Adis, a Wolters Kluwer Business, Auckland, New Zealand.
Drugs. 2011 Dec 24;71(18):2457-89. doi: 10.2165/11208240-000000000-00000.
Celecoxib (Celebrex®) was the first cyclo-oxygenase (COX)-2 selective inhibitor (coxib) to be introduced into clinical practice. Coxibs were developed to provide anti-inflammatory/analgesic activity similar to that of nonselective NSAIDs, but without their upper gastrointestinal (GI) toxicity, which is thought to result largely from COX-1 inhibition. Celecoxib is indicated in the EU for the symptomatic treatment of osteoarthritis, rheumatoid arthritis and ankylosing spondylitis in adults. This article reviews the clinical efficacy and tolerability of celecoxib in these EU-approved indications, as well as overviewing its pharmacological properties. In randomized controlled trials, celecoxib, at the recommended dosages of 200 or 400 mg/day, was significantly more effective than placebo, at least as effective as or more effective than paracetamol (acetaminophen) and as effective as nonselective NSAIDs and the coxibs etoricoxib and lumiracoxib for the symptomatic treatment of patients with active osteoarthritis, rheumatoid arthritis or ankylosing spondylitis. Celecoxib was generally well tolerated, with mild to moderate upper GI complaints being the most common body system adverse events. In meta-analyses and large safety studies, the incidence of upper GI ulcer complications with recommended dosages of celecoxib was significantly lower than that with nonselective NSAIDs and similar to that with paracetamol and other coxibs. However, concomitant administration of celecoxib with low-dose cardioprotective aspirin often appeared to negate the GI-sparing advantages of celecoxib over NSAIDs. Although one polyp prevention trial noted a dose-related increase in cardiovascular risk with celecoxib 400 and 800 mg/day, other trials have not found any significant difference in cardiovascular risk between celecoxib and placebo or nonselective NSAIDs. Meta-analyses and database-derived analyses are inconsistent regarding cardiovascular risk. At recommended dosages, the risks of increased thrombotic cardiovascular events, or renovascular, hepatic or hypersensitivity reactions with celecoxib would appear to be small and similar to those with NSAIDs. Celecoxib would appear to be a useful option for therapy in patients at high risk for NSAID-induced GI toxicity, or in those responding suboptimally to or intolerant of NSAIDs. To minimize any risk, particularly the cardiovascular risk, celecoxib, like all coxibs and NSAIDs, should be used at the lowest effective dosage for the shortest possible duration after a careful evaluation of the GI, cardiovascular and renal risks of the individual patient.
塞来昔布(西乐葆)是首个被应用于临床的环氧化酶-2(COX-2)选择性抑制剂(昔布类药物)。昔布类药物的研发目的是提供与非选择性 NSAIDs 相似的抗炎/镇痛活性,但没有其胃肠道(GI)毒性,这种毒性主要归因于 COX-1 抑制。塞来昔布在欧盟被批准用于治疗成人骨关节炎、类风湿关节炎和强直性脊柱炎的症状。本文综述了塞来昔布在这些已获欧盟批准的适应证中的临床疗效和耐受性,并概述了其药理学特性。在随机对照试验中,塞来昔布在推荐剂量 200 或 400mg/天时,与安慰剂相比,疗效显著更优,至少与扑热息痛(对乙酰氨基酚)相当,与非选择性 NSAIDs 以及昔布类药物依托考昔和罗非昔布相当,用于治疗活动性骨关节炎、类风湿关节炎或强直性脊柱炎患者的症状。塞来昔布通常具有良好的耐受性,最常见的不良事件为轻中度的胃肠道不良反应。在荟萃分析和大型安全性研究中,塞来昔布推荐剂量下上胃肠道溃疡并发症的发生率显著低于非选择性 NSAIDs,与扑热息痛和其他昔布类药物相当。然而,塞来昔布与低剂量心脏保护用阿司匹林合用,往往会使塞来昔布相较于 NSAIDs 的胃肠道保护优势不复存在。虽然一项息肉预防试验注意到塞来昔布 400mg 和 800mg/天剂量与心血管风险呈剂量相关性增加,但其他试验未发现塞来昔布与安慰剂或非选择性 NSAIDs 之间存在任何心血管风险差异。荟萃分析和数据库衍生分析在心血管风险方面并不一致。在推荐剂量下,塞来昔布增加血栓性心血管事件或肾血管、肝脏或超敏反应的风险似乎较小,与 NSAIDs 相当。塞来昔布似乎是一种治疗 NSAIDs 诱导的胃肠道毒性高危患者的有用选择,或者是那些对 NSAIDs 反应不佳或不耐受的患者。为了降低任何风险,特别是心血管风险,塞来昔布与所有昔布类药物和 NSAIDs 一样,应在对个体患者的胃肠道、心血管和肾脏风险进行仔细评估后,以最低有效剂量最短时间使用。