Product Information
Registration Status: ActiveKYTRIL TABLET 1mg is approved to be sold in Singapore with effective from 1994-07-21. It is marketed by DKSH SINGAPORE PTE LTD, with the registration number of SIN07800P.
This product contains Granisetron 1.12mg (eqv 1mg) in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Roche S.p.A. in ITALY.
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
A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic and antinauseant for cancer chemotherapy patients. [PubChem]
Indication
For the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy (including high dose cisplatin), postoperation, and radiation (including total body irradiation and daily fractionated abdominal radiation).
Mechanism of Action
Granisetron is a potent, selective antagonist of 5-HT3 receptors. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.
Pharmacokinetics
- Absorption
- Absorption of is rapid and complete, though oral bioavailability is reduced to about 60% as a result of first pass metabolism.
- Distribution
- Metabolism
- Primarily hepatic; undergoes N -demethylation and aromatic ring oxidation followed by conjugation. Animal studies suggest that some of the metabolites may have 5-HT 3 receptor antagonist activity.
- Elimination
Clearance
* 0.52 L/h/kg [Cancer Patients with 1 mg bid for 7 days] * 0.41 L/h/kg [Healthy subject with a single 1 mg dose]
Toxicity
LD50>2000 mg/kg (rat, oral)
Active Ingredient/Synonyms
granisétron | granisetrón | granisetronum | Granisetron |
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.