$368.00
Manufacturer: Bulgaria
As part of combination therapy: prevention of acute and delayed nausea and vomiting associated with anti-cancer chemotherapy based on cisplatin with a high emetogenic risk in adults, prevention of nausea and vomiting associated with the use of anti-cancer chemotherapy with a moderate emetogenic risk in adults.
Description
Emend Storage:
active substance: aprepitant;
1 capsule contains 80 mg or 125 mg of aprepitant;
Emend excipients: sucrose, microcrystalline cellulose, hydroxypropylcellulose, sodium lauryl sulfate.
The capsule shell – gelatin, titanium dioxide (E 171).
The 125 mg capsule shell also contains red iron oxide (E 172) and yellow iron oxide (E 172).
Emend Dosage form.
Capsules.
Basic physical and chemical properties:
80 mg capsules: white opaque hard gelatin capsule with “461” and “80 mg”, printed radially in black ink;
125 mg capsules: an opaque hard gelatin capsule with a white body and a pink cap with “462” and “125 mg” printed in radially black ink.
Pharmacotherapeutic group.
Antibiotics and drugs that eliminate nausea.
ATX code A04A D12.
Pharmacological properties.
Pharmacodynamics.
Aprepitant is a selective antagonist of neurokinin 1 (NK1) receptors with a high degree of affinity for substance P (P-neuropeptide of the tachykinin family). Additional screening studies have shown that aprepitant was at least 3,000-fold more selective for NK1 receptors for other enzymes, transporters, ion channels, and receptor localization, including dopamine and serotonin receptors, which are targeted for chemotherapy-induced nausea and vomiting.
NK1 receptor antagonists inhibit the gag reflex caused by cytotoxic chemotherapeutic drugs such as cisplatin due to their effects on the central nervous system. Preclinical and positron emission tomography (PET) studies of aprepitant have shown that it enters the brain and binds to NK1 receptors in the brain. The effect of aprepitant on the central nervous system is quite long, it suppresses the acute and delayed phase of the gag reflex caused by cisplatin, and increases the antiemetic activity of the 5HT3-receptor antagonist ondansetron and the corticosteroid dexamethasone.
Clinical characteristics.
Indication.
As part of combination therapy:
prevention of acute and delayed nausea and vomiting associated with cisplatin-based anticancer chemotherapy in adults;
prevention of nausea and vomiting associated with the use of anticancer chemotherapy with moderate emetogenic risk in adults.
Contraindication.
Emend® is contraindicated in patients with hypersensitivity to any component of the drug.
Emend® should not be used concomitantly with pimozide, terfenadine, astemizole and cisapride.
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