Emend IV

Fosaprepitant dimeglumine

Prevention of acute & delayed nausea & vomiting associated w/ highly emetogenic cisplatin-based cancer chemotherapy. Prevention of nausea & vomiting associated w/ moderately emetogenic cancer chemotherapy.

Adult Initiate approx 30 min prior to chemotherapy. Highly emetogenic chemotherapy regimen 150 mg IV infusion over 20-30 min on day 1, in conjunction w/ dexamethasone & standard dose of 5-HT₃ antagonist. Dexamethasone on day 1: 12 mg orally; day 2: 8 mg orally in the morning; days 3-4: 8 mg orally bd (morning & evening). Moderately emetogenic chemotherapy regimen 150 mg IV infusion over 20-30 min on day 1, in conjunction w/ dexamethasone 12 mg orally & standard dose of 5-HT₃ antagonist.

Hypersensitivity to fosaprepitant dimeglumine, polysorbate 80 or any other excipients. Co-administration w/ pimozide, terfenadine, astemizole, cisapride.

Use w/ caution in patients receiving concomitant active substances that are metabolised primarily through CYP3A4 & w/ a narrow therapeutic range eg, cyclosporine, tacrolimus, sirolimus, everolimus, alfentanil, ergot alkaloid derivatives, fentanyl, & quinidine. Concomitant administration w/ irinotecan might result in increased toxicity. In patients on chronic warfarin therapy, closely monitor INR for 14 days following the use of fosaprepitant. Potential reduced effect of hormonal contraceptives. Hypersensitivity reactions. Infusion site reactions. Should not be given as bolus inj, IM or SC. Patients w/ moderate to severe hepatic impairment. Minor influence on the ability to drive & use machines. Pregnancy & lactation.

Hiccups, increased ALT, dyspepsia, constipation, headache, decreased appetite, fatigue.

Transient increase in plasma conc of drugs metabolised through CYP3A4 eg, cyclosporine, tacrolimus, sirolimus, everolimus, alfentanil, diergotamine, ergotamine, fentanyl, quinidine. Increased AUC of dexamethasone. Transient moderate increase followed by mild decrease in exposure of immunosuppressants metabolised by CYP3A4 (eg, cyclosporine, tacrolimus, everolimus, sirolimus). Potential increased plasma conc of midazolam or other benzodiazepines metabolised via CYP3A4 eg, alprazolam, triazolam. Potential small decrease in BP w/ diltiazem. Caution when co-administered w/ warfarin, acenocoumarol, tolbutamide, phenytoin & other drugs metabolised by CYP2C9. Efficacy of hormonal contraceptives may be reduced. Increased plasma conc of aprepitant w/ CYP3A4 inhibitors (eg, ketoconazole, itraconazole, voriconazole, posaconazole, clarithromycin, telithromycin, nefazodone, PIs). Reduced plasma conc of aprepitant w/ strong CYP3A4 inducers (eg, rifampicin, phenytoin, carbamazepine, phenobarb); St. John's Wort.

Antiemetics / Supportive Care Therapy

A04AD12 - aprepitant ; Belongs to the class of other antiemetics.

P₁S₁S₃