Cardiotonic drugs are medications that increase the efficiency and improve the contraction of

the heart muscle, thereby enhancing cardiac output. They are primarily used in conditions like
heart failure and certain arrhythmias.

Classification of Cardiotonic Drugs (In Short):

1. Cardiac Glycosides

• Example: Digoxin, Digitoxin

• Mechanism: Inhibit Na⁺/K⁺-ATPase → ↑ intracellular Ca²⁺ → stronger heart contraction

2. Sympathomimetic Amines (Beta-adrenergic Agonists)

• Examples: Dobutamine, Dopamine

• Mechanism: Stimulate β1 receptors → ↑ cAMP → ↑ heart contractility

3. Phosphodiesterase Inhibitors (PDE-3 Inhibitors)

• Examples: Milrinone, Inamrinone

• Mechanism: Inhibit PDE-3 → ↑ cAMP → ↑ Ca²⁺ → increased cardiac output

4. Calcium Sensitizers

• Example: Levosimendan
• Mechanism: Increases sensitivity of cardiac myofilaments to calcium

Mechanism of Action of Digitalis (e.g., Digoxin):

Digitalis primarily works by inhibiting the Na⁺/K⁺-ATPase pump in heart cells, leading to increased
calcium inside the cells, which improves the force of heart contractions.

Step-by-Step Mechanism:

1. Inhibition of Na⁺/K⁺-ATPase Pump

Digitalis binds to and blocks a pump (called Na⁺/K⁺-ATPase) that normally moves sodium and
potassium in and out of heart cells. Inhibition of this pump results in accumulation of sodium in
the heart cell.

2. Activity of Na⁺/Ca²⁺ Exchanger

Normally, this exchanger brings Na⁺ in and pumps Ca²⁺ out. With high Na⁺ inside, this exchanger
becomes less active. This causes more calcium to stay in the cell too
 3. Calcium helps the heart muscle squeeze better. So, with more calcium inside, the heart
contracts more strongly with stronger and more efficient heartbeats.

4. Digitalis stimulates vagus nerve, which reduces the activity of the heart's natural
pacemaker (SA node) and slows signals at the AV node. This decreases the heart rate

Key Actions of Digitalis on the Heart:

1. Positive Inotropic Effect (Stronger Heartbeat):

• Digitalis helps the heart beat more strongly.

• It blocks a pump (Na⁺/K⁺-ATPase) in heart cells, causing more sodium to build up inside.
• This leads to more calcium in the cells, which makes heart muscles contract harder.

2. Negative Chronotropic Effect (Slower Heart Rate):

• Digitalis slows down the heart rate.

• It does this by stimulating the vagus nerve, which reduces the activity of the heart's
natural pacemaker (SA node) and slows signals at the AV node.
• This is helpful in fast heart rhythms like atrial fibrillation.

3. Negative Dromotropic Effect (Slower Signal Conduction):

• Digitalis slows the speed of electrical signals, especially through the AV node.
• This helps prevent too many signals from reaching the lower chambers of the heart,
keeping the heart rhythm more regular.

4. Mild Diuretic Effect (More Urine Output):

• By making the heart pump better, digitalis improves blood flow to the kidneys.
• This helps the kidneys remove extra water and salt, which reduces swelling and fluid
buildup in heart failure.
Therapeutic Uses of Digitalis:

1. Congestive Cardiac Failure: Increases heart pumping power, relieving symptoms like
fatigue and swelling.
2. Atrial Fibrillation: Slows heart rate and helps regulate rhythm.

Adverse Effects of Digitalis:

1. Cardiac: Arrhythmias, heart block, digoxin toxicity (can cause dangerous irregular
heartbeats).
2. Gastrointestinal: Nausea, vomiting, loss of appetite, diarrhea.
3. Neurological: Confusion, dizziness, visual disturbances (e.g., yellow-green halos).
4. Other: Fatigue, weakness, headache, electrolyte imbalances.

