Aderjan R, Bösche J, Schmidt G
Z Rechtsmed. 1982;88(4):263-70. doi: 10.1007/BF00198661.
Several poisonings by diphenhydramine were reported shortly after it had been introduced as an antihistamine in 1945. In the Federal Republic of Germany its combination with 8-chlorotheophylline (dimenhydrinate) is available as a hypnotic without prescription. Replacing the dangerous diethylpentenamide diphenhydramine is a drug which is also often abused. Fatal poisonings, suicide attempts, and traffic accidents were increasingly observed. In seven cases drug-influenced road users caused traffic accidents. We observed blood concentrations of diphenhydramine as high as in four cases of clinically treated patients after ingestion of large doses. This indicates a serious drug abuse. The measurement of the concentration of diphenhydramine and its major metabolite (diphenmethoxy acetic acid) in blood and urine is a means of recognizing chronic use and misuse of diphenhydramine. As the metabolite accumulates in blood one may find an elevated level after multiple dosing. Shortly after taking a single dose no or only low metabolite concentration is found. The concentration of diphenhydramine and its metabolite was measured in several fatal cases. In one of these cases the concentration in body fluids and tissues was in a range not observed until now.
1945年苯海拉明作为抗组胺药被引入后不久,就有几起苯海拉明中毒的报告。在德意志联邦共和国,它与8-氯茶碱(茶苯海明)的组合作为一种催眠药无需处方即可获得。取代危险的二乙戊酰胺的苯海拉明也是一种经常被滥用的药物。致命中毒、自杀未遂和交通事故越来越多地被观察到。在七起案件中,受药物影响的道路使用者引发了交通事故。我们观察到,在四例大剂量摄入后接受临床治疗的患者中,苯海拉明的血药浓度也很高。这表明存在严重的药物滥用情况。测量血液和尿液中苯海拉明及其主要代谢物(二苯甲氧基乙酸)的浓度是识别苯海拉明长期使用和滥用的一种方法。由于代谢物在血液中积累,多次给药后可能会发现其水平升高。单次服药后不久,代谢物浓度无或仅低。在几起致命案件中测量了苯海拉明及其代谢物的浓度。在其中一起案件中,体液和组织中的浓度处于迄今为止未观察到的范围。