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Pharmacokinetics of Captopril in Elderly Healthy Male Volunteers
Author(s) -
Creasey William A.,
Funke Phillip T.,
McKinstry Doris N.,
Sugerman A. Arthur
Publication year - 1986
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1986.tb03521.x
Subject(s) - captopril , pharmacokinetics , urine , medicine , population , chemistry , excretion , endocrinology , blood pressure , environmental health
The pharmacokinetics of captopril were studied in 12 healthy male volunteers aged 65 to 76 years, who each received a single 100‐mg oral dose. Blood and urine samples were collected over a 24‐hour period, and assayed for unchanged captopril (CAP), S‐methyl captopril (Me‐CAP, plasma concentrations from 2 subjects only), and total captopril levels (TOT, a mixture of CAP and its dimer and mixed disulfides with endogenous thiolcontaining compounds such as glutathione and cysteine). Mean values for the maximum concentration (C max ) were 803 and 66.3 ng/mL for CAP and Me‐CAP, respectively. Mean time to maximum concentration (t max ) was determined as 1.0, 1.4, and 1.0 for CAP, TOT, and Me‐CAP, respectively. Mean areas under the plasma concentration‐time curve (AUC) were 1,394 hr‐ng/mL (CAP, 0–8 hr) and 17,316 hr‐ng/mL (TOT, 0–24 hr). The mean estimated half‐life (t 1/2 ) for CAP was 1.4 hr, and its renal clearance was 187 mL/hr/kg. Mean urinary excretion over 24 hr was 20.8 and 53.1 for CAP and TOT, respectively. C max , and AUC for CAP were 9% less and 13% greater, respectively, than in a historical control group of 18–35‐year‐old men, treated in the same clinic, by the same personnel, using the same analytic procedures, whereas the 24‐hour urinary excretion was 25% lower and eight‐hour renal clearance 36% lower in the older population. Since the values for C max , AUC, and t 1/2 were similar in the two populations, it does not appear that the pharmacokinetics of CAP are altered markedly with age alone .