etoricoxib临床药代动力学和药效学的状况。

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Takemoto JK,雷诺兹JK Remsberg厘米,Vega-Villa KR,戴维斯海里

etoricoxib临床药代动力学和药效学的状况。

47 Pharmacokinet。2008; (11): 703 - 20。

PubMed ID

18840026 (在PubMed

]

文摘

非甾体抗炎药etoricoxib是选择性cyclo-oxygenase 2 (cox - 2)抑制剂,批准用于治疗慢性关节病患者和肌肉骨骼和牙齿疼痛。吸收的速率etoricoxib适中时口服(最大血浆药物浓度发生后约1小时),和吸收的程度与口服给药和静脉注射的剂量是相似的。Etoricoxib广泛蛋白质绑定,主要是血浆白蛋白,和有一个表观分布容积120升的人类。血浆浓度时间曲线下的面积(AUC) etoricoxib增加成比例增加口服剂量之间的5和120毫克。消除半衰期约20小时在健康受试者可以每天换一次剂量。Etoricoxib消除生物转化后羧酸和葡糖苷酸代谢物排出的尿液和粪便,几乎被消除的药物(< 1%)不变的尿液。Etoricoxib是代谢主要由细胞色素P450 (CYP) 3 a4同工酶。等离子体浓度(AUC) etoricoxib出现不不同的慢性肾功能不全患者与人正常的肾功能。与健康受试者相比,据报道,AUC是中度肝损害患者增加了大约40%。没有对CYP2C9抑制性影响,2 c19, 2 d6 2 e1或3 a4 etoricoxib预计将出现。 Coadministration of etoricoxib with other drugs has been examined only to a limited extent, thus further assessment is necessary. Etoricoxib has been assessed for the management of several specific disease states, including pain, osteoarthritis, and rheumatoid arthritis, and has shown similar efficacy in comparison with traditional NSAIDs (including naproxen, diclofenac and ibuprofen) in these conditions. Etoricoxib has demonstrated a significant reduction in gastrointestinal toxicity compared with many traditional NSAIDs. The renal adverse effects of etoricoxib appear to be similar to those of other NSAIDs, and the cardiovascular adverse effects of this selective COX-2 inhibitor require further clinical scrutiny. Further study is necessary to delineate the relevance of the pharmacokinetic disposition in terms of the clinical benefits and risks of etoricoxib compared with other options in the clinical arsenal.

DrugBank数据引用了这篇文章

药物酶

药物	酶	类	生物	药理作用	行动
Etoricoxib	细胞色素P450 3 a4	蛋白质	人类	未知的	底物 抑制剂	细节