Description

Simple

A medication used to lower blood pressure.

Clinical

An ACE inhibitor used for the management of essential or renovascular hypertension, congestive heart failure, left ventricular dysfunction following myocardial infarction, and nephropathy.

Overview

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.

Pharmacology

Indication

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 i... Read more

Pharmacodynamic

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 juxt... Read more

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 A... Read more

Absorption

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

Protein binding

25-30% bound to plasma proteins, primarily albumin

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

2 hours

Route of elimination

Information currently not available.

Toxicity

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.

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

  • Avoid hypertensive herbs (e.g. bayberry, blue cohosh, cayenne, ephedra, and licorice).
  • Avoid potassium-containing products. Potassium products increase the risk of hyperkalemia.
  • Limit salt intake. Salt may attenuate the antihypertensive effect.
  • Take separate from meals. The presence of food decreases absorption. Take one hour prior to meals.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-benzylimidazole
1-benzylimidazole may decrease the antihypertensive activities of Captopril.
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Captopril.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may decrease the antihypertensive activities of Captopril.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Captopril.
4-Methoxyamphetamine
4-Methoxyamphetamine may decrease the antihypertensive activities of Captopril.
5-methoxy-N,N-dimethyltryptamine
5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Captopril.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Captopril.
Abediterol
Abediterol may decrease the antihypertensive activities of Captopril.
Aceclofenac
The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Aceclofenac is combined with Captopril.
Acemetacin
The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Acemetacin is combined with Captopril.
Acepromazine
Acepromazine may decrease the antihypertensive activities of Captopril.
Acetazolamide
The excretion of Captopril can be decreased when combined with Acetazolamide.
Acetyldigoxin
The serum concentration of Acetyldigoxin can be increased when it is combined with Captopril.
Acetylsalicylic acid
The therapeutic efficacy of Captopril can be decreased when used in combination with Acetylsalicylic acid.
Acipimox
The risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Captopril is combined with Acipimox.
Acyclovir
The excretion of Captopril can be decreased when combined with Acyclovir.
Adefovir dipivoxil
The excretion of Captopril can be decreased when combined with Adefovir dipivoxil.
Adrafinil
Adrafinil may decrease the antihypertensive activities of Captopril.
Agmatine
The risk or severity of hyperkalemia can be increased when Captopril is combined with Agmatine.
Agrostis gigantea pollen
The risk or severity of adverse effects can be increased when Captopril is combined with Agrostis gigantea pollen.
3 References
  1. 1 . Atkinson AB, Robertson JI: Captopril in the treatment of clinical hypertension and cardiac failure. Lancet. 1979 Oct 20;2(8147):836-9.PubMed: 90928
  2. 2 . Patchett AA, Harris E, Tristram EW, Wyvratt MJ, Wu MT, Taub D, Peterson ER, Ikeler TJ, ten Broeke J, Payne LG, Ondeyka DL, Thorsett ED, Greenlee WJ, Lohr NS, Hoffsommer RD, Joshua H, Ruyle WV, Rothrock JW, Aster SD, Maycock AL, Robinson FM, Hirschmann R, Sweet CS, Ulm EH, Gross DM, Vassil TC, Stone CA: A new class of angiotensin-converting enzyme inhibitors. Nature. 1980 Nov 20;288(5788):280-3.PubMed: 6253826
  3. 3 . Smith CG, Vane JR: The discovery of captopril. FASEB J. 2003 May;17(8):788-9.PubMed: 12724335