Captopril

ACE Inhibitor · ACE inhibitor

Indications

Mild to moderate hypertension as adjunct to thiazide diuretics. Severe hypertension where other measures have failed. Adjunct to diuretics and, where appropriate, digitalis in congestive cardiac failure. Short-term treatment within 24 hrs of onset of MI. Diabetic neuropathy in type 1 DM.

Dosage

Adults: Hypertension: Mild to moderate hypertension: Initially 12.5 mg twice daily with a thiazide. Maintenance, 25 mg twice daily increasing gradually at 2-4 wk intervals if necessary to max 50 mg twice daily. Severe hypertension: Initially 12.5 mg twice daily increasing if necessary to 50 mg three times daily; see literature. Congestive cardiac failure: Initially 6.25 mg or 12.5 mg; usual maintenance, 25 mg three times daily. Max 150 mg daily. See literature. Short-term treatment within 24 hrs of onset of MI: Initially 6.25 mg, increased to 12.5 mg after 2 hrs, followed by 25 mg after 12 hrs; increased if tolerated to 50 mg two times daily for 4 wks. Diabetic neuropathy in type 1 DM: 75-100 mg daily in divided doses. Children: Not recommended.

Adverse Effects

Neutropenia, agranulocytosis, proteinuria, angioedema, pancreatitis, tachycardia, angina, anorexia, drowsiness, headache, paraesthesia, hepatic failure, hypotension, rash, loss of taste, cough (rare), sleep disorders, dizziness, dyspnoea, GI upset, dry mouth, pruritus, alopecia, blood dyscrasias.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Aortic stenosis. Renal impairment, angioedema, history of angioedema associated with previous ACE inhibitor therapy. Precautions: Collagen vascular disease, anaesthesia, diabetes. Elderly. Salt or volume depletion; correct before commencing therapy with a lower dose, aortic and mitral valve stenosis, outflow obstruction, renovascular hypertension, severe CHF, haemodialysis, renal impairment; monitor renal function, serum electrolytes, white cell count and urinary protein before and during therapy.

Interactions

K+ sparing diuretics or K+ supplements, NSAID, vasodilators, clonidine, allopurinol, procainamide, probenecid, immunosuppressants, other antihypertensives, trimethoprim, heparin, lithium, antidiabetic agents, TCADs, antipsychotics, sympathomimetics, hyposensitising agents, anaesthetics, high flux dialysis memebranes, alcohol.

Advice to Patient

Take 1 hour before or 2 hours after meals. Contact prescriber if there is chest pain or palpitations; mouth sores; fever; chills; swelling of feet, ankles, face, mouth, tongue; skin rash; numbness; tingling; muscle pain; difficulty in breathing or unusual cough. Do not take potassium supplements or salt substitutes without consulting prescriber. Change position slowly.

Pharmacokinetics

Onset of action: Within 15 min. Peak effect: Blood pressure reduction: 1-1.5 hrs after dose. Max effect: Antihypertensive: 60-90 min. Duration: Dose related. Absorption: 60%-75%; rapid. Bioavailability: Approx. 60%-75%; decreased 30%-40% by food. Metabolism: 50% metabolized. Half-life elimination: Infants with CHF: 3.3 hrs. Children: 1.5 hrs. Adults (healthy): Approx. 1.7 hrs. Time to peak: Within 1-2 hrs. Excretion: Urine (>95%) within 24 hrs.

Unlicensed Use

Children: Hypertension, heart failure, proteinuria in nephritis: Neonate, test dose, 10-50 mcg/kg (10 mcg/kg in neonate less than 37 wk corrected gestational age), monitor blood pressure carefully for 1-2 hr; if tolerated give 10-50 mcg/kg 2-3 times daily increased as necessary to max. 2 mg/kg daily in divided doses (max 300 mcg/kg daily in divided doses in neonate less than 37 wk (corrected gestational age); 1 mth-12 yr, test dose, 100 mcg/kg (max 6.25 mg), monitor blood pressure carefully for 1-2 hr; if tolerated give 100-300 mcg/kg 2-3 times a day, increased as necessary to max 6 mg/kg daily in divided doses (max 4 mg/kg daily in divided doses for child 1 mth-1 yr); 12-18 yr, test dose, 100 mcg/kg or 6.25 mg, monitor blood pressure carefully for 1-2 hr; if tolerated give 12.5-25 mg 2-3 times a day, increased as necessary to max. 150 mg daily in divided doses. Diabetic nephropathy:…

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