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依托考昔

Etoricoxib.

作者信息

Matsumoto Alan K, Cavanaugh Paul F

机构信息

Arthritis and Rheumatism Associates, Wheaton, Maryland 20902, USA.

出版信息

Drugs Today (Barc). 2004 May;40(5):395-414.

Abstract

Etoricoxib (Arcoxia, Merck & Co., Inc.) is a selective inhibitor of cyclooxygenase-2 (COX-2), an enzyme involved in pain and inflammation. It is a member of the COX-2-selective (coxib) class of nonsteroidal antiinflammatory drugs (NSAIDs). Extensive clinical trials have confirmed its analgesic and antiinflammatory efficacy to be at least as good as and in some cases superior to nonselective NSAIDs in a number of disease and patient treatment settings. Etoricoxib displays improved gastrointestinal safety compared with nonselective NSAIDs and has a favorable overall safety and tolerability profile. It is rapidly and completely absorbed following oral administration providing a rapid onset of action. Its long plasma half-life allows for once-daily dosing. Etoricoxib is currently approved in a number of countries for various indications including the treatment of acute pain, acute gouty arthritis, chronic low back pain, primary dysmenorrhea, and chronic treatment for the signs and symptoms of osteoarthritis and rheumatoid arthritis. In countries where it is approved, the highest recommended daily dose for chronic use is 90 mg for rheumatoid arthritis and 60 mg for osteoarthritis and chronic low back pain. The recommended daily dose for acute pain relief treatment from primary dysmenorrhea and acute gouty arthritis is 120 mg. This review summarizes the published preclinical and clinical data relevant to the use of etoricoxib in clinical practice.

摘要

依托考昔(Arcoxia,默克公司)是一种环氧化酶-2(COX-2)的选择性抑制剂,COX-2是一种参与疼痛和炎症反应的酶。它属于COX-2选择性(昔布类)非甾体抗炎药(NSAIDs)。大量临床试验已证实,在多种疾病和患者治疗情况下,其镇痛和抗炎疗效至少与非选择性NSAIDs相当,在某些情况下甚至优于非选择性NSAIDs。与非选择性NSAIDs相比,依托考昔显示出更好的胃肠道安全性,并且具有良好的总体安全性和耐受性。口服给药后,它能迅速且完全吸收,起效迅速。其较长的血浆半衰期允许每日给药一次。依托考昔目前在多个国家被批准用于多种适应症,包括治疗急性疼痛、急性痛风性关节炎、慢性下腰痛、原发性痛经,以及骨关节炎和类风湿关节炎体征和症状的慢性治疗。在其获批的国家,类风湿关节炎慢性使用的最高推荐日剂量为90毫克,骨关节炎和慢性下腰痛为60毫克。原发性痛经和急性痛风性关节炎急性疼痛缓解治疗的推荐日剂量为120毫克。本综述总结了已发表的与依托考昔在临床实践中应用相关的临床前和临床数据。

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