Product Information
Registration Status: ActiveEMEND TRI-PACK CAPSULE is approved to be sold in Singapore with effective from 2003-07-26. It is marketed by MSD PHARMA (SINGAPORE) PTE LTD, with the registration number of SIN12371P.
This product contains Aprepitant 125mg in the form of CAPSULE. It is approved for ORAL use.
This product is manufactured by MERCK SHARP & DOHME CORP. in UNITED STATES,MERCK SHARP & DOHME (AUSTRALIA) PTY LTD (Primary and Secondary Packager) in IRELAND,Alkermes Pharma Ireland Limited in AUSTRALIA, andPT. Merck Sharp Dohme Pharma Tbk. (Primary and Secondary Packager) in INDONESIA REP OF.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Aprepitant, an antiemetic, is a substance P/neurokinin 1 (NK1) receptor antagonist which, in combination with other antiemetic agents, is indicated for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CI NV).
Indication
For the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy, including high-dose cisplatin (in combination with other antiemetic agents).
Mechanism of Action
Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with Aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that Aprepitant augments the antiemetic activity of the 5-HT3-receptor antagonist ondansetron and the corticosteroid ethasone and inhibits both the acute and delayed phases of cisplatin induced emesis.
Pharmacokinetics
- Absorption
- The mean absolute oral bioavailability of aprepitant is approximately 60 to 65%.
- Distribution
- * 70 L
- Metabolism
- Aprepitant is metabolized primarily by CYP3A4 with minor metabolism by CYP1A2 and CYP2C19. Seven metabolites of aprepitant, which are only weakly active, have been identified in human plasma.
- Elimination
Clearance
* Apparent plasma cl=62-90 mL/min
Active Ingredient/Synonyms
3-(((2R,3S)-3-(P-Fluorophenyl)-2-(((alphar)-alpha-methyl-3,5-bis(trifluoromethyl)benzyl)oxy)morpholino)methyl)-delta(2)-1,2,4-triazolin-5-one | Aprepitant | Aprépitant | Aprepitantum | Aprepitant |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.