Richter E, Breimer D D, Zilly W
Eur J Clin Pharmacol. 1980;17(3):197-202. doi: 10.1007/BF00561900.
The pharmacokinetics of intravenously infused hexobarbital was studied in 10 patients with intrahepatic cholestasis and in 9 with extrahepatic biliary obstruction. The results were compared with those obtained in 16 healthy young volunteers and 5 older patients with normal liver function. After infusion, the plasma concentrations showed a rapid initial decline (alpha-phase) and subsequently a slower decrease (beta-phase). The half-life of a latter phase was 323 +/- 84 min in the healthy group, 357 +/- 151 min in the patients with intrahepatic cholestasis and 344 +/- 115 min in the group with biliary obstruction; the clearances were 3.41 +/- 0.90, 4.08 +/- 1.95 and 3.81 +/- 1.97 ml x min-1 x kg-1, respectively. The differences were not statistically significant. The mean volume of the central compartment of distribution and the steady state volume of distribution were not significantly different. In two patients hexobarbital clearance during cholestasis was greater than after it had subsided. After treatment of 11 patients with cholestasis with drug metabolism-inducing agents (phenobarbital, rifampicin or phenytoin), the half-life of hexobarbital was significantly shortened and the mean value of hexobarbital clearance was more than doubled.
对10例肝内胆汁淤积患者和9例肝外胆管梗阻患者静脉输注己巴比妥的药代动力学进行了研究。将结果与16名健康年轻志愿者和5名肝功能正常的老年患者的结果进行了比较。输注后，血浆浓度最初迅速下降（α期），随后下降较慢（β期）。健康组后一阶段的半衰期为323±84分钟，肝内胆汁淤积患者为357±151分钟，胆管梗阻组为344±115分钟；清除率分别为3.41±0.90、4.08±1.95和3.81±1.97 ml·min⁻¹·kg⁻¹。差异无统计学意义。中央室分布容积和稳态分布容积的平均值无显著差异。2例胆汁淤积患者在胆汁淤积期间己巴比妥的清除率高于胆汁淤积消退后。用药物代谢诱导剂（苯巴比妥、利福平或苯妥英）治疗11例胆汁淤积患者后，己巴比妥的半衰期显著缩短，己巴比妥清除率的平均值增加了一倍多。
