In the same study, the authors observed that astemizole
clearly prevented HCC development in vivo.
Danazol , decursin , hydroxyebastine , thelephoric acid , telmisartan , TSAHC  inhibited CYP2J2-mediated astemizole
O-demethylation activity with [IC.
In vitro studies have shown ketoconazole, a potent inhibitor of CYP3A4 activity, to be at least 100 times more potent than paroxetine as an inhibitor of the metabolism of several substrates for CYP3A4, including astemizole
, triazolam, and cyclosporine.
The two compounds are already marketed as the drugs tacrolimus and astemizole
haematological values) of phenylhydantoin, astemizole
, calcium channel blockers, cisapride, oral hypoglycemiants, rifampicin, zidovudine, rifabutin, cyclosporine, sulfonylureas and warfarin.
From the Food and Drug Administration Warnings Issued on Nonse-dating Antihistamines Teffenadine and Astemizole
Se debe de tener cuidado cuando se usan concomitantemente drogas que interactuen sobre la citocromo P450, CYP3A4 como el alfentanil, astemizole
, cisapride, ciclosporina, ergotamina (derivados del ergot), fentanyl pimozide, quinidina, tacrolimus debido a que pueden ser modificadas sus concentraciones plasmaticas por el uso de dastinib.
Torsades de pointes associated with astemizole
Dual effect of the anti-allergic astemizole
Initial reports of cardiac arrhythmias, including torsades de pointes, were predominately associated with high blood concentrations subsequent to overdoses Given the metabolic pathway of these drugs, arrhythmias were eventually reported subsequent to coadministration with drugs that slowed the metabolism of terfenadine and astemizole
(also resulting in high blood concentrations).
Coadministration is contraindicated for ergot alkaloids, terfenadine, astemizole
, cisapride, pimozide, halofantrine, and quinidine.
Special Considerations: Emend is a weak to moderate CYP3A4 inhibitor, so it should not be used with pimozide, terfenadine, astemizole
, or cisapride.