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Anti-hypertensive Agents (Med Chem:- 2) Notes Download

A condition in which the blood pressure of systemic artery increases beyond the normal pressure is known as hypertension. Therefore, to deliver blood to tissues, the heart works harder to overcome the increased systemic pressure. This increased systemic arterial pressure puts strain on the heart and other arteries, thus resulting in high blood pressure. Based on the degree of severity, hypertension can be graded as:

1. Mild: Diastole up to 104 mmHg,
2. Moderate: Diastole 105-114 mmHg, and
3. Severe: Diastole more than 115 mmHg.

Therapy for hypertensive patients aims at reducing the increased blood pressure. This is accomplished by the administration of drugs from different classes; treatment is often given in the form of a combination of several agents. If left untreated, it would result in end-organ damage, an increased risk for MI, and stroke.

6.1.2. Classification

Antihypertensive drugs are classified as follows:

1. Diuretics
   • Thiazides: Hydrochlorothiazide, Chlorthalidone, and Indapamide.
   • Loop Diuretics: Furosemide, Bumetanide, and Torsemide.
   • Potassium Sparing Diuretics: Spironolactone, Amiloride, and Triamterene.
2. Angiotensin Converting Enzyme Inhibitors: Captopril, Enalapril, Lisinopril, Ramipril, Perindopril, Fosinopril, Trandolapril, Quinapril, and Benazepril.
3. Angiotensin II Receptor Antagonists: Losartan, Candesartan, Valsartan, Eprosartan, and Irbesartan.
4. Ganglion Blockers: Trimethaphan.
5. Adrenergic Drugs
   • Centrally Acting Drugs: Clonidine, Methyldopa, Guanabenz, and Guanfacine.
   • Adrenergic Neuron Blockers: Guanethidine and Reserpine.
   • Sympatholytics (Adrenergic Receptor Blockers)
     • α-Blockers: Prazosin, Terazosin, Doxazin, Phenoxybenzamine, and Phentolamine.
     • β-Blockers: Propranolol, Atenolol, Esmolol, and Metoprolol.
     • α & β-Blockers: Labetalol and Carvedilol.
6. Calcium Channel Blockers: Verapamil, Nifedipine, Nicardipine, Nimodipine, Amlodipine, and Felodipine.
7. Vasodilators
   • Arteriolar Dilators: Hydralazine, Minoxidil, and Diazoxide.
   • Arteriolar and Venular Dilators: Sodium nitroprusside.

Detailed Explanation of Anti-hypertensive Agents

Hypertension, or high blood pressure, is a chronic medical condition that significantly increases the risk of heart disease, stroke, and kidney failure. Anti-hypertensive agents are drugs used to manage and treat hypertension by lowering blood pressure. These drugs work through various mechanisms, including reducing blood volume, relaxing blood vessels, and decreasing the heart's workload.

Diuretics: These drugs help the kidneys eliminate excess sodium and water from the body, reducing blood volume and pressure. Thiazide diuretics are commonly used for mild to moderate hypertension, while loop diuretics are reserved for severe cases or patients with kidney dysfunction. Potassium-sparing diuretics are used to prevent potassium loss, which can be a side effect of other diuretics.

Angiotensin-Converting Enzyme (ACE) Inhibitors: These drugs block the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor. By inhibiting this process, ACE inhibitors reduce blood pressure and decrease the workload on the heart. They are particularly effective in patients with diabetes or kidney disease.

Angiotensin II Receptor Blockers (ARBs): ARBs work by blocking the action of angiotensin II at its receptors, leading to vasodilation and reduced blood pressure. They are often used as an alternative to ACE inhibitors, especially in patients who experience side effects like a dry cough.

Calcium Channel Blockers: These drugs prevent calcium from entering the cells of the heart and blood vessels, leading to relaxation of the vessels and reduced blood pressure. They are effective in treating hypertension and angina.

Vasodilators: These drugs directly relax the muscles in the walls of blood vessels, causing them to dilate and lower blood pressure. They are often used in combination with other anti-hypertensive agents for better control of blood pressure.

Anti-hypertensive therapy is tailored to the individual patient, taking into account the severity of hypertension, the presence of other medical conditions, and potential side effects of the drugs. Proper management of hypertension can significantly reduce the risk of cardiovascular events and improve overall health.

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