Dale O
Biochem Pharmacol. 1986 Feb 15;35(4):557-61. doi: 10.1016/0006-2952(86)90347-3.
The interaction of the volatile anaesthetics enflurane, halothane and the halothane metabolite trifluoroacetic acid with the binding of two highly bound acidic drugs (warfarin, phenytoin) to albumin has been studied in vitro by equilibrium dialysis. Trifluoroacetic acid (TFA) inhibited the binding of both drugs to human serum albumin (HSA). Halothane, on the other hand, increased the binding of warfarin to HSA, while enflurane inhibited only the binding of phenytoin. It seems that the binding of the acidic drugs warfarin and phenytoin to HSA is more sensitive to the structures of the gases than for the basic drug diazepam which was previously shown to be equally affected by both gases. Furthermore, it seems that drugs competing for the same binding site (warfarin, phenytoin) may respond differently to conformational changes of the site. It is suggested that drugs bound to the "diazepam site" are more easily affected by the volatile anaesthetics than drugs bound to the "warfarin site".
通过平衡透析法在体外研究了挥发性麻醉剂恩氟烷、氟烷以及氟烷代谢产物三氟乙酸与两种高度结合的酸性药物（华法林、苯妥英）和白蛋白结合的相互作用。三氟乙酸（TFA）抑制了这两种药物与人血清白蛋白（HSA）的结合。另一方面，氟烷增加了华法林与HSA的结合，而恩氟烷仅抑制苯妥英的结合。似乎酸性药物华法林和苯妥英与HSA的结合比碱性药物地西泮对气体结构更敏感，先前已表明地西泮受这两种气体的影响相同。此外，似乎竞争相同结合位点的药物（华法林、苯妥英）对该位点的构象变化可能有不同反应。有人提出，与“地西泮位点”结合的药物比与“华法林位点”结合的药物更容易受到挥发性麻醉剂的影响。
