Comprehensive Overview of Antihypertensive Drugs

 Antihypertensive Drugs

Introduction to Hypertension

  • Hypertension: A chronic condition characterized by elevated blood pressure.
  • Importance of management: Reduces risk of cardiovascular events such as stroke, heart attack, and kidney damage.
  • Antihypertensive drugs: Key to controlling blood pressure and preventing complications.

Classification of Antihypertensive Drugs

  1. Diuretics
    • Thiazide diuretics
    • Loop diuretics
    • Potassium-sparing diuretics
  2. Beta Blockers
    • Atenolol
    • Metoprolol
    • Propranolol
    • Esmolol
    • Carvedilol
    • Nebivolol
  3. Calcium Channel Blockers (CCBs)
    • Dihydropyridines (e.g., amlodipine)
    • Non-dihydropyridines (e.g., verapamil)
  4. Renin-Angiotensin-Aldosterone System (RAAS) Inhibitors
    • ACE inhibitors (e.g., enalapril)
    • ARBs (e.g., losartan)
    • Direct renin inhibitors (e.g., aliskiren)
  5. Alpha Blockers
    • Terazosin
    • Prazosin
    • Tamsulosin
  6. Central Alpha Agonists
    • Methyldopa
    • Clonidine
  7. Vasodilators
    • Hydralazine
    • Sodium nitroprusside

Mechanism of Action (MOA)

1. Diuretics

  • Increase renal excretion of sodium and water.
  • Reduce blood volume and cardiac output.

2. Beta Blockers

  • Block beta-adrenergic receptors.
  • Reduce heart rate and cardiac output.

3. Calcium Channel Blockers

  • Inhibit calcium entry into vascular smooth muscle and myocardium.
  • Cause vasodilation and reduce cardiac workload.

4. RAAS Inhibitors

  • ACE inhibitors: Block conversion of angiotensin I to angiotensin II.
  • ARBs: Block angiotensin II receptors.
  • Renin inhibitors: Directly inhibit renin activity.

5. Alpha Blockers

  • Block alpha-adrenergic receptors, leading to vasodilation.

6. Central Alpha Agonists

  • Decrease sympathetic outflow from the CNS.

7. Vasodilators

  • Relax vascular smooth muscle to decrease peripheral resistance.

Clinical Indications

  • Diuretics: First-line for hypertension, heart failure, and edema.
  • Beta Blockers: Hypertension with comorbid angina, post-MI, or arrhythmias.
  • CCBs: Hypertension, angina, arrhythmias.
  • ACE Inhibitors/ARBs: Hypertension with heart failure, diabetic nephropathy.
  • Alpha Blockers: Resistant hypertension, BPH.
  • Vasodilators: Severe or refractory hypertension.

Adverse Effects

  • Diuretics: Electrolyte imbalance, dehydration.
  • Beta Blockers: Bradycardia, fatigue, bronchospasm.
  • CCBs: Peripheral edema, headache, dizziness.
  • ACE Inhibitors: Dry cough, hyperkalemia, angioedema.
  • ARBs: Similar to ACE inhibitors but without cough.
  • Alpha Blockers: Orthostatic hypotension, dizziness.
  • Vasodilators: Reflex tachycardia, headache.

Contraindications

  • Diuretics: Severe electrolyte disturbances, anuria.
  • Beta Blockers: Asthma, severe bradycardia.
  • CCBs: Severe heart failure (non-dihydropyridines).
  • ACE Inhibitors: Pregnancy, bilateral renal artery stenosis.
  • ARBs: Pregnancy.
  • Alpha Blockers: Hypotension.
  • Vasodilators: Hypotension, coronary artery disease.

Drug Interactions

  • Diuretics: Increased risk of lithium toxicity.
  • Beta Blockers: Enhanced effect with CCBs; reduced effect with NSAIDs.
  • CCBs: Potentiated effect with grapefruit juice.
  • ACE Inhibitors/ARBs: Risk of hyperkalemia with potassium supplements.
  • Alpha Blockers: Additive hypotensive effects with other antihypertensives.

References

  • Goodman & Gilman’s The Pharmacological Basis of Therapeutics.
  • Rang & Dale’s Pharmacology.
  Presentation for Antihypertension Drugs   

                                                                END OF THE CHAPTER

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