PMID: 9549653Apr 29, 1998Paper

Stereoselective pharmacokinetics and inversion of (R)- ketoprofen in healthy volunteers

Journal of Clinical Pharmacology
A C RudyS D Hall

Abstract

The pharmacokinetics of ketoprofen enantiomers were evaluated after 25-, 50-, and 100-mg doses of (R)- ketoprofen and 100 mg of racemic ketoprofen in 25 healthy volunteers (12 male and 13 female). The fractional inversion (Finv) of (R)- ketoprofen was 8.9 +/- 3.3% using plasma data and 10.0 +/- 2.2% using urine data. There were small (< 5%) but significant differences between the enantiomers for areas under the plasma concentration-time curve (AUC) after the racemic dose (P < 0.005). Half-lives were 130-144 minutes for (R)- ketoprofen and 132-209 minutes for (S)- ketoprofen. Dose proportionality in AUC and maximum plasma concentration (Cmax) values was noted for both enantiomers. A total of 69% of the dose was recovered in the urine as (R)- and (S)- ketoprofen and conjugates. The elimination rate constant of (R)- ketoprofen was significantly different (P < 0.05) between men and women. Exposure to cyclooxygenase inhibiting (S)- ketoprofen was approximately 10% of the dose after the administration of pure (R)- ketoprofen and was independent of gender.

References

Dec 1, 1992·Therapeutic Drug Monitoring·A C RudyS D Hall
Sep 1, 1990·Clinical Pharmacokinetics·F Jamali, D R Brocks
Jun 1, 1989·Agents and Actions·G GeisslingerK Brune
Jan 1, 1985·Journal of Pharmaceutical Sciences·A RubinR L Wolen
Nov 1, 1980·Journal of Pharmaceutical Sciences·R A UptonS Riegelman
Mar 1, 1994·Chemico-biological Interactions·S D Hall, X Quan
Apr 1, 1993·Clinical Pharmacology and Therapeutics·S D HallD C Brater
Aug 1, 1995·Drugs·R Z HarrisJ B Schwartz

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Citations

Apr 26, 2011·European Journal of Drug Metabolism and Pharmacokinetics·Franciszek GłówkaWojciech Romanowski
Nov 7, 2001·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·J L DorneA G Renwick
Sep 1, 2011·Pain Management·Jean-Sébastien Walczak
Feb 14, 2006·Archives of Toxicology·Takashi NakazawaMasaharu Yamamoto
Mar 8, 2005·Drug Metabolism Reviews·Haiping HaoJianguo Sun
Nov 24, 2011·The Veterinary Journal·Eva NeirinckxChris Vervaet
Mar 15, 2011·Journal of Veterinary Pharmacology and Therapeutics·T K FosseB Ranheim
Oct 19, 2010·Journal of Veterinary Pharmacology and Therapeutics·T K FosseB Ranheim
Nov 23, 2015·European Journal of Drug Metabolism and Pharmacokinetics·Marianela LorierPietro Fagiolino
Nov 21, 2014·Journal of Veterinary Pharmacology and Therapeutics·E PlessersS Croubels
Dec 7, 2000·Journal of Veterinary Pharmacology and Therapeutics·E CastroO Tapia
Jun 18, 1999·Journal of Veterinary Pharmacology and Therapeutics·N A AlkatheeriM Lambert
Jan 29, 2000·Journal of Veterinary Pharmacology and Therapeutics·M F LandoniP Lees
Oct 25, 2016·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Misato UrakiMasahiro Iwaki
Jan 20, 2017·European Journal of Drug Metabolism and Pharmacokinetics·Pietro FagiolinoMarta Vázquez
Jan 9, 2004·Clinics in Chest Medicine·Vidya Krishnan, Patrick Murray
Jul 23, 2014·Knee Surgery, Sports Traumatology, Arthroscopy : Official Journal of the ESSKA·Sevtap Hekimoglu SahinNecdet Sut
Nov 21, 2016·Analytical and Bioanalytical Chemistry·Miguel Peñín-IbáñezLuis María Polo-Díez
Dec 1, 2004·Clinical Pharmacokinetics·Fried Faassen, Herman Vromans
May 4, 2011·Journal of Enzyme Inhibition and Medicinal Chemistry·Başak GökçeFeray Köçkar
Dec 1, 1998·Journal of Clinical Pharmacology·Francesc CabréDavid Mauleón
Dec 1, 1998·Journal of Clinical Pharmacology·Manel J BarbanojDavid Mauleón
Dec 1, 1998·Journal of Clinical Pharmacology·Francisco Javier López-MuñozDavid Mauleón
Dec 1, 1998·Journal of Clinical Pharmacology·Mark McGurkDavid Mauleón
Dec 1, 1998·Journal of Clinical Pharmacology

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