ONDANSETRON

Details

Stereochemistry	RACEMIC
Molecular Formula	C18H19N3O
Molecular Weight	293.363
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN1C2=C(C3=C1C=CC=C3)C(=O)C(CN4C=CN=C4C)CC2

InChI

InChIKey=FELGMEQIXOGIFQ-UHFFFAOYSA-N

InChI=1S/C18H19N3O/c1-12-19-9-10-21(12)11-13-7-8-16-17(18(13)22)14-5-3-4-6-15(14)20(16)2/h3-6,9-10,13H,7-8,11H2,1-2H3

HIDE SMILES / InChI

Molecular Formula	C18H19N3O
Molecular Weight	293.363
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2005/020103s008s025,020605s008lbl.pdf
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/mesh/68017294 | https://www.ncbi.nlm.nih.gov/pubmed/11474424

Ondansetron (ZOFRAN®) is a selective 5-HT3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by radiotherapy, anesthesia, surgery or cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties. While its mechanism of action has not been fully characterized, ondansetron is not a dopamine-receptor antagonist. It is not certain whether ondansetron's antiemetic action is mediated centrally, peripherally, or in both sites. However, cytotoxic chemotherapy appears to be associated with release of serotonin from the enterochromaffin cells of the small intestine. The released serotonin may stimulate the vagal afferents through the 5-HT3 receptors and initiate the vomiting reflex.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Serotonin 3a (5-HT3a) receptor 48 Target ID: CHEMBL1899 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2005/020103s008s025,020605s008lbl.pdf	Antagonist 2849		8.31 null [pKi]

Conditions

Condition	Modality	Highest Phase	Product
Postoperative nausea and vomiting 31 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2005/020103s008s025,020605s008lbl.pdf	Preventing	Approved 8583	ZOFRAN Approved Use Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy, including cisplatin ≥50 mg/m2. Prevention of nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy. Prevention of nausea and vomiting associated with radiotherapy in patients receiving either total body irradiation, single high-dose fraction to the abdomen, or daily fractions to the abdomen. Prevention of postoperative nausea and/or vomiting. As with other antiemetics, routine prophylaxis is not recommended for patients in whom there is little expectation that nausea and/or vomiting will occur postoperatively. In patients where nausea and/or vomiting must be avoided postoperatively, ZOFRAN® is recommended even where the incidence of postoperative nausea and/or vomiting is low. Launch Date 1992
Nausea 63 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2005/020103s008s025,020605s008lbl.pdf	Preventing	Approved 8583	ZOFRAN Approved Use Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy, including cisplatin ≥50 mg/m2. Prevention of nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy. Prevention of nausea and vomiting associated with radiotherapy in patients receiving either total body irradiation, single high-dose fraction to the abdomen, or daily fractions to the abdomen. Prevention of postoperative nausea and/or vomiting. As with other antiemetics, routine prophylaxis is not recommended for patients in whom there is little expectation that nausea and/or vomiting will occur postoperatively. In patients where nausea and/or vomiting must be avoided postoperatively, ZOFRAN® is recommended even where the incidence of postoperative nausea and/or vomiting is low. Launch Date 1992
Vomiting 38 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2005/020103s008s025,020605s008lbl.pdf	Preventing	Approved 8583	ZOFRAN Approved Use Prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy, including cisplatin ≥50 mg/m2. Prevention of nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy. Prevention of nausea and vomiting associated with radiotherapy in patients receiving either total body irradiation, single high-dose fraction to the abdomen, or daily fractions to the abdomen. Prevention of postoperative nausea and/or vomiting. As with other antiemetics, routine prophylaxis is not recommended for patients in whom there is little expectation that nausea and/or vomiting will occur postoperatively. In patients where nausea and/or vomiting must be avoided postoperatively, ZOFRAN® is recommended even where the incidence of postoperative nausea and/or vomiting is low. Launch Date 1992

