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First‐pass metabolism of imipramine in man
Author(s) -
Gram Lars F.,
Christiansen Johannes
Publication year - 1975
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt1975175555
Subject(s) - demethylation , metabolism , imipramine , metabolite , urine , oral administration , first pass effect , excretion , pharmacology , chemistry , pharmacokinetics , endocrinology , medicine , biochemistry , gene expression , alternative medicine , pathology , dna methylation , gene
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.