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Chapter 3 (Nervous System Vol II) (Encrypted)

The document discusses analgesics and anesthetics, detailing their classifications, mechanisms of action, and indications. It highlights the differences between opioid and non-opioid analgesics, the role of NSAIDs, and the importance of general anesthetics in surgical procedures. Additionally, it addresses potential adverse effects, contraindications, and the responsibilities of healthcare professionals in managing these medications.

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0% found this document useful (0 votes)
21 views87 pages

Chapter 3 (Nervous System Vol II) (Encrypted)

The document discusses analgesics and anesthetics, detailing their classifications, mechanisms of action, and indications. It highlights the differences between opioid and non-opioid analgesics, the role of NSAIDs, and the importance of general anesthetics in surgical procedures. Additionally, it addresses potential adverse effects, contraindications, and the responsibilities of healthcare professionals in managing these medications.

Uploaded by

Maheboob Sutar
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PDF, TXT or read online on Scribd
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UNIT

3
DRUGS ACTING ON
NERVOUS SYSTEM
ANALGESICS AND ANAESTHETICS
ANALGESICS
❑ Pain is the most common symptom which brings the patient to a
hospital.
❑ The word “algesia” means “pain” and word “analgesia” means
“absence of pain”.
❑Drugs which are used to bring relief from pain are non-steroidal anti-
inflammatory drugs (NSAIDs) called analgesics.
Analgesic drugs may be of two types:

❑Opioids analgesics: Drugs which cause sedation and are used for
moderate to severe type of pain. e.g. Morphine.

❑Non-opioids analgesics: Drugs which don’t cause sedation and are


used for mild to moderate type of pain. e.g., NSAIDs.
Role of Prostaglandins (PGs) in the body
Pathological: Pain, Fever, Inflammation, Asthma, Ulcers, Diarrhea,
Dysmenorrhea.
Physiological: Temperature control, Bronchial tone, Intestinal
mobility, Myometrial tone Labor, Semen viability.
Characteristics of NSAIDs
❑ NSAIDs are NOT steroids.
❑They are weak analgesics than opioid/narcotic analgesics.
❑NSAIDs do not have any central depressant or sedative activity.
❑They have additional anti-inflammatory, antipyretic effects.
❑NSAIDs do not cause any physical dependence, thus, have no abuse
liability.
Pharmacological actions of NSAIDs
Anti-inflammatory Action
Arachidonic acid with help of cyclooxygenase (COX), is converted to
prostaglandins (PG). PGs play a very important role in causing
inflammation. NSAIDs exert anti-inflammatory action by inhibiting
enzyme cyclooxygenase (COX) and hence inhibit PG synthesis.
Antipyretic Effect
NSAIDs exert antipyretic effect by inhibiting PGE2 synthesis - by
increasing dissipation of heat through vasodilatation of superficial
blood vessels, which leads to profuse sweating. NSAIDS lower the
body temperature only when it is raised.
Classification of NSAIDS
I. Non-selective COX Inhibitors
Salicylates
Propionic acid derivative
Anthranilic acid derivatives
Acetic acid Derivative
II. Preferential COX-2 Inhibitors
III. Analgesic-Antipyretic with Poor Anti-inflammatory Action
IV. Selective COX-2 Inhibitors
Harmful Effects due to PG Synthesis Inhibition
✓Gastric mucosal damage.
✓ Renal effect- sodium retention and edema.
✓Asthma and anaphylactoid reactions-due to diversion of arachidonic
acid to LOX pathway.
Indications
✓Antipyretic
✓Analgesic
✓Anti-inflammatory
✓Anti-platelet
Adverse Effects
❑Gastric mucosal damage- nausea, vomiting, epigastric distress, occult blood
loss and peptic ulceration, dyspepsia, bleeding.
❑Frontal headache (especially with indomethacin).
❑Hypersensitivity reactions.
❑Renal toxicity.
Drug Interactions
❑NSAIDs + Probenecid: may cause decrease in uricosuric effect of Probenecid
as Aspirin inhibits secretion of uric acid. However, aspirin is uricosuric at
>5g/day.
❑NSAIDs + Lithium increases lithium toxicity.
❑ NSAIDs + Oral Antidiabetic drugs increases risk of hypoglycemia.
Contraindications
❑Hypersensitivity
❑Peptic ulcer
❑Bleeding tendency
❑Children with varicella, influenza
❑Chronic liver disease
Drug Toxicity
GI bleeding, hypertension, hepatotoxicity, and renal damage, anion gap
metabolic acidosis, coma.
Selective COX 2 Inhibitors
✓Also called as COXIBs.
✓Celecoxib, rofecoxib, valedocoxib.
✓Highly selective for COX2.
✓ Incidence of gastric ulcer are less than other NSAIDs. (Gastric
ulcers are due to COX-1 inhibition in gastric cells).
ANTIPYRETIC
Paracetamol is acetaminophen. It is commonly used as Over The Counter (OTC)
drug for pain, headache and dysmenorrhea, osteoarthritis. It is available as crocin/
paracetamol 500 mg, 1000 mg/650 mg.
Paracetamol
This drug have prompt antipyretic effect but weak anti-inflammatory effect. It
does not have any effect on respiration, cardiovascular system, platelet
aggregation, clotting factors and acid base balance, but it has insignificant gastric
irritation.
Administration: Oral, Rectal, Intravenous
Mechanism of Action
Acetaminophen is thought to inhibit the synthesis of prostaglandins in the central
nervous system, leading to its analgesic and antipyretic effects. The analgesic
properties may be due to a stimulating effect on the descending serotonergic
pathways in the central nervous system (CNS).
Side Effects
❑Skin rash, hypersensitivity reactions.
❑Nephrotoxicity (elevations in BUN, creatinine).
❑Hematological: anemia, leukopenia, neutropenia,
❑pancytopenia.
Indications

