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The Clinical Pharmacokinetics of Quinapril

Ann Marie Horvath

Barbara M. Michniewicz

Allen J. Sedman, M.D., Ph.D.

Wayne A. Colburn, Ph.D.

Peter G. Welling, Ph.D., D.Sc.

Stephen C. Olson, Ph. D.

Parke-Davis Pharmaceutical Research Division Warner-Lambert Company 2800 Plymouth Road Ann Arbor, MI 48105

Quinapril (Q) and quinaprilat (QT) pharmacokinetics are dose pro portional following single oral 2.5- to 80-mg Q doses. Q absorption and hy drolysis 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 follow ing 40-mg Q). Dose-proportional QT area under the curve and dose-inde pendent percent of dose excreted in urine as QT demonstrate that the ex tent of Q conversion to QT is con stant 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 clear ances of 1,850 and 220 mL/min, re spectively, 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 radioactiv ity circulating in plasma and 56% of that excreted in urine. Metabolism to compounds other than QT is not extensive. Two diketo piperazine metabolites of Q have been identified in plasma and urine, with approximately 6% of an admin istered 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 ex cretion profiles indicate the presence of other minor metabolites. In summary, the absorption of Q and conversion to QT is rapid and dose-proportional, subsequent clear ance of both Q and QT is independ ent of dose, and metabolism to compounds other than QT is not ex tensive.

Angiology, Vol. 40, No. 4 part_2, 351-359 (1989)
DOI: 10.1177/000331978904000404


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				H. R. Kaplan, D. G. Taylor, S. C. Olson, L. K. Andrews, and H. R. Kaplan Quinapril--A Preclinical Review of the Pharmacology, Pharmacokinetics, and Toxicology Angiology, January 1, 1989; 40(4_part_2): 335 - 350. [Abstract] [PDF]