Captopril

ATC code

C09AA01

Therapeutic class

Angiotensin-Converting Enzyme (ACE) Inhibitor · ACE inhibitor

Forms

oral tablet

Brand names

Capoten (Global) · Captopril Cinfa (ES) · Captopril Viatris (FR)

Overall confidence

high

Regulatory sources consulted

openfda-label-0ea90fd4-0da6-4ad2-ab83-6cfbe0ae515e
aemps-cima-ft-62304
ansm-bdpm-rcp-69283419
PubMed PMID:34924198 ↗
PubMed PMID:37417783 ↗
PubMed PMID:38771738 ↗
PubMed PMID:40835369 ↗
OpenFDA · C09AA01
RxNorm rxcui 1998 ↗

Approved indications

Treatment of hypertension.
Treatment of chronic heart failure with reduction of systolic ventricular function, in combination with diuretics and, where appropriate, digitalis and beta-blockers.
Post-myocardial infarction treatment in clinically stable patients with asymptomatic or symptomatic ventricular dysfunction (ejection fraction ≤ 40%).
Treatment of macroproteinuric diabetic nephropathy in patients with type 1 diabetes.
Captopril challenge test for the confirmatory diagnosis of primary aldosteronism. · off-label

Contraindications

Absolute

Hypersensitivity to captopril or any other ACE inhibitor.
History of angioedema related to previous ACE inhibitor therapy.
Hereditary or idiopathic angioedema.
Concomitant use with sacubitril/valsartan. Do not initiate captopril until 36 hours after the last dose of sacubitril/valsartan.
Second and third trimesters of pregnancy.
Concomitant use with aliskiren in patients with diabetes or renal impairment (GFR < 60 ml/min/1.73 m²).

Clinical warnings

Boxed warning · Pregnancy: ACE inhibitors can cause fetal and neonatal morbidity and death when administered during the second and third trimesters of pregnancy. Discontinue as soon as pregnancy is detected. — FDA
Major warning · Angioedema: Angioedema of the face, extremities, lips, tongue, glottis and/or larynx has been reported. Intestinal angioedema is also possible. The risk is higher in black patients and with concomitant use of mTOR inhibitors or sacubitril. — FDA
Major warning · Neutropenia/Agranulocytosis: Risk of neutropenia has been observed, especially in patients with renal impairment, collagen vascular diseases (e.g., lupus, scleroderma), or on immunosuppressive therapy. Monitor white blood cell counts. — ANSM
Hypotension: Symptomatic hypotension may occur, especially in volume-depleted patients (diuretic therapy, dialysis, salt restriction). — FDA

Drug interactions

HighSacubitril/ValsartanC09DX04
Mechanism: Concomitant use is contraindicated due to an increased risk of angioedema from additive inhibition of neprilysin and ACE, leading to increased bradykinin levels.
Recommendation: Contraindicated. Do not co-administer. Allow a washout period of at least 36 hours when switching from one drug to the other.
ANSM RCP
HighPotassium-sparing diuretics and potassium supplementsC03D
Mechanism: ACE inhibitors decrease aldosterone production, which reduces potassium excretion. The combination can lead to severe hyperkalemia.
Recommendation: Combination not recommended. Use only for documented hypokalemia and with frequent monitoring of serum potassium.
FDA labelANSM RCP
HighAliskirenC09XA02
Mechanism: Dual blockade of the renin-angiotensin-aldosterone system (RAAS), which increases the risk of hypotension, hyperkalemia, and renal failure.
Recommendation: Contraindicated in patients with diabetes or renal impairment (GFR < 60 ml/min). Not recommended in other patients.
ANSM RCP
HighLithiumN05AN01
Mechanism: ACE inhibitors reduce the renal clearance of lithium, increasing its serum concentration and risk of toxicity.
Recommendation: Combination not recommended. If necessary, monitor lithium levels closely.
ANSM RCP

Adverse events

Common (≥1%)

dry cough · dizziness · skin rash · taste disturbance · hypotension

Rare but serious

angioedema · agranulocytosis · hyperkalemia · acute renal failure · hepatotoxicity

Pregnancy and lactation

FDA category: Contraindicated in 2nd/3rd trimester

Pregnancy: Contraindicated in the second and third trimesters. Can cause fetal injury (hypotension, renal failure, oligohydramnios, cranial hypoplasia) and death. Discontinue as soon as pregnancy is detected. Lactation: Excreted in breast milk in low levels; risk to the infant is considered low, but caution is advised.

Recent literature (PubMed)

Evidentiary Landscape of Heart Failure Therapies, Regulatory Decisions, and Translation Into Guidelines.
Kaul S · J Am Coll Cardiol · 2025 · Relevance 5/5
Este artículo de revisión destaca que captopril fue uno de los 11 fármacos fundamentales aprobados antes de 2015 para la insuficiencia cardíaca con fracción de eyección reducida (ICFEr) que demostró reducir la mortalidad y la morbilidad, a diferencia de muchos tratamientos más nuevos.
Angiotensin-converting enzyme inhibitor induced cough compared with placebo, and other antihypertensives: A systematic review, and network meta-analysis.
Hu Y, et al. · J Clin Hypertens (Greenwich) · 2023 · Relevance 4/5
Una revisión sistemática y metaanálisis en red de 135 ECA encontró que los IECA tienen un riesgo 2.21 veces mayor de tos en comparación con el placebo. Dentro de la clase de los IECA, captopril se clasificó como uno de los que tienen menor propensión a inducir tos en comparación con otros como ramipril o moexipril.
Drugs for hypertension.
Unknown · Med Lett Drugs Ther · 2024 · Relevance 4/5
Este artículo señala que debido a los bajos niveles de captopril en la leche materna, las cantidades ingeridas por el lactante son pequeñas y no se espera que causen efectos adversos, lo que sugiere que es relativamente seguro durante la lactancia.
Diagnosis of primary hyperaldosteronism.
Araujo-Castro M, et al. · Med Clin (Barc) · 2022 · Relevance 3/5
Esta revisión sobre el diagnóstico del hiperaldosteronismo primario menciona la prueba de supresión con captopril como una de las pruebas de confirmación comúnmente utilizadas después de un cribado positivo, destacando un uso diagnóstico específico del fármaco.