Klotz U, Ziegler G, Reimann I W
Eur J Clin Pharmacol. 1984;27(1):115-7.
The pharmacokinetics of the selective benzodiazepine antagonist Ro 15-1788 has been studied in 6 healthy male volunteers following a single intravenous dose of 2.5 mg. The drug was only slightly bound to plasma proteins (40 +/- 8%, mean +/- SD). A negligible amount (less than 0.2% of the dose) of unchanged drug was recovered in urine. Hepatic elimination was rapid, as shown by a short t1/2 of 0.9 +/- 0.2 h, and high total plasma and blood clearances of 691 +/- 216 ml/min and 716 +/- 199 ml/min, respectively. The fast decline of plasma levels from about 60 to 2 ng/ml accounts for the short-lasting reversal of benzodiazepine-induced sedation by Ro 15-1788.
在6名健康男性志愿者单次静脉注射2.5毫克选择性苯二氮䓬拮抗剂Ro 15 - 1788后，对其药代动力学进行了研究。该药物与血浆蛋白的结合程度较低（平均±标准差为40±8%）。尿液中回收的原形药物量可忽略不计（少于给药剂量的0.2%）。肝脏消除迅速，半衰期短，为0.9±0.2小时，总血浆清除率和血液清除率较高，分别为691±216毫升/分钟和716±199毫升/分钟。血浆浓度从约60纳克/毫升快速下降至2纳克/毫升，这解释了Ro 15 - 1788对苯二氮䓬诱导的镇静作用的短期逆转。