Acetaminophen is a non-opioid analgesic and antipyretic agent used to


treat pain and fever. Clinicians can use it for their patients as a single
agent for mild to moderate pain and in combination with an opioid
analgesic for severe pain.

Contraindications

Hypersensitivity to acetaminophen, severe hepatic impairment, or


severe active hepatic disease.
OPIOIDS & OTHER CENTRAL ANALGESICS
Natural source of morphine and Codeine: Opium Poppy
(Papaver somniferum).
Classification
Morphine, Codeine, Pethidine, Methadone, Tramadol
Morphine
❑CNS actions: Stimulant or depressant
✓Depressant action:
❖Analgesia: Strong analgesic, increases threshold of pain. Degree increases
with dose.
❖ Sedation
❖Mood calming effect: Pleasurable for addicts and patients in pain or
anxiety.
✓Stimulant action:
❖ Chemoreceptor Trigger Zone : Cause Nausea and vomiting.
❖Edinger Westphal Nucleus: Miosis (not on topical application).
❖Vagal Center : Bradycardia.
Administration
Orally (PO), Intravenously (IV), Epidural, Intrathecal.
Uses: Pre-anesthetic medication, Balanced anesthesia and surgical
analgesia, Relief of anxiety and apprehension.
Contraindications
GI obstruction, respiratory depression, asthma, hypersensitivity
reaction.
Adverse Effects
Sedation, mental clouding, lethargy, vomiting, constipation,
respiratory depression, blurring of vision, urinary retention, itching (at
site of injection).
Opioid Dependence
✓Opioid addiction causes both psychological and physical
dependence. There is intense craving in morphine addicts/dependent
patients.
✓On sudden stoppage of opioid in these patients, there occurs
withdrawal symptoms (Abstinence syndrome). The patient may have
irritability, yawning, anxiety, body shakes, gooseflesh, tremors,
restlessness, lacrimation, sweating, fever, diarrhoea, dehydration,
abdominal colic, palpitation, insomnia, rise in BP, mydriasis, loss of
weight, tremors.
Opioid drugs: Methadone, Codeine, Pethidine, Pentazocine
Drug Toxicity
Severe respiratory depression is the most feared complication of
morphine in cases of overdose.
Drug Interaction
❑When morphine is combined with other opioids or sedatives, it can
cause increased sedation, respiratory depression, and even coma.
❑MAOIs, a type of antidepressant, can interact with morphine and
cause potentially life-threatening side effects such as hypertensive
crisis and serotonin syndrome. Patients taking MAOIs should avoid
morphine.
Naloxone
It is competitive antagonist on all types of opioid receptors. It has no
agonistic action and it does not cause dependence and have no subjective
effect. It is not orally effective and given intravenously.
Dose/administration
Naloxone administration is usually via IV, but if no IV access is available, it
can also be administered via an IO line, subcutaneously (SQ), IM, or via the
intranasal (IN) route.
A small initial dose, usually 0.04 mg to 0.1 mg IV, is recommended in
opioid-dependent patients with symptoms of opioid overdose to avoid
opioid withdrawal symptoms.
Side effects/ Adverse effects
anxiety, aggression, nausea, vomiting, diarrhea, abdominal pain, and
rhinorrhea. In rare cases, the use of naloxone can precipitate
noncardiogenic pulmonary edema.

Mechanism of action
Naloxone is a pure, competitive opioid antagonist with a high affinity
for the mu-opioid receptor, allowing for reversal of the effects of
opioids. The onset of action varies depending on the route of
administration but can be as fast as one minute when delivered
intravenous (IV) or intraosseous (IO).
Drug interaction
Naloxone may be less effective in reversing the effects of opioids if the
patient has taken an opioid agonist, such as methadone, buprenorphine.

