Journal of Antimicrobial Chemotherapy, Vol 39, 129-138, Copyright © 1997 by The British Society for Antimicrobial Chemotherapy
M Bergeron and G Montay
The pharmacokinetics of quinupristin/dalfopristin have been studied in
rats, monkeys and humans following intravenous infusion of radiolabelled
and unlabelled drug. In rats and monkeys quinupristin and dalfopristin
undergo rapid elimination from the blood and wide tissue distribution.
Nevertheless, they do not penetrate the central nervous system or cross the
placenta to any significant degree and they do not appear to be subject to
significant body retention following cessation of administration. The blood
elimination half-life of quinupristin was approximately 0.6 h in rats and
0.5 h in monkeys, and that of dalfopristin was approximately 0.6 h and 0.2
h, respectively. Both compounds are primarily eliminated through the bile
into the faeces; quinupristin is mainly excreted unchanged whereas
dalfopristin is extensively metabolized beforehand. The metabolites include
the microbiologically active pristinamycin PIIA for dalfopristin and the
microbiologically active glutathione- and cysteine-conjugated derivatives
for quinupristin. Quinupristin and dalfopristin appear to be handled in a
similar manner by humans. Following intravenous administration both
compounds are rapidly cleared from the blood with elimination half-lives of
approximately 1 h for quinupristin and 0.4- 0.5 h for dalfopristin. The
pharmacokinetic profile of quinupristin is dose-independent and so is that
of dalfopristin and RP 12536 when considered together. Extravascular
diffusion of quinupristin/dalfopristin has been assessed in human
non-inflammatory interstitial fluid.
ORIGINAL ARTICLES
The pharmacokinetics of quinupristin/dalfopristin in laboratory animals and in humans
Department de Microbiologie, Universtite Laval, Quebec, Canada.
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