Class: ACE-I, Antihypertensive
Dosage Forms. Oral Tablet: 2.5 mg, 5 mg, 10 mg, 20 mg; Oral Solution: 1 mg/mL
Common FDA Label Indication, Dosing, and Titration.
Heart failure: Infants ≥4 d of age and Adolescents, 0.1-0.5 mg/kg po daily, max 0.94 mg/kg po daily; Adults, 2.5 mg po daily, titrate to 20-40 mg po daily in divided doses
Hypertension: Infants ≥1 mo of age and Adolescents, 0.08 mg/kg up to 5 mg po daily, max 0.58 mg/kg or 40 mg po daily; Adults, 5 mg po daily, max 40 mg po daily in divided doses
Kidney disease, nondiabetic: Children 7-18 y of age, 0.1-0.5 mg/kg po daily, max 20 mg po daily; Adults, 5 mg po daily, max 20 mg po daily
Diabetic nephropathy: 5-20 mg po daily
MI: 2.5 mg po daily, may titrate to 20 mg po daily
MOA. Enalapril is a prodrug that is rapidly converted to its active metabolite, enalaprilat, a competitive ACE-I. It reduces serum aldosterone, leading to decreased sodium retention, potentiates the vasodilator kallikrein-kinin system, inhibits the sympathetic nervous system, and inhibits the tissue renin-angiotensin system. The net effect is reduction in total peripheral resistance and blood pressure in hypertensive patients, and reduction of elevated afterload in patients with heart failure.
Drug Characteristics: Enalapril
Dose Adjustment Hepatic Not required Absorption F = 60%, no effect of food on absorption
Dose Adjustment Renal CrCl <30 mL/min, initial dose 2.5 mg po daily, max 40 mg po daily Distribution 50-60% protein bound
Dialyzable Yes Metabolism Extensive hepatic to 1 active metabolite
Pregnancy Category D Elimination Renal 61% with a half-life of 1.3 h (parent drug), 11 h (metabolite)
Lactation Weigh risks and benefits Pharmacogenetics None known
Contraindications Hypersensitivity to enalapril, history of angioedema, pregnancy, concurrent sacubitril Black Box Warnings Pregnancy