DMD Simcyp

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Rodrigues, A. D.
Right arrow Articles by Agrawal, N. G. B.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Rodrigues, A. D.
Right arrow Articles by Agrawal, N. G. B.

Vol. 31, Issue 2, 224-232, February 2003

Absorption, Metabolism, and Excretion of Etoricoxib, a Potent and Selective Cyclooxygenase-2 Inhibitor, in Healthy Male Volunteers

A. David Rodrigues, Rita A. Halpin, Leslie A. Geer, Donghui Cui, Eric J. Woolf, Catherine Z. Matthews, Keith M. Gottesdiener, Patrick J. Larson, Kenneth C. Lasseter, and Nancy G. B. Agrawal

Departments of Drug Metabolism (A.D.R., R.A.H., L.A.G., D.C., E.J.W., C.Z.M., N.G.B.A.), Clinical Pharmacology (K.M.G.), and BARDS (P.J.L.), Merck Research Laboratories, West Point, Pennsylvania and Rahway, New Jersey; and Clinical Pharmacology Associates, Miami, Florida (K.C.L.)

[14C]Etoricoxib (100 µCi/dose) was administered to six healthy male subjects (i.v., 25 mg; p.o., 100 mg). Following the i.v. dose, the plasma clearance was 57 ml/min, and the harmonic mean half-life was 24.8 h. Etoricoxib accounted for the majority of the radioactivity (~75%) present in plasma following both i.v. and p.o. doses. The oral dose, administered as a solution in polyethylene glycol-400, was well absorbed (absolute bioavailability of ~83%). Total recovery of radioactivity in the excreta was 90% (i.v.) and 80% (p.o.), with 70% (i.v.) and 60% (p.o.) excreted in urine and 20% in feces after either route of administration. Radiochromatographic analysis of the excreta revealed that etoricoxib was metabolized extensively, and only a minor fraction of the dose (<1%) was excreted unchanged. Radiochromatograms of urine and feces showed that the 6'-carboxylic acid derivative of etoricoxib was the major metabolite observed (>= 65% of the total radioactivity). 6'-Hydroxymethyl-etoricoxib and etoricoxib-1'-N-oxide, as well as the O-beta -D-glucuronide conjugate and the 1'-N-oxide derivative of 6'-hydroxymethyl-etoricoxib, were present in the excreta also (individually, <= 10% of the total radioactivity). In healthy male subjects, therefore, etoricoxib is well absorbed, is metabolized extensively via oxidation (6'-methyl oxidation >1'-N-oxidation), and the metabolites are excreted largely in the urine.

Copyright © 2003 by The American Society for Pharmacology and Experimental Therapeutics


This article has been cited by other articles:


Home page
 J Public Health (Oxf)Home page
E. Chilet-Rosell, M. T. Ruiz-Cantero, and J. F. Horga
Women's health and gender-based clinical trials on etoricoxib: methodological gender bias
J. Public Health Med., September 1, 2009; 31(3): 434 - 445.
[Abstract] [Full Text] [PDF]

Home page
 Drug Metab. Dispos.Home page
A. D. Rodrigues
IMPACT OF CYP2C9 GENOTYPE ON PHARMACOKINETICS: ARE ALL CYCLOOXYGENASE INHIBITORS THE SAME?
Drug Metab. Dispos., November 1, 2005; 33(11): 1567 - 1575.
[Abstract] [Full Text] [PDF]

Home page
 The Annals of PharmacotherapyHome page
S. D Martina, K. S Vesta, and T. L Ripley
Etoricoxib: A Highly Selective COX-2 Inhibitor
Ann. Pharmacother., May 1, 2005; 39(5): 854 - 862.
[Abstract] [Full Text] [PDF]

Home page
 J Clin PharmacolHome page
N. G. B. Agrawal, C. Z. Matthews, R. S. Mazenko, E. J. Woolf, A. G. Porras, X. Chen, J. L. Miller, N. Michiels, M. Wehling, A. Schultz, et al.
The Effects of Modifying In Vivo Cytochrome P450 3A (CYP3A) Activity on Etoricoxib Pharmacokinetics and of Etoricoxib Administration on CYP3A Activity
J. Clin. Pharmacol., October 1, 2004; 44(10): 1125 - 1131.
[Abstract] [Full Text] [PDF]

Home page
 Anesth. Analg.Home page
D. J. Chang, P. J. Desjardins, T. R. King, T. Erb, and G. P. Geba
The Analgesic Efficacy of Etoricoxib Compared with Oxycodone/Acetaminophen in an Acute Postoperative Pain Model: A Randomized, Double-Blind Clinical Trial
Anesth. Analg., September 1, 2004; 99(3): 807 - 815.
[Abstract] [Full Text] [PDF]

Home page
 J Clin PharmacolHome page
N. G. B. Agrawal, M. J. Rose, C. Z. Matthews, E. J. Woolf, A. G. Porras, L. A. Geer, P. J. Larson, J. Cote, S. C. Dilzer, K. C. Lasseter, et al.
Pharmacokinetics of Etoricoxib in Patients with Hepatic Impairment
J. Clin. Pharmacol., October 1, 2003; 43(10): 1136 - 1148.
[Abstract] [Full Text] [PDF]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 2003 by the American Society for Pharmacology and Experimental Therapeutics.