Captopril
- Atc Codes:C09AA01
- CAS Codes:62571-86-2
- PHARMGKB ID:62571-86-2
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Captopril, Debax; Belgium: Capoten, Captopril, Doccaptopri; Bulgaria: Alkadil, Captopril; Cyprus: Aceprotin, Acrodin, Capoten, Epsitron, Rilcapton, Ropril; Czech Republic: Tensiomin; Denmark: Capoten, Captol, Captopril; Estonia: Captohexal, Kaptopril; Finland: Captopril, Lopril; France: Captopril, Lopril; Germany: ACE-Hemmer, Adocor, Capto, Captobeta, Captodoc, Captoflux, Captogamma, Captopress, Captopril, Captowieb, Cardiagen, Coronorm, Jucapt, Lopirin, Tensiomin, Tensobon, Tensostad; Greece: Capoten, Captopril, Hypotensor, Normolose, Pertacilon; Hungary: Aceomel, Captogamma, Tensiomin; Ireland: Aceomel, Capoten, Captor; Italy: Capoten, Captopril; Latvia: Captogamma, Kaptopril; Lithuania: Captohexal, Kaptopril; Luxembourg: Capoten, Captohexal; Malta: Captopril, Epsitron, Normolose, Rilcapton, Ropril; Netherlands: Captopril; Poland: Captopril; Portugal: Capoten, Captopril, Hipotensil, Vidapril; Romania: Captopril; Slovakia: Tensiomin; Slovenia: Kaptopril; Spain: Capoten, Captopril, Captosina, Cesplon, Tensoprel; Sweden: Captopril; UK: Capoten.
North America
Canada: Apo-Capto, Capoten, Captopril, Nu-Capto; USA: Capoten, Captopril.
Latin America
Brazil: Capobal, Capoten, Capotrat, Capox, Capril, Captolab, Captomed, Captopiril, Captopril, Captopron, Captrizin, Catoprol, Ductopril, Hipoten, Pressomax, Prilpressin, Repril; Mexico: Altiver, Atrisol, Biodezil, Bioxil, Brucap, Bugazon, Capotena, Captopril, Captoser, Captral, Cardipril, Catona, Cryopril, Eca Presan, Ecaten, Enlace, Hipertex, Kenolan, Lenpryl, Midrat, Novapress, Precaptil, Prinarten, Proldin, Ranpres, Reductel, Reduprec, Romir, Tensin, Toprifar, Toprilem, Varaxil.
Asia
Japan: Apopril, Brealin, Capotec, Captopril, Captoril, Captowa, Dowpril, Kapuseal, Katonaplon, Kobapril, Ktplon, Onfrule.
Drug combinations
Captopril and Hydrochlorothiazide
Chemistry
Captopril: C~9~H~15~NO~3~S. Mw: 217.29. (1) L-Proline, 1-[(2S)-3-mercapto-2-methyl-1-oxopropyl]-; (2) 1-[(2S)-3-Mercapto-2-methylpropionyl]-L-proline. CAS-62571-86-2 (1978).

Pharmacologic Category
Angiotensin-Converting Enzyme Inhibitors. Antihypertensive Agent. (ATC-Code: C09AA01).
Mechanism of action
Competitive inhibitor of angiotensin-converting enzyme (ACE). Prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, resulting in lower levels of angiotensin II, which causes an increase in plasma renin activity and a reduction in aldosterone secretion. By decreasing local angiotensin II production, ACE inhibitors may decrease vascular tone by reducing direct angiotensin II-induced vasoconstriction and/or angiotensin II-induced increases in sympathetic activity. In hypertensive patients, captopril reduces blood pressure by decreasing total peripheral resistance with no change or an increase in heart rate, stroke volume, or cardiac output (these effects are independent of pre-treatment blood pressure/cardiac output). Causes arterial and possibly venous dilation. In patients with congestive heart failure, captopril decreases total peripheral resistance, pulmonary vascular resistance, pulmonary capillary wedge pressure, and mean arterial and right atrial pressures (cardiac index, cardiac output, stroke volume, and exercise tolerance are increased; heart rate decreases or is unchanged). The drug may also cause regional redistribution of blood flow, principally increasing renal blood flow (glomerular filtration rate is usually unchanged) with slight or no increase in flow in the forearm or hepatic vasculature, respectively. The hypotensive effect of captopril persists longer than inhibition of ACE in blood (unknown whether ACE is inhibited longer in vascular endothelium than in blood). Captopril alone is apparently more effective in reducing blood pressure in high or normal renin hypertension. Serum prolactin concentration has been reported to increase during captopril therapy.
Therapeutic use
Hypertension. Heart failure, left ventricular dysfunction after myocardial infarction. Diabetic nephropathy.
Pregnancy and lactiation implications
Captopril crosses the placenta and may affect ACE activity in the fetus. First trimester exposure to ACE inhibitors may cause major congenital malformations (cardiovascular and/or central nervous system malformations). Second and third trimester use of an ACE inhibitor is associated with oligohydramnios (risk of fetal limb contractures, craniofacial deformation, and hypoplastic lung development), anuria, hypotension, renal failure (reversible or irreversible), skull hypoplasia, and death in the fetus/neonate. ACE inhibitors are not recommended during pregnancy to treat maternal hypertension or heart failure. Not recommended during lactation.
Unlabeled use
To delay the progression of nephropathy and reduce risks of cardiovascular events in hypertensive patients with type 1 or 2 diabetes mellitus. Hypertensive crisis. Rheumatoid arthritis. Diagnosis of anatomic renal artery stenosis, hypertension secondary to scleroderma renal crisis, aldosteronism, idiopathic edema, Bartter’s syndrome, postmyocardial infarction for prevention of ventricular failure. Raynaud’s phenomenon. Hypertension secondary to Takayasu’s disease.
Contraindications
Hypersensitivity to captopril, any other ACE inhibitor, or any component of the formulation. Angioedema related to previous treatment with an ACE inhibitor.
Warnings and precautions
Angioedema might occur (especially following first dose), and may involve the head and neck (potentially compromising airway) or the intestine (presenting with abdominal pain)(higher risk in African-Americans and idiopathic or hereditary angioedema). May cause cholestatic jaundice (risk of fulminant hepatic necrosis). A dry, hacking, nonproductive cough might occur. Hyperkalemia is possible (risk factors: renal dysfunction, diabetes mellitus, concomitant use of potassium-sparing diuretics, potassium supplements, and/or potassium-containing salts). Anaphylactic/anaphylactoid reactions might occur. Symptomatic hypotension with or without syncope may also occur. Captopril has been associated with rare cases of agranulocytosis, neutropenia, or leukopenia with myeloid hypoplasia (higher risk in renal impairment and collagen vascular disease). May be associated with deterioration of renal function and/or increases in serum creatinine, particularly in low renal blood flow. Use with caution in the following situations: severe aortic stenosis (may reduce coronary perfusion resulting in ischemia), in ischemic heart disease or cerebrovascular disease (potential consequences posed by falling blood pressure), in hypertrophic cardiomyopathy and outflow tract obstruction (may worsen symptoms associated with reduction in afterload), in unstented unilateral/bilateral renal artery stenosis (risk of deterioration in renal function), and before, during, or immediately after major surgery (cardiopulmonary bypass, intraoperative blood loss or vasodilating anesthesia increases endogenous renin release). May cause drowsiness or insomnia. A syndrome which may include fever, myalgia, arthralgia, interstitial nephritis, vasculitis, rash, eosinophilia, and elevated ESR has been reported for captopril and other ACE inhibitors.