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别嘌醇及其剂量大小对痛风患者中保泰松代谢的影响。

The influence of allopurinol and size of dose on the metabolism of phenylbutazone in patients with gout.

作者信息

Horwitz D, Thorgeirsson S S, Mitchell J R

出版信息

Eur J Clin Pharmacol. 1977 Oct 14;12(2):133-6. doi: 10.1007/BF00645134.

DOI:10.1007/BF00645134
PMID:923626
Abstract

Administration of allopurinol 300 mg/day produced minimal changes in the disappearance of phenylbutazone in each of five subjects following single doses (6 mg/kg) in clinical range and caused some prolongation (21%, 52%) of drug half-lives in two of six subjects after single small doses (0.5 mg/kg); mean half-life was not significantly altered by allopurinol at either dose level (means of 52 versus 48 at 0.5 mg/kg and 68 versus 70 h at 6 mg/kg). Size of dose altered half-life when phenylbutazone was used alone; three subjects showed considerably longer half-lives at the higher dose (86 versus 47, 91 versus 41, 65 versus 38 h). Allopurinol caused a greater than 50% prolongation of half-lives in two of five subjects who received single 0.5 g doses of probenecid. These preliminary data do not indicate a need to change the dose of phenylbutazone when subjects are receiving allopurinol.

摘要

在五名受试者单次给予临床剂量范围的苯基丁氮酮(6毫克/千克)后,每天服用300毫克别嘌醇对苯基丁氮酮的消除产生的变化极小;在六名受试者中的两名单次给予小剂量(0.5毫克/千克)后,别嘌醇使药物半衰期延长了一些(分别为21%、52%);在任一剂量水平下,别嘌醇均未显著改变平均半衰期(0.5毫克/千克时分别为52小时和48小时,6毫克/千克时分别为68小时和70小时)。单独使用苯基丁氮酮时,剂量大小会改变半衰期;三名受试者在较高剂量下的半衰期明显更长(分别为86小时对47小时、91小时对41小时、65小时对38小时)。在五名接受单次0.5克丙磺舒剂量的受试者中,有两名受试者的半衰期因别嘌醇而延长超过50%。这些初步数据表明,当受试者接受别嘌醇治疗时,无需改变苯基丁氮酮的剂量。

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引用本文的文献

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Clinical pharmacokinetics of probenecid.丙磺舒的临床药代动力学。
Clin Pharmacokinet. 1981 Mar-Apr;6(2):135-51. doi: 10.2165/00003088-198106020-00004.
2
Prediction of the disposition of nine weakly acidic and six weakly basic drugs in humans from pharmacokinetic parameters in rats.根据大鼠药代动力学参数预测九种弱酸性和六种弱碱性药物在人体内的处置情况。
J Pharmacokinet Biopharm. 1985 Oct;13(5):477-92. doi: 10.1007/BF01059331.
3
Clinical pharmacokinetics of phenylbutazone.保泰松的临床药代动力学

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The physiological disposition of dicumarol in man.双香豆素在人体中的生理处置。
J Pharmacol Exp Ther. 1950 Aug;99(4:1):409-20.
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Observations on the disposition of probenecid in patients receiving allopurinol.对接受别嘌醇治疗的患者中丙磺舒处置情况的观察。
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