captopril (Capoten)
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Introduction
Tradename: Capoten.
Indications
- hypertension
- treatment of hypertensive urgency
- congestive heart failure:
- left ventricular systolic dysfunction after myocardial infarction
- diabetic nephropathy
- nondiabetic proteinuric nephropathy
- cystinuria, cystine renal calculi[7] Contradindications:
- pregnancy:
- teratogenic in 1st trimester[8]
- fetal or neonatal renal failure in 2nd or 3rd trimester
- scleroderma renal crisis is exception[8]
- safe in lactation[8]
- pregnancy:
Dosage
Tabs: 12.5, 25, 50, 100 mg.
Pharmacokinetics
- oral bioavailability is about 60%
- food impairs absorption[6]
- 30% is bound to plasma proteins
- 50% is metabolized by the liver
- 30% is excreted into the urine
- onset of action: (single dose) 15-60 minutes
- duration of action: (single dose) 6-12 hours
- 1/2 life is 1.7 hours[4] in healthy individuals, but is prolonged in patients with renal failure or CHF
elimination via liver
elimination via kidney
1/2life = 6-8 hours
1/2life = 1.7 hours
Adverse effects
- common (> 10%)
- transient, non-productive, dry cough
- not common (1-10%)
- uncommon (< 1%)
- hypotension, hyperkalemia, neutropenia, agranulocytosis*, angioedema*, proteinuria, worsening of renal failure, disturbances in taste
* side effects of angioedema & agranulocytosis may be more common in captopril than in other ACE inhibitors because of sulfhydryl group, especially in patients with connective tissue disease or serum creatinine > 1.5 mg/dL
- drug adverse effects of renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
- drug adverse effects of ACE inhibitors
- drug adverse effects of antihypertensive agents
Drug interactions
- NSAIDs may reduce hypotensive effect
- phenothiazines may increase pharmacologic effects of captopril
- high risk of hypersensitivity reactions when used in combination with allopurinol
- captopril increases serum levels of lithium & digoxin
- agents that increase serum K+
- drug interaction(s) of fluticasone with HIV1 protease inhibitors
- drug interaction(s) of calcineurin inhibitors with ACE inhibitors
- drug interaction(s) of calcium channel blockers with ACE inhibitors
- drug interaction(s) of renin-angiotensin-aldosterone inhibitors with trimethoprim-sulfamethoxazole
- drug interaction(s) of lithium carbonate with ACE inhibitors
- drug interaction(s) of ACE inhibitor with trimethoprim
- drug interaction(s) of ACE inhibitors with potassium-sparing diuretics
- drug interaction(s) of ACE inhibitors with aliskiren
- drug interaction(s) of ACE inhibitors with angiotensin II receptor antagonists
- drug interaction(s) of potassium chloride with ACE inhibitors
- drug interaction(s) of spironolactone with ACE inhibitors
- drug interaction(s) of diuretics with ACE inhibitors
- drug interaction(s) of beta blockers with ACE inhibitors
- drug interaction(s) of NSAIDs, diuretics & ACE inhibitors
- drug interaction(s) of NSAIDs with ACE inhibitors
- drug interaction(s) of NSAIDs & antihypertensives
Mechanism of action
- ACE inhibitors block conversion of angiotensin-1 to angiotensin-2 by inhibiting angiotensin converting enzyme
Notes
- captopril improves symptoms of heart failure, improves exercise tolerance & improves functional capacity in patients with heart failure
- captopril also attenuates ventricular enlargement & improves hemodynamics & survival in patients with left ventricular dysfunction secondary to myocardial infarction
- it is likely that other ACE inhibitors have similar beneficial effects, but have been less well studied.
More general terms
- pyrrolidine; tetrahydropyrrole
- carboxylic acid
- thiol; sulhydryl compound; mercaptan
- angiotensin-converting enzyme (ACE) inhibitor
Additional terms
- angiotensin converting enzyme (ACE)
- angiotensin II (Giapreza)
- Captopril Prevention Project (CAPPP)
- captopril scan; ACE inhibitor renography; renal scintigraphy
- captopril-renin stimulation test
- ELITE II Study
Component of
References
- ↑ Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1990. pg 760-1
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Manual of Medical Therapeutics, 28th ed, Ewald & McKenzie (eds), Little, Brown & Co, Boston, 1995, pg 117
- ↑ 4.0 4.1 Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 6.0 6.1 Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 470
- ↑ 7.0 7.1 Deprecated Reference
- ↑ 8.0 8.1 8.2 8.3 Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
- ↑ 9.0 9.1 NEJM Knowledge+ Question of the Week. Sept 18, 2018 https://knowledgeplus.nejm.org/question-of-week/15/