Captopril

Captopril treatment for hypertension and heart failure. Captopril is an inhibitor of angiotensin converting enzyme (ACE), which converts angiotensin I to angiotensin II, a potent endogenous vasoconstrictor subtance. Captopril is designated chemically as 1-[(2 S)-3-mercapto-2-methylpropionyl]-Lproline. Healthy subjects given captopril intravenously, the body clearance of captopril and steady-state volume of distribution were about 0.7 L/h/kg and 0.8 L/kg, respectively. The elimination half-life of unchanged captopril was approximately 2 hours. The primary route of elimination of captopril is the kidney. The renal clearance of unchanged captopril exceeds the glomerular filtration rate, due to active tubular secretion of the drug. In healthy subjects, about 70 to 75% of an oral dose is absorbed and the bioavailability of captopril is approximately 65%. Peak blood concentrations are reached about 45 to 60 minutes after oral administration
Indication Of Captopril :
Hypertension
Management of hypertension alone or with other antihypertensive agents, especially thiazide-type diuretics. The Blood Pressure lowering effects of captopril and thiazides are approximately additive.
Captopril may be used as initial therapy for patients with normal renal function. In patients with impaired renal function, particularly those with collagen vascular disease reserve captopril for hypertensive patients who have either developed unacceptable side effects on other drusgs, or have failed to respond satisfactorily to drug combination.
Heart Failure
For the treatment of Congestive Heart Failure ( CHF ) usually in combination with diuretics and digitalis. The beneficial effects of captopril in heart failure does not require the presence of digitalis; However, Most controlled clinical trial experience with captopril has been in patients receiving digitalis, as well as diuretic treatment.