Imamura Y, Nomura T, Katsuki Y, Kojima Y, Otagiri M
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
Pharmacol Toxicol. 1990 Nov;67(5):415-9. doi: 10.1111/j.1600-0773.1990.tb00855.x.
The interaction of acetohexamide (AH) with phenylbutazone (PBZ) was investigated in rabbits. Orally administered PBZ caused a potentiation of hypoglycaemic action after oral administration of AH. This can be explained by the fact that the co-administration of PBZ significantly increased both the serum concentrations of AH and its pharmacologically active metabolite. (-)-hydroxyhexamide [(-)-HH], after AH administration. The co-administration of PBZ decreased the renal clearance (Clr) and non-renal clearance (Clnr) of AH. PBZ inhibited the in vitro reduction of AH to (-)-HH and decreased the accumulation of (-)-HH by the kidney cortical slices. These results indicate that the mechanism of in vivo interaction of AH with PBZ is complicated.
在兔体内研究了醋磺己脲（AH）与保泰松（PBZ）的相互作用。口服PBZ会导致口服AH后低血糖作用增强。这可以用以下事实来解释：PBZ与AH联合给药显著提高了AH及其药理活性代谢物（-）-羟基己脲[（-）-HH]的血清浓度。PBZ与AH联合给药降低了AH的肾清除率（Clr）和非肾清除率（Clnr）。PBZ抑制AH在体外还原为（-）-HH，并减少肾皮质切片对（-）-HH的蓄积。这些结果表明AH与PBZ在体内相互作用的机制很复杂。
