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Captopril kinetics
Author(s) -
Duchin Kenneth L,
Singhvi Sampat M,
Willard David A,
Migdalof Bruce H,
McKinstry Doris N
Publication year - 1982
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1982.59
Subject(s) - captopril , volume of distribution , bioavailability , pharmacology , urine , pharmacokinetics , dosing , chemistry , oral administration , distribution (mathematics) , angiotensin converting enzyme , half life , absorption (acoustics) , medicine , blood pressure , mathematical analysis , physics , mathematics , acoustics
Captopril, an angiotensin‐converting enzyme inhibitor with antihypertensive properties, was given by mouth and intravenously in 10‐mg doses to five healthy subjects. After intravenous dosing, semilogarithmic plots of captopril blood levels:time showed a triexponential decay. Data were analyzed using an open three‐compartment model. The average volume of distribution (Vd) was 0.2 l/kg for the central compartment and 2 l/kg for the elimination (β) phase. The Vd at steady‐state was 0.7 l/kg. The total body clearance of captopril averaged 0.8 l/kg/hr and the mean blood half‐life during the β phase was 1.9 hr. In the 0‐ to 96‐hr urine, after intravenous and oral drug, excretion of radioactivity accounted for 87% and 61% of dose. In the 0‐ to 24‐hr urine, averages of 38% (intravenous) and 24% (oral) of the doses were excreted as unchanged captopril. Absolute absorption of the radioactive oral dose was 71 % and the absolute oral bioavailability of captopril was 62%. Clinical Pharmacology and Therapeutics (1982) 31, 452–458; doi: 10.1038/clpt.1982.59