Products
Granisetron is commercially available as film-coated tablets and as an infusion concentrate (Kytril, generic). It has been approved in many countries since 1991. A transdermal patch was approved in the EU in 2012 (Sancuso).
Structure and properties
Granisetron (C18H24N4O, Mr = 312.4 g/mol) is an indazole derivative. It is present in drugs as granisetron hydrochloride, a white powder that is soluble in water.
Effects
Granisetron (ATC A04AA02) has antiemetic properties. The effects are due to selective and potent sertotonin antagonism at the 5-HT3 receptor.
Indications
For the prevention of nausea and vomiting induced by cytostatic chemotherapy or radiotherapy. For the treatment of nausea and vomiting after surgery.
Dosage
According to the professional information leaflet.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Granisetron is biotransformed by CYP3A4 and CYP1A1. Drug-drug interactions have been described with ketoconazole and phenobarbital, among others.
Adverse effects
The most common potential adverse effects include headache. Occasionally, constipation and flu-like symptoms occurred. Hypersensitivity reactions and rare serious cardiovascular adverse reactions (eg, prolongation of the QT interval) have been reported.