Desipramine hydroxylation: variability and effect of antipsychotic drugs.
Steady-state plasma concentrations of desipramine (DMI), unconjugated 2-OH DMI, and total 2-OH DMI were measured in 82 depressed inpatients, 35 of whom were concurrently receiving a phenothiazine or butyrophenone antipsychotic drug. In the patients not on an antipsychotic, the ratio of unconjugated metabolite to parent varied from 0.01 to 1.5, with a median of 0.48, and was inversely related to the parent drug level. Antipsychotic drug was associated with higher DMI levels and a lower proportion of OH-metabolite (median, 0.23). In both groups the unconjugated form accounted for only about 10% of the total metabolite. No relationship of age, sex, drinking history, or smoking to DMI or 2-OH DMI levels was found.
D000328:Adult; D000368:Aged; D014150:Antipsychotic Agents / Q000494:pharmacology*; D002849:Chromatography, Gas; D002851:Chromatography, High Pressure Liquid; D003891:Desipramine / Q000031:analogs & derivatives / Q000097:blood / Q000378:metabolism*; D004347:Drug Interactions; D005260:Female; D006801:Humans; D006900:Hydroxylation; D008297:Male; D008875:Middle Aged; D010546:Perphenazine / Q000494:pharmacology
D014150:Antipsychotic Agents; D010546:Perphenazine; D003891:Desipramine; C028653:2-hydroxydesipramine