title: Acute kinetic and dynamic interactions of zimelidine with ethanol.
abstract: The acute interaction of zimelidine (Z) with ethanol (E) was examined in six healthy men aged 20 to 37 yr who randomly received each of four treatments 1 wk apart: Z, 200 mg by mouth, preceded by 1 hr and followed for 7 hr of oral E in juice dosed to maintain blood alcohol concentrations between 800 and 1000 mg/l; placebo Z and E; Z and juice; and placebo Z and juice. E decreased the rate of biotransformation of Z to norzimelidine (NZ) by 46%, but the AUCs of Z, NZ, and their total concentration over 8 hr were not altered by E. Acetaldehyde concentrations did not change and no aversive alcohol-sensitizing reaction was detected. E-induced impairments in memory, body sway, and a manual tracking task were further enhanced by Z, as was the E-induced decrease in friendliness. Data suggest Z and E interact kinetically and dynamically and suggest a mechanism whereby Z may decrease E intake in man.
mesh_terms: D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D001711:Biotransformation; D004347:Drug Interactions; D004644:Emotions / Q000187:drug effects; D000431:Ethanol / Q000378:metabolism* / Q000494:pharmacology; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007700:Kinetics; D008297:Male; D011939:Mental Recall / Q000187:drug effects; D011597:Psychomotor Performance / Q000187:drug effects; D015031:Zimeldine / Q000031:analogs & derivatives / Q000097:blood / Q000378:metabolism* / Q000494:pharmacology
chemical_list: D015031:Zimeldine; D000431:Ethanol; C017578:norzimelidine