布洛芬:药理学、疗效和安全性。
文章的细节
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引用
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Rainsford KD
布洛芬:药理学、疗效和安全性。
Inflammopharmacology。2009年12月,17 (6):275 - 342。doi: 10.1007 / s10787 - 009 - 0016 - x。Epub 2009年11月21日。
- PubMed ID
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19949916 (在PubMed]
- 文摘
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目的:本文试图从大量汇集信息最近的研究在临床使用安全性和布洛芬的药理特性。布洛芬被广泛使用在许多国家为缓解疼痛的症状,炎症和发烧。布洛芬的作用模式的证据被认为是与它的行为在控制炎症,疼痛和发烧,以及药物的副作用。总结的结果:在低剂量(800 - 1200 mg(1))在许多国家批准的非处方药(场外)销售布洛芬有良好的安全性与扑热息痛可比。其镇痛活性与抗炎作用及其与降低血液的体外生产cyclo-oxygenase (COX) 1和COX - 2前列腺素类派生而来。更高的处方剂量(大约1800 - 2400毫克(1))长期治疗风湿性和其他更严重的musculo-skeletal的条件。最近的证据从大规模临床试验新coxibs,布洛芬是一个comparator,证实了早期的研究表明,布洛芬与coxibs和其他非甾体类抗炎药比较疗效。长期使用(6 +个月)有更多的辍学生由于减少治疗的有效性,与非甾体抗炎药是常见的一个特征。自发报告的不良事件和药品不良反应(adr)在临床路径从长期coxib比较研究,以及在流行病学研究中,表明,布洛芬胃肠道(GI)相对较低的风险,hepato-renal和其它药物不良反应少见,而与其他非甾体抗炎药和coxibs。心血管风险略高(CV)事件据报道在一些,但不是所有的研究,但风险是一般低于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.
beplay体育安全吗DrugBank数据引用了这篇文章
- 药物
- 药物酶
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药物 酶 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 2 c19 蛋白质 人类 未知的底物细节