to inflammation or injury.)
• Contraindication:
Open wounds, known allergy.
• Adverse Effects:
Mild irritation, dryness, redness, itching, brown or black staining.
• Dose:
0.1% as needed.
• Dosage Form:
Solution, lotion
 6. Aromatic Water (e.g., Rose Water)
• Indication:
Used as a soothing agent in eye or skin preparations. Mild astringent action also.
• Contraindication:
Hypersensitivity.
• Adverse Effects:
Rare irritation or allergic reactions.
• Dose:
As required.
• Dosage Form:
Aqueous solution.

7. Spirit (e.g., Ethanol 70%, Camphorated Spirit)

• Indication:
Antiseptic, cooling agent, counter-irritant(A counter-irritant is a substance applied to the skin that
causes mild inflammation or irritation with the goal of relieving deeper pain or inflammation), rubbing
alcohol(used to disinfect skin and surfaces.)
• Contraindication:
Broken or inflamed skin, hypersensitivity.
• Adverse Effects:
Burning, stinging, drying of skin, systemic absorption in large amounts.
• Dose:
Apply to area with cotton swab as needed.
• Dosage Form:
Liquid.
 8. Calamine Powder
• Indication:
Pruritus, sunburn, chickenpox, insect bites. Has mild astringent and soothing properties.
• Contraindication:
Broken or infected skin.
• Adverse Effects:
Chalky residue, dryness, rare skin irritation.
• Dose:
Apply as dusting powder as needed.
• Dosage Form:
Fine powder.

9. Zinc Oxide
• Indication:
Skin protectant , minor burns, eczema(itchy, dry, and scaly patches on the skin). Astringent, soothing,
protective.
• Contraindication:
Known sensitivity.
• Adverse Effects:
Mild irritation, rarely allergic reaction, dryness, itching, burning sensation.
• Dose:
10% , 25% Apply thin layer to affected area 2–3 times daily.
• Dosage Form:
Ointment, cream, paste, powder.

10. Zinc Sulphate

• Indication:
Used for acne, eczema, conjunctivitis, dermatitis.
• Contraindication:
Hypersensitivity.
• Adverse Effects:
Burning eye, stinging, irritation, itching
• Dose:
Topical application or eye drops 2–3 times daily.
• Dosage Form:
Solution (0.25–0.5%), lotion, eye drop

11. Calamine Lotion

• Indication:
Relief of itching due to insect bites, sunburn, allergic dermatitis, chickenpox.
• Contraindication:
Hypersensitivity, oozing skin lesions.( Oozing skin lesions are those where the skin is weeping or discharging fluid,)
• Adverse Effects:
Mild skin irritation or flaking, redness, burning, staining.
• Dose:
Apply to affected area 2–3 times daily.
• Dosage Form:
Lotion (mixture of zinc oxide 1-2% +calamine 5%).

12. Sulfur
• Indication:
Acne, dermatitis, scabies. Antibacterial, antifungal, and keratolytic.
• Contraindication:
Hypersensitivity, inflamed skin.
• Adverse Effects:
Skin dryness, peeling, photosensitivity, has a characteristic unpleasant smell
• Dose:
Apply 1–2 times daily, or leave overnight for scabies.
• Dosage Form:
Ointment, soap, lotion.(2%-10%)

13. Benzoic Acid

• Indication:
Antifungal agent (used in combination with salicylic acid in Whitfield ointment).
• Contraindication:
Hypersensitivity, broken skin.
• Adverse Effects:
Skin irritation, peeling, burning, redness, staining.
• Dose:
Apply twice daily.
• Dosage Form:
Ointment (usually 6%).

14. Whitfield Ointment

• Indication:
Fungal infections such as ringworm, athlete’s foot.
• Contraindication:
Sensitive or inflamed skin.
• Adverse Effects:
Burning, peeling, irritation, redness, staining.
• Dose:
Apply to infected skin twice daily.
• Dosage Form:
Ointment (Benzoic acid 6% + Salicylic acid 3%).
 15. Benzyl Benzoate
• Indication:
Scabies, pediculosis (lice).
• Contraindication:
Inflamed or broken skin; infants (risk of neurotoxicity).
• Adverse Effects:
Severe burning, stinging, itching, systemic absorption in infants.
• Dose:
for scabies-Apply to whole body (except face) , leave overnight; repeat after 7 days if needed.
For pediculosis-apply on the scalp, leave overnight; repeat after 7 days if needed.
• Dosage Form:
Emulsion or lotion (25% in adults, 10% in children).

16. Chlorhexidine
• Indication:
Preoperative skin disinfection, wound cleansing, oral rinse (0.12%).
• Contraindication:
Hypersensitivity, ototoxic if used in ear.
• Adverse Effects:
Tooth staining (oral), skin irritation, allergic reactions, burning.
• Dose:
Use 15 ml mouth rinse twice daily; apply solution to skin as needed.
• Dosage Form:
Solution, mouthwash, gel. ( 0.5% to 4%)
 17. Cetrimide
• Indication:
Wound antiseptic, cleansing agent, burn treatment.
• Contraindication:
Deep wounds, mucosal use.
• Adverse Effects:
Burning, allergic dermatitis, redness, itching.
• Dose:
0.5–1% solution applied topically.
• Dosage Form:
Solution, cream.

