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哺乳期妇女乳汁和唾液中安替比林的代谢情况

Antipyrine disposition in milk and saliva of lactating women.

作者信息

Berlin C M, Vesell E S

出版信息

Clin Pharmacol Ther. 1982 Jan;31(1):38-44. doi: 10.1038/clpt.1982.6.

Abstract

Widely used to study hepatic drug metabolism, antipyrine rapidly distributes in total body water. Antipyrine distribution was studied in seven lactating women. Duration of lactation ranged from 2 to 19 mo. In all subjects the drug was rapidly absorbed; in five women peak concentrations were attained in milk and saliva by 1 hr and in the other two women by 3 hr (first point at which collections were made). In two women in whom antipyrine was measured at 10-min intervals during the first hour, peak concentrations in both milk and saliva were attained by 10 min after antipyrine. The time course for antipyrine disappearance from milk paralleled that from saliva for each subject. Antipyrine half-life (t1/2) varied from 5.6 to 20.3 hr for saliva (mean +/- SD = 11.5 +/- 4.8) and from 5.7 to 21.7 hr for milk (mean +/- SD = 11.6 +/- 5.4). In the two women with the shortest salivary antipyrine t1/2 (5.6 and 7.5 hr), antipyrine was readministered many months later, after they had stopped lactating. The salivary antipyrine t1/2 rose from 5.6 to 13.3 hr in one subject and from 7.5 to 14.6 hr in the other. The corresponding decrease in antipyrine clearance was 0.93 to 0.55 and 1.41 to 0.60 ml/min/kg. This observation suggests that in some subjects lactation may influence drug metabolism. The amount of antipyrine available to each nursing infant was estimated by assuming the the infant nursed 3 ounces every 4 hr for 24 hr after maternal antipyrine administration. The amount of antipyrine available to the nursing infant was calculated to range from 3.0 to 11.1 mg (mean +/- SD = 6.4 +/- 2.9 mg) or from 0.25% to 1.07% (mean +/- SD = 0.59 +/- 0.29%) of the maternal dose.

摘要

安替比林被广泛用于研究肝脏药物代谢,它能迅速分布于全身水分中。对7名哺乳期妇女的安替比林分布情况进行了研究。哺乳期从2个月至19个月不等。所有受试者体内药物均迅速吸收;5名妇女在1小时时乳汁和唾液中达到峰值浓度,另外2名妇女在3小时时达到峰值浓度(首次采集样本的时间点)。在2名妇女中,在第1小时内每隔10分钟测量一次安替比林,乳汁和唾液中的峰值浓度在服用安替比林后10分钟时达到。每位受试者体内安替比林从乳汁中消失的时间过程与从唾液中消失的时间过程相似。安替比林半衰期(t1/2)在唾液中为5.6至20.3小时(平均值±标准差 = 11.5±4.8),在乳汁中为5.7至21.7小时(平均值±标准差 = 11.6±5.4)。在唾液中安替比林半衰期最短的2名妇女(5.6小时和7.5小时)中,在她们停止哺乳数月后再次给予安替比林。其中一名受试者唾液中安替比林半衰期从5.6小时升至13.3小时,另一名受试者从7.5小时升至14.6小时。安替比林清除率相应地从0.93降至0.55以及从1.41降至0.60 ml/min/kg。这一观察结果表明,在某些受试者中,哺乳可能会影响药物代谢。通过假设婴儿在母亲服用安替比林后24小时内每4小时哺乳3盎司,估算了每个哺乳婴儿可获得的安替比林量。计算得出哺乳婴儿可获得的安替比林量为3.0至11.1毫克(平均值±标准差 = 6.4±2.9毫克),或占母亲剂量的0.25%至1.07%(平均值±标准差 = 0.59±0.29%)。

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