P - Contraindicated in pregnancy
L - Caution when used during lactation
LI - Lab *
Enalapril is an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension and some types of chronic heart failure. Enalapril was the first member of the group of ACE inhibitors known as the dicarboxylate-containing ACE inhibitors. It is marketed by Merck & Co. (Merck, Sharp & Dohme) under the trade names, Renitec and Vasotec. The primary effect of enalapril, as with all ACE inhibitors, is to lower blood pressure.
Enalapril is de-esterified into the active enalaprilat resulting in potent inhibition of ACE thus leading to reduced levels of angiotensin II and aldosterone. Clinically, BP is reduced, salt and water retention is corrected. Ventricular hypertrophy is reversed. Renal blood flow is increased but in patients with renal impairment there may be oliguria or acute renal failure.
Absorption 60% of dose is absorbed from the GI tract (oral); peak plasma concentrations after 1 hr (enalapril), 3-4 hr (enalaprilat).
Distribution Protein-binding: 50-60% (enalaprilat).
Metabolism Hepatic: Hydrolysed to enalaprilat.
Excretion Via urine (60% as enalaprilat and unchanged drug); via faeces (remaining dose); 11 hr (elimination half-life). Removed by haemodialysis and peritoneal dialysis.
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Initial hypotension may be severe and prolonged. Dizziness, headache, fatigue, persistent dry cough, abnormal taste, lassitude, rash, neutropenia, renal impairment or failure. Potentially Fatal: Angioedema.
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Impaired renal function. Hyperkalaemia, hypovolaemia, collagen vascular disease, valvular stenosis, during or immediately before or after anaesthesia, unilateral renal artery stenosis. Hypotension due to volume depletion, diuretic therapy. Monitor WBC count. Lactation, children.
Diuretics potentiate hypotensive action. May increase lithium levels. Other antihypertensives potentiate enalapril action. Potentially Fatal: Increased risk of bone marrow suppression when used with immunosuppressive drugs. Hyperkalaemia with potassium-sparing diuretics or potassium supplements especially in the presence of renal failure. Probenecid delays excretion. Potentiates analgesia and respiratory depression produced by morphine. NSAIDs may result in further deterioration of renal function.
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Oral Hypertension Adult: Initially, 5 mg at bedtime. Maintenance: 10-20 mg once daily increased up to 40 mg in divided doses in severe hypertension. Max: 40 mg/day. Child: 80 mcg/kg once daily. Max: 5 mg/day. Elderly: May initiate at lower doses at 2.5 mg daily. Renal impairment: Initial dose should be halved. Oral Heart failure Adult: Initially, 2.5 mg daily. Maintenance: 20 mg once daily as a single or in 2 divided doses, up to 40 mg daily in 2 divided doses. Renal impairment: Initial dose should be halved. Intravenous Hypertension Adult: 1.25 mg by slow inj over 5 minutes repeated every 6 hr if needed. Renal impairment: Initial dose should be halved. Special Populations Patients on diuretics: Initial dose should be halved.
May be taken with or without food
Contraindicated in pregnancy. Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus. In 2nd & 3rd trimesters Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Caution when used during lactation
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Hypersensitivity. History of angioedema due to previous treatment with ACE inhibitors; bilateral renal artery stenosis. Pregnancy.
Intravenous Store below 30 ℃ Oral Store below 30 ℃
Intravenous Store below 30 ℃ Oral Store below 30 ℃
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