18. Chloroxylenol (e.g., Dettol)

• Indication:
Skin antiseptic, used for wounds, cuts, and hygiene.
• Contraindication:
Hypersensitivity.
• Adverse Effects:
Skin irritation, dermatitis, burn if applied in eye, dryness .
• Dose:
4.8%
• Dosage Form:
Liquid antiseptic.

19. Iodine (Tincture or Povidone-Iodine)

• Indication:
Disinfection of wounds, preoperative skin preparation.
• Contraindication:
Iodine allergy, prolonged use in neonates.
• Adverse Effects:
Skin irritation, staining, allergic dermatitis, burning.
• Dose:
Apply small amount to affected area once or twice daily.
• Dosage Form:
Tincture (2%), povidone-iodine solution (5–10%).

20. Nystatin
• Indication:
Candidiasis (oral thrush, skin, vaginal). Antifungal.
• Contraindication:
Hypersensitivity.
• Adverse Effects:
Mild irritation, rare allergic reaction, burning, dryness, staining.
• Dose:
Apply 2–3 times daily for skin infections.
• Dosage Form:
Cream, ointment, oral suspension.( 0.1%)

21. Clotrimazole
• Indication:
Fungal infections – tinea, candidiasis, athlete's foot, vaginal yeast infection.
• Contraindication:
Hypersensitivity.
• Adverse Effects:
Burning, itching, redness, stinging.
• Dose:
Apply thin layer twice daily for 2–4 weeks.
• Dosage Form:
Cream, lotion, vaginal tablet.( 1%)
 Unit -8
Drugs used in Gastrointestinal System

A peptic ulcer is a sore or lesion that forms in the lining of the stomach, duodenum (first part of the small
intestine), or sometimes the esophagus due to the damaging effects of gastric acid and pepsin.
It occurs when the protective mucosal barrier is weakened, allowing acid to erode the lining.
Common causes:
• Helicobacter pylori infection
• NSAID use
• Excess gastric acid secretion (e.g., in Zollinger-Ellison syndrome)
• Stress, smoking, alcohol, etc.

Antiulcer Drugs:
Antiulcer drugs are medications used to prevent or treat peptic ulcers by:
• Reducing gastric acid secretion
• Neutralizing acid
• Protecting the mucosal lining
• Eradicating H. pylori infection
•
Classification

1. Drugs That Reduce Gastric Acid Secretion

a. Proton Pump Inhibitors (PPIs)
• Omeprazole
• Esomeprazole
• Pantoprazole
• Lansoprazole
• Rabeprazole
• Ilaprazole
b. H₂-Receptor Antagonists
• Ranitidine
• Famotidine
• Nizatidine
• Cimetidine
c. Anticholinergics (Antimuscarinics)
• Pirenzepine (selective M1 antagonist, rarely used)
• Propantheline
d. Prostaglandin Analogues
• Misoprostol (also protects mucosa, used with NSAIDs)
2. Drugs That Neutralize Gastric Acid (Antacids)
a. Systemic Antacids
• Sodium bicarbonate
b. Non-Systemic Antacids
• Magnesium hydroxide
• Aluminum hydroxide
• Magnesium trisilicate
• Calcium carbonate

3. Ulcer Protectives (Mucosal Protective Agents)

• Sucralfate
• Bismuth subsalicylate / Bismuth subcitrate
• Carbenoxolone (rarely used)

4. Drugs Used to Eradicate Helicobacter pylori

(Usually used in combination therapy)
• Antibiotics:
o Clarithromycin
o Amoxicillin
o Metronidazole
o Tetracycline
H2 receptor antagonist

MOA common

Step 1: H2 receptor antagonist

↓
Step 2: Competitively blocks H₂ receptor
↓
Step 3: Decrease cAMP formation
↓
Step 4: Decrease acid secretion
↓
Step 5: Healing of ulcer

1.Ranitidine
Indications:
• Treatment of active duodenal and gastric ulcers
• Maintenance therapy to prevent ulcer recurrence
• Gastroesophageal reflux disease (GERD)
• Zollinger-Ellison syndrome (A rare disorder caused by gastrin-secreting tumors (gastrinomas), usually
in the pancreas or duodenum, leading to excessive gastric acid production.)
• Erosive esophagitis(Inflammation and damage (erosions) of the esophageal lining)
• Prevention of stress ulcers in critically ill patients
Side Effects:
• Headache, Dizziness, Diarrhea or constipation
• Abdominal discomfort, Rash or itching
• Rare: gynecomastia (with prolonged use)
• Rare: blood dyscrasias (thrombocytopenia, neutropenia)
• Elevated liver enzymes (rare)
Contraindications:
• Hypersensitivity to ranitidine or other H2 receptor antagonists
• Caution in patients with severe renal or hepatic impairment
Dose and Dosage Forms:
• Adult oral dose for duodenal ulcer: 150 mg twice daily or 300 mg once at bedtime
• Adult oral dose for gastric ulcer: 150 mg twice daily or 300 mg once at bedtime
• IV dose: 50 mg every 6 to 8 hours (in hospitalized patients)
• Dosage forms: Tablets (75 mg, 150 mg, 300 mg), oral syrup, injectable solution