Nurses responsibilities
-Nurses are responsible for monitoring the patient's response to
treatment and administering additional doses as necessary.
-Nurses are responsible for monitoring the patient's response to
treatment and administering additional doses as necessary.
-Nurses must monitor patients who have been treated with naloxone
for signs of relapse, withdrawal symptoms, or adverse reactions to the
medication.
GENERAL ANESTHETICS
It is defined as drug that brings about a reversible loss of
consciousness and all sensations. It is administered to
induce or maintain general anesthesia to facilitate surgery.
Essential Components of Anesthesia
•Analgesia: Perception of pain is eliminated
•Hypnosis-unconsciousness
•Muscle relaxation
•Depression of reflexes
Stages of General Anesthesia

❑Stage 1: Analgesia phase- the patient will be unconscious, heart rate,


blood pressure and respiration will be more than normal.
❑Stage 2: Excitement phase- the patient will have loss of
consciousness and vital signs will be increased.
❑ Stage 3: Surgical phase- the patient will be unconscious and surgery
is going on.
❑ Stage 4: Medullary phase- this is toxic and dangerous phase. Patient
should not go in this phase as respiratory/cardiac arrest can occur.
Classification of General Anesthetic Drugs
❑Inhalational Drugs
❑Intravenous Drugs
✓Inducing agents: Thiopentone sodium, Propofol, Etomidate
✓Slower acting agents: Ketamine, Benzodiazepines
Phases of Anesthesia
During surgery, general anesthetic drugs are given in two phases:
•Induction phase: Intravenous anesthetic drugs are given at the start
of surgery.
•Maintenance phase: Inhalational drugs are for maintaining
anaesthesia during surgery.
General Actions of Anesthetics

•Respiration: Depressed respiration and response to CO2.

• Kidney: Depression of renal blood flow and urine output.

•Muscle: High enough concentrations will relax skeletal muscle.

•Cardiovascular system: Generalized reduction in arterial pressure and


peripheral vascular resistance. Isoflurane maintains CO2 and coronary
function better than other agents.
Adverse Effects
Fall in BP, arrhythmias, respiratory depression, asphyxia, laryngospasm,
salivation, delirium, convulsions. Nausea, vomiting, pneumonia, sedation,
Hepatic toxicity, Renal toxicity (with methoxyflurane), Nerve palsy.
Role of a Nurse
•Administer these medications at time as prescribed.
•Exact time of drug administration should be recorded on patient's record that has
to go inside operation theatre.
•Monitor vital signs of the patient.
Preoperative Medication/Pre-anaesthetic Medication (PAM)

These medications are given prior to inducing general or local anesthesia. Opioids,
benzodiazepines, and anticholinergic drugs or antibiotics may be given to the patient, so that

✓ The patient will be stress free and calm.

✓ Help in provide general anesthesia.

✓ Counteract adverse effects of general anesthesia.

✓These drugs are given to make the experience of the patient more pleasant & safe, as it:

❖Ensures patient’s comfort

❖Minimize adverse effects of anesthetic drugs


Drugs used in pre-anesthetic medication are given:

❑Antihistaminics/Proton Pump Inhibitors: Ranitidine, Omeprazole

❑Anticholinergics: Glycopyrrolate, hyoscine

❑Sedative and hypnotics: Benzodiazpeines like diazepam

❑Analgesics: NSAIDs, opioids

❑Anti-emetics: Domperidone, metoclopramide

❑Neuroleptics: Haloperidol, chlorpromazine


Antihistaminic drugs (H2 blockers)/Proton Pump Inhibitors:

❑Ranitidine, Famotidine, Omeprazole.

❑Given one night before and in morning.

Anticholinergic drugs (Glycopyrolate, Atropine/ Hyoscine)

Uses: Reduce salivary and tracheobronchial secretions, prevent vagal bradycardia and
hypotension, prophylaxis of laryngospasm.

Sedative hypnotics (Benzodiazepines like diazepam, lorazepam, midazolam)

Uses: To produce tranquility, smoothen induction and to induce post-operative amnesia.


Analgesics (NSAIDs like diclofenac, Opioids like Morphine, Pethidine)

Uses: Allay anxiety and apprehension, pre- and post-operative analgesia,


smoothen induction, reduce the anesthetic dose.
Inhalational Anesthetics
Oxygen
❑Oxygen is not typically used as a general anesthetic gas on its own. Instead, it
is often used as a carrier gas to deliver other anesthetic gases, such as nitrous
oxide or volatile anesthetics like sevoflurane or desflurane.
❑Anesthetic gases work by depressing the central nervous system, reducing
consciousness and pain perception. However, they can also depress respiratory
function, so oxygen is added to ensure that the patient maintains adequate
oxygenation.
❑ While oxygen itself is not an anesthetic gas, it is an important component of
general anesthesia because it helps to prevent hypoxemia, which is a decrease
in the concentration of oxygen in the blood. Hypoxemia can lead to serious
complications, such as brain damage, heart failure, and even death. Therefore,
oxygen is essential during general anesthesia to ensure that the patient's body is
receiving enough oxygen to function properly.
It's important to note that while oxygen is essential during anesthesia, too much
oxygen can also be harmful. High concentrations of oxygen can cause oxygen
toxicity, which can damage the lungs and other organs. Therefore, the amount of
oxygen administered during anesthesia must be carefully monitored to ensure
that the patient is receiving enough oxygen, but not too much.
Carbon dioxide
Carbon dioxide is not typically used as a general anesthetic gas to produce
unconsciousness or pain relief during surgery. It has important physiological
effects on the body. For example, inhaled carbon dioxide can cause blood vessels
to dilate, which can increase blood flow to certain tissues. Carbon dioxide can
also stimulate the respiratory drive, which can be useful during certain types of
surgery where the patient's breathing must be temporarily interrupted.
Nitrous Oxide (N2O)
❑ Laughing gas
❑ Colorless, odorless, cheap.
❑ Commonly used
• It is poor muscle relaxant, so neuromuscular blockers often required.
• Weak anesthetic, powerful analgesic other agents are required for surgical
anesthesia
• Second gas effect and diffusion hypoxia (only with N2O).
Ether
❑ Colorless, highly volatile liquid, inflammable and explosive, often given by
open drop method.
❑ Cheap and relatively safe.
❑Explosion risk (diathermy cannot be used).
❑Not used normally except in periphery.
Halothane
❑Not a good analgesic (use N2O/opioids) or muscle relaxation (use
neuromuscular blockers).
❑ 20% metabolized in liver, rest exhaled.
❑Direct depression of myocardial contractility decreases cardiac output and
heart rate.
❑Sensitizes heart to arrhythmogenic action of adrenaline.
Enflurane
•Potent anesthetic.
•Better muscle relaxation than halothane.
•Slight decrease in cardiac output, heart rate and blood pressure.
• Greater depressant action on respiration, assistance needed.
Intravenous Agents
Used in combination with inhaled anesthetics to:
Supplement general anesthesia:
•Maintain general anesthesia
• Provide sedation
•Control blood pressure
•Protect the brain
Inducing Agents
Thiopentone
Ultra short acting barbiturate
•Commonest inducing agent.
• Crosses BBB rapidly.
• Short effect due to redistribution.
Etomidate
• Minimal cardiovascular effects.
•Potential adrenocortical suppression (0.2-0.5 mg/kg).
Balanced Anesthesia

