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Beacon Pharmaceuticals LtdProduct Description
Palonosetron is a highly potent, second-generation 5-HT3 receptor antagonist primarily utilized for the prevention of chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV). It distinguishes itself from first-generation antagonists, such as ondansetron, through its significantly higher binding affinity for the 5-HT3 receptor and a remarkably prolonged plasma half-life of approximately 40 hours. Its unique mechanism involves allosteric binding and receptor internalization, which provides sustained inhibition of the emetic reflex by blocking serotonin receptors on the terminals of the vagus nerve in the periphery and within the chemoreceptor trigger zone in the central nervous system. Palonosetron is particularly effective in managing both acute and delayed emesis, a feat many earlier agents fail to achieve consistently. Clinically, it is administered as a single intravenous or oral dose prior to the start of emetogenic chemotherapy. While generally well-tolerated, common adverse effects include headache, constipation, and occasionally diarrhea. Unlike some other medications in its class, palonosetron has a lower propensity for causing clinically significant QT interval prolongation, though it should still be monitored in patients with pre-existing cardiac conditions. It is metabolized primarily by the hepatic enzyme CYP2D6, with its metabolites and the unchanged drug being excreted via the renal system.
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