Active Substance: aprepitant
Common Name: aprepitant
ATC Code: A04AD12
Marketing Authorisation Holder: Merck Sharp & Dohme Ltd.
Active Substance: aprepitant
Authorisation Date: 2003-11-11
Therapeutic Area: Postoperative Nausea and Vomiting Vomiting Cancer
Pharmacotherapeutic Group: Anti-emetics and antinauseants
Emend 40 mg is indicated for the prevention of postoperative nausea and vomiting (PONV) in adults.
Emend 80 mg, 125 mg and 165 mg are indicated for prevention of acute and delayed nausea and vomiting associated with highly emetogenic cisplatin based cancer chemotherapy in adults and prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy in adults.
Emend 80 mg, 125 mg and 165 mg are given as part of combination therapy.
What is Emend?
Emend is a medicine containing the active substance aprepitant. It is available as capsules (40, 80, 125 and 165 mg).
What is Emend used for?
Emend is an anti-emetic (a medicine that prevents nausea [feeling sick] and vomiting).
Emend 80-, 125- and 165-mg capsules are used with other medicines to prevent nausea and vomiting caused by chemotherapy (medicines used to treat cancer) in adults. Emend works with chemotherapy containing cisplatin (a strong trigger of nausea and vomiting) and with chemotherapy that is a moderate trigger of nausea and vomiting (such as cyclophosphamide, doxorubicin or epirubicin). Emend makes chemotherapy more tolerable for the patient.
Emend 40-mg capsules are used to prevent postoperative nausea and vomiting (PONV) in adults. This is nausea and vomiting that a patient can experience after surgery.
The medicine can only be obtained with a prescription.
How is Emend used?
In chemotherapy, the usual dose of Emend is one 125-mg capsule by mouth one hour before the start of chemotherapy. After chemotherapy, one 80-mg capsule is taken each day for the next two days. It must be given with other medicines that also prevent nausea and vomiting, including a corticosteroid (such as dexamethasone) and a ‘5HT3 antagonist’ (such as ondansetron).
Emend 165 mg is given only once one hour before the start of chemotherapy. It is only given on the first day of the chemotherapy and is followed by treatment involving a corticosteroid and a 5-HT3 antagonist.
In PONV, the usual dose is one 40-mg capsule given within the three hours before the patient is anaesthetised (‘put to sleep’).
Emend capsules should be swallowed whole, with or without food.
How does Emend work?
Emend is a neurokinin-1 (NK1)-receptor antagonist. It stops a chemical in the body (substance P) from binding to the NK1 receptors. When substance P attaches to these receptors, it causes nausea and vomiting. By blocking the receptors, Emend can prevent nausea and vomiting, which often happens after chemotherapy or as a complication of surgery.
How has Emend been studied?
In chemotherapy, three main studies have been carried out for Emend 80 and 125 mg. The first two studies involved a total of 1,094 adults receiving chemotherapy including cisplatin, and the third involved 866 patients with breast cancer who were receiving cyclophosphamide, with or without doxorubicin or epirubicin. All three studies compared the effectiveness of Emend, taken in combination with dexamethasone and ondansetron, with that of the standard combination of dexamethasone and ondansetron. The main measure of effectiveness was the number of patients who had nausea and vomiting in the five days after receiving chemotherapy.
Emend 165 mg was compared with the authorised intravenous medicine Ivemend 150 mg. Ivemend contains a substance called fosaprepitant which is converted in the body into aprepitant. Tests were performed to determine that Emend 165 mg produces the same amount of aprepitant in the body as a single dose of 150 mg Ivemend.
In PONV, two studies were carried out in a total of 1,727 patients, most of whom were women undergoing gynaecological operations. Two doses of Emend (40 and 125 mg) were compared with ondansetron given as an injection. The studies measured how many patients had a ‘complete response’, which was defined as no vomiting and no need for any other medication to control nausea and vomiting in the 24 hours after the operation.
What benefit has Emend shown during the studies?
In the chemotherapy studies, adding Emend to the standard combination was more effective than the standard combination alone. Looking at the results of the two cisplatin studies taken together, 68% of the patients taking Emend had no nausea or vomiting over five days (352 out of 520), compared with 48% of the patients who did not take it (250 out of 523). The effectiveness of Emend was also seen during a further five cycles of chemotherapy. In the study of chemotherapy that is a moderate trigger of nausea and vomiting, 51% of the patients taking Emend had no nausea or vomiting (220 out of 433), compared with 43% of the patients who did not take it (180 out of 424).
Emend 165 mg was shown to be bioequivalent to Ivemend 150 mg, which means that like Ivemend it can also be used to prevent nausea and vomiting caused by chemotherapy.
In PONV, Emend was as effective as ondansetron. Looking at the results of both studies together, 55% of the patients taking Emend at a dose of 40 mg were ‘complete responders’ (298 out of 541), compared with 49% of the patients who received ondansetron (258 out of 526).
What is the risk associated with Emend?
The most common side effect of Emend at all doses (seen in between 1 and 10 patients in 100) is increased liver enzymes. At doses of 80, 125 and 165 mg, the other side effects seen in between 1 and 10 patients in 100 are headache, dizziness, hiccups, constipation, diarrhoea, dyspepsia (indigestion), eructation (burping), anorexia (loss of appetite), and asthenia (weakness) or fatigue (tiredness). For the full list of all side effects reported with Emend, see the package leaflet.
Emend should not be used in people who may be hypersensitive (allergic) to aprepitant or any of the other ingredients. Emend 80 mg and 125 mg must not be taken with the following medicines:
- pimozide (used to treat mental illness);
- terfenadine, astemizole (commonly used to treat allergy symptoms - these medicines may be available without a prescription):
- cisapride (used to relieve certain stomach problems).
Emend should be used with caution when taking with some other medicines. Oral contraceptives may become less effective in patients taking Emend. For more information, see the summary of product characteristics (also part of the EPAR).
Why has Emend been approved?
The CHMP decided that Emend’s benefits are greater than its risks and recommended that it be given marketing authorisation.
Other information about Emend:
The European Commission granted a marketing authorisation valid throughout the European Union for Emend on 11 November 2003.
For more information about treatment with Emend, read the package leaflet (also part of the EPAR) or contact your doctor or pharmacist.
Source: European Medicines Agency
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