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月经周期中的安替比林代谢

Antipyrine metabolism during the menstrual cycle.

作者信息

Riester E F, Pantuck E J, Pantuck C B, Passananti G T, Vesell E S, Conney A H

出版信息

Clin Pharmacol Ther. 1980 Sep;28(3):384-91. doi: 10.1038/clpt.1980.177.

Abstract

Two studies were initiated to determine the effect of the menstrual cycle on antipyrine metabolism. In the first study a relatively large oral dose of antipyrine (15 mg/kg) was given on days, 3, 5, 10, 14, 16, 20, and 25 after the onset of menstruation. Salivary antipyrine half-lifes (t1/2S) declined progressively, suggesting that the long-term administration of this dose had stimulated antipyrine metabolism. To minimize this possible induction, in the second study a much smaller dose of antipyrine (1 mg/kg) was given on the same days of the cycle as in the first study. There was no induction. In both experiments, the menstrual cycle had little or no effect on the mean salivary t1/2, mean metabolic clearance rate, or apparent volume of distribution of antipyrine. In the second, men served as controls. The mean kinetic parameters for the men did not differ from those for the women. Although individuals of each sex varied from day to day in each kinetic parameter, the magnitude of the intraindividual variability in antipyrine metabolism was the same for both. The mean intraindividual coefficient of variation for antipyrine t1/2S was 14.4 +/- 1.6% (SE) in women and 12.4 +/- 1.3% (SE) in men. No consistent pattern for either sex was observed in the day-to-day variations in the means of the kinetic parameters investigated. Several women in whom the t1/2 rose or fell at midcycle were found to have a different pattern when reexamined 6 mo later.

摘要

开展了两项研究以确定月经周期对安替比林代谢的影响。在第一项研究中,在月经开始后的第3、5、10、14、16、20和25天给予相对大剂量的口服安替比林(15毫克/千克)。唾液安替比林半衰期(t1/2S)逐渐下降,表明长期给予该剂量刺激了安替比林代谢。为尽量减少这种可能的诱导作用,在第二项研究中,在与第一项研究相同的月经周期日子里给予小得多的安替比林剂量(1毫克/千克)。未出现诱导作用。在两项实验中,月经周期对安替比林的平均唾液t1/2、平均代谢清除率或表观分布容积几乎没有影响。在第二项研究中,男性作为对照。男性的平均动力学参数与女性的无差异。尽管每种性别的个体在每个动力学参数上每天都有变化,但安替比林代谢的个体内变异性大小对两者而言是相同的。女性安替比林t1/2S的平均个体内变异系数为14.4±1.6%(标准误),男性为12.4±1.3%(标准误)。在所研究的动力学参数均值的每日变化中,未观察到任何一种性别的一致模式。发现几名t1/2在月经周期中期升高或降低的女性在6个月后重新检查时具有不同的模式。

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