ETORICOXIB IS A NEW SELECTIVE CYCLOOXYGENASE-2 INHIBITOR

Absorption, metabolism, and excretion of etoricoxib, a potent and selective cyclooxygenase-2 inhibitor, in healthy male volunteers.

[(14)C]Etoricoxib (100 microCi/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 (approximately 75%) present in plasma following both i.v. and p.o. doses. The oral dose, administered as a solution in po...

Role of human liver cytochrome P4503A in the metabolism of etoricoxib, a novel cyclooxygenase-2 selective inhibitor.

Etoricoxib, a potent and selective cyclooxygenase-2 inhibitor, was shown to be metabolized via 6'-methylhydroxylation (M2 formation) when incubated with NADPH-fortified human liver microsomes. In agreement with in vivo data, 1'-N'-oxidation was a relatively minor pathway. Over the etoricoxib concentration range studied (1-1300 microM), the rate of hydroxylation conformed to saturable Michaelis-...

Selective Cyclooxygenase-2 Inhibitor Compound 11b Improves Haloperidol-Induced Catatonia by Enhancing the Striatum Dopaminergic Neurotransmission

The aim of this research was to investigate the Cyclooxygenase-2 (COX-2) selective inhibition effect on haloperidol-induced catatonia. In this study, the effect of orally, acutely and Sub-chronically administrations of compound 11b [1-(phenyl)-5-(4-methylsulfonylphenyl)-2-ethylthioimidazole] (2, 4 and 8 mg/kg), a newly selective COX-2 inhibitor, was investigated against the haloperidol-induced ...

Selective Cyclooxygenase-2 Inhibitor Compound 11b Improves Haloperidol-Induced Catatonia by Enhancing the Striatum Dopaminergic Neurotransmission

The aim of this research was to investigate the Cyclooxygenase-2 (COX-2) selective inhibition effect on haloperidol-induced catatonia. In this study, the effect of orally, acutely and Sub-chronically administrations of compound 11b [1-(phenyl)-5-(4-methylsulfonylphenyl)-2-ethylthioimidazole] (2, 4 and 8 mg/kg), a newly selective COX-2 inhibitor, was investigated against the haloperidol-induced ...

Update on the clinical pharmacology of etoricoxib, a potent cyclooxygenase-2 inhibitor