PMID: 8971676Dec 1, 1996Paper

Pharmacokinetics and pharmacodynamics of ketoprofen enantiomers in the horse

Journal of Veterinary Pharmacology and Therapeutics
M F Landoni, P Lees

Abstract

Pharmacokinetic and pharmacodynamic parameters were established for enantiomers of the non-steroidal anti-inflammatory drug (NSAID) ketoprofen (KTP), each administered separately at a dose level of 1.1 mg/kg to a group of six New Forest geldings, in a three-period cross-over study using a tissue cage model of inflammation. For both S(+)-and R(-)-KTP, penetration into tissue cage fluid (transudate) and inflamed tissue cage fluid (exudate) was rapid, and clearances from exudate and transudate were much slower than from plasma. AUC values were, therefore, higher for exudate and, to a lesser degree, transudate than for plasma. Unidirectional chiral inversion of R(-)-to S(+)-KTP was demonstrated. Administration of both enantiomers produced marked, time-dependent inhibition of synthesis of serum thromboxane B2 and exudate prostaglandin E2, indicating non-selective inhibition of cyclo-oxygenase (COX) isoenzymes COX-1 and COX-2 respectively. Administration of both enantiomers also produced partial inhibition of beta-glucuronidase release into inflammatory exudate and of bradykinin-induced skin oedema. It is suggested that, although S(+)-KTP is generally regarded as the eutomer, R(-)-KTP was probably at least as active in inhibiting bra...Continue Reading

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Citations

Mar 6, 2003·The Veterinary Journal·P LeesC Waters
Jan 29, 2000·Journal of Veterinary Pharmacology and Therapeutics·M F LandoniP Lees
Dec 7, 2000·Journal of Veterinary Pharmacology and Therapeutics·E CastroO Tapia
Jul 10, 2001·Journal of Veterinary Pharmacology and Therapeutics·C R VerdeM F Landoni
Nov 7, 2001·Journal of Veterinary Pharmacology and Therapeutics·J Y KimB C Chung
Dec 18, 2002·Journal of Veterinary Pharmacology and Therapeutics·P Lees, M F Landoni
Nov 10, 2000·The Journal of Small Animal Practice·L S Slingsby, A E Waterman-Pearson
Dec 30, 2008·Journal of Zoo and Wildlife Medicine : Official Publication of the American Association of Zoo Veterinarians·Robert P Hunter, Ramiro Isaza
Jan 3, 2008·American Journal of Veterinary Research·Marja R RaekallioOuti M Vainio
Feb 1, 1996·Journal of Veterinary Pharmacology and Therapeutics·M F Landoni, P Lees
Nov 24, 2011·The Veterinary Journal·Eva NeirinckxChris Vervaet
Dec 17, 2004·Journal of Veterinary Pharmacology and Therapeutics·P LeesP L Toutain
Aug 13, 2004·Journal of Veterinary Pharmacology and Therapeutics·E-I Lepist, W J Jusko
Feb 22, 2005·Journal of Veterinary Pharmacology and Therapeutics·A L SoraciJ Garcia
Apr 2, 2003·Journal of Veterinary Pharmacology and Therapeutics·A K ArifahP Lees
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
Mar 22, 2014·Drug Development Research·José Carlos Aguilar-CarrascoFrancisco Javier Flores-Murrieta
Nov 21, 2014·Journal of Veterinary Pharmacology and Therapeutics·E PlessersS Croubels
Jun 18, 1999·Journal of Veterinary Pharmacology and Therapeutics·P LeesP V Rens
Sep 26, 2000·Journal of Dairy Science·P M Faulkner, D M Weary
Feb 24, 2001·American Journal of Veterinary Research·A K ArifahP Lees
May 2, 2019·The Veterinary Record·Alexandra SchoosDominiek Gd Maes
Jul 16, 2002·Equine Veterinary Journal·P Lees, F Shojaee Aliabadi
Jan 14, 2021·Drug Testing and Analysis·Fernando MoreiraMaria de Lourdes Bastos
May 30, 2020·Journal of Medicinal Chemistry·Mateusz P CzubWladek Minor

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