| The clinical pharmacokinetics of quinapril. | |
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MedLine Citation:
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PMID: 2705643 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Quinapril (Q) and quinaprilat (QT) pharmacokinetics are dose proportional following single oral 2.5- to 80-mg Q doses. Q absorption and hydrolysis to QT is rapid with peak Q and QT concentrations occurring one and two hours postdose, respectively. Peak plasma QT concentrations were approximately fourfold higher than those of Q (923 vs 207 ng/mL following 40-mg Q). Dose-proportional QT area under the curve and dose-independent percent of dose excreted in urine as QT demonstrate that the extent of Q conversion to QT is constant over the dose range studied. Q and QT were eliminated from plasma with apparent half-lives of 0.8 and 1.9 hours and apparent plasma clearances of 1,850 and 220 mL/min, respectively, over the 2.5- to 80-mg dose range. Following oral 14C-Q, 61% and 37% of radiolabel was recovered in urine and feces, respectively. Q plus QT accounted for 46% of radioactivity circulating in plasma and 56% of that excreted in urine. Metabolism to compounds other than QT is not extensive. Two diketopiperazine metabolites of Q have been identified in plasma and urine, with approximately 6% of an administered dose excreted in urine as each of these metabolites. Peak plasma concentrations of these metabolites are similar to that of Q, and each is eliminated rapidly with a half-life of approximately one hour. Urinary excretion profiles indicate the presence of other minor metabolites. In summary, the absorption of Q and conversion to QT is rapid and dose-proportional, subsequent clearance of both Q and QT is independent of dose, and metabolism to compounds other than QT is not extensive. |
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Authors:
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S C Olson; A M Horvath; B M Michniewicz; A J Sedman; W A Colburn; P G Welling |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Angiology Volume: 40 ISSN: 0003-3197 ISO Abbreviation: Angiology Publication Date: 1989 Apr |
Date Detail:
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Created Date: 1989-05-18 Completed Date: 1989-05-18 Revised Date: 2004-11-17 |
Medline Journal Info:
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Nlm Unique ID: 0203706 Medline TA: Angiology Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 351-9 Citation Subset: IM |
Affiliation:
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Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, Michigan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Absorption Adult Angiotensin-Converting Enzyme Inhibitors / blood, pharmacokinetics*, urine Half-Life Humans Isoquinolines / blood, pharmacokinetics*, urine Male Random Allocation Tetrahydroisoquinolines* |
| Chemical | |
Reg. No./Substance:
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0/Angiotensin-Converting Enzyme Inhibitors; 0/Isoquinolines; 0/Tetrahydroisoquinolines; 82586-55-8/quinapril; 82768-85-2/quinaprilat |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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