Altman Roy, Barkin Robert L
David Geffen School of Medicine, Department of Rheumatology and Immunology, University of California, Los Angeles, CA 90024, USA.
Postgrad Med. 2009 Mar;121(2):139-47. doi: 10.3810/pgm.2009.03.1986.
Nonsteroidal anti-inflammatory drugs (NSAIDs) have shown efficacy in patients with osteoarthritis (OA) pain but are also associated with a dose-dependent risk of gastrointestinal, cardiovascular, hematologic, hepatic, and renal adverse events (AEs). Topical NSAIDs were developed to provide analgesia similar to their oral counterparts with less systemic exposure and fewer serious AEs. Topical NSAIDs have long been available in Europe for the management of OA, and guidelines of the European League Against Rheumatism and the Osteoarthritis Research Society International specify that topical NSAIDs are preferred over oral NSAIDs for patients with knee or hand OA of mild-to-moderate severity, few affected joints, and/or a history of sensitivity to oral NSAIDs. In contrast, the guidelines of the American Pain Society and American College of Rheumatology have in the past recommended topical methyl salicylate and topical capsaicin, but not topical NSAIDs. This reflects the fact that the American guidelines were written several years before the first topical NSAID was approved for use in the United States. Neither salicylates nor capsaicin have shown significant efficacy in the treatment of OA. In October 2007, diclofenac sodium 1% gel (Voltaren Gel) became the first topical NSAID for OA therapy approved in the United States following a long history of use internationally. Topical diclofenac sodium 1% gel delivers effective diclofenac concentrations in the affected joint with limited systemic exposure. Clinical trial data suggest that diclofenac sodium 1% gel provides clinically meaningful analgesia in OA patients with a low incidence of systemic AEs. This review discusses the pharmacology, clinical efficacy, and safety profiles of diclofenac sodium 1% gel, salicylates, and capsaicin for the management of hand and knee OA.
非甾体抗炎药（NSAIDs）已被证明对骨关节炎（OA）疼痛患者有效，但也与胃肠道、心血管、血液、肝脏和肾脏不良事件（AE）的剂量依赖性风险相关。局部用NSAIDs的研发目的是提供与口服NSAIDs相似的镇痛效果，同时减少全身暴露和严重AE的发生。局部用NSAIDs在欧洲长期用于OA的治疗，欧洲抗风湿病联盟和国际骨关节炎研究学会的指南规定，对于轻度至中度严重程度、受累关节较少和/或对口服NSAIDs敏感的膝或手OA患者，局部用NSAIDs优于口服NSAIDs。相比之下，美国疼痛学会和美国风湿病学会的指南过去推荐使用局部用的水杨酸甲酯和辣椒素，但不包括局部用NSAIDs。这反映了美国的指南是在第一种局部用NSAIDs在美国获批使用的几年前编写的这一事实。水杨酸酯和辣椒素在OA治疗中均未显示出显著疗效。2007年10月，1%双氯芬酸钠凝胶（扶他林凝胶）在国际上长期使用后，成为美国首个获批用于OA治疗的局部用NSAIDs。1%双氯芬酸钠凝胶可在受累关节中提供有效的双氯芬酸浓度，同时全身暴露有限。临床试验数据表明，1%双氯芬酸钠凝胶可为OA患者提供具有临床意义的镇痛效果，且全身AE的发生率较低。本综述讨论了1%双氯芬酸钠凝胶、水杨酸酯和辣椒素用于手部和膝部OA治疗的药理学、临床疗效和安全性。
