Captopril

Indications
Oral
Hypertension
Adult: Initially, 12.5 mg bid or 6.25 mg bid in combination with a diuretic, at bedtime to avoid precipitous fall in BP, gradually increased at 2-4-wk intervals according to response. Maintenance: 25-50 mg bid. Max: 50 mg tid.
Child: Neonate: Test dose: 10-50 mcg/kg (for neonates <37 wk postmenstrual age: 10 mcg/kg), monitor BP for 1-2 hr; if tolerated give 10-50 mcg/kg 2-3 times daily, increased if needed. Max: 2 mg/kg daily in divided doses (for neonates <37 wk postmenstrual age: 300 mcg/kg daily in divided doses). 1 mth-12 yr: Test dose: 100 mcg/kg (max: 6.25 mg), monitor BP for 1-2 hr; if tolerated give 100-300 mcg/kg 2-3 times daily, increased if needed. Max: 6 mg/kg daily in divided doses (for 1-12 mth: Max: 4 mg/kg daily in divided doses). 12-18 yr: Test dose: 100 mcg/kg or 6.25 mg, monitor BP for 1-2 hr; if tolerated give 12.5-25 mg 2-3 times daily, increased if needed. Max: 150 mg daily in divided doses.
Elderly: Initially, 6.25 mg bid.
CrCl (ml/min)Dosage Recommendation
21-40Initially, 25 mg daily. Max: 100 mg daily.
10-20Initially, 12.5 mg daily. Max: 75 mg daily.
<10Initially, 6.25 mg daily. Max: 37.5 mg daily.

Oral
Heart failure
Adult: Initially, 6.25-12.5 mg bid-tid. Maintenance: 25 mg bid-tid. Max: 50 mg tid.
Child: Neonate: Test dose: 10-50 mcg/kg (for neonates <37 wk postmenstrual age: 10 mcg/kg), monitor BP for 1-2 hr; if tolerated give 10-50 mcg/kg 2-3 times daily, increased if needed. Max: 2 mg/kg daily in divided doses (for neonates <37 wk postmenstrual age: 300 mcg/kg daily in divided doses). 1 mth-12 yr: Test dose: 100 mcg/kg (max: 6.25 mg), monitor BP for 1-2 hr; if tolerated give 100-300 mcg/kg 2-3 times daily, increased if needed. Max: 6 mg/kg daily in divided doses (for 1-12 mth: Max: 4 mg/kg daily in divided doses). 12-18 yr: Test dose: 100 mcg/kg or 6.25 mg, monitor BP for 1-2 hr; if tolerated give 12.5-25 mg 2-3 times daily, increased if needed. Max: 150 mg daily in divided doses.
CrCl (ml/min)Dosage Recommendation
21-40Initially, 25 mg daily. Max: 100 mg daily.
10-20Initially, 12.5 mg daily. Max: 75 mg daily.
<10Initially, 6.25 mg daily. Max: 37.5 mg daily.

Oral
Post myocardial infarction
Adult: May be started 3 days after MI. Initially, 6.25 mg/day increased after several wk to 150 mg daily in divided doses if tolerated.
CrCl (ml/min)Dosage Recommendation
21-40Initially, 25 mg daily. Max: 100 mg daily.
10-20Initially, 12.5 mg daily. Max: 75 mg daily.
<10Initially, 6.25 mg daily. Max: 37.5 mg daily.