❑There is combination of intravenous & inhalational anesthetic agents.

❑The combination is used taking advantage of their favourable properties and


minimizing their adverse effects.

First intravenous agents and then, inhalational anaesthetic agents are used:

❖Inducing agent: Intravenous (Thiopentone sodium).

❖Maintained by inhalational anesthetic.

❖Supplemented by benzodiazepines.
LOCAL ANESTHESIA (LA)

• Drugs for topical/local application with reversible loss of sensory perception in


a restricted area of body.

• Block nerve impulse at all part of neuron in contact, that is loss of sensory,
motor and autonomic control.

Classification of Local Anesthesia

Procaine, Chlorprocaine, Lignocaine, Prilocaine, Tetracaine, Bupivacine,


Benzocaine
Mechanism of Action
Inhibit or decrease the entry of Na+ ion during upstroke of action potential.
Thus, block action potential generation by blocking Na+ channels.
Adverse Effect
Toxicity dependent upon rate of absorption and metabolism.
❑ CNS effects: Light headedness, dizziness, visual disturbances, mental
confusion, shivering, involuntary movements, convulsion, respiratory arrest.
❑ CVS: Bradycardia, hypotension, arrhythmia.
❑Local: Painful, delayed wound healing. Addition of vasoconstrictor may cause
necrosis of hands, feet, fingers, toes, penis and pinna of ear.
❑Hypersensitivity with esters.
Indications
•Minor surgeries.
•Diagnostic procedures (biopsies, lumbar punctures, and endoscopies).
Contraindications
• Cardiovascular disease
•Hepatic disease
•Renal dysfunction
•History of allergy to any of constituents of local anesthetics.
Drug Interaction

❑MAO inhibitors

❑Anticoagulants

❑opioids, benzodiazepines, and muscle relaxants.

Uses and Techniques of Local Anesthesia: Surface anesthesia, Infiltration

anesthesia, Conduction block, Spinal anesthesia, Epidural anesthesia.


SEDATIVE-HYPNOTICS
Definition
❑Sedative: Decreases excitement and calms a person without inducing sleep.
❑Hypnotic: Induces or maintains sleep.
Classification
Barbiturates
Long acting (DOA: 12-16 hours)
Short acting (DOA: 2-3 hours)
Ultra-short acting (DOA: 15-30 min)
Benzodiazepines
Hypnotics
Antianxiety
Non-Benzodiazepines
Melatonin and its congeners
Barbiturates
Barbiturates are a group of sedative-hypnotic medications used for treating
seizure disorder, insomnia, preoperative anxiety, and induction of coma for
increased intracranial pressure. They are also useful for inducing anesthesia.
Uses
•Phenobarbitone: Epilepsy
• Thiopentone: In general anesthesia, as a inducing agent (ultra short acting).
Adverse effects
drowsiness, hangover, vertigo, marked respiratory depression, amnesia, impaired
judgement, renal failure, coma.
Benzodiazepines
Barbiturates are a group of sedative-hypnotic medications used for treating seizure
disorder, neonatal withdrawal, insomnia, preoperative anxiety, and induction of coma
for increased intracranial pressure. They are also useful for inducing anesthesia.
Mechanism of Action
✓Acts on GABA-BZD receptor Cl- channel complex → increase the frequency of Cl-
channel opening induced by GABA.
✓ At high concentrations may be GABA-mimetic.
Indications
✓Insomnia
✓Anxiety disorder
✓Preoperative sedation
✓Restless leg syndrome
✓Muscle spasm tension
✓ Epilepsy
✓Panic disorder
Adverse effects: Sedation or even euphoria, drowsiness, confusion, impaired
motor co-ordination, impaired learning, restlessness, delirium may occur on
therapeutic dose.

