Rannou François, Pelletier Jean-Pierre, Martel-Pelletier Johanne
Rehabilitation Unit, Rheumatology Department, Hôpital Cochin, AP-HP, INSERM UMR-S 1124, Université Paris Descartes, 27 rue de faubourg saint Jacques, 75014 Paris, France.
Osteoarthritis Research Unit, University of Montreal Hospital Research Centre (CRCHUM), Montreal, Quebec, Canada.
Semin Arthritis Rheum. 2016 Feb;45(4 Suppl):S18-21. doi: 10.1016/j.semarthrit.2015.11.007. Epub 2015 Dec 2.
Topical non-steroidal anti-inflammatory drugs (NSAIDs) are recommended in international and national guidelines as an early treatment option for the symptomatic management of knee and hand osteoarthritis (OA), and may be used ahead of oral NSAIDs due to their superior safety profile. The European Society for Clinical and Economic Aspects of Osteoporosis and Osteoarthritis (ESCEO) treatment algorithm recommends topical NSAIDs for knee OA in addition to the pharmacological background of symptomatic slow-acting drugs for osteoarthritis (SYSADOAs) and rescue analgesia with paracetamol and non-pharmacological treatment, if the patient is still symptomatic. Topical NSAIDs have a moderate effect on pain relief, with efficacy similar to that of oral NSAIDs, with the advantage of a better risk:benefit ratio. In real-life studies, topical and oral NSAIDs demonstrate an equivalent effect on knee pain over 1 year of treatment, with fewer adverse events due to lower systemic absorption of topical NSAIDs compared with oral NSAIDs. As a result, topical NSAIDs may be the preferred treatment option, especially in OA patients aged ≥75 years, and those with co-morbidities or at an increased risk of cardiovascular, gastrointestinal, or renal side effects. Furthermore, using topical NSAIDs in inflammatory rheumatic diseases leads to a 40% reduction in the need for concomitant oral NSAIDs. When selecting a topical NSAID, absorption and bioavailability are important because of heterogeneity among topical drug formulations. Molecules like etofenamate have a bioavailability of >20% and evidence for accumulation in synovial tissues, with efficacy demonstrated as improvement in pain and function in real-life studies of OA patients. Diclofenac also shows good efficacy alongside evidence that diclofenac accumulates in the synovium.
局部用非甾体抗炎药(NSAIDs)在国际和国内指南中被推荐作为膝关节和手部骨关节炎(OA)症状管理的早期治疗选择,由于其安全性更高,可在口服NSAIDs之前使用。欧洲骨质疏松症和骨关节炎临床与经济学会(ESCEO)的治疗算法建议,对于膝关节OA,除了使用骨关节炎症状性慢作用药物(SYSADOAs)的药理背景以及使用对乙酰氨基酚进行急救镇痛和非药物治疗外,如果患者仍有症状,可使用局部用NSAIDs。局部用NSAIDs对缓解疼痛有中等效果,疗效与口服NSAIDs相似,且优势在于风险效益比更好。在现实生活研究中,局部用和口服NSAIDs在1年的治疗期内对膝关节疼痛显示出等效效果,与口服NSAIDs相比,局部用NSAIDs全身吸收较低,不良事件较少。因此,局部用NSAIDs可能是首选治疗选择,尤其是在年龄≥75岁的OA患者以及患有合并症或心血管、胃肠道或肾脏副作用风险增加的患者中。此外,在炎性风湿性疾病中使用局部用NSAIDs可使口服NSAIDs的联合使用需求减少40%。选择局部用NSAIDs时,由于局部药物制剂之间存在异质性,吸收和生物利用度很重要。依托芬那酯等分子的生物利用度>20%,且有证据表明其在滑膜组织中蓄积,在OA患者的现实生活研究中显示出对疼痛和功能有改善作用。双氯芬酸也显示出良好的疗效,同时有证据表明双氯芬酸在滑膜中蓄积。