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Description: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat. [PubChem]
Drug Type: Small Molecule; Approved
Pharmacology: Ramipril is an angiotensin-converting enzyme (ACE) inhibitor similar to benazepril, fosinopril, and quinapril. An inactive prodrug, ramipril is converted to ramiprilat in the liver and is used to treat hypertension and heart failure, to reduce proteinuria and renal disease in patients with nephropathies, and to prevent stroke, myocardial infarction, and cardiac death in high-risk patients.
Mechanism of Action: Ramiprilat, the active metabolite, competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and an increase in plasma renin. Ramiprilat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin.
Indication: For diuretics and digitalis in congestive heart failure as adjunctive therapy and for use in prophylaxis in post MI.
Half Life: 2-4 hours
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