Source: Health Products Regulatory Authority (ZA) Revision Year: 2022 Publisher: Acino Pharma (Pty) Ltd, 106 16th Road, Midrand, 1686
A 5.7.2 Anti-emetics and anti-vertigo preparations
ATC code: A04AA02
Granisetron is a selective 5-HT3 receptor-antagonist with anti-emetic properties. Chemotherapeutic agents and radiotherapy may cause release of 5-HT in the small intestine initiating a vomiting reflex by activating vagal afferents via 5-HT3 receptors. The initiation of this reflex is blocked by granisetron. Activation of vagal afferents may also cause a release of 5-HT in the area postrema, located on the floor of the fourth ventricle, and this may also promote emesis through a central mechanism.
Granisetron has an apparent volume of distribution of about 3 litres/kg. Plasma protein binding is approximately 65%.
The pharmacokinetics of granisetron exhibit considerable inter-individual variation. The elimination half-life after an intravenous dose is reported to be around 4 to 5 hours in healthy subjects but about 9 to 12 hours in cancer patients. It is metabolised in the liver, primarily by N-demethylation, with less than 20% of a dose recovered unchanged in urine, the remainder being excreted in faeces and urine as metabolites. Granisetron clearance is not affected by renal impairment, but is lower in the elderly and in patients with hepatic impairment.
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