Za Pharmacy
Drugs, Supplies and Delivery
Palonosetron
Palonosetron is a second-generation selective serotonin 5-HT3 receptor antagonist used to prevent and treat nausea and vomiting caused by chemotherapy and surgery. It is particularly effective in managing acute and delayed chemotherapy-induced nausea and vomiting (CINV) due to its long half-life and high receptor-binding affinity. This article synthesizes information from the British National Formulary (BNF), Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology to provide a detailed overview of palonosetron, including its mechanism, uses, dosing, side effects, precautions, and drug interactions.
Palonosetron works by selectively blocking 5-HT3 receptors in the chemoreceptor trigger zone (CTZ) and the gastrointestinal (GI) tract. By inhibiting these receptors, palonosetron:
- Prevents the stimulation of the vomiting center in the brain, reducing nausea and vomiting.
- Blocks serotonin release from enterochromaffin cells in the GI tract, which is often triggered by chemotherapy or radiation (Lippincott, Lange).
Palonosetron has a long half-life (40 hours) and a high affinity for 5-HT3 receptors, making it effective for both acute and delayed CINV (BNF).
