消炎痛的临床药物动力学。

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Helleberg L

消炎痛的临床药物动力学。

Jul-Aug Pharmacokinet。1981; 6 (4): 245 - 58。doi: 10.2165 / 00003088-198106040-00001。

PubMed ID

7249487 (在PubMed

]

文摘

吲哚美辛(1 - (p-chlorobenzoyl) 5-methoxy-2-methylindole-3-acetic酸)是一种anit-in-flammatory退热的药物常用的疼痛和僵硬的症状缓解风湿性疾病。口服药物的吸收后快速和完整的,但重要的国际米兰和个体内的变化。在一般情况下,血浆浓度峰值的2到3微克/毫升实现1到2小时,但同时摄入的食物减少了峰值浓度和延迟没有减少吸收。直肠政府早些时候但降低血浆浓度峰值,栓剂不完全吸收形式,并没有提供临床优势相比,相当于口服剂量。在等离子体的90%消炎痛必定会在治疗性血浆白蛋白浓度。吲哚美辛分布到滑液,是人类母乳分泌,在大量穿过胎盘。是代谢O-desmethylindomethacin, N-deschlorobenzoylindomethacin O-desmethy-N-deschlorobenzoylindomethacin,是缺乏抗炎活动和存在大量的等离子体。大约60%的口服剂量glucuronidated形式主要由尿排出,虽然大约40%是在粪便中排出后胆汁分泌。大量的剂量进行胆道回收。生物转化是独立于政府的路线。 A 2-compartment open model with correction for biliary recycling can be used to describe the disposition of indomethacin. The drug has a biological half-life of about 5 to 10 hours and a plasma clearance of 1 to 2.5ml/kg/min. In premature infants the half-life of indomethacin is inversely correlated with gestational age and is significantly prolonged as compared with adults. Renal failure does not affect the serum concentrations of indomethacin. Probenecid results in increased plasma concentrations of indomethacin with enhanced pain relief without increasing the incidence of side effects. There seem to be no significant pharmacokinetic interactions between indomethacin and aspirin or warfarin. To date it has not been possible to identify a relationship between the clinical effects and plasma concentration of indomethacin.

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药物

吲哚美辛