What Pain Medicines are OK to Take with Imatinib (Gleevec)?
response from Kavita Bhagat/PH/Novartis 08/22/2008 01:11 PM Our drug interaction letter shows drugs known to be metabolized by CYP450 isoenzyme 2D6 (beta blockers – substrates), CYP450 isoenzyme 2C9 (NSAIDS – substrates), and CYP450 isoenzyme 3A 4/5 (benzodiazepines – substrates). Gleevec is primarily metabolized to its active metabolite, an N-demethylated piperazine derivative, as well as to various inactive metabolites by the human P450 cytochrome isoenzyme CYP3A4. Cytochrome P450 enzymes, including CYP1A2, CYP2D6, CYP2C9 and CYP2C19 also play a minor role in the metabolism of Gleevec. In addition, in vitro human liver microsome studies demonstrate that Gleevec is a potent competitive inhibitor of the cytochrome P450 isoenzymes CYP3A4/5 and CYP2D6, as well as CYP2C9. Therefore, interactions with Gleevec are possible and caution is recommended when Gleevec is administered with drugs whose metabolism is dependent on or which alter levels of these isoenzymes.
