Small molecule
PubChem CID 44093
Captopril
Capoten
- Mechanism of action
- ACE (angiotensin-converting enzyme) inhibitor
- In plain language
- Blocks the enzyme that converts a mild hormone into a powerful blood-vessel-tightening one, so vessels relax and blood pressure drops.
- How it works
- Captopril inhibits angiotensin-converting enzyme (ACE), blocking conversion of angiotensin I to angiotensin II, a potent vasoconstrictor that also stimulates aldosterone secretion from the adrenal cortex. The resulting suppression of the renin-angiotensin-aldosterone system decreases plasma angiotensin II and aldosterone while plasma renin activity rises due to loss of negative feedback, together lowering peripheral vascular resistance and blood pressure. Because ACE is identical to kininase II, the enzyme that degrades the vasodilator peptide bradykinin, captopril inhibition may also raise bradykinin and prostaglandin E2 levels, which may contribute to the drug's therapeutic effect. The manufacturer's label notes that captopril's mechanism has not been fully elucidated and that there is no consistent correlation between renin levels and response to the drug.
- Therapeutic applications
- Indicated for the treatment of hypertension, alone or in combination with other antihypertensive agents, particularly thiazide-type diuretics; for the treatment of heart failure, usually in combination with diuretics and digitalis; to improve survival following myocardial infarction in clinically stable patients with left ventricular dysfunction (ejection fraction ≤ 40%), and to reduce the incidence of overt heart failure and subsequent heart-failure-related hospitalizations in these patients; and for the treatment of diabetic nephropathy (proteinuria > 500 mg/day) in patients with type 1 insulin-dependent diabetes mellitus and retinopathy.
- Class
- Small molecule
- Therapeutic area
- Cardiovascular
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