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Disposition of captopril in normal subjects
Author(s) -
Kripalani Kishin J,
McKinstry Doris N,
Singhvi Sampat M,
Willard David A,
Vukovich Robert A,
Migdalof Bruce H
Publication year - 1980
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.1980.90
Subject(s) - captopril , cmax , chemistry , urine , pharmacokinetics , metabolite , pharmacology , active metabolite , angiotensin converting enzyme , half life , oral administration , absorption (acoustics) , endocrinology , medicine , biochemistry , blood pressure , physics , acoustics
The disposition of Captopril, an angiotensin‐converting enzyme inhibitor with antihypertensive properties, was studied in 10 normal male subjects after a single 100‐mg tablet of 35 S‐labeled drug. Average absorption parameters for unchanged Captopril in blood were T max 0.93 ± 0.08 hr and C max 800 ± 76 ng/ml. For total radioactivity in blood the values were T max 1.05 ± 0.08 hr and C max 1,580 ± 90 ng/ml (as Captopril equivalents). Because of the curvilinearity of the semilogarithmic plots of blood concentrations of Captopril: time, elimination half‐life (t½) of unchanged drug could not be determined. At 1 hr unchanged Captopril accounted for about 52% of total radioactivity in blood, and the dimeric disulfide metabolite of Captopril accounted for about 10%. In the first 5 days after dosing, an average of about 68% of the radioactive dose was recovered in urine and 18% in feces. The distribution of radioactivity in the first 24‐hr urine sample (66% of the dose) was 58% Captopril (38% of dose), 2% Captopril disulfide (1.5% of dose), and 40% unidentified polar metabolites (26% of dose). Clinical Pharmacology and Therapeutics (1980) 27, 636–641; doi: 10.1038/clpt.1980.90