Presentation and Status in Health Basket
1 x 125 mg + 2 x 80 mg
This product is given for 3 days as part of a regimen that includes a corticosteroid and a 5-HT3 antagonist. The recommended posology is 125 mg orally once daily one hour before start of chemotherapy on Day 1 and 80 mg orallyonce daily on Days 2 and 3 in the morning.
For rrecommended regimens for the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy, please refer to at the attached doctor’s leaflet.
General: Efficacy data in combination with other corticosteroids and 5-HT3 antagonists are limited. For additional information on the co-administration with corticosteroids, see section 4.5 at the attached doctor’s leaflet . Please refer to the Summary of Product Characteristics of co-administered 5-HT3 antagonist medicinal products.
Elderly (≥65 years): No dose adjustment is necessary for the elderly.
Gender: No dose adjustment is necessary based on gender.
Renal impairment: No dose adjustment is necessary for patients with renal impairment or for patients with end stage renal disease undergoing haemodialysis.
Hepatic impairment: No dose adjustment is necessary for patients with mild hepatic impairment. There are limited data in patients with moderate hepatic impairment and no data in patients with severe hepatic impairment.
Aprepitant should be used with caution in these patients.
Paediatric population: EMEND is not approved for use in paediatric patients.
Method of administration: The capsule should be swallowed whole. EMEND may be taken with or without food.
In combination with other antiemetic agents, for the prevention of acute and delayed nausea and vomiting associated with initial and repeated courses of highly emetogenic cancer chemotherapy, including high-dose cisplatin.
Prevention of nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy.
Hypersensitivity to the active substance or to any of the excipients.
Co-administration with pimozide, terfenadine, astemizole or cisapride.
Patients with moderate to severe hepatic impairment: There are limited data in patients with moderate hepatic impairment and no data in patients with severe hepatic impairment. EMEND should be used with caution in these patients.
CYP3A4 interactions: EMEND should be used with caution in patients receiving concomitant orally administered active substances that are metabolised primarily through CYP3A4 and with a narrow therapeutic range, such as cyclosporine, tacrolimus, sirolimus, everolimus, alfentanil, ergot alkaloid derivatives, fentanyl, and quinidine. Additionally, concomitant administration with irinotecan should be approached with particular caution as the combination might result in increased toxicity.
Co-administration with warfarin (a CYP2C9 substrate): In patients on chronic warfarin therapy, the International Normalised Ratio (INR) should be monitored
closely during treatment with EMEND and for 14 days following each 3-day course of EMEND.
Co-administration with hormonal contraceptives: The efficacy of hormonal contraceptives may be reduced during and for 28 days after administration of EMEND. Alternative non-hormonal back-up methods of contraception should be used during treatment with EMEND and for 2 months following the last dose of EMEND.
Excipients: EMEND capsules contains sucrose. Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.
The most common adverse reactions reported at a greater incidence in adults treated with the aprepitant regimen than with standard therapy in patients receiving Highly Emetogenic Chemotherapy (HEC) were: hiccups (4.6 % versus 2.9 %), alanine aminotransferase (ALT) increased (2.8 % versus 1.1 %), dyspepsia (2.6 % versus 2.0 %), constipation (2.4 % versus 2.0 %), headache (2.0 % versus 1.8 %), and decreased appetite (2.0 % versus 0.5 %). The most common adverse reaction reported at a greater incidence in patients treated with the aprepitant regimen than with standard therapy in patients receiving Moderately Emetogenic Chemotherapy (MEC) was fatigue (1.4 % versus 0.9 %).
See prescribing information for full details.
Aprepitant (125 mg/80 mg) is a substrate, a moderate inhibitor, and an inducer of CYP3A4. Aprepitant is also an inducer of CYP2C9. During treatment with EMEND, CYP3A4 is inhibited. After the end of treatment, EMEND causes a transient mild induction of CYP2C9, CYP3A4 and glucuronidation.
Aprepitant does not seem to interact with the P-glycoprotein transporter, as suggested by the lack of interaction of aprepitant with digoxin.
See prescribing information for full details.
Pregnancy and Lactation
Pregnancy: For aprepitant no clinical data on exposed pregnancies are available. The potential for reproductive toxicity of aprepitant has not been fully characterized, since exposure levels above the therapeutic exposure in humans at the 125 mg/80 mg dose could not be attained in animal studies. These studies did not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development. The potential effects on reproduction of alterations in neurokinin regulation are unknown. This product should not be used during pregnancy unless clearly necessary.
Lactation: Aprepitant is excreted in the milk of lactating rats. It is not known whether aprepitant is excreted in human milk; therefore, breast-feeding is not recommended during treatment with EMEND.
In the event of overdose, this product should be discontinued and general supportive treatment and monitoring should be provided. Because of the antiemetic activity of aprepitant, emesis -induced by a medicinal product may not be effective. Aprepitant cannot be removed by haemodialysis.