2.Famotidine

Indications:
• Treatment and maintenance of duodenal and gastric ulcers
• GERD and erosive esophagitis, Zollinger-Ellison syndrome
• Prevention of NSAID-induced gastric ulcers
• Stress ulcer prophylaxis in critically ill patients
Side Effects:
• Headache, Dizziness, Constipation or diarrhea, Fatigue
• Rare: rash, muscle pain, arrhythmias (IV use)
• Very rare: blood dyscrasias (agranulocytosis, thrombocytopenia)
Contraindications:
• Hypersensitivity to famotidine or other H2 blockers
• Caution in renal impairment (dose adjustment needed)
Dose and Dosage Forms:
• Adult oral dose for duodenal ulcer: 40 mg once daily at bedtime or 20 mg twice daily
• Adult oral dose for gastric ulcer: 40 mg once daily at bedtime
• GERD: 20 mg twice daily for 6 to 12 weeks
• Zollinger-Ellison syndrome: Initial 20 mg twice daily, may increase as needed
• Dosage forms: Tablets (10 mg, 20 mg, 40 mg), oral suspension, injectable solution
Proton Pump Inhibitors

MOA
Proton Pump Inhibitor (PPI) (e.g., Omeprazole)
↓
Absorbed in small intestine (Prodrug form)
↓
Enters bloodstream → reaches parietal cells in stomach lining
↓ ↓
Irreversibly binds to H+/K+ ATPase enzyme ("proton pump")
↓
Inhibits the final step of gastric acid secretion
↓
↓ Hydrogen ion (H+) secretion into gastric lumen
↓
Reduced gastric acid production → increased gastric pH

1. Omeprazole
Indications:
• Peptic ulcers (gastric and duodenal)
• GERD and erosive esophagitis
• Zollinger-Ellison syndrome
• Helicobacter pylori eradication (with antibiotics)
• Prevention of NSAID-induced ulcers
Side Effects:
• Headache
• Abdominal pain, nausea, diarrhea
• Flatulence
• Rare: Vitamin B12 deficiency (long-term use), hypomagnesemia
• Rare: Increased risk of fractures
Contraindications:
• Hypersensitivity to omeprazole or other PPIs
Dose and Dosage Forms:
• Oral: 20-40 mg once daily (can be increased for Zollinger-Ellison syndrome)
• IV form available (usually 40 mg once daily)
• Dosage forms: Capsules, tablets, oral suspension, IV injection
2. Pantoprazole
Indications:
• GERD, erosive esophagitis
• Peptic ulcer disease
• Zollinger-Ellison syndrome
• NSAID-associated ulcers
Side Effects:
• Headache
• Diarrhea, nausea, abdominal pain
• Rare: Hypomagnesemia, vitamin B12 deficiency (long-term use)
Contraindications:
• Hypersensitivity to pantoprazole or other PPIs
Dose and Dosage Forms:
• Oral: 20,40 mg once daily
• IV: 40 mg once daily (for hospitalized patients)
• Dosage forms: Tablets, IV injection
3. Rabeprazole
Indications:
• GERD and erosive esophagitis
• Peptic ulcers
• Zollinger-Ellison syndrome
• H. pylori eradication (with antibiotics)
Side Effects:
• Headache
• Diarrhea, nausea, abdominal pain
• Rare: Rash, dizziness

Contraindications:
• Hypersensitivity to rabeprazole or other PPIs
Dose and Dosage Forms:
• Oral: 20 mg once daily
• Dosage forms: Tablets, delayed-release capsules
4. Esomeprazole
Indications:
• GERD and erosive esophagitis
• Peptic ulcer disease
• Zollinger-Ellison syndrome
• H. pylori eradication (with antibiotics)
Side Effects:
• Headache
• Diarrhea, nausea, abdominal pain, flatulence
• Rare: Vitamin B12 deficiency (long-term use)
Contraindications:
• Hypersensitivity to esomeprazole or other PPIs
Dose and Dosage Forms:
• Oral: 20-40 mg once daily
• IV: 20-40 mg once daily
• Dosage forms: Capsules, oral suspension, IV injection
5. Ilaprazole
Indications:
• GERD and erosive esophagitis
• Peptic ulcer disease
• Zollinger-Ellison syndrome
Side Effects:
• Headache
• Diarrhea, nausea, abd pain, dizziness, flatulence, Rash

Contraindications:
• Hypersensitivity to ilaprazole or other PPIs
Dose and Dosage Forms:
• Oral: 10-20 mg once daily
• Dosage forms: Tablets
Triple Drug Therapy for H. pylori Eradication

Triple drug therapy is a standard treatment regimen for Helicobacter pylori (H. pylori) infection, which is a major cause of peptic
ulcer disease, gastritis, and even gastric cancer.

