Palonosetron: Difference between revisions

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Palonosetron
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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VisualWikitext

Latest revision as of 13:54, 9 April 2015

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

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

Template:Gastrointestinal-drug-stub

[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]

@@ Line 1: / Line 1: @@
-{{drugbox
+{{Drugbox
-|IUPAC_name=(3''aR'')-2-[(3''S'')-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3''a'',<br>4,5,6-hexahydro-1''H''-benz[''de'']isoquinolin-1-one
+| Verifiedfields = changed
-|image=Palonosetron.svg
+| Watchedfields = changed
-|image2 = Palenosetron_3D.png
+| verifiedrevid = 464197120
-|CAS_number=119904-90-4
+| IUPAC_name = (3''aS'')-2-[(3''S'')-1-Azabicyclo[2.2.2]oct-3-yl]-2,3,3''a'',4,5,6-hexahydro-1''H''-benz[''de'']isoquinolin-1-one
-|ATC_prefix=A04
+| image = Palonosetron Wiki Str.png
-|ATC_suffix=AA05
+| width = 200
-|ATC_supplemental=
-|PubChem=148211
+<!--Clinical data-->
-|DrugBank=APRD00351
+| tradename =
-|C=19|H=24|N=2|O=1
+| Drugs.com = {{drugs.com|monograph|palonosetron-hydrochloride}}
-|molecular_weight=296.407 g/mol
+| MedlinePlus = a610002
-|bioavailability=Low (oral)
+| licence_US = Palonosetron
-|protein_bound=62%
+| pregnancy_AU = B1
-|metabolism=[[Liver|Hepatic]], 50% (mostly [[CYP2D6]]-mediated, [[CYP3A4]] and [[CYP1A2]] also involved)
+| pregnancy_US = B
-|elimination_half-life=Approximately 40 hours
+| legal_AU = <!-- Unscheduled / S2 / S4 / S8 -->
-|excretion=[[Kidney|Renal]], 80% (of which 49% unchanged)
+| legal_UK = <!-- GSL / P / POM / CD -->
-|pregnancy_AU=B1
+| legal_US = Rx-only
-|pregnancy_US=B
+| routes_of_administration = [[Intravenous therapy|Intravenous]], oral
-|pregnancy_category=
-|legal_AU=<!-- Unscheduled / S2 / S4 / S8 -->
+<!--Pharmacokinetic data-->
-|legal_UK=<!-- GSL / P / POM / CD -->
+| bioavailability = 97% (oral)
-|legal_US=Rx-only
+| protein_bound = 62%
-|legal_status=
+| metabolism = [[Liver|Hepatic]], 50% (mostly [[CYP2D6]]-mediated, [[CYP3A4]] and [[CYP1A2]] also involved)
-|routes_of_administration=[[Intravenous therapy|Intravenous]]
+| elimination_half-life = Approximately 40 hours
+| excretion = [[Kidney|Renal]], 80% (of which 49% unchanged); fecal (5 to 8%)
+<!--Identifiers-->
+| CAS_number_Ref = {{cascite|changed|??}}
+| CAS_number = 135729-61-2
+| ATC_prefix = A04
+| ATC_suffix = AA05
+| PubChem = 148211
+| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
+ | DrugBank = DB00377
+| ChEBI_Ref = {{ebicite|correct|EBI}}
+| ChEBI = 85161
+| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
+| ChemSpiderID = 4892289
+| UNII_Ref = {{fdacite|correct|FDA}}
+| UNII = 5D06587D6R
+| ChEMBL_Ref = {{ebicite|changed|EBI}}
+| ChEMBL = 1189679
+<!--Chemical data-->
+| C=19 | H=24 | N=2 | O=1
+| molecular_weight = 296.407 g/mol
+| smiles = O=C5N([C@H]2C1CCN(CC1)C2)C[C@@H]4c3c5cccc3CCC4
+| InChI = 1/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
+| InChIKey = CPZBLNMUGSZIPR-NVXWUHKLBP
+| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
+| StdInChI = 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
+| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
