Paloxiron is indicated for:
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Palonosetron is a 5-HT3 receptor antagonist with a high affinity for the receptor. Chemotherapy triggers the release of serotonin from enterochromaffin cells in the small intestine, activating 5-HT3 receptors in the vagus nerve and the brain's chemoreceptor trigger zone, which leads to nausea and vomiting. Palonosetron blocks serotonin at 5-HT3 receptors, preventing this emetic response. It acts both in the small intestine and the brain.
Palonosetron demonstrates linear pharmacokinetics over 1-90 mcg/kg. After IV administration, 40% is excreted unchanged in urine within 144 hours. It has a volume of distribution of 6.9–7.9 L/kg, with about 62% plasma protein binding. Approximately 50% is metabolized into inactive metabolites via renal pathways and CYP enzymes (CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2D6, CYP2E1, and CYP3A4/5). Its half-life is approximately 40 hours, indicating prolonged receptor binding.
Use medication under the guidance of a registered physician.
Paloxiron is generally safe with corticosteroids, analgesics, antiemetics, antispasmodics, and metoclopramide, with no significant pharmacokinetic interactions. It does not inhibit or induce CYP enzymes, minimizing drug interaction risks. No effect on cisplatin, cyclophosphamide, cytarabine, doxorubicin, or mitomycin C efficacy in tumor models.
Palonosetron is contraindicated in patients with hypersensitivity to the drug or its components.
Store in a cool, dry place, protected from light.
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