Rimonabant Ketoconazole

RIMONABANT ANTIFUNGALS- KETOCONAZOLE t rimonabant levels Ketoconazole inhibits CYP3A4-mediated metabolism of rimonabant Avoid co-administration... 

Clinically important, potentially hazardous interactions with alfentanil, alfuzosin, alprazolam, amiodarone, amprenavir, aprepitant, astemizole, atazanavir, bepridil, buprenorphine, bupropion, carbamazepine, chlordiazepoxide, ciclesonide, clozapine, conivaptan, cyclosporine, cyproterone, dasatinib, diazepam, dihydroergotamine, ergot alkaloids, estazolam, eszopidone, etravirine, ezetimibe, fentanyl, fesoterodine, flecainide, flurazepam, fluticasone, halazepam, ivabradine, ixabepilone, ketoconazole, lapatinib, levothyroxine, meperidine, meptazinol, methysergide, midazolam, nifedipine, nilotinib, oral contraceptives, phenytoin, pimozide, piroxicam, propafenone, propoxyphene, quazepam, quinidine, ranolazine, rifabutin, rifampin, rifapentine, rimonabant, rivaroxaban, saquinavir, sildenafil, silodosin, simvastatin, solifenacin, St John s wort, tadalafil, temsirolimus, trabectedin, triazolam, vardenafil, voriconazole, zolpidem... 

Ketoconazole doubled the AUC of rimonabant, and other potent CYP3A4 inhibitors are also expected to raise rimonabant levels. Potent CYP3A4 inducers are expected to lower rimonabant levels. Due to a lack of information the manufacturers suggest that rimonabant should not be taken with antidepressants. Rimonabant does not appear to affect the levels of oral contraceptives, di-goxin, midazolam or warfarin, and alcohol, lorazepam, and orlistat do not appear to alter rimonabant levels. 

Rimonabant is partly metabolised by the cytochrome P450 isoenzyme C YP3A4. Ketoconazole, a potent CYKIA4 inhibitor, doubles the AUC of rimonabant. The manufacturers therefore expect that other potent CYP3A4 inhibitors (they name clarithromycin, itraconazole, nefazo-done, ritonavir, and teUthromycin) will also raise rimonabant levels, and they therefore advise caution on concurrent use. They similarly suggest that potent CYP3A4 inducers (such as carbamazepine, phenobarbital, phenytoin, rifampicin (rifampin) and St John s wort) may lower rimonabant levels. If concurrent use is necessary monitor to ensure that rimonabant remains effective. See Table 1.4 , (p.6), for a list of clinically relevant CYE 3A4 inducers and inhibitors. 

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See also in sourсe #XX -- [ ]

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