Nordgren I, Bengtsson E, Holmstedt B, Pettersson B M
Acta Pharmacol Toxicol (Copenh). 1981;49 Suppl 5:79-86. doi: 10.1111/j.1600-0773.1981.tb03256.x.
A method for the simultaneous quantitation of metrifonate (0,0-dimethyl-(1-hydroxy-2,2,2-trichloroethyl)-phosphonate) and dichlorvos (2,2-dichlorovinyl dimethyl phosphate, DDVP) in human blood has been worked out. It is based upon multiple labelling of the compounds with deuterium and gas phase analysis using the mass spectrometer as a selective detector. The amount of DDVP in plasma is about 1% of the amount of metrifonate. In erythrocytes the corresponding amount of DDVP is 0.5% or less of metrifonate. Both compounds reach peak levels in blood within two hours after oral dosing and are detectable for at least eight hours. Cholinesterase activity in plasma reaches zero levels within 15 min. and remains inhibited for more than eight hours. Red blood cell cholinesterase is inhibited only 60-80%. According to kinetic calculations, clearance of metrifonate occurs primarily via dichlorvos. If dichlorvos is the only active component, which in all likelihood it is, it's slow release may be important in the schistosomicidal effect. Clinical data in seven metrifonate treated patients revealed that mild vertigo subsiding in a few hours was the most common side effect.
已研究出一种同时定量测定人血液中敌百虫（0,0 - 二甲基 -（1 - 羟基 - 2,2,2 - 三氯乙基） - 膦酸酯）和敌敌畏（2,2 - 二氯乙烯基二甲基磷酸酯，DDVP）的方法。该方法基于用氘对化合物进行多重标记，并使用质谱仪作为选择性检测器进行气相分析。血浆中敌敌畏的量约为敌百虫量的1%。在红细胞中，敌敌畏的相应量为敌百虫的0.5%或更少。口服给药后两小时内，两种化合物在血液中均达到峰值水平，并且至少八小时内可检测到。血浆中的胆碱酯酶活性在15分钟内降至零水平，并在超过八小时内保持抑制状态。红细胞胆碱酯酶仅被抑制60 - 80%。根据动力学计算，敌百虫的清除主要通过敌敌畏进行。如果敌敌畏是唯一的活性成分（很可能如此），其缓慢释放可能在杀血吸虫作用中起重要作用。七名接受敌百虫治疗的患者的临床数据显示，数小时内消退的轻度眩晕是最常见的副作用。
