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効能
鎮痛薬, 抗炎症薬, シクロオキシゲナーゼ2阻害薬
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化学的特性
Off-White Powder
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使用
Labeled Etoricoxib, intended for use as an internal standard for the quantification of Etoricoxib by GC- or LC-mass spectrometry.
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定義
ChEBI: A member of the class of bipyridines that is 2,3'-bipyridine which is substituted at the 3, 5, and 6' positions by 4-(methylsulfonyl)phenyl, chlorine, and methyl groups, respectively.
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薬物動態学
Etoricoxib is rapidly
absorbed, with an oral bioavailability of 80 to 100%, and reaches maximum plasma concentrations in 1 to 2 hours
after dosing. Food decreases the rate of absorption but has no effect on the extent of absorption. It exhibits a long
elimination half-life of approximately 22 hours, demonstrating linear plasma pharmacokinetics with no accumulation
during multiple dosing.
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臨床応用
Etoricoxib is a selective COX-2 inhibitor being developed for postsurgical treatment of dental pain (120
mg) and osteoarthritis. It has a methylsulfonyl group common to the other coxib inhibitors.
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代謝
Etoricoxib is metabolized involving oxidation of its 6′-methyl group primarily by CYP3A4 but is
not an inhibitor of CYP3A4. Other metabolites include 1′-N-oxide and glucuronides. Etoricoxib is primarily excreted as
metabolites into the urine.
