Update on the clinical pharmacology of etoricoxib, a potent cyclooxygenase-2 inhibitor
نویسنده
چکیده
منابع مشابه
Formulation Design and In Vitro Characterization of Etoricoxib Cream for the Treatment of Rheumatoid Arthritis
Non-Steroidal Anti-inflammatory drugs (NSAIDs), including selective cyclooxygenase (COX)-2 inhibitors, have come to play an important role in the pharmacologic management of musculoskeletal disorders. Clinical trials have established the efficacy of etoricoxib in Osteoarthritis, Rheumatoid Arthritis, Acute Gouty Arthritis, Ankylosing Spondylitis, Low back pain, acute postoperative pain, and pri...
متن کاملTolerability to etoricoxib in patients with aspirin-exacerbated respiratory disease.
BACKGROUND The use of selective cyclooxygenase (COX) 2 inhibitors as an alternative to aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) has been suggested for patients with aspirin-exacerbated respiratory disease (AERD). OBJECTIVE To evaluate tolerability to etoricoxib, a second-generation COX-2 inhibitor with high in vitro selectivity for COX-2 in patients with AERD. METHODS...
متن کاملAbsorption, 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...
متن کاملRole 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-...
متن کاملEtoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2.
We report here the preclinical profile of etoricoxib (MK-0663) [5-chloro-2-(6-methylpyridin-3-yl)-3-(4-methylsulfonylphenyl) pyridine], a novel orally active agent that selectively inhibits cyclooxygenase-2 (COX-2), that has been developed for high selectivity in vitro using whole blood assays and sensitive COX-1 enzyme assays at low substrate concentration. Etoricoxib selectively inhibited COX...
متن کامل