7cited
checked 2026-08-05
what it isThe first ACE inhibitor, largely superseded but still stocked because it is active as given and works sublingually within about a quarter of an hour; never in pregnancy
what it doesActs as a competitive active-site inhibitor at Angiotensin-converting enzyme, one of 5 targets.what you would noticeWorks sublingually within about fifteen minutesActive as given rather than a prodrugThe first ACE inhibitor ever brought to market
is it safecontraindicated in pregnancy; the sulfhydryl group gives it a higher rate of rash, taste disturbance, proteinuria and neutropenia than later ACE inhibitors, and it shares the hyperkalaemia…in its favour: human data in the cited literature
CardiovascularPrescription
classCardiovascular · ACE inhibitor · Antihypertensive · RAAS inhibitor
key targetAngiotensin-converting enzyme (ACE / peptidyl-dipeptidase A, kininase II) · Competitive active-site inhibitor; the free sulfhydryl group coordinates the catalytic zinc, the design insight that made captopril the first orally active ACE inhibitor · Strong
targets5
literature1982 to 2003 · 6 journals
also known asCapoten, Kaptopril, Acepril, Lopirin and 1 more
outlets1 outlet
spec sheet7 rows
classCardiovascular · ACE inhibitor · Antihypertensive · RAAS inhibitor
key targetAngiotensin-converting enzyme (ACE / peptidyl-dipeptidase A, kininase II) · Competitive active-site inhibitor; the free sulfhydryl group coordinates the catalytic zinc, the design insight that made captopril the first orally active ACE inhibitor · Strong
targets5
literature1982 to 2003 · 6 journals
also known asCapoten, Kaptopril, Acepril, Lopirin and 1 more
outlets1 outlet
all namesCapoten, Kaptopril, Acepril, Lopirin, SQ 14225
evidence over time
19821 in 19922003
Captopril is the first ACE inhibitor, short acting and dosed two or three times a day; it survives mainly as a sublingual option for acute rises in blood pressure and in paediatric and renal practice.
works for
- Works sublingually within about fifteen minutes
- No later ACE inhibitor manages that sublingual speed
- Active as given rather than a prodrug
- The first ACE inhibitor ever brought to market
- Still used in paediatric and renal practice
- Short acting, so the dose can be titrated closely
Gallery
did you know
- Captopril was the first orally active ACE inhibitor and one of the earliest successes of structure-based drug design, built from the observation that Brazilian pit viper venom peptides potentiated bradykinin, then optimised around a zinc-binding sulfhydryl (PMID 6176105, PMID 14668810).
- SAVE showed captopril reduced mortality and morbidity in patients with left ventricular dysfunction after myocardial infarction, establishing ACE inhibition as post-infarction standard care [1].
- The Collaborative Study Group trial showed captopril slows the progression of diabetic nephropathy in type 1 diabetes independently of its blood-pressure effect, the trial that made ACE inhibitors renoprotective drugs rather than merely antihypertensives (PMID 8413456; this record carries an erratum).
- CAPPP compared ACE inhibition with conventional diuretic and beta-blocker therapy in over 10,000 hypertensive patients; the benefit was clearest in the diabetic subgroup (PMID 10030325, PMID 11723089).
- Captopril's sulfhydryl group is unique among the common ACE inhibitors and is responsible for its distinctive adverse effects, taste disturbance and rash, and for its short half-life and multiple daily dosing, which is why it has largely been replaced by longer-acting agents.
- A rise in serum creatinine of up to about 30% after starting an ACE inhibitor is expected haemodynamic efferent arteriolar dilation and is not by itself a reason to stop; a larger or progressive rise should prompt investigation for renal artery stenosis or volume depletion.
