Palonosetron
Encyclopedia
Palonosetron is a 5-HT3 antagonist
5-HT3 antagonist
The 5-HT3 antagonists are a class of medications that act as receptor antagonists at the 5-HT3 receptor, a subtype of serotonin receptor found in terminals of the vagus nerve and in certain areas of the brain....

 used in the prevention and treatment of chemotherapy
Chemotherapy
Chemotherapy is the treatment of cancer with an antineoplastic drug or with a combination of such drugs into a standardized treatment regimen....

-induced nausea
Nausea
Nausea , is a sensation of unease and discomfort in the upper stomach with an involuntary urge to vomit. It often, but not always, precedes vomiting...

 and vomiting
Vomiting
Vomiting is the forceful expulsion of the contents of one's stomach through the mouth and sometimes the nose...

 (CINV). It is the most effective of the 5-HT3 antagonists in controlling delayed CINV—nausea and vomiting that appear more than 24 hours after the first dose of a course of chemotherapy—and is the only drug of its class approved for this use by the U.S. Food and Drug Administration
Food and Drug Administration
The Food and Drug Administration is an agency of the United States Department of Health and Human Services, one of the United States federal executive departments...

. , it is the most recent 5-HT3 antagonist to enter clinical use.

Palonosetron is administered intravenously
Intravenous therapy
Intravenous therapy or IV therapy is the infusion of liquid substances directly into a vein. The word intravenous simply means "within a vein". Therapies administered intravenously are often called specialty pharmaceuticals...

, as a single dose, 30 minutes before chemotherapy, or as a single oral capsule one hour before chemotherapy. The oral formulation was approved on August 22, 2008 for prevention of acute CINV alone, as a large clinical trial did not show oral administration to be as effective as intravenous use against delayed CINV.

See also

  • 5-HT3 receptor antagonist: Drug discovery and development
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