Trade name Capoten
Oral agent with a bioavailability of 70–75%.
Undergoes hepatic metabolism, with half-life of 1.9 hours.
Excretion by renal system.
An angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of congestive heart failure.
It prevents the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, resulting in lower aldosterone secretion.
It is rapidly absorbed, but bioavailability is significantly reduced with food intake.
Achieves a peak concentration in 1 hour and has a short half-life.
The drug is cleared by the kidney; impaired renal function requires reduction of the dosage.
Captopril is absorbed well orally.
Uses primarily: Hypertension, for congestive heart failure and after myocardial infarction. and preservation of kidney function in diabetic nephropathy.
Has mood-elevating properties in some patients.
Not a prodrug, like the majority of ACE inhibitors.
Adverse drug reaction includes cough, rash and taste changes.
Short half-life necessitates two or three times per day dosing.
Adverse effects include: cough due to increase in the plasma levels of bradykinin, angioedema, agranulocytosis, proteinuria, hyperkalemia, taste alteration, teratogenicity, postural hypotension, acute renal failure, leukopenia, itching, headache, tachycardia, chest pain, palpitations and weakness.
Cough is the most common adverse effect.
Hyperkalemia can occur, especially if used with other drugs which elevate potassium levels.
Overdose can be antagonized with naloxone.