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Enalapril

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From Pharmacopedia
Enalapril (and enalaprilat IV)
Vasotec, Vasotec IV, Epaned

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Summary
Common uses
Hypertension0, Heart failure0, Asymptomatic LV systolic dysfunction0
Pharmacy
Starting dose
5-10 mg PO once daily (2.5 mg if on diuretic or in heart failure); titrate to 10-20 mg BID for HFrEF
Preparations
2.5, 5, 10, 20 mg tablets; 1 mg/mL oral solution (Epaned); 1.25 mg/mL IV (enalaprilat)
US FDA Max
40 mg/d
Pharmacology
Routes
Oral, IV
Onset
BP effect 1 hour; max at 4-6 hours
Duration
12-24 hours
Half-life
~11 hours (enalaprilat, the active metabolite)[1]
Bioavailability
~60% (oral; food does not affect absorption)[1]
Pregnancy
Contraindicated in pregnancy (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension. Stop on detection[1]
Legal status
Rx-only in US
Purported mechanism
Enalapril is an inactive prodrug hydrolyzed by hepatic carboxylesterases to enalaprilat, an ACE inhibitor that blocks conversion of angiotensin I to angiotensin II, reducing vasoconstriction, aldosterone secretion, and renal sodium retention.0 The IV form (enalaprilat) bypasses the prodrug activation step. Raises bradykinin, driving the characteristic dry cough and rare angioedema common across the ACE inhibitor class. The CONSENSUS (1987) and SOLVD (1991) trials made enalapril a cornerstone of evidence-based HFrEF therapy[1].

References

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  1. 1.0 1.1 1.2 1.3 FDA Prescribing Information, Vasotec (enalapril maleate), Valeant/Bausch, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018998s080lbl.pdf