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2018 Price of Palonosetron
Aloxi 0.075 mg/1.5 ml vial
* price without discount in nearest pharmacy. Price may vary.
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Palonosetron volume of distribution
* 8.3 2.5 L/kg
Discount Cards 16,000+
Clients Benefit 29%
Total savings $4,735,080
What is Palonosetron
Palonosetron (INN, trade name Aloxi) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (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. As of 2008, it is the most recent 5-HT3 antagonist to enter clinical use. (wikipedia)
Palonosetron mechanism of action
Palonosetron is a selective serotonin 5-HT sub 3 /sub receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT sub 3 /sub receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT sub 3 /sub receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone. Alternative mechanisms appear to be primarily responsible for delayed nausea and vomiting induced by emetogenic chemotherapy, since similar temporal relationships between between serotonin and emesis beyond the first day after a dose have not been established, and 5-HT sub 3 /sub receptor antagonists generally have not appeared to be effective alone in preventing or ameliorating delayed effects. It has been hypothesized that palonosetron’s potency and long plasma half-life may contribute to its observed efficacy in preventing delayed nausea and vomiting caused by moderately emetogenic cancer chemotherapy.
Dosage forms of Palonosetron
|Capsule, gelatin coated||oral||.5 mg/1|
(3aS)-2-((3S)-1-azabicyclo(2.2.2)oct-3-yl)-2,3,3a, 4,5,6-hexahydro-1H-benz(de)isoquinolin-1-one (3aS)-2,3,3a,4,5,6-hexahydro-2-((3S)-3-quinuclidinyl)-1H-benz(de)isoquinolin-1-one
Humans and other mammals
Indication of Palonosetron
For the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy, as well as prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy. Also used for the prevention of postoperative nausea and vomiting for up to 24 hours post operation.
Toxicity of Palonosetron
A single intravenous dose of palonosetron at 30 mg/kg (947 and 474 times the human dose for rats and mice, respectively, based on body surface area) was lethal to rats and mice. The major signs of toxicity were convulsions, gasping, pallor, cyanosis and collapse.
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