Drug Toxicity
Overdose: Taking too much benzodiazepine can lead to an overdose, which can
cause respiratory depression, coma, and even death.
Cognitive impairment: This can lead to problems with memory, attention, and
executive function.
Respiratory depression: Benzodiazepines can cause respiratory depression,
particularly when taken in high doses or in combination with other substances
that depress the central nervous system.
Newer Sedative Hypnotics
Zaleplon, Zopiclone and Zolpidem (Z-drugs)
Non-Benzodiazepines or Type 1 Benzodiazepines receptor agonists.
•These drugs have anticonvulsant, muscle relaxant effect but have less anxiolytic
effect.
•Less rebound, tolerance and risk for dependence.
Nursing Responsibilities
❑Advise the patient to take medicine with food to prevent GI disturbances.
Patient has to swallow the sustained release tablet as a whole.
❑ Advice the patient that he should not drive and indulge in hazardous activity
as these drugs can cause CNS depression.
❑Patient has to inform immediately to the physician if he experience
excitement, rage and extreme anxiety.
❑ Advice the patient to avoid alcohol and other opioids as they all are CNS
depressants.
MUSCLE RELAXANTS
Skeletal Muscle
❑ Contraction is under voluntary control.
❑ Contraction controlled by the nervous system.
Action of Skeletal Muscle Relaxants
❑Most relaxants
❑Work in the brain and spinal cord.
❑Interfere with cycle of muscle spasm and pain.
❑Botulinum toxins and dantrolene: Enters muscle fibers directly.
Indications
❑Relief of painful musculoskeletal conditions.
❑Muscle spasms
❑Management of spasticity of severe chronic disorders.
Classification of Musculoskeletal Drug
Agents/Skeletal Muscle Relaxants (SMRs)
▪ Peripherally acting SMRs
❑Neuromuscular Blocking Agents (NMBAs).
❑Directly acting agents: Dantrolene.
▪ Centrally acting SMRs: Diazepam, Methocarbamol, Chlorzoxazone, Tizanidine,
Baclofen, Gabapentin.
Neuromuscular Blocking Agents Dose
✓Non depolarizing: (competitive)
▪ Long acting: d-tubocurarine, Pancuronium (2mg/ml Injection), Doxacurium.
▪ Intermediate acting: Vecuronium (4 mg/ampoule), Atracurium (10 mg/ml Injection).
▪ Short acting: Mivacurium
✓Depolarizing type (Non Competitive)
▪ Succinylcholine (50 mg/ml Injection), Decamethonium
Adverse Effects/Side Effects
Respiratory paralysis
Fall in BP
Tachycardia
Cardiac arrhythmias
Post operative muscle soreness
Uses
All are given IV.
❑ In surgeries: As an adjuvant to general anesthesia.
❑ Electroconvulsive therapy (SCh).
❑ Severe tetanus.
❑ Complicated status epilepticus.
Drug Toxicity
✓Prolonged paralysis.
✓Anaphylactic reactions.
✓Cardiovascular toxicity (including hypotension, bradycardia, and arrhythmias).

