Eigenberg D A, Pazdernik T L, Doull J
Fundam Appl Toxicol. 1983 Nov-Dec;3(6):496-501. doi: 10.1016/s0272-0590(83)80094-3.
A gas chromatographic method for quantifying methamidophos in plasma was developed and used to study the kinetics of methamidophos in the rat and to evaluate the efficacy of hemoperfusion therapy for treating organophosphate insecticide poisoned individuals. Intravenous administration of methamidophos resulted in a plasma decay curve which corresponded to a one compartment pharmacokinetic model with the following pharmacokinetic parameters: t1/2 = 1.5 hr; Vd = 0.81 L/kg; C1 = 5.8 mL/min/kg; kel = 0.45 hr-1. Hemoperfusion with activated charcoal effectively removed methamidophos from the blood of intoxicated rats, and significantly decreased the body burden of methamidophos; 27% of the administered dose of methamidophos was removed during five hours of perfusion. Despite a rapid reduction in the body burden of the insecticide, rats were not protected against a lethal dose of the insecticide. Because of the rapid and slowly reversible inhibition of acetylcholinesterase by organophosphate insecticides, hemoperfusion alone will not improve the clinical status of organophosphate insecticide poisoned patients.
建立了一种气相色谱法用于定量测定血浆中的甲胺磷，并用于研究大鼠体内甲胺磷的动力学以及评估血液灌流疗法治疗有机磷杀虫剂中毒患者的疗效。静脉注射甲胺磷后，血浆衰减曲线符合一室药代动力学模型，其药代动力学参数如下：t1/2 = 1.5小时；Vd = 0.81升/千克；C1 = 5.8毫升/分钟/千克；kel = 0.45小时-1。用活性炭进行血液灌流可有效清除中毒大鼠血液中的甲胺磷，并显著降低甲胺磷的体内负荷；在灌流5小时期间，27%的甲胺磷给药剂量被清除。尽管杀虫剂的体内负荷迅速降低，但大鼠并未免受致死剂量杀虫剂的影响。由于有机磷杀虫剂对乙酰胆碱酯酶的抑制作用迅速且可逆性缓慢，单纯的血液灌流并不能改善有机磷杀虫剂中毒患者的临床状况。
