Enalaprilat

Summary

Enalaprilat is the active diacid form of enalapril and the only ACE inhibitor available for intravenous administration. It is used for the management of hypertensive urgencies and emergencies when oral therapy is not feasible. It acts by directly inhibiting ACE without requiring hepatic conversion.

Mechanism of Action

Active diacid metabolite that competitively inhibits angiotensin-converting enzyme (ACE), preventing conversion of angiotensin I to angiotensin II, thereby reducing vasoconstriction and aldosterone secretion, leading to decreased blood pressure and reduced cardiac afterload.

Routes of Administration

Goals & Uses

• Reduction of proteinuria in renal diseaseRenalModerate
• Hypertensive emergency/urgency managementCardiovascularHigh
• Heart failure management (acute)CardiovascularModerate
• Blood pressure control in hospitalized patientsCardiovascularHigh

Contraindications

• Hereditary or idiopathic angioedemaImmunologic/AllergicHigh
• Hypersensitivity to enalaprilat or any ACE inhibitorHypersensitivityHigh
• Pregnancy (2nd and 3rd trimester)ObstetricHigh
• Concomitant use with sacubitril/valsartanDrug InteractionHigh
• History of ACE inhibitor-induced angioedemaImmunologic/AllergicHigh
• Severe bilateral renal artery stenosisRenalHigh

Adverse Effects

• Injection site reactionsLocalUncommon
• Acute kidney injuryRenalUncommonSudden decline in kidney function
• HypotensionCardiovascularCommonLow blood pressure
• Headache / dizzinessNeurologicalCommon
• HyperkalemiaElectrolyte ImbalanceUncommon
• AngioedemaImmunologicRare

Drug Interactions

• Potassium-sparing diuretics / potassium supplementsModerate
• Diuretics (loop/thiazide)Moderate
• Sacubitril/valsartan (Entresto)High
• AliskirenHigh
• NSAIDsModerateMay increase renal risk in susceptible patients
• LithiumModerate

Population Constraints

• PregnancyReproductive SafetyAbsolute
• Bilateral renal artery stenosis or single functioning kidney with renal artery stenosisRenalAbsolute
• Renal impairmentOrgan ImpairmentRelative
• Elderly patientsAgeRelative
• Neonates and infants (premature/newborn)PediatricAbsolute

Regulatory Status

• European UnionApprovedApproved: Hypertensive crises, Acute heart failure (when oral therapy not feasible)Available as intravenous formulation across EU member states for acute hypertension management.
• United StatesApprovedApproved: Hypertension (intravenous treatment when oral therapy not feasible)FDA-approved as Vasotec IV. The oral prodrug enalapril maleate is also separately approved for hypertension and heart failure.
• United KingdomApprovedApproved: Hypertension (IV, when oral therapy is not appropriate)Licensed in the UK for parenteral management of acute hypertension.

Approved by the FDA for intravenous treatment of hypertension. Enalaprilat IV is indicated when oral therapy is not practical. The oral prodrug enalapril is more widely used for chronic hypertension and heart failure.

Evidence & Sources

No sources recorded yet.