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Home / Drugs / Starting with C / Captopril

Captopril is a potent, competitive inhibitor of angiotensin-converting enzyme (ACE), the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Captopril may be used in the treatment of hypertension.
CategoriesAntihypertensive Agents
Angiotensin-converting Enzyme Inhibitors
ManufacturersPar pharmaceutical inc
Apotex inc
Apothecon inc div bristol myers squibb
Clonmel healthcare ltd
Egis pharmaceuticals ltd
Endo laboratories inc div dupont merck pharmaceutical co
Huahai us inc
Ivax pharmaceuticals inc sub teva pharmaceuticals usa
Mylan laboratories inc
Purepac pharmaceutical co
Sandoz inc
Stason industrial corp
Teva pharmaceuticals usa inc
Teva pharmaceuticals usa
Watson laboratories inc
West ward pharmaceutical corp
Wockhardt americas inc
PackagersAdvanced Pharmaceutical Services Inc.
Amerisource Health Services Corp.
Apotex Inc.
Apotheca Inc.
AQ Pharmaceuticals Inc.
A-S Medication Solutions LLC
Bristol-Myers Squibb Co.
Bryant Ranch Prepack
Cardinal Health
Caremark LLC
Changzhou Pharmaceutical Factory
Comprehensive Consultant Services Inc.
Dept Health Central Pharmacy
Direct Dispensing Inc.
Dispensing Solutions
Diversified Healthcare Services Inc.
E.R. Squibb and Sons LLC
Egis Pharmaceuticals Public Ltd. Co.
Eon Labs
Heartland Repack Services LLC
Innovative Manufacturing and Distribution Services Inc.
Lake Erie Medical and Surgical Supply
Legacy Pharmaceuticals Packaging LLC
Liberty Pharmaceuticals
Major Pharmaceuticals
Medisca Inc.
Murfreesboro Pharmaceutical Nursing Supply
Neuman Distributors Inc.
Novopharm Ltd.
Nucare Pharmaceuticals Inc.
Par Pharmaceuticals
PD-Rx Pharmaceuticals Inc.
Pharmaceutical Utilization Management Program VA Inc.
Pharmacy Service Center
Physicians Total Care Inc.
Preferred Pharmaceuticals Inc.
Prepackage Specialists
Prepak Systems Inc.
Prescript Pharmaceuticals
Rebel Distributors Corp.
Remedy Repack
Resource Optimization and Innovation LLC
Sandhills Packaging Inc.
Southwood Pharmaceuticals
Stason Pharmaceuticals Inc.
Teva Pharmaceutical Industries Ltd.
Tya Pharmaceuticals
UDL Laboratories
Vangard Labs Inc.
West-Ward Pharmaceuticals
Wockhardt Ltd.
SynonymsCaptoprilum [INN-Latin]


For the treatment of essential or renovascular hypertension (usually administered with other drugs, particularly thiazide diuretics). May be used to treat congestive heart failure in combination with other drugs (e.g. cardiac glycosides, diuretics, β-adrenergic blockers). May improve survival in patients with left ventricular dysfunction following myocardial infarction. May be used to treat nephropathy, including diabetic nephropathy.


Captopril, an ACE inhibitor, antagonizes the effect of the RAAS. The RAAS is a homeostatic mechanism for regulating hemodynamics, water and electrolyte balance. During sympathetic stimulation or when renal blood pressure or blood flow is reduced, renin is released from the granular cells of the juxtaglomerular apparatus in the kidneys. In the blood stream, renin cleaves circulating angiotensinogen to ATI, which is subsequently cleaved to ATII by ACE. ATII increases blood pressure using a number of mechanisms. First, it stimulates the secretion of aldosterone from the adrenal cortex. Aldosterone travels to the distal convoluted tubule (DCT) and collecting tubule of nephrons where it increases sodium and water reabsorption by increasing the number of sodium channels and sodium-potassium ATPases on cell membranes. Second, ATII stimulates the secretion of vasopressin (also known as antidiuretic hormone or ADH) from the posterior pituitary gland. ADH stimulates further water reabsorption from the kidneys via insertion of aquaporin-2 channels on the apical surface of cells of the DCT and collecting tubules. Third, ATII increases blood pressure through direct arterial vasoconstriction. Stimulation of the Type 1 ATII receptor on vascular smooth muscle cells leads to a cascade of events resulting in myocyte contraction and vasoconstriction. In addition to these major effects, ATII induces the thirst response via stimulation of hypothalamic neurons. ACE inhibitors inhibit the rapid conversion of ATI to ATII and antagonize RAAS-induced increases in blood pressure. ACE (also known as kininase II) is also involved in the enzymatic deactivation of bradykinin, a vasodilator. Inhibiting the deactivation of bradykinin increases bradykinin levels and may sustain its effects by causing increased vasodilation and decreased blood pressure.

mechanism of action

There are two isoforms of ACE: the somatic isoform, which exists as a glycoprotein comprised of a single polypeptide chain of 1277; and the testicular isoform, which has a lower molecular mass and is thought to play a role in sperm maturation and binding of sperm to the oviduct epithelium. Somatic ACE has two functionally active domains, N and C, which arise from tandem gene duplication. Although the two domains have high sequence similarity, they play distinct physiological roles. The C-domain is predominantly involved in blood pressure regulation while the N-domain plays a role in hematopoietic stem cell differentiation and proliferation. ACE inhibitors bind to and inhibit the activity of both domains, but have much greater affinity for and inhibitory activity against the C-domain. Captopril, one of the few ACE inhibitors that is not a prodrug, competes with ATI for binding to ACE and inhibits and enzymatic proteolysis of ATI to ATII. Decreasing ATII levels in the body decreases blood pressure by inhibiting the pressor effects of ATII as described in the Pharmacology section above. Captopril also causes an increase in plasma renin activity likely due to a loss of feedback inhibition mediated by ATII on the release of renin and/or stimulation of reflex mechanisms via baroreceptors. Captopril’s affinity for ACE is approximately 30,000 times greater than that of ATI.


Symptoms of overdose include emesis and decreased blood pressure. Side effects include dose-dependent rash (usually maculopapular), taste alterations, hypotension, gastric irritation, cough, and angioedema.


Hepatic. Major metabolites are captopril-cysteine disulfide and the disulfide dimer of captopril. Metabolites may undergo reversible interconversion.


60-75% in fasting individuals; food decreases absorption by 25-40% (some evidence indicates that this is not clinically significant)

half life

2 hours

drug interactions

Amiloride: Increased risk of hyperkalemia

Aprotinin: In study of nine patients with untreated hypertension, aprotinin infused intravenously in a dose of 2 million KIU over two hours blocked the acute hypotensive effect of 100mg of captopril.

Drospirenone: Increased risk of hyperkalemia

Lithium: The ACE inhibitor increases serum levels of lithium

Potassium: Increased risk of hyperkalemia

Spironolactone: Increased risk of hyperkalemia

Terbinafine: Terbinafine may reduce the metabolism and clearance of Captopril. Consider alternate therapy or monitor for therapeutic/adverse effects of Captopril if Terbinafine is initiated, discontinued or dose changed.

Tizanidine: Tizanidine increases the risk of hypotension with the ACE inhibitor

Tobramycin: Increased risk of nephrotoxicity

Treprostinil: Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.

Triamterene: Increased risk of hyperkalemia