Contraindications
✓Myasthenia gravis
✓Hypersensitivity
Directly Acting Muscle Relaxants
Example/Dose
Dantrolene (25-100 mg four times a day).
Mechanism of Action
Decreases calcium from sarcoplasmic reticulum, does not effect neuromuscular
junction.
Side Effects
Muscle weakness, sedation, lightheadedness, malaise.
Uses
✓ Drug of choice for malignant hyperthermia (given IV)
✓Upper motor neuron disorder
✓Hemiplegia
✓Paraplegia
✓ Cerebral Palsy
✓Multiple sclerosis
Drug Toxicity
✓ Respiratory depression
✓ Hypotension, bradycardia, and tachycardia
✓ Prolonged paralysis
✓Myopathy
✓Allergic reactions
Centrally Acting Muscle Relaxants
Classification/Dose
•• Mephensin group
➢Mephensin, Carisoprodol (350 mg three times to four times daily).
➢Cholorzoxanone (250-500 mg three to four times daily).
➢Chlormezanone (100-200 mg three times a day).
➢Methocarbamol (500 mg three times daily).
•• GABA agonist
➢Baclofen (10-25 mg two to three times daily).
•• Central α2 agonist
➢Tizandine (2 mg three times a day).
•• Benzodiazepines
➢Diazepam (5 mg three times a day; 10-40 mg IV route).
Mechanism of Action
✓Depress reflex impulse conduction within SC.
✓ Decrease number of impulses (CNS) available to produce contract.
✓ Inhibits reflexes at the spinal level.
✓Do not alter function of skeletal muscle fibers.
✓ Typically used with analgesics.
Uses
✓Acute muscle spasm
✓Torticollis, lumbago, backache
✓Anxiety and tension (Cholrmezanone)
Contraindications
Hypersensitivity, Hepatic impairment, Renal impairment, Cardiovascular
disease
DRUGS USED IN PSYCHIATRY
Antipsychotic Drugs
It also called as Psychotropics/Neuroleptics/Major tranquilizers. Neuroleptics are
used to treat and manage symptoms of many psychiatric disorders.
They fall into two classes:
1. First-generation or “typical” antipsychotics.
2. Second-generation or “atypical” antipsychotics.
Both first and second-generation antipsychotics are used in various
neuropsychiatric conditions.
Drug toxicity
➢Hepatotoxicity.
➢ CNS depression (Sedation, drowsiness, and impaired cognitive function).
➢ Renal toxicity.
➢ Allergic reactions.
Role of nurse
➢Assessment of the patient must be done for pain, muscle stiffness, and range of
motion before and periodically throughout therapy.
➢Provide safety measures as indicated and supervise ambulation and transfer of
patients.
➢Encourage the patient to comply with additional therapies prescribed for
muscle spasm (rest, physical therapy, heat).
Classification/Dose/Route
Antipsychotic medications can be administered through different routes, including oral, intramuscular (IM), and
intravenous (IV) administration.
•Phenothiazines
Chlorpromazine (100-800 mg per day)
Triflupromazine (10-30 mg per day)
Thioridazine (100-400 mg per day)
Trifluoperazine (5-10 mg per day)
• Butyrophenones
Haloperidol (2-20 mg per day)
Droperidol, Penfluridol (20-60 mg once weekly)
• Thioxanthenes: Thiothixene, Flupenthixol (3-5 mg per day)
• Other heterocyclics
Pimozide (2-6 mg per day)
Loxapine (10-100 mg per day)
Reserpine
• Atypical neuroleptics
Clozapine (2.5-10 mg per day)
Pharmacological Actions
Central Nervous System
In Psychotics: Reduces irrational behavior, agitation, aggression, psychotic
symptomatology. There is normalization of thought and behavior, reduced
hallucination and delirium–action takes weeks to develop.
Autonomic Nervous System
α adrenergic blocking activity, weak anticholinergic action, antihistaminic and
anti 5-HT action.
Cardiovascular System
Hypotension, reflex tachycardia, high dose produce – QT prolongation.
Indications
• Psychoses (Schizophrenia)
• Mania: For rapid control.
•Organic brain syndrome: To avoid mental confusion, hypotension, and
prophylaxis treatment of seizure.
•Anxiety, antiemetic

Contraindications
Liver damage, coronary artery disease, cerebrovascular disease, parkinsonism,
bone marrow depression.
Drug Toxicity
Extrapyramidal symptoms include acute dystonia (tongue protrusion, facial
grimacing, trismus, and oculogyric crisis) and akathisia (feeling of inner
restlessness). Tachycardia, dry mucous membranes, dry skin, decreased bowel
sounds, and delirium.
Adverse Effects
CNS: Drowsiness, lethargy, mental confusion, increased appetite, weight gain,
aggravation of seizures.
α adrenergic blockade: Postural hypotension, palpitation, inhibition of
ejaculation.
Anticholinergics: Dry mouth, blurring of vision, constipation, urinary
hesitancy.
Extrapyramidal Disturbances
Parkinsonism
Acute Muscular Dystonia
Malignant neuroleptic syndrome
Tardive dyskinesia
Nursing Responsibilities
•Advise the patient and their attendants to take the medicine as prescribed, it
should not be changed at own will without consulting the physician.
• Oral preparation should be protected from light. Patient can dilute the
concentrated solution with juice to improve taste.
•Advice the patient to clean the area immediately if liquid preparation spills as it
can cause contact dermatitis.
•Advise the patient to observe extrapyramial symptoms like parkinsonism, acute
muscular dystonia, malignant neuroleptic syndrome.
Antianxiety Drugs
Antianxiety drugs, also known as anxiolytics, are medications that are used to
treat anxiety disorders and other conditions that involve anxiety. These
medications work by reducing excessive activity in the central nervous system,
which can help to decrease feelings of anxiety and promote relaxation.

Classification/Dose
•Benzodiazepines: Diazepam (5-20 mg per day), Chlordiazepoxide (25-100 mg
per day), Alprazolam (0.25-1 mg per day), Lorazepam (1-6 mg per day),
Oxazepam (30-60 mg per day).
•Azapirones: Buspirone (5-15 mg once-thrice daily), Gepirone, Ispapirone.
•Beta blockers: Propanolol.
Benzodiazepines
•Act through GABAA receptor: Cl– channel complex –opening of chloride
channels hyperpolarization decreased firing rate of neurons.
•CNS depressants: Occurs at low dose, relieve anxiety, more selective on limbic
system, at low dose, less CVS and respiratory depression.
•Better than barbiturates: Little effect on other body system, lower
dependence producing liability, less withdrawal symptoms, relatively safe in
gross overdose.
•Adverse effects: Sedation, light headedness, psychomotor and cognitive
impairment, vertigo, confusional state, increased appetite, altered sexual
function.
Side Effects/Adverse Effects
Drowsiness, Dizziness, Fatigue, Headache, Nausea, Blurred vision, Dry mouth,
Constipation, Sexual dysfunction.

