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The following message was posted to: PharmPK
It depends on species. According the work done by Cashman and
coworkers, FMO is involved in the metabolism of chlorpheniramine in
hog liver....causing mainly N-oxidation. On the other hand, Nomura
and coworkers have shown that...in rat liver micorsomes CYP2B and
CYP2C11 are involved in the N-demethylation reaction. There is
indirect evidence of the contribution of CYP2D6 in the metabolism in
humans (Yasuda et al.). Chlorpheniramine has been shown to inhibit
CYP2D6 in vitro (mixed inhibition of bufuralol metabolism..Ki 10.8
uM) ...Hamelin et al. Given the involvement of FMO, cimetedine
should inhibit its metabolism as well.
My two cents
>Is chlorpheniramine and/or dexchlorpheniramine metabolised extensively by
>the cytochrome P450 system?
>If so, then which enzyme system does it act in?
>I am specifically looking for drug interaction information between these
>antihistamines and CYP3A4 substrates.
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