Enalapril

Summary

Enalapril is an oral ACE inhibitor prodrug widely used for hypertension, heart failure, and asymptomatic left ventricular dysfunction. It is one of the most commonly prescribed antihypertensives and has extensive evidence for cardiovascular morbidity and mortality reduction.

Mechanism of Action

Enalapril is a prodrug hydrolyzed to enalaprilat, which competitively inhibits angiotensin-converting enzyme (ACE), preventing conversion of angiotensin I to angiotensin II. This reduces vasoconstriction and aldosterone secretion, lowering blood pressure and cardiac afterload.

Routes of Administration

Goals & Uses

• Hypertension managementCardiovascularHigh
• Diabetic nephropathyRenalModerate
• Asymptomatic LV dysfunctionCardiovascularHigh
• Post-MI LV remodeling preventionCardiovascularModerate
• Heart failure (reduced EF)CardiovascularHigh

Contraindications

• Hereditary or idiopathic angioedemaImmunologic/AllergicHigh
• Pregnancy (2nd and 3rd trimester)ObstetricHigh
• Concurrent aliskiren use in diabetes or CKD (eGFR <60)Drug InteractionHigh
• History of ACE inhibitor-induced angioedemaImmunologic/AllergicHigh
• Bilateral renal artery stenosisVascular/RenalHigh

Adverse Effects

• Renal impairment (acute)RenalUncommon
• Hypotension (first-dose)CardiovascularCommon
• HyperkalemiaElectrolyte ImbalanceUncommon
• Dry coughRespiratoryCommon
• AngioedemaImmunologicRare
• Dizziness/headacheNeurologicalCommon

Drug Interactions

• Potassium-sparing diuretics / potassium supplementsHigh
• Sacubitril (Entresto combination)High
• AliskirenHigh
• NSAIDsModerateMay increase renal risk in susceptible patients
• Antidiabetic agents (insulin, sulfonylureas)Low
• LithiumModerate

Population Constraints

• Chronic kidney disease (severe, eGFR <30)RenalRelative
• PregnancyReproductive SafetyAbsolute
• Neonates and infantsPediatricRelative
• Elderly (>75 years)GeriatricRelative
• Bilateral renal artery stenosisVascularAbsolute

Regulatory Status

• European UnionApprovedApproved: Hypertension, Symptomatic heart failure, Prevention of symptomatic heart failure in LV dysfunctionApproved via national procedures; available as generic in all EU member states (e.g., Renitec, Xanef).
• United StatesApprovedApproved: Hypertension, Heart failure, Asymptomatic left ventricular dysfunctionFDA approved 1985 (Vasotec, Merck); widely available as generic. IV enalaprilat approved for hypertensive urgency.
• United KingdomApprovedApproved: Hypertension, Heart failure, Prevention of symptomatic heart failure in asymptomatic LV dysfunctionMHRA approved; widely available as generic on NHS formulary.

Approved by the FDA in 1985 (Vasotec). Available as generic worldwide. IV form (enalaprilat) also approved for hypertensive urgency.

Evidence & Sources

No sources recorded yet.