Name the drug contraindicated in Congestive cardiac failure and Hypokalemia ?

The drug contraindicated in Congestive Heart Failure (CHF) and Hypokalemia is:

Digoxin (or Digitalis)

• In CHF: While digoxin can be used to treat heart failure, it is contraindicated or used
with caution in severe heart failure with ventricular arrhythmias or acute
decompensated heart failure, as it may worsen arrhythmias.
• In Hypokalemia: Digoxin is contraindicated in hypokalemia (low potassium) because
low potassium levels increase the risk of digoxin toxicity. It can lead to dangerous
arrhythmias (e.g., ventricular arrhythmias), making it unsafe.

Digitalis (Digoxin) Toxicity:

Digitalis toxicity occurs when the level of digoxin in the body becomes too high, leading to
harmful effects. It is particularly dangerous because digoxin has a narrow therapeutic index,
meaning the difference between a therapeutic dose and a toxic dose is small.

Symptoms of Digitalis Toxicity:

1. Cardiac: Cardiac Arrhythmias

2. Gastrointestinal:
o Nausea, vomiting, loss of appetite, diarrhea.
3. Neurological:
o Confusion, dizziness, visual disturbances
Antidote for Digitalis Toxicity:

The antidote for digoxin toxicity is Digoxin Immune Fab (brand name Digibind).

Mechanism of Action of the Antidote (Digoxin Immune Fab):

• Digoxin immune fab binds to digoxin molecules in the bloodstream, preventing them
from binding to the cardiac Na⁺/K⁺-ATPase pump.
• By binding to digoxin, it inactivates the drug and accelerates its elimination from the
body.
• This reduces digoxin's toxic effects, especially the risk of arrhythmias and other life-
threatening symptoms.

why digitilis called cardiotonics ?

cardiotonics are drugs that improve heart function by enhancing its contractility (the strength of the
heart's contractions). Digitalis (or digoxin) is called a cardiotonic because it increases the force of heart
contractions (i.e., it strengthens the heart's ability to pump blood). Digitalis achieves this by increasing
the calcium available to heart muscle cells, making the heart pump more efficiently, which is especially
helpful in conditions like heart failure.

What is Cardiac Arrhythmia?

Cardiac arrhythmia refers to any abnormality in the heart rhythm. It occurs when the
electrical signals that control the heartbeat are irregular, leading to the heart beating too fast, too
slow, or in an irregular pattern.

Types of Cardiac Arrhythmias:

• Tachycardia: Rapid heart rate

• Bradycardia: Slow heart rate
• Fibrillation: Chaotic and irregular heartbeat

Atrial fibrillation or ventricular fibrillation

• Heart Block: Delay or complete block of the electrical signal between the atria and
ventricles.(Atropine in emergency)
Antiarrhythmic Drugs:

Antiarrhythmic drugs are medications used to treat or prevent arrhythmias. They work by
modifying the electrical impulses in the heart to restore a normal rhythm.

Classification of Antiarrhythmic Drugs:

Antiarrhythmic drugs are classified into four main classes based on their mechanism of action:

Class I: Sodium Channel Blockers

• Mechanism: They block sodium channels, which slows down the electrical conduction
of the heart.
• Subtypes:
o Class Ia: Moderate sodium channel block (e.g., Quinidine, Procainamide).
o Class Ib: Weak sodium channel block (e.g., Lidocaine, Mexiletine).
o Class Ic: Strong sodium channel block (e.g., Flecainide, Propafenone).

Class II: Beta-Blockers

• Mechanism: They block the effects of adrenaline on beta receptors, slowing the heart
rate and reducing the electrical activity in the heart.
• Examples: Propranolol, Atenolol, Metoprolol.

Class III: Potassium Channel Blockers

• Mechanism: These drugs block potassium channels, which prolongs the repolarization
phase of the cardiac action potential, helping to restore normal rhythm.
• Examples: Amiodarone, Sotalol, Dofetilide.