Components of Triple Therapy (Classic Regimen):

1. Proton Pump Inhibitor (PPI)
o e.g., Omeprazole, Esomeprazole, Pantoprazole, Rabeprazole, etc.
o Reduces gastric acid → improves antibiotic efficacy and ulcer healing
2. Clarithromycin
o A macrolide antibiotic that inhibits bacterial protein synthesis
3. Amoxicillin (or Metronidazole if allergic to penicillin)
o Amoxicillin: inhibits bacterial cell wall synthesis
o Metronidazole: disrupts DNA synthesis in anaerobic organisms

Example Regimen:
• Omeprazole 20 mg twice daily
• Amoxicillin 1 g twice daily
• Clarithromycin 500 mg twice daily
• Duration: 10–14 days (commonly 14 days for better efficacy)
•
Ulcer Protectives (Mucosal Protective Agents)

1.Sucralfate
Mechanism of Action (MOA):
• In acidic pH (<4), sucralfate undergoes polymerization to form a viscous, sticky gel
• This gel binds to ulcer base, forming a protective barrier over the lesion
• Prevents further damage by acid, pepsin, and bile salts

Indications:
• Duodenal ulcer (short-term treatment)
• Gastric ulcer
• Prevention of stress ulcers (off-label)
• GERD (mild cases or during pregnancy, as it's non-systemic)
• Mucositis (oral or esophageal, especially in cancer patients – off-label)
• Rectal ulcerations (as enema – off-label)

Dose and Dosage Forms:

• Tablet: 500 mg, 1 g
• Oral suspension: 1 g/10 mL
• Rectal suspension (off-label use)
Adult dose:
• 1 g orally, 4 times daily (1 hour before meals and at bedtime)
• Maintenance: 1 g twice daily

Adverse Drug Reactions (ADRs):

Common:
• Constipation (most frequent; due to aluminum content)
• Dry mouth
• Nausea
• Indigestion
Rare:
• Aluminum toxicity (in renal failure patients)
• Hypophosphatemia (with long-term use)
• Bezoar formation (rare; in patients with gastric stasis)

Contraindications:
• Hypersensitivity to sucralfate
• Severe chronic kidney disease (risk of aluminum accumulation)
Antiemetic drugs

Antiemetic drugs are medications used to prevent or treat nausea and vomiting caused by various conditions such
as motion sickness, pregnancy, gastrointestinal disorders, chemotherapy, or post-operative recovery.

Classification of Antiemetic Drugs :

1. Serotonin (5-HT₃) Receptor Antagonists

• Ondansetron, Granisetron, Palonosetron, Tropisetron
2. Dopamine (D₂) Receptor Antagonists
• Metoclopramide
• Domperidone
• Prochlorperazine
• Chlorpromazine
3. Histamine (H₁) Receptor Antagonists
• Promethazine, Diphenhydramine, Meclizine, Cyclizine, Dimenhydrinate
4. Muscarinic (M₁) Receptor Antagonists
• Hyoscine (Scopolamine)
5. Neurokinin-1 (NK₁) Receptor Antagonists
• Aprepitant, Fosaprepitant,Rolapitant
6. Cannabinoids
• Dronabinol, Nabilone
7. Corticosteroids
• Dexamethasone
• Methylprednisolone
8. Benzodiazepines
• Lorazepam
• Diazepam
• Midazolam
1. Metoclopramide
Mechanism of Action (MOA):
• Blocks D₂ receptors in the chemoreceptor trigger zone (CTZ) → prevents nausea and vomiting
• Enhances acetylcholine release in GI tract → increases gastric motility and emptying
• At higher doses, blocks 5-HT₃ receptors → added antiemetic effect
Indications:
• Nausea & vomiting
• Gastroparesis(Gastroparesis is a condition characterized by delayed gastric emptying)
• GERD (as prokinetic)
• Migraine-associated nausea
Dose:
• 10–15 mg orally/IV/IM 3–4 times daily before meals
• Max: 40 mg/day
• Tablets (10 mg)
• Oral solution / syrup
• Injection (IV/IM)
•
Adverse Effects:
• Extrapyramidal symptoms (Involuntary muscle spasms, tremors, rigidity, or restlessness due to dopamine receptor blockade in
the CNS)
• Tardive dyskinesia (Late-onset, often irreversible involuntary repetitive movements)
• Drowsiness
• Diarrhea
• Galactorrhea- excessive milk production unassociated preganacy.
Contraindications:
• GI obstruction
• Parkinson’s disease
• Epilepsy
• Pheochromocytoma- A rare tumor of the adrenal medulla
2. Domperidone
Mechanism of Action (MOA):
• Blocks D₂ receptors in the chemoreceptor trigger zone (CTZ) (outside blood-brain barrier)
• Increases GI motility and gastric emptying by increasing acetylcholine release
• Less CNS side effects due to poor brain penetration
Indications:
• Nausea and vomiting
• Functional dyspepsia- upper abdominal discomfort or pain, bloating, early satiety, and nausea
• Gastroparesis- Delayed gastric emptying without mechanical obstruction
• Lactation enhancement
Dose:
• 10 mg orally 3–4 times/day (before meals)
• Max: 30 mg/day
• Tablets (10 mg)
• Oral suspension / syrup
• Suppositories (less common)

Adverse Effects:
• QT prolongation (especially in elderly), Arrhythmias (rare)
• Hyperprolactinemia
• Headache, dry mouth
Contraindications:
• Prolonged QT interval
• Severe hepatic or cardiac disease
• Concomitant use with QT-prolonging drugs

