Detail

Palonosetron

Description

Name: Palonosetron
Type: small molecule
Groups: Array
Indication: 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.
Accession Number: DB00377 ( APRD00351)
Description: 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]
Structure:
Prescription Products:
NameDosageStrengthRouteMarketing StartMarketing EndCountry
AkynzeocapsuleArrayoral13-10-2014US
Aloxiinjection.25 mg/5mLintravenous28-05-2014US
Aloxiinjection.075 mg/1.5mLintravenous28-05-2014US
Aloxicapsule, gelatin coated.5 mg/1oral22-08-2008US
Aloxisolution0.25 mgintravenous19-07-2012Canada
Aloxicapsule0.5 mgoral07-08-2012Canada

Generic Prescription Products: Not Available
Over the Counter Products: Not Available
International Brands
  • No Brands

Brand Names
  • No Brands

Brand Mixtures
Brand NameIngredients
AkynzeoNetupitant + Palonosetron
AloxiPalonosetron
AloxiPalonosetron
AloxiPalonosetron
AloxiPalonosetron
AloxiPalonosetron

Categories
  • No Category

Pharmacology

Indication: 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.
Pharmacodynamics: Not Available
Mechanism of action: Palonosetron is a selective serotonin 5-HT3 receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 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-HT3 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.
Absorption: Low oral bioavailability.
Volume of distribution:
  • 8.3 ± 2.5 L/kg

Protein binding: 62%
Metabolism: Not Available
Route of elimination: After a single intravenous dose of 10 mcg/kg [14C]-palonosetron, approximately 80% of the dose was recovered within 144 hours in the urine
Half life: Approximately 40 hours
Clearance: Not Available
Toxicity: 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.
Affected organisms
  • Not Available

SNP Mediated Adverse Drug Reactions
  • Not Available

Pharmacoeconomics

Manufacturers:
  • Helsinn healthcare sa

Packagers:
Dosage forms
FormRouteStrength
Capsuleoral
Capsuleoral0.5 mg
Capsule, gelatin coatedoral.5 mg/1
Injectionintravenous.075 mg/1.5mL
Injectionintravenous.25 mg/5mL
Solutionintravenous0.25 mg

Prices
Unit descriptionCostUnit
Aloxi 0.075 mg/1.5 ml vial$52.8ml

Patents
CountryPatent NumberApprovedExpires (estimated)
5202333United States1995-04-132015-04-13

Interactions

Drug Interactions
DrugInteraction
ApomorphinePalonosetron may increase the hypotensive activities of Apomorphine.
BexaroteneThe serum concentration of Palonosetron can be decreased when it is combined with Bexarotene.
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Palonosetron.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Palonosetron.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Palonosetron.
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Palonosetron.
FluvoxaminePalonosetron may increase the serotonergic activities of Fluvoxamine.
PhenytoinThe serum concentration of Palonosetron can be decreased when it is combined with Phenytoin.
St. John's WortThe serum concentration of Palonosetron can be decreased when it is combined with St. John's Wort.
TapentadolPalonosetron may decrease the analgesic activities of Tapentadol.
TramadolPalonosetron may decrease the analgesic activities of Tramadol.

Food Interactions:
  • Not Available

Taxonomy

Kingdom: Organic compounds
Super Class: Not Available
Class: Not Available
Sub Class: Not Available
Direct Parent: Not Available
Alternative Parents:
  • Aminopiperidines
  • Azacyclic compounds
  • Carbonyl compounds
  • Carboxylic acid amides
  • Hydrocarbon derivatives
  • Lactams
  • Quinuclidines
  • Tetrahydroisoquinolines
  • Tetralins
  • Trialkylamines

substituent:
  • 3-aminopiperidine
  • Amine
  • Aromatic heteropolycyclic compound
  • Azacycle
  • Benzenoid
  • Carbonyl group
  • Carboxamide group
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Isoquinolone
  • Lactam
  • Organonitrogen compound
  • Organooxygen compound
  • Piperidine
  • Quinuclidine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Tetrahydroisoquinoline
  • Tetralin

References

Synthesis Reference: Pierluigi Rossetto, Peter MacDonald, Ettore Bigatti, Gaia Banfi, Dario Tentorio, "Processes for preparing palonosetron salts." U.S. Patent US20080200681, issued August 21, 2008.
General Reference: # De Leon A: Palonosetron (Aloxi): a second-generation 5-HT(3) receptor antagonist for chemotherapy-induced nausea and vomiting. Proc (Bayl Univ Med Cent). 2006 Oct;19(4):413-6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17106506 # Stoltz R, Cyong JC, Shah A, Parisi S: Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjects. J Clin Pharmacol. 2004 May;44(5):520-31. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15102873 # Rubenstein EB: Palonosetron: a unique 5-HT3 receptor antagonist indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting. Clin Adv Hematol Oncol. 2004 May;2(5):284-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16163194 # Yang LP, Scott LJ: Palonosetron: in the prevention of nausea and vomiting. Drugs. 2009 Nov 12;69(16):2257-78. doi: 10.2165/11200980-000000000-00000. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19852528 # Siddiqui MA, Scott LJ: Palonosetron. Drugs. 2004;64(10):1125-32; discussion 1133-4. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15139789 # Eisenberg P, MacKintosh FR, Ritch P, Cornett PA, Macciocchi A: Efficacy, safety and pharmacokinetics of palonosetron in patients receiving highly emetogenic cisplatin-based chemotherapy: a dose-ranging clinical study. Ann Oncol. 2004 Feb;15(2):330-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/14760130 # Stoltz R, Parisi S, Shah A, Macciocchi A: Pharmacokinetics, metabolism and excretion of intravenous [l4C]-palonosetron in healthy human volunteers. Biopharm Drug Dispos. 2004 Nov;25(8):329-37. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15378559
External Links:
ResourceLink
RxListhttp://www.rxlist.com/cgi/generic/aloxi.htm
Drugs.comhttp://www.drugs.com/cdi/palonosetron.html

ATC Codes:
  • Array

AHFS Codes:
  • Not Available

MSDS: Download
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