Trevive Drug Interactions

Compatibilities: Active substances that may increase imatinib plasma concentrations: Substances that inhibit the cytochrome P450 isoenzyme CYP3A4 activity (e.g. protease inhibitors such as indinavir, lopinavir/ritonavir, ritonavir, saquinavir, telaprevir, nelfinavir, boceprevir; azole antifungals including ketoconazole, itraconazole, posaconazole, voriconazole; certain macrolides such as erythromycin, clarithromycin and telithromycin) could decrease metabolism and increase imatinib concentrations. There was a significant increase in exposure to imatinib when it was co-administered with a single dose of ketoconazole (a CYP3A4 inhibitor). Caution should be taken when administering Imatinib Tablets with inhibitors of the CYP3A4 family.
Active substances that may decrease imatinib plasma concentrations: Substances that are inducers of CYP3A4 activity (e.g. dexamethasone, phenytoin, carbamazepine, rifampicin, phenobarbital, fosphenytoin, primidone or Hypericum perforatum, also known as St. John's Wort) may significantly reduce exposure to Imatinib Tablets, potentially increasing the risk of therapeutic failure. Concomitant use of rifampicin or other strong CYP3A4 inducers and imatinib should be avoided.
Active substances that may have their plasma concentration altered by Imatinib Tablets: Caution is recommended when administering Imatinib Tablets with CYP3A4 substrates with a narrow therapeutic window (e.g. cyclosporine, pimozide, tacrolimus, sirolimus, ergotamine, diergotamine, fentanyl, alfentanil, terfenadine, bortezomib, docetaxel and quinidine).
Imatinib Tablets may increase plasma concentration of other CYP3A4 metabolised drugs (e.g. triazolobenzodiazepines, dihydropyridine calcium channel blockers, certain HMG-CoA reductase inhibitors, i.e. statins, etc.).
Because of known increased risks of bleeding in conjunction with the use of imatinib (e.g. haemorrhage), patients who require anticoagulation should receive low-molecular-weight or standard heparin, instead of coumarin derivatives such as warfarin.
In vitro Imatinib Tablets inhibits the cytochrome P450 isoenzyme CYP2D6 activity at concentrations similar to those that affect CYP3A4 activity. Dose adjustments do not seem to be necessary when imatinib is co-administrated with CYP2D6 substrates, however caution is advised for CYP2D6 substrates with a narrow therapeutic window such as metoprolol. In patients treated with metoprolol clinical monitoring should be considered.
In vitro, Imatinib Tablets inhibits paracetamol O-glucuronidation. Caution should be exercised when using high doses of Imatinib Tablets and paracetamol concomitantly.
In thyroidectomy patients receiving levothyroxine, the plasma exposure to levothyroxine maybe decreased when Imatinib Tablets is co-administered. Caution is therefore recommended. Drug-drug interactions between imatinib and chemotherapy regimens are not well characterised. Imatinib adverse events, i.e. hepatotoxicity, myelosuppression or others may increase and it has been reported that concomitant use with L-asparaginase could be associated with increased hepatotoxicity. Therefore, the use of Imatinib Tablets in combination requires special precaution.