3. Ondansetron
Mechanism of Action (MOA):
• Selectively blocks 5-HT₃ receptors in:
o GI tract (vagal afferents)
o Chemoreceptor trigger zone (CTZ) and vomiting center in CNS
• This prevents serotonin-mediated nausea and vomiting, especially after chemotherapy
Indications:
• Chemotherapy-induced nausea and vomiting (CINV)
• Postoperative nausea and vomiting (PONV)
• Radiation-induced nausea
Dose:
• 4–8 mg orally or IV before chemotherapy or surgery
• Repeat every 8–12 hours as needed
• Tablets (4 mg, 8 mg)
• Orally disintegrating tablets (ODT)
• Oral solution / syrup
• Injection (IV/IM)
•
Adverse Effects:
• Headache
• Constipation
• QT prolongation
• Dizziness
• Rare: serotonin syndrome
Contraindications:
• Congenital long QT syndrome
• Hypersensitivity to ondansetron

4. Promethazine
Mechanism of Action (MOA):
• Blocks H₁ receptors in the vestibular system and vomiting center
• Also blocks muscarinic (M₁) receptors in the CNS
• Strong sedative and anti-motion sickness effects

Indications:
• Motion sickness
• Nausea and vomiting
 • Allergy symptoms
• Preoperative sedation
• Vertigo
Dose:
• 12.5–25 mg orally, IM, or IV every 4–6 hours as needed
• For motion sickness: 25 mg at bedtime or 30–60 min before travel
• Tablets (12.5 mg, 25 mg)
• Syrup / oral solution
• Suppositories
• Injection (IM, IV)

Adverse Effects:
• Sedation, dizziness
• Dry mouth, blurred vision
• Urinary retention
• Respiratory depression (especially in children <2 years)
Contraindications:
• Children under 2 years (risk of fatal respiratory depression)
• Glaucoma
• CNS depression

Drugs used in constipation(Laxatives)

Definition of Constipation:
Constipation is a condition characterized by infrequent, difficult, or incomplete bowel movements. Clinically, it is often defined as
having fewer than three bowel movements per week, along with symptoms such as hard or lumpy stools, straining during defecation,
and a sensation of incomplete evacuation.

Classification of Drugs Used in Constipation:

Drugs used to treat constipation are called laxatives or cathartics, and they are classified based on their mechanism of action:
1. Bulk-forming Laxatives (Fiber supplements)
o Psyllium (Ispaghula)
o Methylcellulose
o Bran
2. Osmotic Laxatives
o Lactulose
o Polyethylene glycol (PEG)
o Magnesium hydroxide
o Magnesium sulfate
o Sorbitol
3. Stimulant Laxatives (Contact laxatives)
o Bisacodyl
o Senna
o Castor oil
4. Stool Softeners (Emollient Laxatives)
o Docusate sodium
o Liquid paraffin (mineral oil)
5. Lubricant Laxatives
o Liquid paraffin
6. Prokinetic Agents
o Prucalopride (5-HT₄ agonist)
o Itopride
7.Guanylate Cyclase-C Agonists
o Linaclotid

1. Ispaghula Husk (Psyllium)

MOA:
• It is a natural fiber that absorbs water in the intestine and swells, forming a soft, bulky stool mass.
• This increases peristalsis (reflex contractions of the bowel) and facilitates easier defecation.
Adverse Drug Reactions (Detailed):
• Bloating and flatulence: Due to fermentation by colonic bacteria.
• Abdominal distension: Common, especially when starting therapy.
• Esophageal or intestinal obstruction: If taken with inadequate water.
• Allergic reactions: Rare, can present as rash or respiratory difficulty.
 Uses:
• constipation
• Irritable bowel syndrome (IBS)( Irritable Bowel Syndrome (IBS) is a functional gastrointestinal (GI) disorder
characterized by chronic abdominal pain, bloating, and altered bowel habits (such as diarrhea, constipation, or both),
without any identifiable structural or biochemical abnormality.)
• Post-anal surgery stool regulation
Contraindications:
• Intestinal obstruction
• Fecal impaction(Fecal impaction is a condition in which a large, hardened mass of stool becomes stuck in the rectum or
distal colon and cannot be passed voluntarily.)
• Difficulty in swallowing
• Hypersensitivity to psyllium
Dose:
• Adults: 3.5–7 g (1–2 teaspoons) mixed in 150–250 mL water, once or twice daily after meals
Dosage Forms:
• Powder (for suspension)
• Granules

2. Bisacodyl
MOA:
• Directly stimulates enteric nerves in the colon, increasing peristalsis.

• Promotes accumulation of water and electrolytes in the intestinal lumen by altering mucosal fluid transport • leading to
softening of stool and increased bowel motility.

