Department of Medicine, McMaster University Faculty of Health Sciences, Hamilton, ON, Canada.
J Pharm Pharmacol. 2012 May;64(5):626-36. doi: 10.1111/j.2042-7158.2012.01456.x. Epub 2012 Feb 7.
We review the pharmacological properties and clinical evidence pertaining to the efficacy of ibuprofen as a first-line treatment in hip and knee osteoarthritis (OA). In the context of our previous paper's exploration of the aetiology and pathogenesis of OA as a basis for pharmacotherapy, we discuss the pharmacokinetics (PK) and clinical pharmacodynamics (PD) of ibuprofen relevant to OA.
Although widely used, the benefits and risks of ibuprofen, especially compared with other non-steroidal anti-inflammatory drugs (NSAIDs) and placebo, have only recently been evaluated in OA of the hip and knee in randomized-controlled clinical trials (RCT). The efficacy and occurrence of adverse reactions from ibuprofen was compared with placebo in a structural review of the literature and systematic review of RCTs in large-scale clinical trials. Ibuprofen has been found to result in approximately 50-60% improvement over placebo in WOMAC scores, including those reflecting inflammatory joint pain in knee and hip OA or other indices of pain, disability and impaired function. Mega-trials performed in comparison with the newer NSAIDs, the coxibs, have shown that ibuprofen has comparable therapeutic benefits and although serious gastrointestinal conditions are sometimes more frequent after short-term treatment, longer-term (several months) therapy in OA reduces the advantages of the coxibs over other NSAIDs including ibuprofen. Cardiovascular risk, though present with coxibs and some NSAIDs in OA, is lower or slightly so with ibuprofen compared with coxibs.
Ibuprofen is effective and relatively safe (especially at low over-the-counter doses and in the short term) for mild-to-moderate OA of the knee and hip. The PK properties of ibuprofen in OA (short plasma t½) confer advantages of this drug for OA, while evidence for clinically relevant PD benefits in joints of patients with OA, though limited, is suggestive of local anti-inflammatory activity.
我们回顾了布洛芬作为髋和膝关节骨关节炎（OA）一线治疗药物的疗效的药理学特性和临床证据。在前一篇论文探讨 OA 的病因和发病机制作为药物治疗基础的背景下，我们讨论了与 OA 相关的布洛芬的药代动力学（PK）和临床药效学（PD）。
尽管布洛芬被广泛应用，但它的益处和风险，尤其是与其他非甾体抗炎药（NSAIDs）和安慰剂相比，最近才在髋和膝关节 OA 的随机对照临床试验（RCT）中得到评估。在文献的结构综述和大规模临床试验的 RCT 系统评价中，比较了布洛芬与安慰剂的疗效和不良反应的发生情况。研究发现，与安慰剂相比，布洛芬可使 WOMAC 评分（包括反映膝和髋 OA 关节炎症疼痛或其他疼痛、残疾和功能障碍指标的评分）提高约 50-60%。与新型 NSAIDs，即昔布类药物进行的大型试验表明，布洛芬具有相当的治疗益处，尽管短期治疗后胃肠道不良事件有时更为常见，但 OA 的长期（数月）治疗降低了昔布类药物相对于其他 NSAIDs（包括布洛芬）的优势。心血管风险在 OA 中与昔布类药物和某些 NSAIDs 有关，但与昔布类药物相比，布洛芬的风险较低或略低。
布洛芬对轻中度膝和髋 OA 是有效且相对安全的（尤其是在低剂量非处方和短期使用时）。OA 中布洛芬的 PK 特性（较短的血浆半衰期）为该药物治疗 OA 带来了优势，尽管有关患者关节临床相关 PD 益处的证据有限，但提示其具有局部抗炎活性。