Oral
Diabetic nephropathy
Adult: Proteinuria >500 mg per 24 hr (in patients with Type 1 diabetes mellitus and retinopathy): 25 mg tid. May be taken with other anti-hypertensives if patient requires further lowering of BP.
Child: Neonate: Test dose: 10-50 mcg/kg (for neonates <37 wk postmenstrual age: 10 mcg/kg), monitor BP for 1-2 hr; if tolerated give 10-50 mcg/kg 2-3 times daily, increased if needed. Max: 2 mg/kg daily in divided doses (for neonates <37 wk postmenstrual age: 300 mcg/kg daily in divided doses). 1 mth-12 yr: Test dose: 100 mcg/kg (max: 6.25 mg), monitor BP for 1-2 hr; if tolerated give 100-300 mcg/kg 2-3 times daily, increased if needed. Max: 6 mg/kg daily in divided doses (for 1-12 mth: Max: 4 mg/kg daily in divided doses). 12-18 yr: Test dose: 100 mcg/kg or 6.25 mg, monitor BP for 1-2 hr; if tolerated give 12.5-25 mg 2-3 times daily, increased if needed. Max: 150 mg daily in divided doses.
CrCl (ml/min)Dosage Recommendation
21-40Initially, 25 mg daily. Max: 100 mg daily.
10-20Initially, 12.5 mg daily. Max: 75 mg daily.
<10Initially, 6.25 mg daily. Max: 37.5 mg daily.


Special Populations: Patients with severe renal impairment: CrCl <30 mL/min: Initially, 12.5 mg bid.
Contraindications
Known hypersensitivity to the drug. Bilateral renal artery stenosis, hereditary angioedema; renal impairment; pregnancy.
Warnings / Precautions
Patients on diuretics or with sodium depletion should discontinue diuretics or increase sodium intake prior to initiation of therapy. Renal impairment, SLE and other autoimmune collagen disorders and during concurrent use of immunosuppressant or leucopenic drugs, monitor WBC count and urinary protein before and during therapy. Lactation. Porphyria. Severe CHF.
Adverse Reactions
Hypotension, tachycardia, chest pain, palpitations, pruritus, hyperkalaemia. Proteinuria; angioedema, skin rashes; taste disturbance, nonproductive cough, headache.
Potentially Fatal: Neutropenia, usually occurs within 3 mth of starting therapy especially in patients with renal dysfunction or collagen diseases. Hyperkalaemia. Anaphylactic reactions.
Overdose Reactions
Treatment includes correction of hypotension. Volume expansion with an IV infusion of normal saline may be used for restoration of BP.
Drug Interactions
Concurrent treatment with diuretics increases the hypotensive action of ACE inhibitors hence, starting dose must be kept low.
Potentially Fatal: Risk of bone marrow depression increased with concomitant therapy with immunosuppressive drugs. Hyperkalaemia may result if used along with potassium supplements and potassium-sparing diuretics especially if renal function is impaired. Probenecid delays excretion of captopril thereby increasing blood levels. Analgesic and respiratory depression of morphine may be accentuated by captopril. NSAIDs may result in further deterioration of renal function.
See Below for More captopril Drug Interactions
Lab Interactions
False-positive test for urinary nitrites and acetone. Increased BUN, creatinine and potassium.
Food Interactions
Concurrent admin with food may reduce serum levels of captopril. Avoid dong quai (if using for hypertension), ephedra, yohimbe, ginseng (may worsen hypertension) and garlic (may increase antihypertensive effect).
Mechanism of Actions
Captopril competitively inhibits the conversion of angiotensin I (ATI) to angiotensin II (ATII), thus resulting in reduced ATII levels and aldosterone secretion. It also increases plasma renin activity and bradykinin levels. Reduction of ATII leads to decreased sodium and water retention. By these mechanisms, captopril produces a hypotensive effect and a beneficial effect in congestive heart failure.
Absorption: 60-75% absorbed from the GI tract (oral); peak plasma concentrations after 1 hr. Absorption may be reduced in the presence of food.
Distribution: Protein-binding: 30%; crosses the placenta and enters breast milk at about 1% of maternal blood concentrations.
Excretion: Via urine (40-50% as unchanged, the rest as disulfide and other metabolites); 2-3 hr (elimination half-life), may be increased in renal impairment. Removed by haemodialysis.
Administration
Should be taken on an empty stomach. (Take on an empty stomach 1 hr before or 2 hr after meals.)
Storage Conditions
Oral: Store below 30°C
ATC Classification
C09AA01 - captopril ; Belongs to the class of ACE inhibitors. Used in the treatment of cardiovascular disease.
Storage
Oral: Store below 30°C
Available As
  • Captopril 12.5 mg
  • Captopril 25 mg
  • Captopril 50 mg
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