Interactions between octreotide and Aprepitant (aprepitant)
octreotide and aprepitant (Moderate Drug-Drug)
MONITOR: Coadministration with inhibitors of CYP450 3A4 may increase the plasma concentrations of aprepitant, which is primarily metabolized by the isoenzyme. According to the manufacturer, coadministration of the potent CYP450 3A4 inhibitor ketoconazole (400 mg/day for 10 days) and a single 125 mg dose of aprepitant on day 5 resulted in a 5-fold increase in the area under the plasma concentration-time curve (AUC) and a 3-fold increase in the mean terminal half-life of aprepitant. In patients with mild to moderate hypertension, coadministration of the moderate inhibitor diltiazem (120 mg three times a day for 5 days) and aprepitant (approximately 230 mg once a day) resulted in a 2-fold increase in the AUC of aprepitant and a 1.7-fold increase in that of diltiazem. No clinically significant changes in ECG, heart rate, or blood pressure were observed beyond those induced by diltiazem alone.
MANAGEMENT: Caution is advised if aprepitant is used with CYP450 3A4 inhibitors, particularly potent ones like protease inhibitors, macrolide antibiotics, itraconazole, ketoconazole, and nefazodone. Pharmacologic response to aprepitant should be monitored more closely whenever a CYP450 3A4 inhibitor is added to or withdrawn from therapy. In addition, many CYP450 3A4 inhibitors are also substrates of the isoenzyme, thus pharmacologic response to these agents should also be monitored during coadministration with aprepitant.
