Desipramine hydroxylation: Variability and effect of antipsychotic drugs

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Abstract
Steady‐state plasma concentrations of desipramine (DM1), unconjugated 2‐OH DM1, and total 2‐OH DM1 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 DM1 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 DM1 or 2‐OH DM1 levels was found. Clinical Pharmacology and Therapeutics (1983) 33, 322–328; doi:10.1038/clpt.1983.40

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