Enalapril
Enalapril. ACE inhibitor prodrug — hydrolyzed in liver to enalaprilat (the active form) by carboxylesterase. Same blockade of angiotensin I → II… Oral half-life 11 h.
ACE inhibitor prodrug — hydrolyzed in liver to enalaprilat (the active form) by carboxylesterase. Same blockade of angiotensin I → II conversion as lisinopril, but oral prodrug strategy gave better bioavailability than the early ACEi captopril.
PK describes ENALAPRILAT, the active diacid — enalapril is a prodrug and the cited paper measures only the metabolite. THE IV ROUTE WAS REMOVED: its cited study administered nothing intravenously, and more fundamentally the marketed intravenous product is enalaprilat, a different molecule, so an enalapril IV row asserting complete availability describes something that does not happen clinically. F corrected 0.6 -> 0.62, verbatim "There was no difference in F between young (0.62 +/- 0.16) and elderly subjects" (PMID:3011046, 9 healthy volunteers, oral enalapril against intravenous enalaprilat) — a true absolute figure. The half-life is re-cited to PMID:6091806, "An average effective half-life for accumulation of approximately 11h", and should be read as an accumulation half-life from urine data rather than a terminal disposition value. ka 1.2 /h and V 70 L dropped as unstated. ANALYTE: the active diacid ENALAPRILAT, confirmed rather than inferred. Its cited crossover measured only enalaprilat on both arms — "After both drugs, a biexponential curve was fitted to the decline in plasma enalaprilat concentration" — so the stored bioavailability of 0.62 is oral enalapril against INTRAVENOUS ENALAPRILAT, and the 11 h is enalaprilat accumulation. The pk block is therefore internally consistent; only the mass is not, since mw 376.45 is the ethyl ester. Caveat retained: 11 h is an ACCUMULATION half-life derived from urine, not a terminal disposition value. MASS: the stored molecular weight described the PARENT while pk_analyte declares the metabolite, so the one field that must name a single species named the wrong one. LATENT RATHER THAN LIVE — this record carries no occupancy rows and is no other record interaction perpetrator — but it is one authored edge away from being live, because both consumers of the field (the micromolar-to-mass conversion for a kinetics edge, and the affinity the app renders from a stored occupancy concentration) want the species that actually circulates, which is the species pk[] already describes.
Pharmacokinetics
- Oral — t½ 11 h · F 62%
Sources: PMID:11523062, PMID:6091806, PMID:3011046