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溴芬酸钠的临床药代动力学与药效学

Clinical pharmacokinetics and pharmacodynamics of bromfenac.

作者信息

Skjodt N M, Davies N M

机构信息

Respiratory Research Group, Faculty of Medicine, University of Calgary, Alberta, Canada.

出版信息

Clin Pharmacokinet. 1999 Jun;36(6):399-408. doi: 10.2165/00003088-199936060-00002.

Abstract

Bromfenac is a nonsteroidal anti-inflammatory drug whose peak plasma concentration is reached 0.5 hours after oral administration. Bromfenac binds extensively to plasma albumin. The area under the plasma concentration-time curve is linearly proportional to the dose for oral doses up to 150 mg. The relationship between the total plasma and analgesic effect has been established. Only small amounts of bromfenac are eliminated unchanged, with the remaining drug being biotransformed into glucuronide metabolites which are excreted in urine and bile. Rapid elimination occurs in healthy individuals (half-life 0.5 to 4.0 h). Renal disease, hepatic disease and aging alter the disposition kinetics of bromfenac, and dosage adjustment may be advisable. Bromfenac modestly decreases free phenytoin concentrations. Bromfenac can cause idiosyncratic hepatic toxicity and has been withdrawn by its manufacturer pending further investigation of these case reports.

摘要

溴芬酸是一种非甾体抗炎药,口服给药后0.5小时达到血浆峰浓度。溴芬酸与血浆白蛋白广泛结合。对于口服剂量高达150毫克的情况,血浆浓度-时间曲线下面积与剂量呈线性比例关系。已确定血浆总量与镇痛效果之间的关系。只有少量溴芬酸以原形消除,其余药物被生物转化为葡萄糖醛酸代谢物,经尿液和胆汁排泄。健康个体中药物消除迅速(半衰期为0.5至4.0小时)。肾脏疾病、肝脏疾病和衰老会改变溴芬酸的处置动力学,可能需要调整剂量。溴芬酸会适度降低游离苯妥英的浓度。溴芬酸可引起特异性肝毒性,其制造商已将其撤出,等待对这些病例报告进行进一步调查。

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