Adverse Drug Reactions (Detailed):

• Abdominal cramping
• Nausea and vomiting
• Diarrhea and dehydration: Especially with high doses.
• Electrolyte imbalance: Hypokalemia with prolonged use.
• Dependence: Risk with long-term use.
• Rectal irritation: With suppositories.
 Uses:
• Short-term relief of constipation
• Bowel evacuation before surgery, colonoscopy, or radiological exam
• Neurogenic bowel disorders
Contraindications:
• Intestinal obstruction,Acute abdominal conditions (e.g., appendicitis)
• Undiagnosed abdominal pain
• Severe dehydration
Dose:
• Oral: 5–10 mg at bedtime
• Rectal suppository: 10 mg once daily (for faster relief)
Dosage Forms:
• Tablets
• Suppositories
• Enemas
3. Lactulose
MOA:
• Not absorbed in the small intestine; reaches the colon where bacteria metabolize it to lactic acid, acetic acid, and formic acid.
• These acids draw water into the colon, softening stool and stimulating motility.
Adverse Drug Reactions (Detailed):
• Flatulence: Common initially due to fermentation.
• Abdominal cramps and bloating
• Nausea
• Diarrhea: Especially if overused or overdosed.
• Electrolyte disturbances: Hyponatremia, hypokalemia (with chronic overuse)
• Sweet taste may be intolerable for some patients.

Uses:
• Chronic constipation
• Hepatic encephalopathy (Hepatic encephalopathy is a neuropsychiatric syndrome that occurs in patients with acute or
chronic liver dysfunction, especially in cirrhosis. It results from accumulation of neurotoxic substances (especially
ammonia) that are normally cleared by the liver.)
 Contraindications:
• Galactosemia (Galactosemia is a rare inherited metabolic disorder in which the body is unable to properly metabolize
galactose, a sugar found in milk and dairy products.)
• Intestinal obstruction
Dose:
• Constipation (Adult): 15–30 mL daily, adjusted up to 60 mL/day
• Children: 5–15 mL daily (age-dependent)
Dosage Forms:
• Syrup
• Oral solution

4. Sorbitol
MOA:
• Poorly absorbed sugar alcohol that draws water into the large intestine by osmosis, softening the stool and inducing bowel
movement.
Adverse Drug Reactions (Detailed):
• Abdominal pain and distension
• Flatulence
• Nausea
• Watery diarrhea
• Dehydration and electrolyte imbalance (if overused)
• Lactic acidosis (rare) with very large doses or in renal failure
Uses:
• Occasional constipation
• Fecal impaction

Contraindications:
• Intestinal obstruction
• Anuria
• Hypersensitivity
Dose:
 • Oral: 30–50 mL of 70% solution once daily
• Rectal enema: 120 mL of 25–30% solution once daily
Dosage Forms:
• Oral liquid
• Enema solution

5. Itopride

MOA:
• Inhibits dopamine D₂ receptors and acetylcholinesterase in the GI tract.
• Enhances the release of acetylcholine, promoting gastric emptying and intestinal motility.
Adverse Drug Reactions (Detailed):
• Diarrhea and abdominal pain
• Nausea
• Headache and dizziness
• Elevated prolactin levels: Rare but may lead to gynecomastia or galactorrhea
• Fatigue
• Rarely: Allergic rash or liver enzyme elevation
Uses:
• Functional constipation
• Functional dyspepsia(discomfort or pain in the upper abdomen)
• Gastroesophageal reflux
Contraindications:
• GI hemorrhage
• Mechanical obstruction
• GI perforation
• Hypersensitivity
Dose:
• Adults: 50 mg orally 3 times a day before meals
Dosage Forms:
• Tablets
• Capsules
ANTACID
Antacids are alkaline substances that neutralize excess hydrochloric acid in the stomach, increasing gastric pH and
providing relief from symptoms of acidity such as heartburn, indigestion, and peptic ulcers.

Classification of Antacids:
1. Systemic Antacids:
These antacids are absorbed into the bloodstream after administration.
o Example: Sodium bicarbonate, potassium bicarbonate
2. Non-Systemic Antacids:
These are not absorbed from the gastrointestinal tract and act locally in the stomach.
o Examples: Magnesium hydroxide, aluminum hydroxide, calcium carbonate, calcium citrate.

MOA
Antacids are alkaline compounds that react with the strong acid (HCl) in the stomach to form water and neutral salts. This
reaction raises the pH of the stomach contents, reducing acidity.
• General reaction example:
Antacid (base)+HCl (acid)→Salt + Water

1. Magnesium Hydroxide

Indications
• Antacid for symptomatic relief of acid indigestion, heartburn, gastric hyperacidity, and peptic ulcer.
• Laxative: Used as an osmotic laxative in constipation.
• Sometimes used to neutralize stomach acid during acid-base imbalance.
Dosage Forms
• Oral suspensions (e.g., Milk of Magnesia)
• Chewable tablets
• Capsules
Dose
• Antacid: 400-800 mg orally, 1-4 times daily as needed.
• Laxative: 30-60 mL of suspension (containing 400 mg/mL), once daily at bedtime or as directed.
• Dose varies with age and clinical situation.
Adverse Drug Reactions (ADR)
• Diarrhea (most common due to osmotic effect)
• Electrolyte imbalance with prolonged use (hypermagnesemia, especially in renal impairment)
• Abdominal cramping
• Nausea
Contraindications
• Renal failure or severe renal impairment (risk of hypermagnesemia)
• Hypersensitivity to magnesium hydroxide
• Intestinal obstruction (due to laxative action)
• Caution in pregnancy/lactation (generally safe but use under medical supervision)