+| StdInChIKey = CPZBLNMUGSZIPR-NVXWUHKLSA-N
 }}
-'''Palonosetron''' ([[International Nonproprietary Name|INN]], trade name '''Aloxi''') is a [[5-HT3 antagonist|5-HT<sub>3</sub> antagonist]] used in the prevention and treatment of [[chemotherapy]]-induced [[nausea]] and [[vomiting]] (CINV). It is the most effective of the 5-HT<sub>3</sub> 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]].<ref name="pmid17106506">{{cite journal |author=De Leon A |title=Palonosetron (Aloxi): a second-generation 5-HT(3) receptor antagonist for chemotherapy-induced nausea and vomiting |journal=Proceedings (Baylor University. Medical Center) |volume=19 |issue=4 |pages=413–6 |year=2006 |pmid=17106506 |doi=}} {{PMC|1618755}}.</ref> [[As of 2007]], it is the most recent 5-HT<sub>3</sub> antagonist to enter clinical use.
+__NOTOC__
+{{SI}}
+{{CMG}}
+== Overview ==
+'''Palonosetron''' ([[International Nonproprietary Name|INN]], trade name '''Aloxi''') is a [[5-HT3 antagonist|5-HT<sub>3</sub> 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]].<ref>{{cite journal|last=Billio|first=A|author2=Morello, E |author3=Clarke, MJ |title=Serotonin receptor antagonists for highly emetogenic chemotherapy in adults.|journal=The Cochrane database of systematic reviews|date=Jan 20, 2010|issue=1|pages=CD006272|pmid=20091591|doi=10.1002/14651858.CD006272.pub2}}</ref>
-Palonosetron is administered [[intravenous therapy|intravenously]], as a single dose, 30 minutes before chemotherapy.<ref name="pmid17106506"/> An oral formulation is in [[Clinical trial#Phase III|Phase III]] [[clinical trial]]s.<ref>{{cite web | url = http://www.mgipharma.com/wt/page/oral_aloxi | title = Aloxi<sup>&reg;</sup> Oral Capsule | year = 2007 | accessdate = 2007-05-16 | publisher = MGI Pharma}}</ref>
+Palonosetron is administered [[intravenous therapy|intravenously]], as a single dose, 30 minutes before chemotherapy,<ref name="pmid17106506">{{cite journal |author=De Leon A |title=Palonosetron (Aloxi): a second-generation 5-HT(3) receptor antagonist for chemotherapy-induced nausea and vomiting |journal=Proceedings (Baylor University. Medical Center) |volume=19 |issue=4 |pages=413–6 |year=2006 |pmid=17106506 |doi= |pmc=1618755}}</ref> or as a single oral capsule one hour before chemotherapy.<ref name=Medscape>{{cite web |url=http://www.medscape.com/viewarticle/580032 |title=FDA Approvals: Nplate, Aloxi, Vidaza |author=Waknine, Yael |date=September 4, 2008 |accessdate=2008-09-04 |publisher=[[Medscape]]}} Freely available with registration.</ref> 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.<ref name=Medscape/>
+==See also==
+* [[5-HT3 receptor antagonist:drug discovery and development|5-HT<sub>3</sub> receptor antagonist: Drug discovery and development]]
 ==References==
-{{Reflist}}
+{{Reflist|2}}
 {{5-HT3 antagonists}}
+{{Serotonergics}}
-{{pharma-stub}}
+[[Category:Drug]]
+[[Category:5-HT3 antagonists]]
+[[Category:Quinuclidines]]
+[[Category:Isoquinolines]]
+[[Category:Lactams]]
-[[de:Palonosetron]]
-{{WikiDoc Help Menu}}
-{{WikiDoc Sources}}
-[[Category:5-HT3 antagonists]]
+{{gastrointestinal-drug-stub}}
-[[Category:Drugs]]

Palonosetron: Difference between revisions

Latest revision as of 13:54, 9 April 2015

Overview

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