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Pharmacokinetics of lisinopril (IV/PO) in healthy volunteers
Author(s) -
Beermann Bjorn,
Till Alice E.,
Gomez Hector J.,
Hichens Martin,
Bolognese James A.,
Junggren IngaLill
Publication year - 1989
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510100407
Subject(s) - lisinopril , pharmacokinetics , enalapril , metabolite , enalaprilat , ace inhibitor , angiotensin converting enzyme , ramipril , active metabolite , chemistry , enzyme inhibitor , half life , pharmacology , steady state (chemistry) , endocrinology , medicine , enzyme , biochemistry , blood pressure
When three intravenous doses of lisinopril were administered to healthy volunteers, area under the curve (to infinity) vs dose was linear with a positive intercept. Subtracting area under the extrapolated terminal phase of the serum profile from zero to infinity retained the linear relationship, but shifted the regression line to a zero intercept. It is postulated that the terminal phase reflects binding of drug to angiotensin‐converting enzyme (ACE). The half‐life for the terminal phase (approximately 40 h) was not predictive of steadystate parameters when ten daily doses (q24h) of lisinopril were administered orally to healthy volunteers. The mean effective half‐life for accumulation was 12·6h. The mean accumulation ratio was 1·38. Steady state was attained after the second daily dose. The observations in these studies with lisinopril are similar to those reported for enalaprilat, the active metabolite of the ACE inhibitor, enalapril maleate.