3. Aluminum Hydroxide

Indications
• Antacid to relieve symptoms of acid indigestion, heartburn, gastroesophageal reflux disease (GERD), and peptic ulcer.
• Used to treat hyperphosphatemia in patients with chronic renal failure by binding phosphate in the gut.
Dosage Forms
• Oral suspension
• Chewable tablets
Dose
• Antacid: 300-600 mg orally 4 times daily, usually 1-3 hours after meals and at bedtime.
• Phosphate binder: Dose adjusted according to serum phosphate levels.
Adverse Drug Reactions (ADR)
• Constipation (most common due to aluminum's effect on bowel motility)
• Hypophosphatemia with prolonged use
• Osteomalacia
• Aluminum toxicity
• Nausea, vomiting, and abdominal discomfort
Contraindications
• Hypersensitivity to aluminum hydroxide
• Severe abdominal pain of unknown cause (risk of intestinal obstruction)
• Caution in renal impairment (risk of aluminum accumulation)
• Long-term use in pregnancy only if benefits outweigh risks
 4. Sodium Bicarbonate

Indications
• Antacid for symptomatic relief of acid indigestion, heartburn, and acid reflux.
• Treatment of metabolic acidosis (systemic alkalinization) in conditions like renal tubular acidosis, diabetic ketoacidosis, or
acidosis due to poisoning.
• Urinary alkalinization to promote excretion of acidic drugs or toxins.
Dosage Forms
• Oral tablets
• Effervescent tablets
• Powder for oral solution
• Injectable form (for systemic alkalinization)
Dose
• Antacid: 325-650 mg orally every 1-2 hours as needed (maximum about 7 doses per day).
• Metabolic acidosis: Dose individualized based on blood bicarbonate levels, typically intravenous in hospital.
• For urinary alkalinization, doses vary widely depending on the target urine pH.
Adverse Drug Reactions (ADR)
• Metabolic alkalosis (if overdosed or prolonged use)
• Sodium overload leading to fluid retention, hypertension, edema
• Flatulence
• Hypokalemia with prolonged use
• Gastric distension (Gastric Distension is the abnormal enlargement or swelling of the stomach due to accumulation of gas,
fluid, or food.), bloating
Contraindications
• Metabolic alkalosis
• Severe renal impairment (risk of sodium and bicarbonate retention)
• Hypertension, heart failure, edema (due to sodium load)
• Hypersensitivity to sodium bicarbonate
• Caution in pregnancy and lactation
Indication, side effect, contraindication, dose and dosage form of:

1. Ipecacuanha

Indications
• Historically used as an emetic to induce vomiting in acute poisoning cases (within 30 minutes of ingestion).
• Note: Its use is largely obsolete and not recommended in many guidelines due to safety concerns and questionable efficacy.
Side Effects
• Prolonged vomiting leading to dehydration and electrolyte imbalance
• Drowsiness or sedation
• Diarrhea
• Aspiration pneumonia if vomiting is not controlled
Contraindications
• Ingestion of corrosive substances (acids, alkalis)
• Hydrocarbon ingestion (risk of aspiration)
• Depressed consciousness or seizure risk
• Delayed presentation (>1 hour after poisoning)
Dose
• Oral syrup: 15 mL (for adults), can be repeated once after 20 minutes if vomiting does not occur.
• Pediatric dose: 3 mL/kg (max 15 mL).
Dosage Forms
• Oral syrup
2. Loperamide
Indications
• Symptomatic treatment of acute non-specific diarrhea
• Chronic diarrhea associated with inflammatory bowel disease (IBD)
• Reduction of ileostomy output
Side Effects
• Constipation
• Abdominal cramps or pain
• Nausea
• Dizziness or drowsiness (rare)
• Risk of toxic megacolon in infectious colitis or IBD flare-ups (use cautiously)
Contraindications
• Acute dysentery, ulcerative colitis flare, bacterial enterocolitis (e.g., C. difficile)
• Children under 2 years (risk of severe adverse effects)
• Hypersensitivity to loperamide
• Abdominal pain without diarrhea of unknown cause
Dose
• Adults: Initial 4 mg orally, then 2 mg after each loose stool (max 16 mg/day)
• Children (2-12 years): 1 mg after each loose stool (max 8 mg/day)
Dosage Forms
• Tablets
• Capsules
• Oral liquid/syrup

3. Hyoscyamine
Indications
• Treatment of irritable bowel syndrome (IBS) with diarrhea and cramping
• Peptic ulcer disease (to reduce gastric motility and secretions)
• Relief of spasmodic abdominal pain and intestinal colic
Side Effects
• Dry mouth
• Blurred vision
• Dizziness
• Urinary retention
• Constipation
• Tachycardia
• Confusion, especially in elderly
Contraindications
• Glaucoma
• Myasthenia gravis
• Severe ulcerative colitis (toxic megacolon risk)
• Ileus or intestinal obstruction
• Hypersensitivity
Dose
• Adults: 0.125 to 0.25 mg orally every 4 hours as needed (max 1.5 mg/day)
• Pediatric dosing varies and requires careful adjustment.
Dosage Forms
• Tablets
• Oral syrup
• Sublingual tablets
• Injectable form