Mechanism of Action
The most common mechanism of action among antianxiety drugs is the
enhancement of the activity of the neurotransmitter gamma-aminobutyric acid
(GABA) in the brain. Benzodiazepines, which include medications such as
alprazolam, clonazepam, diazepam, and lorazepam, work by binding to specific
GABA receptors and increasing the activity of GABA. This results in a calming
effect, reduces anxiety, promotes relaxation, and can also induce sleep.
Indications
•Generalized anxiety disorder
•Panic disorder
•Post-traumatic stress disorder
•Obsessive-compulsive disorder
Contraindications
•Hypersensitivity to the drug or any of its components.
Drug Toxicity
•Confusion
•Drowsiness
•Difficulty breathing
•Loss of consciousness
•Seizures
•Irregular heartbeat
•Nausea and vomiting
•Blurred vision
Antimaniac drugs (mood stabilizers)
Mood stabilizers are a class of medications used in the management and
treatment of bipolar disorder. They work by regulating the levels of
neurotransmitters in the brain, such as serotonin and dopamine, which can affect
mood and behavior.
Lithium Carbonate (750-2000 mg per day)
Action
CNS: No acute effect. On prolonged administration. Lithium acts as mood
stabilizer, gradually suppress the episode taking 1-2 weeks, normalizes sleep
time.
Indications
•Acute manic episode (neuroleptic with benzodiazepines by IM/IV route).
•Prophylaxis in BPD (bipolar disorders).
•Inappropriate ADH secretion.
Contraindications
•Patients over the age of 60 and those with renal failure.
•Cardiac failure
•Pregnancy
Adverse Effects
•Initial (nausea, vomiting, diarrhea).
•Thirst and polyuria, fine tremor and seizures.
Drug Toxicity
•Lithium: Tremors, twitching, drowsiness, a feeling of sluggishness, vomiting,
diarrhea, and loss of appetite.
•Valproic acid: Toxicity is manifested most commonly as central nervous system
depression and potential cerebral edema, potentially leading to coma and
respiratory depression.
Antidepressants
Introduction
•Depression is feeling of sadness, loss of interest, self neglect, anorexia, sleep
disturbances. There may be suicidal feelings in severe cases of depression.
•Antidepressants are agents used to treat depression. They affect monoaminergic
transmission in the brain.
Classification/Dose
•Reversible Inhibitor of MOA-A (RIMA): Moclobemide
(150-300 mg twice-thrice daily), Clorgyline
•Tricyclic Antidepressants (TCA)
Imipramine (50-200 mg per day)
Amitryptiline (50-200 mg per day)
Dothiepin (50-150 mg per day)
Desipramine, Nortryptiline (50-150 mg per day)
Amoxapine (100-300 mg per day)
•Selective Serotonin Reuptake Inhibitor (SSRI)
Fluoxetine (20-50 mg per day)
Citalopram (20-40 mg per day)
Sertraline (50-200 mg per day)
Paroxetine (20-50 mg per day)
•Atypical Antidepressants
Mirtazapine (15-45 mg per day)
Venlafaxine (75-150 mg per day)
Bupropion (150-300 mg per day)
Trazodone (50-200 mg per day)
Indications
Depressive disorders include unipolar major depression, persistent depressive
disorder (dysthymia), premenstrual dysphoric disorder, and depressive disorder
due to another medical condition.
Contraindications
• Seizure disorder.
•Liver injury.
•Aneurysmal vascular disease.
Adverse Effects
Sexual dysfunction, drowsiness, weight gain, insomnia, Potential for serotonin
syndrome anxiety,

US Boxed Warning (FDA).


Suicidal thoughts and behaviors: Antidepressants increased the risk of suicidal
thoughts and behavior in pediatric and young adult patients. Closely monitor all
antidepressant-treated patients for clinical worsening and the emergence of
suicidal thoughts and behavior.)
Nursing Responsibilities for Antidepressants

•Advise the patient to take medicine as prescribed.

•After starting the antidepressants drugs, patient may feel sleepy but after few
weeks this effect will be less.

• Products containing caffeine, like tea, coffee and cola and cigarette smoking
should be avoided as these products decrease the efficacy of these drugs.
DRUGS USED IN EPILEPSY
Classification/Dose of Anti-epiletic Drugs
• Barbiturates: Phenobarbitone (30-60 mg once to thrice daily; 100-200 mg by
IM/IV).
• Deoxybarbiturates: Primidone (250-500 mg twice daily).
• Hydantoin: Phenytoin (100 mg twice daily), Fosphenytoin (20 mg/kg IV
route).
• Iminostilbene: Carbamazepine (200-400 mg thrice daily).
• Succinimide: Ethosuximide (20-30 mg/kg/day).
• Aliphatic carboxylic acid: Valproic acid (200-600 mg thrice daily).
Indications
➢Seizures.
➢Certain seizure medications have been used off-label for a variety of other
indications, including but not limited to: Mood stabilizer.
➢Neuropathic pain relief.
➢Antiparkinsonian agent.

Side Effects/Adverse Effects


Headaches, fatigue, dizziness, blurry vision, nausea, weight gain or loss, mood
disorders, and neurocognitive problems.
Drug Interaction

❑Birth control pills: Some AEDs, such as carbamazepine, phenytoin, and topiramate, can
reduce the effectiveness of birth control pills, increasing the risk of unintended pregnancy.

