布洛芬:药理学、疗效和安全性。

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Rainsford KD

布洛芬:药理学、疗效和安全性。

炎症药理学。2009 Dec;17(6):275-342。doi: 10.1007 / s10787 - 009 - 0016 - x。Epub 2009 11月21日。

PubMed ID

19949916 (PubMed视图

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摘要

目的:本综述试图收集大量关于布洛芬的临床用途、安全性和药理特性的最新研究资料。布洛芬在许多国家被广泛用于缓解疼痛、炎症和发烧症状。布洛芬作用方式的证据与它在控制炎症、疼痛和发热方面的作用以及药物的不良反应有关。结果总结:在许多国家被批准非处方(非处方)销售的低剂量(800- 1200毫克/天(-1))布洛芬具有与扑热息痛相当的良好安全性。其镇痛活性与其抗炎作用有关，并与血液中环加氧酶(COX)-1和COX-2衍生前列腺素的体外生产减少有关。较高的处方剂量(约1,800-2,400毫克每天(-1))被长期用于治疗风湿病和其他更严重的肌肉骨骼疾病。最近来自新型coxibs的大规模临床试验的证据，其中布洛芬作为比较剂，证实了早期的研究，这些研究表明布洛芬与coxibs和其他非甾体抗炎药具有相当的治疗效果。对于长期使用(6个月以上)，由于治疗效果降低，退出的人数更多，这是非甾体抗炎药常见的特征。长期coxib比较研究和流行病学研究的临床试验中不良事件和药物不良反应(adr)的自发报告表明，与其他非甾体抗炎药和coxib相比，布洛芬的胃肠道(GI)、肝肾和其他不良反应的风险相对较低，更罕见。在一些研究中，但不是所有的研究都报道了心血管(CV)事件的风险略高，但风险总体上低于一些coxibs和双氯芬酸。 The possibility that ibuprofen may interfere with the anti-platelet effects of aspirin, though arguably of low grade or significance, has given rise to caution on its use in patients that are at risk for CV conditions that take aspirin for preventing these conditions. Paediatric use of ibuprofen is reviewed and the main results are that the drug is relatively safe and effective as a treatment of acute pain and fever. It is probably more effective than paracetamol as an antipyretic. CONCLUSIONS: This assessment of the safety and benefits of ibuprofen can be summarized thus: (1) Ibuprofen at OTC doses has low possibilities of serious GI events, and little prospect of developing renal and associated CV events. Ibuprofen OTC does not represent a risk for developing liver injury especially the irreversible liver damage observed with paracetamol and the occasional liver reactions from aspirin. (2) The pharmacokinetic properties of ibuprofen, especially the short plasma half-life of elimination, lack of development of pathologically related metabolites (e.g. covalent modification of liver proteins by the quinine-imine metabolite of paracetamol or irreversible acetylation of biomolecules by aspirin) are support for the view that these pharmacokinetic and notably metabolic effects of ibuprofen favour its low toxic potential. (3) The multiple actions of ibuprofen in controlling inflammation combine with moderate inhibition of COX-1 and COX-2 and low residence time of the drug in the body may account for the low GI, CV and renal risks from ibuprofen, especially at OTC doses.

引用本文的药物库数据

药物

布洛芬

药物酶

药物	酶	种类	生物	药理作用	行动
Dexibuprofen	Alpha-methylacyl-CoA消旋酶	蛋白质	人类	没有	底物	细节
布洛芬	Alpha-methylacyl-CoA消旋酶	蛋白质	人类	没有	底物	细节
布洛芬	细胞色素P450 2C19	蛋白质	人类	未知的	底物	细节