Nordgren I
Fundam Appl Toxicol. 1981 Mar-Apr;1(2):230-7. doi: 10.1016/s0272-0590(81)80063-2.
Metrifonate (0,0-dimethyl-(1-hydroxy-2,2,2-trichloroethyl)-phosphonate) is an organophosphorus compound where there are excellent possibilities to make studies in man. Metrifonate and its rearrangement product dichlorvos (2,2-dichlorovinyl dimethyl phosphate, DDVP) were studied in human blood from schistosomiasis patients treated with Bilarcil. A mass fragmentographic technique was employed. Deuterium labelled variants of the substances were used, both as internal standards and to compensate for DDVP formed during the workup procedure. The amount of DDVP in plasma was about 1% of the amount of metrifonate. In erythrocytes the corresponding amount of DDVP in percent of metrifonate was half or less. Both compounds reached peak levels within two hours and were detectable for at least eight hours. The results were compared to erythrocyte and plasma cholinesterase determinations. Levels of metrifonate and DDVP, together with cholinesterase activity, have also been studied in mouse brain, liver and kidney. It is proposed that metrifonate acts as a slow release formulation for DDVP. Clearance of metrifonate in man occurs primarily via DDVP. Mild vertigo subsiding in a few hours was the most common side-effect.
敌百虫（0,0 - 二甲基 -（1 - 羟基 - 2,2,2 - 三氯乙基） - 膦酸酯）是一种有机磷化合物，在人体研究方面有很好的可能性。对接受血防846治疗的血吸虫病患者的血液中的敌百虫及其重排产物敌敌畏（2,2 - 二氯乙烯基二甲基磷酸酯，DDVP）进行了研究。采用了质量碎片图谱技术。使用了这些物质的氘标记变体，既作为内标，也用于补偿后处理过程中形成的敌敌畏。血浆中敌敌畏的量约为敌百虫量的1%。在红细胞中，敌敌畏相对于敌百虫的相应量为一半或更少。两种化合物在两小时内达到峰值水平，并且至少八小时内可检测到。将结果与红细胞和血浆胆碱酯酶测定结果进行了比较。还对小鼠脑、肝和肾中的敌百虫和敌敌畏水平以及胆碱酯酶活性进行了研究。有人提出敌百虫可作为敌敌畏的缓释制剂。人体中敌百虫的清除主要通过敌敌畏进行。最常见的副作用是几小时内缓解的轻度眩晕。
