Anadón A, Martinez-Larrañaga M R, Díaz M J, Bringas P, Fernandez M C
Department of Pharmacology, CSIC, Faculty of Medicine, Complutense University, Madrid, Spain.
Arch Toxicol. 1991;65(2):156-9. doi: 10.1007/BF02034944.
The effect of deltamethrin pretreatment on the pharmacokinetics and metabolism of antipyrine was studied in male rats. The total plasma clearance of antipyrine was significantly decreased by deltamethrin pretreatment (20 mg/kg and 40 mg/kg daily for 6 days prior to antipyrine administration), while the elimination half-life at beta phase, the area under the concentration-time curve and the mean residence time of antipyrine were significantly increased. The magnitude of the observed changes was dose dependent. The urinary excretion of norantipyrine, 4-hydroxyantipyrine and 3-hydroxymethylantipyrine was decreased by 39%, 32% and 26%, respectively (p less than 0.001) in the presence of deltamethrin. In addition, the rate constants for formation of each of these metabolites were significantly decreased by an average of approximately 71%. These results suggest that deltamethrin is capable of inhibiting oxidative metabolism, a finding which could be of clinical and toxicological significance.
在雄性大鼠中研究了溴氰菊酯预处理对安替比林药代动力学和代谢的影响。在给予安替比林前6天,每日用溴氰菊酯(20mg/kg和40mg/kg)预处理,安替比林的总血浆清除率显著降低,而β相消除半衰期、浓度-时间曲线下面积和安替比林的平均驻留时间显著增加。观察到的变化幅度呈剂量依赖性。在有溴氰菊酯存在的情况下,去甲安替比林、4-羟基安替比林和3-羟甲基安替比林的尿排泄分别减少了39%、32%和26%(p<0.001)。此外,这些代谢物各自的生成速率常数平均显著降低了约71%。这些结果表明溴氰菊酯能够抑制氧化代谢,这一发现可能具有临床和毒理学意义。