PALONOSETRON

Palonosetron is a 5-HT3 antagonist, an antinauseant and antiemetic agent. It is used to prevent vomiting and nausea in patients who are on chemotherapy for moderately-emetogenic cancer and for preventing postoperative nausea and vomiting. Palonosetron is specific and selective serotonin 5-HT3 receptor antagonist that is related to other 5-HT3 receptor antagonists, except for structural difference.

Palonosetron is used in intensive care medicine like pneumonia & peritonitis, some diabetes-related foot infections, and as therapy for febrile neutropenia post-chemotherapy. Prolonged infusions can maximize the duration that serum concentration is maintained at a minimum inhibitory concentration of the bacteria causing the infection. As a post-chemotherapy drug, it is given to prevent nausea and vomiting which may occur within 24 hours post-chemotherapy or surgery. It also prevents delayed nausea and vomiting that may occur several days after receiving certain chemotherapies.

Palonosetron is sold under the brand names such as Aloxi Tazocin and Zosyn among others. Helsinn Healthcare SA developed Palonosetron and was approved for this use by the U.S. Food and Drug Administration. It is the most recent 5-HT3 antagonist to enter clinical use and the only drug of its class.

Dosage Forms & Strengths:

Palonosetron is available as an injectable solution in single-use vials of 0.05mg/mL concentrations. For preventing acute Nausea and Vomiting associated with moderately or highly emetogenic chemotherapeutics and for delayed N/V agents, the dose is 0.25 mg, given through IV over 30 seconds, 30 minutes before chemotherapy begins. And for prevention of Postoperative Nausea & Vomiting, the dose is 0.075 mg, administered through an IV infused over 10 seconds immediately before anaesthesia is given.

The price of Palonosetron:

In the USA, the consumers have to pay around $72 for a supply of 2 millilitres of intravenous solution with 0.25 mg of drug in the 2 mL solution. The price for the same supply is significantly cheaper in countries like India, where it costs only USD2.

How does Palonosetron work?

Palonosetron’s actions block serotonin. Serotonin causes vomiting. Palonosetron has a strong binding affinity as 5-HT3 receptor antagonist and little or no affinity for any other receptors. Cancer chemotherapy sees a high incidence of nausea and vomiting, particularly when agents, such as cisplatin, are used.

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