Class IV: Calcium Channel Blockers

• Mechanism: They block calcium channels, which reduces the electrical conduction and
slows down the heart rate.
• Examples: Verapamil, Diltiazem.

Other Antiarrhythmic Drugs: Adenosine, Digoxin

METION THE DRUG OF CHOICE

• Tachycardia: Adenosine
• Bradycardia: Atropine
• Atrial fibrillation: Digoxin
• ventricular fibrillation: Defibrillation, followed by Epinephrine, then Amiodarone
• Heart Block: Atropine in emergency

Angina pectoris is a medical term for chest pain or discomfort that occurs when the heart muscle
doesn't get enough oxygen-rich blood because of the narrowing or blockage of the coronary arteries .

• Type of Pain: Often described as pressure, squeezing, heaviness, or tightness in the chest.

• Location: Usually felt behind the breastbone and may radiate to the shoulders, arms, neck,
jaw, or back.

Types of Angina:

1. Stable Angina: Predictable pattern; occurs during exertion and is relieved by rest.
2. Unstable Angina: Unpredictable and more severe; can occur at rest and may signal an
impending heart attack. It’s a medical emergency.
3. Variant Angina: Caused by a spasm in a coronary artery; occurs mostly at rest and often
at night.

Drugs for Angina Pectoris

1. Nitrates: e.g. Nitroglycerin/GTN

• Action: Dilate blood vessels, reduce chest pain, provides immediate relief in acute attacks

2. Beta-Blockers: e.g. Metoprolol

• Action: Decrease heart rate and contractility → reduce oxygen demand

3. Calcium Channel Blockers : e.g. Amlodipine

• Action: Relax blood vessels and reduce cardiac workload

4. Antiplatelets: e.g. Aspirin,

• Action: Prevent clot formation

5. Statins: e.g. Atorvastatin

• Action: Lower cholesterol

6. Anticoagulants (in unstable angina): e.g: Heparin

• Action: Prevents clots
Therapeutic use, dosage, Route of administration, and adverse effect of GTN
/Glyceryl Trinitrate/ Nitroglycerine

Therapeutic Uses of Nitroglycerin:

1. Angina pectoris – to relieve or prevent chest pain.

2. Acute myocardial infarction (MI) – helps reduce heart workload and relieve chest pain.
3. Hypertensive emergencies –to quickly lower blood pressure.
4. Before coronary angioplasty (PCI) – to improve coronary blood flow and reduce chest
discomfort.

Dosage & Route of Administration (GTN):

• Sublingual spray/tablet:
0.3–0.6 mg under the tongue
Repeat every 5 minutes (max 3 doses)
• Transdermal patch : 0.3–0.6 mg/hour, Apply once daily, remove after 12–14 hours
• Oral :
2.5–9 mg twice or thrice daily
• IV infusion:
Start at 5 mcg/min, increase gradually as needed

Adverse Effects:

• Headache (very common)

• Hypotension (especially orthostatic)
• Dizziness, lightheadedness

What is Hypertension?

Hypertension is a chronic medical condition where the blood pressure in the arteries is
consistently elevated above normal levels.

• Normal BP: < 120/80 mmHg

• Hypertension: ≥ 140/90 mmHg (in most guidelines)

It increases the risk of heart disease, stroke, kidney failure, and other complications.

Antihypertensive drugs are medications used to lower high blood pressure and maintain it
within a normal range to reduce the risk of cardiovascular events.
 Classification of Antihypertensive Drugs:

1. Diuretics

• Example: Hydrochlorothiazide, Furosemide

• Action: Promote salt and water excretion to reduce blood volume.

2. Alpha-blockers

• Example: Prazosin, Doxazosin

• Action: Relax arterial and venous smooth muscle.

