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RX BIN: 015558RX PCN: HTGroup ID: DDN6600Card Holder ID: DDN6600
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2019 Price of Aloxi

$456.871 vial (5ml) 0.25mg
price without discount in nearest pharmacy. Price may vary.

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Palonosetron volume of distribution

Palonosetron has a volume of distribution of approximately 8.3 ± 2.5 L/kg. Approximately 62% of palonosetron is bound to plasma proteins. Palonosetron is eliminated by multiple routes with approximately 50% metabolized to form two primary metabolites: N-oxide-palonosetron and 6-S-hydroxy-palonosetron.

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2018 Statistics

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Discount Cards 16,000+

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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

FormRouteStrength
Capsuleoral
Capsuleoral0.5 mg
Capsule, gelatin coatedoral.5 mg/1

Prescription Generics

false

International Brands

Akynzeo

Synonyms

(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

Manufacturers

Eisai Inc.

CAS number

135729-56-5

UNII

29WVV1OJ05

State

solid

Affected organisms

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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