❑Warfarin: AEDs, particularly phenytoin and valproic acid, can interact with the blood-
thinning.

Drug Toxicity

❑Liver toxicity.

❑Blood disorders: Some AEDs, such as carbamazepine and phenytoin, can cause a decrease
in the number of white blood cells, red blood cells, and platelets, leading to an increased
risk of infection, anemia, and bleeding.

❑Bone density loss.


DRUGS USED IN PARKINSON’S DISEASE
➢Dopamine Precursor’s—Levodopa
➢Peripheral decarboxylase inhibitors—Carbidopa, Benserazide (25 mg with
Levodopa).
➢Dopaminergic Agonist
➢MAO-B inhibitors: Selegiline (5 mg at breakfast and lunch).
➢COMT inhibitor
Mechanism of Action
Anti-Parkinson drugs work by increasing the levels of dopamine in the brain,
either by increasing its production or by blocking its breakdown.
Side Effects
Nausea, vomiting, dizziness, hypotension, dyskinesia, psychiatric
symptoms(hallucinations, delusions, and confusion),
COGNITION ENHANCERS
Indications
➢Senile dementia.
➢Common symptoms of elderly.
➢Mental retardation in children.
➢Transient ischemic attack.
Mechanism of Action
The mechanism of action is by increasing global/regional cerebral blood flow, direct support
of neuronal metabolism, enhancement of neurotransmission, improvement of discrete cerebral
function.
Classification
➢Nootropics (cognition enhancer)—Piracetam
➢Metabolic enhancer—Dihydroergotoxin, Nicergoline, Piribedil
➢Cholinergic activators—Tacrine, Rivastigmine, Donezepil, Galantamine.
➢Vasoactive cerebral protector—Pyritinol, Ginkgo.
Indications
ADHD, sleep disorders, Alzheimer's disease, stroke and traumatic brain injury,
general cognitive enhancement.
Contraindications
Allergies, pregnancy and breastfeeding, liver or kidney disease, cardiovascular
disease, history of psychiatric disorders (anxiety, depression, or psychosis).
Nurses Responsibilities
Assess the patient's medical history, including any allergies, current medications,
and underlying medical conditions that may affect the safety or effectiveness of
the drug.
CNS STIMULANTS
These drugs stimulant specific area in brain and spinal cord and are used to elevate mood, energy and alertness.
Mechanism of Action
The general mechanism of stimulants revolves around increased catecholamine levels and increased agonistic
activity at adrenergic receptors.
Indications
❑Narcolepsy
❑ADHD
❑Asthma
❑Obesity
❑Depression
Contraindications
Untreated hyperthyroidism, glaucoma, and a recent stroke, advanced arteriosclerosis, younger patients under the
age of 12 and pregnant patients.
Side Effects
▪ Anxiety
▪ Jitteriness
▪ Headaches
▪ Weight loss
▪ Insomnia
▪ Psychosis
▪ Pruritus
Drug Interaction
➢Monoamine oxidase inhibitors (MAOIs): Taking CNS stimulants with MAOIs can
increase the risk of developing a hypertensive crisis.
➢Antihypertensive drugs: CNS stimulants can decrease the effectiveness of
antihypertensive drugs, leading to an increase in blood pressure.
➢Antidepressants: CNS stimulants can interact with antidepressants, including selective
serotonin reuptake inhibitors (SSRIs) and tricyclic antidepressants, leading to a higher risk
of serotonin syndrome.
Central Nervous System (CNS) Stimulants
➢CNS stimulants are classified as—Convulsant, analeptics and
psychostimulants.
➢Convulsant: Strychnine, Picrotoxin, Pentylenetetrazol (PTZ), Bicuculline.
➢Analeptics: Doxapram, Prethcamide.
➢Psychostimulants: Amphetamine, Methylphenidate, Pemoline, Cocaine,
Caffeine.
TREATMENT OF METHYL ALCOHOL POISONING
Methyl Alcohol Poisoning
▪ Methyl alcohol poisoning occurs when an individual ingests or inhales large
amounts of the toxic alcohol, leading to a range of symptoms and potentially
life-threatening complications.
▪ Symptoms of methyl alcohol poisoning typically develop within hours of
exposure and can include:
▪ Abdominal pain
▪ Nausea and vomiting
▪ Headache
▪ Blurred vision or blindness
▪ Seizures
▪ Respiratory distress
▪ Coma
➢Sodium hydrocarbon can is used to treat respiratory acidosis.
➢Folic acid or folinic acid is given to accelerate metabolism of formate.
➢Hemodialysis
➢Correction of acidosis: Methyl alcohol poisoning can cause metabolic
acidosis, which must be corrected with sodium bicarbonate or other
appropriate agents.
➢Correction of hypoglycemia
➢Ophthalmologic consultation
Role of nurse

❑Administration of antidote: The nurse may be responsible for administering


the antidote fomepizole or ethanol as ordered by the physician. The nurse
should monitor the patient closely for adverse reactions or complications from
the antidote.

❑Supportive care: The nurse should provide supportive care to the patient,
including administering fluids, electrolytes, and glucose to correct metabolic
imbalances. The nurse should also monitor the patient's respiratory function
and provide oxygen therapy if necessary.

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