3. Beta-blockers

• Example: Propranolol, Metoprolol

• Action: Reduce heart rate and cardiac output.

3. Calcium Channel Blockers (CCBs)

• Example: Amlodipine, Verapamil

• Action: Relax blood vessels by blocking calcium entry.

4. ACE Inhibitors (Angiotensin-Converting Enzyme Inhibitors)

• Example: Enalapril, Lisinopril

• Action: Prevent formation of angiotensin II (a vasoconstrictor).

5. ARBs (Angiotensin II Receptor Blockers)

• Example: Losartan, Valsartan

• Action: Block angiotensin II receptors to relax blood vessels.

7. Central acting agents

• Example: Clonidine, Methyldopa

• Action: Reduce sympathetic outflow from the brain.

8. Vasodilators

• Example: Hydralazine
• Action: Directly relax blood vessels.
Propranolol:

• Uses: Hypertension, angina pectoris,Cardiac arrhythmias, migraine, anxiety

• Dose: 40–80 mg twice daily for hypertension, 10–40 mg 2–3 times daily for
migraine/anxiety
• Side Effects: Bradycardia, hypotension, fatigue, dizziness, cold limbs, Nightmare

Metoprolol:

• Uses: Hypertension, angina pectoris,Cardiac arrhythmias, myocardial infarcation

• Dose: 50–100 mg once or twice daily for hypertension/angina, 5–15 mg by IV route in
myocardial infarcation
• Side Effects: Bradycardia, hypotension, fatigue, dizziness, Cold limbs, Nightmares

Vasomotor reversal of Dale is a phenomenon observed when the effects of vasoconstriction

(narrowing of blood vessels) caused by adrenaline (epinephrine) are reversed by the
administration of alpha-adrenergic blockers.

Here's how it works:

1. Vasoconstriction by Adrenaline:
o Adrenaline (epinephrine) is a neurotransmitter and hormone that primarily
stimulates alpha (α) and beta (β) adrenergic receptors.
o When adrenaline binds to alpha-1 adrenergic receptors on the smooth muscle of
blood vessels, it causes vasoconstriction (narrowing of blood vessels), which
increases blood pressure.
2. Action of Alpha Blockers:
o Alpha blockers are drugs that block alpha-1 adrenergic receptors.
o By blocking these receptors, they prevent vasoconstriction induced by
adrenaline.
o This leads to vasodilation (widening of blood vessels), lowering blood pressure.

3. Vasomotor Reversal:
o Under normal conditions, adrenaline causes vasoconstriction by stimulating
alpha-1 receptors.
o If alpha blockers are administered before or along with adrenaline, the
vasoconstriction effects of adrenaline are reversed. In other words, the presence
of alpha blockers prevents adrenaline from acting on alpha-1 receptors, so the
vasoconstriction is negated, and instead, vasodilation may occur.

vasomotor reversal of Dale illustrates how an antagonist (alpha blockers) can change the physiological
effects of a neurotransmitter (adrenaline) on blood vessels, from vasoconstriction to vasodilation.
why hypertensives are given along with Diuretics?

Antihypertensives are often given with diuretics because they work in different ways to lower
blood pressure more effectively.

• Antihypertensive drugs (like ACE inhibitors or beta-blockers) help relax blood vessels
or slow the heart to reduce pressure.
• Diuretics (water pills) help the body get rid of extra salt and water, including sodium.
This reduces blood volume, which helps lower blood pressure. Also, High sodium levels
are one of the important causes of hypertension.

When used together:

• They give better blood pressure control.

• Diuretics help prevent fluid buildup that some antihypertensive drugs might cause.
• The combination allows for lower doses, which means fewer side effects.

Drug Linked to Suicidal Thoughts:

Reserpine depletes brain neurotransmitters like serotonin, dopamine, and norepinephrine

— chemicals that are important for mood regulation. This depletion can lead to:

• Depression
• Severe mood changes
• Suicidal ideation,