II. Indications

III. Mechanism

  1. See ACE Inhibitor
  2. Captopril is a sulfhydryl-containing analog of Proline
  3. Angiotensin-converting enzyme (ACE) inhibitor
  4. Possible antineoplastic activity
    1. May decrease tumor Angiogenesis by inhibiting endothelial cell matrix metalloproteinases (MMPs) and endothelial cell migration

IV. Dosing: Adults

  1. Hypertension
    1. Start 25 mg orally twice to three times daily
    2. Target 25 to 150 mg orally twice to three times daily
    3. Maximum 450 mg/day
  2. Congestive Heart Failure (CHF)
    1. Start 6.25 - 12.5 mg orally three times daily
    2. Target 50 to 100 mg orally three times daily
    3. Maximum 450 mg/day
  3. Diabetic Nephropathy
    1. Take 25 mg orally three times daily
  4. Hypertensive Urgency (not FDA approved)
    1. Take 12.5 to 25 mg orally every 30 to 60 minutes as needed up to 2 doses

V. Dosing: Children (not FDA approved)

  1. Newborns
    1. Give 0.1 to 0.4 mg/kg/day orally divided every 6 to 8 hours
  2. Infants
    1. Start 0.15 to 0.3 mg/kg/dose and titrate
    2. Maximum 6 mg/kg/day divided two to four times daily
  3. Children
    1. Start 0.3 to 0.5 mg/kg/dose and titrate
    2. Maximum 6 mg/kg/day up to 450 mg/day divided two to four times daily

VI. Supplied

  1. Available as scored generic tablets: 12.5, 25, 50 and 100 mg
  2. To make Captopril solution (1 mg/ml)
    1. Disolve tablet in flavored syrup (e.g. 25 mg tablet in 25 ml syrup)
    2. Stable at room Temperature for up to 7 days

VII. Metabolism

  1. Primarily renal excretion

VIII. Adverse Effects

IX. Safety

  1. See ACE Inhibitor
  2. Pregnancy Category X
  3. Captopril is among only two ACE Inhibitors labeled by AAP as compatible with Breast Feeding
    1. However, Captopril is excreted in Breast Milk and may be associated with newborn adverse effects

XI. References

  1. (2016) Presc Lett, Resource #321151, ACE Inhibitor Antihypertensive Dose Comparison
  2. (2020) Med Lett Drugs Ther 62(1598): 73-80
  3. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 68-9
  4. Hamilton (2020) Tarascon Pocket Pharmacopoeia

Images: Related links to external sites (from Bing)

Related Studies

Cost: Medications

captopril (on 11/23/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
CAPTOPRIL 100 MG TABLET Generic $1.38 each
CAPTOPRIL 12.5 MG TABLET Generic $0.45 each
CAPTOPRIL 25 MG TABLET Generic $0.38 each
CAPTOPRIL 50 MG TABLET Generic $0.68 each

Ontology: Captopril (C0006938)

Definition (NCI_NCI-GLOSS) A drug used to treat high blood pressure that is also being studied in the prevention of side effects caused by radiation therapy used in the treatment of cancer. It belongs to the family of drugs called ACE inhibitors.
Definition (NCI) A sulfhydryl-containing analog of proline with antihypertensive activity and potential antineoplastic activity. Captopril competitively inhibits angiotensin converting enzyme (ACE), thereby decreasing levels of angiotensin II, increasing plasma renin activity, and decreasing aldosterone secretion. This agent may also inhibit tumor angiogenesis by inhibiting endothelial cell matrix metalloproteinases (MMPs) and endothelial cell migration. Captopril may also exhibit antineoplastic activity independent of effects on tumor angiogenesis. (NCI04)
Definition (MSH) 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.
Definition (CSP) potent and specific inhibitor of peptidyl dipeptidase A; it acts to suppress the renin-angiotensin system and inhibits blood pressure responses to exogenous angiotensin.
Definition (PDQ) A sulfhydryl-containing analog of proline with antihypertensive activity and potential antineoplastic activity. Captopril competitively inhibits angiotensin converting enzyme (ACE), thereby decreasing levels of angiotensin II, increasing plasma renin activity, and decreasing aldosterone secretion. This agent may also inhibit tumor angiogenesis by inhibiting endothelial cell matrix metalloproteinases (MMPs) and endothelial cell migration. Captopril may also exhibit antineoplastic activity independent of effects on tumor angiogenesis. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=37824&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=37824&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C340" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116)
MSH D002216
SnomedCT 29439004, 387160004
LNC LP32689-9, LP18914-9, MTHU006862
English captopril, (S)-1-(3-Mercapto-2-methyl-1-oxopropyl)-L-proline, L-Proline, 1-(3-mercapto-2-methyl-1-oxopropyl)-, (S)-, captopril (medication), CAPTOPRIL, Captopril [Chemical/Ingredient], Captopril (product), Captopril (substance), CPT, Captopril
Swedish Kaptopril
Czech kaptopril
Finnish Kaptopriili
Russian KAPTOPRIL, SQ 14225, КАПТОПРИЛ
Japanese カプトプリル
French (S)-1-(3-Mercapto-2-méthyl-1-oxopropyl)-L-proline, Captopril
Croatian KAPTOPRIL
Polish Kaptopryl
Spanish captopril (producto), captopril (sustancia), captoprilo, captopril, Captopril
German Captopril
Italian Captopril
Portuguese Captopril

Ontology: Capoten (C0591224)

Concepts Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116)
MSH D002216
English capoten, Capoten