PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
captopril

2D structure

Overview

Generic Names: Captoprilum [INN-Latin]; Captopryl; L-Captopril
Trade Names: Acediur; Aceplus; Acepress; Acepril; Alopresin; Apopril; Capoten; Captolane; Captoril; Cesplon; Dilabar; Garranil; Hipertil; Hypertil; Lopirin; Lopril; Tenosbon; Tensobon; Tensoprel
PharmGKB Accession Id: PA448780

Description

A potent and specific inhibitor of peptidyl-dipeptidase A. It blocks the conversion of angiotensin I to angiotensin II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the renin-angiotensin system and inhibits pressure responses to exogenous angiotensin. PubChem (source: Drug Bank)

Indication

For the treatment of hypertension. It may be used alone or in combination with thiazide diuretics. (source: Drug Bank)

ATC Therapeutic Category

  • C09AA:ACE inhibitors, plain

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Captopril competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. As angiotensin II is a vasoconstrictor and a negative feedback mediator for renin activity, lower angiotensin II levels results in a decrease in blood pressure, an increase in renin activity, and stimulation of baroreceptor reflex mechanisms. Kininase II, an enzyme which degrades the vasodilator bradykinin, is identical to ACE and may also be inhibited. (source: Drug Bank)

Pharmacology

Captopril, an angiotensin-converting enzyme (ACE) inhibitor, is used to treat hypertension, congestive heart failure, and renal syndromes such as diabetic nephropathy and scleroderma. The adverse effect and pharmacokinetic limitations of captopril stimulated the development enalapril and subsequent ACE inhibitors. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Avoid natural licorice.
Avoid salt substitutes containing potassium.
Do not take calcium, aluminum, magnesium or Iron supplements within 2 hours of taking this medication.
Take on empty stomach: 1 hour before or 2 hours after meals, food decreases absorption by 30 to 55%. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic (source: Drug Bank)

Protein Binding

About 25-30% of the circulating drug is bound to plasma proteins (source: Drug Bank)

Absorption

75% without food (the presence of food in the gastrointestinal tract reduces absorption by about 30 to 40 percent). (source: Drug Bank)

Toxicity

Symptoms of overdose include coma, lethargy, low blood pressure, sluggishness, and stomach and intestinal irritation and hyperactivity. (source: Drug Bank)

Isomeric SMILES Code:

C[C@H](CS)C(=O)N1CCC[C@H]1C(=O)O (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs5182 at chr3:149942085 in AGTR1
    The C allele carriers tend to have reduced risk of myocardial infarction in patients taking ACE inhibitors.
    Variant Name:
    AGTR1: 573C/T; 573C>T
    Related Drugs:
    Ace Inhibitors, Plain, captopril, enalapril, fosinopril, imidapril, lisinopril
    Related Diseases:
    Hypertension, Myocardial Infarction, Stroke
    Evidence:
    PMID:18347611
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ACE
  • CO
  • PD
  •   
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
ACE2
  • CO
  • PD
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
AGT
  •   
  • PD
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
AGTR1
  • CO
  • PD
  •   
  •   
  • GN
Publications, Variants
No phenotype data Genotype Data Available Literature annotations available Not annotated
BDKRB2
  •   
  •   
  •   
  • FA
  •   
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ATP1A1 Uncurated Annotation (source: Drug Bank)
ALB Uncurated Annotation (source: Drug Bank)
ACE Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
amiloride Uncurated Annotation Increased risk of hyperkaliemia (source: Drug Bank)
lithium Uncurated Annotation The ACE inhibitor increases serum levels of lithium (source: Drug Bank)
potassium Uncurated Annotation Increased risk of hyperkaliemia (source: Drug Bank)
spironolactone Uncurated Annotation Increased risk of hyperkaliemia (source: Drug Bank)
tizanidine Uncurated Annotation Tizanidine increases the risk of hypotension with the ACE inhibitor (source: Drug Bank)
triamterene Uncurated Annotation Increased risk of hyperkaliemia (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Angioedema
  •   
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Cardiomyopathies
  •   
  • PD
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Cough
  •   
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Diabetes Mellitus
  •   
  • PD
  •   
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Hypertension
  • CO
  • PD
  •   
  •   
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Myocardial Infarction
  • CO
  • PD
  •   
  •   
  • GN
Publications, Variants
Phenotype data available No genotype data Literature annotations available Not annotated
Stroke
  • CO
  • PD
  •   
  •   
  • GN
Publications, Variants

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01197
ChEBI ID:
3380
KEGG Drug ID:
D00251
PubChem Compound ID:
44093
PubChem Substance ID:
7847317

Common Searches

Search PubMed
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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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