4. Sulfasalazine
Indications
• Treatment of ulcerative colitis (mild to moderate)
• Crohn’s disease (colonic involvement)
• Rheumatoid arthritis (extra-GI use)
Side Effects
• Nausea, vomiting
• Headache
• Rash and hypersensitivity reactions
• Hemolytic anemia, leukopenia, agranulocytosis (rare but serious)
• Photosensitivity
• Orange-yellow discoloration of urine and skin
• Reversible male infertility
Contraindications
• Hypersensitivity to sulfasalazine or sulfonamides
• Porphyria
• Severe hepatic or renal impairment
• Intestinal or urinary obstruction
Dose
• Ulcerative colitis: Initial 500 mg to 1 g orally 3-4 times daily (total 2-4 g/day), maintenance 2-2.5 g/day
• Dose adjustment required based on tolerance and clinical response.
Dosage Forms
• Tablets
• Extended-release tablets
Oral Rehydration Therapy (ORT)

Oral Rehydration Therapy (ORT) is the medical treatment of dehydration, especially caused by diarrhea, by giving the patient a
specific mixture of clean water, salts, and glucose (called Oral Rehydration Solution or ORS) by mouth.

Dehydration

Dehydration is a condition that occurs when the body loses more water and electrolytes than it takes in, resulting in an insufficient
amount of fluid to carry out normal body functions.

Causes of Dehydration

• Diarrhea (most common in children)

• Vomiting
• Sweating (fever, hot weather, exercise)
• Urination (due to diabetes or diuretics)
• Bleeding

• Not drinking enough water

• Difficulty drinking (e.g., illness, unconsciousness)
• Infants or elderly who depend on others for fluids

Oral Rehydration Solution (ORS)

Definition:

ORS is a pre-mixed powder containing glucose and electrolytes that, when dissolved in clean water, is used to replace
fluids and salts lost during diarrhea, vomiting, or dehydration.
WHO-Recommended ORS Composition (Low Osmolarity Formula)

Ingredient Amount per Liter Purpose

Glucose (Anhydrous) 13.5 g Enhances sodium and water absorption via co-transport
Sodium Chloride (NaCl) 2.6 g Replaces sodium and chloride lost in stool
Potassium Chloride 1.5 g Replaces potassium lost in diarrhea
Trisodium Citrate 2.9 g Buffer to correct metabolic acidosis

Indications of ORS
• Dehydration due to diarrhea (mild to moderate)
• Vomiting
• Heat exhaustion
• Cholera
• Any fluid and electrolyte loss
Contraindications of ORS
• Severe dehydration with shock (needs IV fluids)
• Inability to drink (e.g., unconscious patients)
• Intestinal obstruction
• Persistent vomiting without oral tolerance
Dosage of ORS (as per WHO guidelines)
• 1 liter of ORS solution over 4–6 hours (or as needed)
• After every loose stool:
o Children: 100–200 mL
o Adults: As much as tolerated
How to Use ORS
1. Dissolve 1 full packet in 1 liter of clean, boiled and cooled water.
2. Stir until fully dissolved.
3. Do not boil after mixing.
4. Use within 24 hours. Discard leftover solution after 24 hours.
Electrolyte Rehydration Therapy

Electrolyte Rehydration Therapy is the administration of fluids containing water, electrolytes (like sodium, potassium, chloride), and
sometimes glucose, usually by the intravenous (IV) route, to correct dehydration, electrolyte imbalance, or fluid loss.
This therapy is used when oral rehydration is not possible or in cases of moderate to severe dehydration.
1. Normal Saline (NS)
(Also called 0.9% Sodium Chloride)
Composition (per 1000 mL):

• Sodium chloride (NaCl): 9 g

• Sodium: 154 mEq/L
• Chloride: 154 mEq/L
Indications:
• Mild to moderate dehydration
• Hypovolemia (low blood volume)
• Shock
• Hyponatremia (low sodium)
• Diluent for IV medications

2. Ringer’s Lactate (RL)

Composition (per 1000 mL):

Component Amount
Sodium (Na⁺) 130 mEq
Potassium (K⁺) 4 mEq
Calcium (Ca²⁺) 2.7 mEq
Chloride (Cl⁻) 109 mEq
Lactate 28 mEq
Lactate is converted to bicarbonate in the liver → helps correct metabolic acidosis
 Indications:
• Burns
• Trauma
• Dehydration with acidosis
• Diarrhea with fluid loss
• Surgical fluid replacement
• Acute blood loss

3. Dextrose Normal Saline (DNS)

(5% Dextrose in 0.9% Sodium Chloride)

Composition (per 1000 mL):

• Dextrose: 50 g (5%)
• Sodium chloride: 9 g
• Sodium: 154 mEq/L
• Chloride: 154 mEq/L
• Calories: ~170 kcal

Provides energy (calories) along with fluid and electrolytes.

Indications:

• Dehydration with hypoglycemia

• Postoperative fluid therapy
• Fluid loss with mild calorie requirement
• Hypernatremia (as it dilutes sodium)
• Not preferred in diabetes or brain injury due to glucose content