[Formation of volatile carcinogenic N-nitroso compounds from drugs under simulated human gastric conditions].
41 commercial drugs approved for peroral application in the GDR, whose active agents contain N,N-dialkylamino groups in their chemical structures, have been investigated under simulated conditions of the human stomach. With the drugs containing aminophenazone, amitriptyline, doxycycline and oxytetracycline as active agents N-nitrosodimethylamine is formed as a result of nitrosation reactions. With the drugs containing clomiphene++, disulfiram, probenecid and a diethylamine-containing liquid hypnoticum, there occurred N-nitrosodiethylamine. In no case N-nitrosodi-n-propylamine or N-nitrosopiperidine were detectable. The isolated active agents amitriptyline, clomiphene++ and probenecid themselves proved not to be nitrosatable. The positive findings with these drugs were caused by not yet identified nitrosatable contaminants of these drugs. The quantitative determination of volatile N-nitroso compounds was done upon steam distillation by means of gas chromatograph and chemiluminescence detector.
D000632:Aminopyrine / Q000378:metabolism; D000639:Amitriptyline / Q000378:metabolism; D002996:Clomiphene / Q000378:metabolism; D004048:Diethylamines / Q000378:metabolism; D004052:Diethylnitrosamine / Q000096:biosynthesis; D004128:Dimethylnitrosamine / Q000096:biosynthesis; D004221:Disulfiram / Q000378:metabolism; D004318:Doxycycline / Q000378:metabolism; D006801:Humans; D008954:Models, Biological; D009603:Nitroso Compounds / Q000096:biosynthesis*; D010118:Oxytetracycline / Q000378:metabolism; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D011339:Probenecid / Q000378:metabolism; D013270:Stomach / Q000502:physiology*
D004048:Diethylamines; D009603:Nitroso Compounds; D004364:Pharmaceutical Preparations; D000632:Aminopyrine; D000639:Amitriptyline; D002996:Clomiphene; D004052:Diethylnitrosamine; C034281:diethylamine; D004128:Dimethylnitrosamine; D004318:Doxycycline; D011339:Probenecid; D004221:Disulfiram; D010118:Oxytetracycline
Bildung flüchtiger kanzerogener N-Nitrosoverbindungen aus Arzneimitteln unter simulierten Bedingungen des menschlichen Magens.