First-pass metabolism of imipramine in man.
The systemic availability of orally administered imipramine (IP) varied from 29 to 77% in 4 subjects. The decrease in availability was due to an excess in metabolism after oral administration. This first-pass metabolism did not correlate with plasma half-life, apparent clearance, or the rate of metabolite excretion in urine. There was close correlation with the excess in formation of demethylated metabolites after oral administration, which suggests that the first-pass metabolism is mediated by demethylation, but does not correlate to the total rate of demethylation.
D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D003891:Desipramine / Q000378:metabolism; D005260:Female; D005965:Glucuronates / Q000378:metabolism; D006207:Half-Life; D006801:Humans; D007099:Imipramine / Q000008:administration & dosage / Q000378:metabolism*; D007275:Injections, Intravenous; D008102:Liver Circulation; D008297:Male; D008745:Methylation; D008875:Middle Aged; D013997:Time Factors
D005965:Glucuronates; D007099:Imipramine; D003891:Desipramine