Hoffman A, Baluom M
Department of Pharmacy, School of Pharmacy, Hebrew University, Jerusalem, Israel.
Acta Anaesthesiol Scand. 1993 Jan;37(1):102-4. doi: 10.1111/j.1399-6576.1993.tb03608.x.
The present study aimed to investigate whether the pharmacodynamics of a lipophilic barbiturate, heptabarbital, is altered by liver dysfunction. Heptabarbital was slowly infused i.v., to rats with liver necrosis induced by carbon-tetrachloride, until the rats lost their righting reflex. The concentrations of the drug in serum, brain and CSF were determined in both the diseased animals and solvent-treated controls. Although the concentrations of heptabarbital in the CSF, serum and brain were not significantly different between controls and diseased rats, the total heptabarbital dose required to induce sleep was markedly lower in the diseased animals. Accordingly, the pharmacodynamics of heptabarbital is unaffected in experimental liver dysfunction in rats.
本研究旨在探讨亲脂性巴比妥类药物庚巴比妥的药效学是否会因肝功能障碍而改变。将庚巴比妥缓慢静脉注射到四氯化碳诱导肝坏死的大鼠体内，直至大鼠失去翻正反射。测定患病动物和溶剂处理对照组血清、脑和脑脊液中的药物浓度。尽管对照组和患病大鼠脑脊液、血清和脑中庚巴比妥的浓度无显著差异，但患病动物诱导睡眠所需的庚巴比妥总剂量明显较低。因此，在大鼠实验性肝功能障碍中，庚巴比妥的药效学未受影响。