Mechanism
Unlike almost every later ACE inhibitor it is active as given rather than being a , which is why it works within about fifteen minutes sublingually. Its sulfhydryl group binds the zinc at the ACE active site directly, and that same group is thought to account for the distinctive metallic taste and the higher rate of rash.
receptor fingerprint
reading the marksactivatesblocks / inhibitsmodulates
01
Angiotensin-converting enzyme (ACE / peptidyl-dipeptidase A, kininase II)Competitive active-site inhibitor; the free sulfhydryl group coordinates the catalytic zinc, the design insight that made captopril the first orally active ACE inhibitor
strong
Blocks conversion of angiotensin I to angiotensin II, lowering blood pressure, afterload and aldosterone drive
02
Free sulfhydryl group (captopril-specific, not a class effect)Direct free-radical scavenging and thiol chemistry not shared by enalapril, lisinopril or ramipril
weak
Proposed antioxidant contribution; also the likely basis of captopril's distinctive taste disturbance, rash and, rarely, neutropenia
03
Bradykinin degradation (ACE is also kininase II)Inhibited, so bradykinin and substance P accumulate
downstream
Contributes and may contribute renal protection, but is also the direct cause of the ACE-inhibitor dry cough and of angioedema
04
Aldosterone secretionReduced secondary to loss of angiotensin II drive
downstream
Reduces sodium and water retention and myocardial fibrosis, but raises serum potassium, which is the main metabolic hazard
05
Glomerular efferent arteriolar toneEfferent arteriolar dilation reduces intraglomerular pressure
downstream
The mechanism of renoprotection in diabetic nephropathy; also why creatinine rises on starting and why bilateral renal artery stenosis is a contraindication (PMID 8413456)
Safetyrisks and cautions, not medical advice
contraindicated in pregnancy; the sulfhydryl group gives it a higher rate of rash, taste disturbance, proteinuria and neutropenia than later ACE inhibitors, and it shares the hyperkalaemia and angioedema risk of the class
Where to buy
recommended
Suppliers
Vendors carrying Captopril, with live product details and codes. Links are affiliate links that support the wiki at no cost to you.
RUPharma🌐
Captopril
From$11
Options$11 to $34
ShipsWorldwide from Russia and India; 3 to 4 weeks to the US and Canada, and 4 to 7 days on the lines that ship express from India, Singapore or China. Europe and Asia are select destinations rather than every country
Research
- 1982first citedDevelopment and design of specific inhibitors of angiotensin-converting enzyme.
- 1992controlled trialEffect of captopril on mortality and morbidity in patients with left ventricular dysfunction af…
- 2003most recentAce revisited: a new target for structure-based drug design.
- 1.Effect of captopril on mortality and morbidity in patients with left ventricular dysfunction after myocardial infarction. Results of the survival and ventricular enlargement trial. The SAVE Investigators.
- 2.The effect of angiotensin-converting-enzyme inhibition on diabetic nephropathy. The Collaborative Study Group.
- 3.Effect of angiotensin-converting-enzyme inhibition compared with conventional therapy on cardiovascular morbidity and mortality in hypertension: the Captopril Prevention Project (CAPPP) randomised trial.
- 4.Reduced cardiovascular morbidity and mortality in hypertensive diabetic patients on first-line therapy with an ACE inhibitor compared with a diuretic/beta-blocker-based treatment regimen: a subanalysis of the Captopril Prevention Project.
- 5.Development and design of specific inhibitors of angiotensin-converting enzyme.
- 6.Ace revisited: a new target for structure-based drug design.
- 7.Captopril. A review of its pharmacology and therapeutic efficacy after myocardial infarction and in ischaemic heart disease.
7 listed here; entry last updated August 2026
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Notes and cautions
- Captopril carries a boxed warning for fetal toxicity: drugs acting on the renin-angiotensin system cause fetal injury and death in the second and third trimesters, and it must be stopped as soon as pregnancy is detected.
- Angioedema is uncommon but can be fatal, is bradykinin-mediated rather than allergic so does not respond to antihistamines, occurs at higher rates in Black patients, and is an absolute contraindication to any future ACE inhibitor.
- Hyperkalaemia is the common metabolic hazard and becomes dangerous when captopril is combined with potassium-sparing diuretics, potassium supplements, trimethoprim or an ARB; check potassium and creatinine within one to two weeks of starting or increasing.
- It is contraindicated in bilateral renal artery stenosis and must never be combined with a direct renin inhibitor such as aliskiren in diabetes, or with sacubitril, where a 36-hour washout is required.
- The dry cough affects roughly one in ten and is a reason to switch to an ARB, not to persist.
reading fda reports