Enhancement of nadolol elimination by activated charcoal and antibiotics
Enhancement of nadolol elimination by activated charcoal and antibiotics
复制标题
活性炭和抗生素增强纳多洛尔的消除
DOI：
10.1038/clpt.1983.79
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发表时间：
1983
影响因子：
6.7
通讯作者：
Pierre Larochelle
中科院分区：
文献类型：
--
作者：
P. Souich;Gilles Caillé;Pierre Larochelle
进行本研究以评估纳多洛尔是否经历肠肝循环。8名健康受试者接受80 mg纳多洛尔口服三次，间隔至少2周。第一个实验是控制。第二组包括纳多洛尔，随后在3小时内给予3 g活性炭，持续9小时。在第三组中，受试者在服用纳多洛尔之前接受0.5 gm红霉素碱和0.5 gm新霉素，每日4次口服，持续2天。活性炭给药后，纳多洛尔AUC从2455 ± 155降至1355 ± 123 ng · hr/ml（平均值± SE），尿液中回收的纳多洛尔百分比（15.4 ± 1.4至10.2 ± 0.7%）和纳多洛尔t½（17.3 ± 1.7至11.8 ± 1.6 h）也是如此。这些数据表明非肾脏消除增加。抗生素给药后，纳多洛尔AUC恒定，尿液中回收的纳多洛尔百分比降至12.7 ± 1.7%，纳多洛尔t½降至11.6 ± 1.3 h，平均峰值纳多洛尔浓度从146 ± 15 ng/ml升至397 ± 52 ng/ml。这些结果表明，纳多洛尔存在肠肝循环，活性炭可能降低纳多洛尔的生物利用度，抗生素可能增加纳多洛尔的作用。临床药理学和治疗学（1983）33，585 -590; doi：10.1038/clpt.1983.79
This study was carried out to assess whether nadolol undergoes enterohepatic circulation. Eight healthy subjects received 80 mg nadolol orally on three occasions at least 2 wk apart. The first experiment was a control. The second consisted of nadolol followed in 3 hr by 3 gm activated charcoal given over a 9‐hr period. In the third, the subjects received 0.5 gm erythromycin base and 0.5 gm neomycin four times a day orally for 2 days before nadolol. After the activated charcoal, the nadolol AUC fell from 2455 ± 155 to 1355 ± 123 ng · hr/ml (mean ± SE), as did the percentage nadolol recovered in urine (15.4 ± 1.4 to 10.2 ± 0.7%) and the nadolol t½ (17.3 ± 1.7 to 11.8 ± 1.6 hr). These data suggest that nonrenal elimination increased. After the antibiotics, nadolol AUC was constant, percentage of nadolol recovered in urine fell to 12.7 ± 1.7%, nadolol t½ fell to 11.6 ± 1.3 hr, and mean peak nadolol concentration rose from 146 ± 15 to 397 ± 52 nglml. These results suggest that there is an enterohepatic circulation for nadolol, that activated charcoal may decrease nadolol bioavailability, and that antibiotics may increase the nadolol effect.Clinical Pharmacology and Therapeutics(1983)33,585–590; doi:10.1038/clpt.1983.79