20. ANTIANGINAL AGENTS AND VASODILATORS

Antianginal agents are medicines used to relieve and prevent angina pectoris — a type of chest pain caused by reduced blood supply to the heart. Vasodilators are a major class of these drugs because they relax blood vessels, improve oxygen supply, and reduce the workload on the heart.

What Is Angina?

Angina occurs when the heart muscle does not receive enough oxygen-rich blood. It is commonly caused by:

  • Coronary artery disease (narrowing of heart vessels)
  • Stress or exertion
  • Increased oxygen demand of the heart

Types of Angina

  • Stable angina – Triggered by exercise or stress
  • Unstable angina – Sudden, unpredictable, and more severe
  • Variant (Prinzmetal’s) angina – Caused by coronary artery spasm

Goals of Antianginal Therapy

  • Reduce heart oxygen demand
  • Increase blood flow to the heart
  • Prevent or relieve chest pain

Classification of Antianginal Agents

1. Nitrates

  • Nitroglycerin
  • Isosorbide dinitrate
  • Isosorbide mononitrate

2. Beta Blockers

  • Atenolol
  • Metoprolol
  • Propranolol

3. Calcium Channel Blockers

  • Verapamil
  • Diltiazem
  • Amlodipine

4. Potassium Channel Activators

  • Nicorandil

5. Miscellaneous / Newer Agents

  • Ranolazine
  • Trimetazidine

Mechanisms of Antianginal Drugs

Nitrates – Vasodilators

Mechanism: Release nitric oxide (NO) which relaxes vascular smooth muscle. This:

  • Reduces preload (venous dilation)
  • Reduces afterload (arterial dilation)
  • Improves blood flow to coronary arteries

Overall, nitrates reduce oxygen demand and increase oxygen supply.

Beta Blockers

Mechanism: Reduce heart rate, blood pressure, and cardiac workload.

Uses: Stable angina (not helpful in variant angina).

Calcium Channel Blockers

Mechanism: Prevent calcium entry into smooth muscle cells, causing vasodilation and reduced heart workload.

Useful for:

  • Stable angina
  • Variant (spasm-related) angina

Nicotinate (Nicorandil)

Mechanism: Opens potassium channels and releases nitric oxide. This causes relaxation of both arteries and veins.

Ranolazine

Mechanism: Inhibits late sodium current in heart cells, reducing oxygen consumption.

Uses: Chronic stable angina.

Trimetazidine

Mechanism: Improves cardiac cell metabolism during low oxygen (cytoprotective).


Drug Profiles

Nitroglycerin

Form: Sublingual tablets, spray, patch, ointment.

Use: Immediate relief of acute angina attacks.

Side effects: Headache, flushing, low blood pressure.

Isosorbide Dinitrate

Long-acting nitrate used for angina prevention.

Atenolol / Metoprolol

Class: Beta-1 selective blockers.

Use: Stable angina and after heart attacks.

Verapamil / Diltiazem

Mechanism: Reduce heart rate and relax blood vessels.

Use: Variant angina and hypertension.

Amlodipine

Primarily vasodilator with minimal effect on heart rate.

Nicorandil

Dual action: Potassium channel opener + nitrate effect.

Ranolazine

Reduces oxygen consumption without altering heart rate or blood pressure.


General Adverse Effects

  • Headache (common with nitrates)
  • Dizziness
  • Low blood pressure
  • Flushing
  • Slow heart rate (beta blockers, some CCBs)
  • Ankle swelling (amlodipine)

Detailed Notes:

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