Metabolism of chlorpheniramine in rat and human by use of stable isotopes.
1. The metabolism of chlorpheniramine (I) was examined in vivo in rats and a human volunteer; in the rats a stable isotope was used. 2. In addition to the unchanged drug (I) and the N-demethylated metabolites (II and III), nine further metabolites were identified in rat urine, four of which were also found in human urine. Chlorpheniramine N-oxide (IV), 3-(p-chlorophenyl)-3-(2-pyridyl) propanol (V), 3-(p-chlorophenyl)-3-(2-pyridyl)-N-acetylaminopropane (VII) and 3-(p-chlorophenyl)-3-(2-pyridyl)-propionic acid (XIII) were identified in rat and human urine. 3. The hydroxylated metabolites of the pyridyl ring of the unchanged drug, II, V and VII, and the glucuronide of XIII were identified only in rat urine. XIII was found in rat urine as long as 6 days after the last dose.
Kasuya
F
F
Faculty of Pharmaceutical Science, Kobegakuin University, Kobe, Japan.
Igarashi
K
K
Fukui
M
M
D000328:Adult; D000818:Animals; D002744:Chlorpheniramine / Q000737:chemistry / Q000378:metabolism* / Q000652:urine; D003903:Deuterium; D005260:Female; D008401:Gas Chromatography-Mass Spectrometry; D006801:Humans; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains
D002744:Chlorpheniramine; D003903:Deuterium