Document Detail


Pharmacokinetics and metabolism of orally administered firocoxib, a novel second generation coxib, in horses.
MedLine Citation:
PMID:  17472652     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The primary objective of this study was to determine the pharmacokinetic profile of firocoxib, a novel second generation coxib, in horses. Horses were administered either a single oral or intravenous dose of firocoxib at 0.1 mg/kg in a two-period crossover study with 12 animals. The dosage was based on previously determined pharmacodynamic parameters. Oral firocoxib was well absorbed with an average bioavailability (absolute) of 79% and a Cmax of 75 ng/mL at 3.9 h. The average elimination half-life was 30 h. Following intravenous administration the average Cmax was 210 ng/mL and the elimination half-life was 34 h. The area under the curve [AUC(0-tlast)] was 1.8 microg.h/mL for the oral dose and 2.3 microg.h/mL for the intravenous dose. Firocoxib was widely distributed with a volume of distribution value of 1.7 L/kg for the intravenous dose. Biotransformation of firocoxib was via dealkylation and glucuronidation to inactive metabolites, namely descyclopropylmethylfirocoxib and its glucuronide conjugate. Urinary excretion was the major route of elimination, and the clearance rate was 37 mL/h/kg.
Authors:
V Kvaternick; M Pollmeier; J Fischer; P D Hanson
Publication Detail:
Type:  Journal Article; Randomized Controlled Trial    
Journal Detail:
Title:  Journal of veterinary pharmacology and therapeutics     Volume:  30     ISSN:  0140-7783     ISO Abbreviation:  J. Vet. Pharmacol. Ther.     Publication Date:  2007 Jun 
Date Detail:
Created Date:  2007-05-02     Completed Date:  2007-06-19     Revised Date:  2012-10-26    
Medline Journal Info:
Nlm Unique ID:  7910920     Medline TA:  J Vet Pharmacol Ther     Country:  England    
Other Details:
Languages:  eng     Pagination:  208-17     Citation Subset:  IM    
Affiliation:
Pharmacokinetics and Drug Metabolism, Merial Limited, North Brunswick, NJ 08902, USA. valerie.kvaternick@merial.com
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MeSH Terms
Descriptor/Qualifier:
4-Butyrolactone / administration & dosage,  analogs & derivatives*,  blood,  pharmacokinetics
Administration, Oral
Animals
Area Under Curve
Cross-Over Studies
Cyclooxygenase 2 Inhibitors / administration & dosage,  blood,  pharmacokinetics*
Female
Horses / metabolism*
Injections, Intravenous
Male
Sulfones / administration & dosage,  blood,  pharmacokinetics*
Chemical
Reg. No./Substance:
0/Cyclooxygenase 2 Inhibitors; 0/Sulfones; 189954-96-9/firocoxib; 96-48-0/4-Butyrolactone

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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