Aprepilor Trio

Aprepitant

In combination therapy for the prevention of nausea & vomiting associated w/ highly & moderately emetogenic cancer chemotherapy in adults & adolescents ≥12.

Recommended dose: 125 mg once daily 1 hr prior to chemotherapy on Day 1 & 80 mg once daily on Days 2 & 3 in the morning. To be given as part of a 3-day regimen that includes a corticosteroid & a 5-HT₃ antagonist. Adult Highly emetogenic chemotherapy regimen Day 1: Aprepitant 125 mg + dexamethasone 12 mg + standard dose of 5-HT₃ antagonist. Days 2 & 3: Aprepitant 80 mg + dexamethasone 8 mg. Day 4: Dexamethasone 8 mg only. Administer dexamethasone 30 min prior to chemotherapy on Day 1 & in the morning on Days 2-4. Moderately emetogenic chemotherapy regimen Day 1: Aprepitant 125 mg + dexamethasone 12 mg + standard dose of 5-HT₃ antagonist. Days 2 & 3: Aprepitant 80 mg only. Administer dexamethasone 30 min prior to chemotherapy on Day 1. Adolescent (12-17 yr) Administer in the morning if no chemotherapy is given on Days 2 & 3. Corticosteroid dose should be administered at 50% of usual dose.

May be taken with or without food: Swallow whole. Do not break, open, or chew.

Hypersensitivity. Co-administration w/ pimozide or cisapride.

Closely monitor INR in patients on chronic warfarin therapy during treatment & for 14 days following each 3-day course. Not to be taken by patients w/ rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltase insufficiency. Concomitant use w/ orally administered cyclosporine, tacrolimus, sirolimus, everolimus, alfentanil, ergot alkaloid derivatives, fentanyl, quinidine); irinotecan; warfarin. Reduced efficacy of hormonal contraceptives during & for 28 days after treatment. Minor influence on ability to drive, cycle & use machines. Moderate to severe hepatic impairment. Use alternative non-hormonal back-up contraceptive methods during treatment & for 2 mth following last dose. Pregnancy. Not recommended to breastfeed during treatment. Childn <12 yr.

Decreased appetite; headache; hiccups; constipation, dyspepsia; fatigue; increased ALT. SJS, TEN.

Increased plasma conc of active substances metabolised through CYP3A4 eg, pimozide, terfenadine, astemizole, or cisapride. Concomitant use w/ active substances metabolised through CYP3A4 & w/ narrow therapeutic range eg, cyclosporine, tacrolimus, sirolimus, everolimus, alfentanil, diergotamine, ergotamine, fentanyl, & quinidine; warfarin. Increased AUC of dexamethasone. Increased or decreased AUC of methylprednisolone. Neurotoxicity w/ ifosfamide. 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 (alprazolam, triazolam). Decreased plasma conc of substances metabolised by CYP2C9 eg, warfarin, acenocoumarol, tolbutamide, phenytoin. Decreased AUC of tolbutamide. Reduced efficacy of hormonal contraceptives eg, ethinyl estradiol, norethindrone. Increased plasma conc 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. Increased AUC & t_½ w/ ketoconazole. Decreased AUC & t_½ w/ rifampicin.

Antiemetics / Supportive Care Therapy

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

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