Palonosetron

Palonosetron
	File:Palonosetron structure.svg
Clinical data
AHFS/Drugs.com	Monograph
MedlinePlus	a610002
[[Regulation of therapeutic goods \|Template:Engvar data]]	US FDA: Palonosetron;
Pregnancy; category	AU: B1 ; US: B (No risk in non-human studies) ; ;
Routes of; administration	Intravenous, oral
ATC code	A04AA05 (WHO) ;
Legal status
Legal status	US: ℞-only ;
Pharmacokinetic data
Bioavailability	97% (oral)
Protein binding	62%
Metabolism	Hepatic, 50% (mostly CYP2D6-mediated, CYP3A4 and CYP1A2 also involved)
Elimination half-life	Approximately 40 hours
Excretion	Renal, 80% (of which 49% unchanged); fecal (5 to 8%)
Identifiers
	IUPAC name (3aS)-2-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one;
CAS Number	135729-61-2 ;
PubChem CID	148211;
DrugBank	DB00377 ;
ChemSpider	4892289 ;
UNII	5D06587D6R;
ChEBI	CHEBI:85161 ;
ChEMBL	ChEMBL1189679 ;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C19H24N2O
Molar mass	296.407 g/mol
3D model (JSmol)	Interactive image;
	SMILES O=C5N([C@H]2C1CCN(CC1)C2)C[C@@H]4c3c5cccc3CCC4;
	InChI InChI=1S/C19H24N2O/c22-19-16-6-2-4-14-3-1-5-15(18(14)16)11-21(19)17-12-20-9-7-13(17)8-10-20/h2,4,6,13,15,17H,1,3,5,7-12H2/t15-,17-/m1/s1 ; Key:CPZBLNMUGSZIPR-NVXWUHKLSA-N ;
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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 used for the control of delayed CINV—nausea and vomiting and there are tentative data to suggest that it may be better than granisetron.^[1]

Palonosetron is administered intravenously, as a single dose, 30 minutes before chemotherapy,^[2] or as a single oral capsule one hour before chemotherapy.^[3] 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.^[3]

References

↑ Billio, A; Morello, E; Clarke, MJ (Jan 20, 2010). "Serotonin receptor antagonists for highly emetogenic chemotherapy in adults". The Cochrane database of systematic reviews (1): CD006272. doi:10.1002/14651858.CD006272.pub2. PMID 20091591.
↑ De Leon A (2006). "Palonosetron (Aloxi): a second-generation 5-HT(3) receptor antagonist for chemotherapy-induced nausea and vomiting". Proceedings (Baylor University. Medical Center). 19 (4): 413–6. PMC 1618755. PMID 17106506.
↑ ^3.0 ^3.1 Waknine, Yael (September 4, 2008). "FDA Approvals: Nplate, Aloxi, Vidaza". Medscape. Retrieved 2008-09-04. Freely available with registration.

Template:5-HT3 antagonists

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[1] Billio, A; Morello, E; Clarke, MJ (Jan 20, 2010). "Serotonin receptor antagonists for highly emetogenic chemotherapy in adults". The Cochrane database of systematic reviews (1): CD006272. doi:10.1002/14651858.CD006272.pub2. PMID 20091591.

[pmid17106506-2] De Leon A (2006). "Palonosetron (Aloxi): a second-generation 5-HT(3) receptor antagonist for chemotherapy-induced nausea and vomiting". Proceedings (Baylor University. Medical Center). 19 (4): 413–6. PMC 1618755. PMID 17106506.

[Medscape-3] 3.0 ^3.1 Waknine, Yael (September 4, 2008). "FDA Approvals: Nplate, Aloxi, Vidaza". Medscape. Retrieved 2008-09-04. Freely available with registration.

[1]

[2]

[3]

Palonosetron

See also

References

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