C_max

Value	Dose	Analyte	Population
32.096 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00934180	8 mg single, oral dose: 8 mg route of administration: oral experiment type: single co-administered:	ONDANSETRON plasma	Homo sapiens
30.196 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00934921	8 mg single, oral dose: 8 mg route of administration: oral experiment type: single co-administered:	ONDANSETRON plasma	Homo sapiens
26.2 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	ONDANSETRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
42.7 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	ONDANSETRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
125.8 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf	24 mg single, oral dose: 24 mg route of administration: Oral experiment type: SINGLE co-administered:	ONDANSETRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
194.4 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf	24 mg single, oral dose: 24 mg route of administration: Oral experiment type: SINGLE co-administered:	ONDANSETRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
237.935 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00934180	8 mg single, oral dose: 8 mg route of administration: oral experiment type: single co-administered:	ONDANSETRON plasma	Homo sapiens
224.155 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00934180	8 mg single, oral dose: 8 mg route of administration: oral experiment type: single co-administered:	ONDANSETRON plasma	Homo sapiens
293.492 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00934921	8 mg single, oral dose: 8 mg route of administration: oral experiment type: single co-administered:	ONDANSETRON plasma	Homo sapiens
270.928 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT00934921	8 mg single, oral dose: 8 mg route of administration: oral experiment type: single co-administered:	ONDANSETRON plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
3.1 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	ONDANSETRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.5 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	ONDANSETRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
4.7 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf	24 mg single, oral dose: 24 mg route of administration: Oral experiment type: SINGLE co-administered:	ONDANSETRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.8 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf	24 mg single, oral dose: 24 mg route of administration: Oral experiment type: SINGLE co-administered:	ONDANSETRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
27% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:		ONDANSETRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946		substrate 1388	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT2 779 OCT1 620 MATE1 415 MATE2 267 OCT3 159	CYP1A1 389 CYP1A2 1197 P-gp 2052

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
OCT1 656	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/21599003/ \| https://pubmed.ncbi.nlm.nih.gov/23241029/	no [IC50 >100 uM]
MATE2 267	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/21599003/ \| https://pubmed.ncbi.nlm.nih.gov/23241029/ \| https://pubmed.ncbi.nlm.nih.gov/26825640/	yes [IC50 0.15 uM]	yes (co-administration study) Comment: [PMID:23241029]: IC50 = 0.3 uM; Ondansetron treatment caused a statistically significantly higher Cmax of metformin compared with placebo and apparently decreased the renal clearance of metformin by 37% Sources: https://pubmed.ncbi.nlm.nih.gov/21599003/ \| https://pubmed.ncbi.nlm.nih.gov/23241029/ \| https://pubmed.ncbi.nlm.nih.gov/26825640/
OCT2 782	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/21599003/ \| https://pubmed.ncbi.nlm.nih.gov/23241029/	yes [IC50 0.89 uM]
OCT3 161	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23241029/	yes [IC50 17.4 uM]
MATE1 416	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/21599003/ \| https://pubmed.ncbi.nlm.nih.gov/23241029/ \| https://pubmed.ncbi.nlm.nih.gov/26825640/	yes [IC50 6.9 uM]	yes (co-administration study) Comment: [PMID:23241029]: IC50 = 0.16 uM; Ondansetron treatment caused a statistically significantly higher Cmax of metformin compared with placebo and apparently decreased the renal clearance of metformin by 37% Sources: https://pubmed.ncbi.nlm.nih.gov/21599003/ \| https://pubmed.ncbi.nlm.nih.gov/23241029/ \| https://pubmed.ncbi.nlm.nih.gov/26825640/

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP1A1 389	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8591723/	yes
P-gp 2052	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8647944/	yes
CYP1A2 1197	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8591723/ \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf	yes	likely (co-administration study) Comment: inducers or inhibitors of CYP1A2 may change the clearance and, hence, the half-life of ondansetron Sources: https://pubmed.ncbi.nlm.nih.gov/8591723/ \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf
CYP2D6 1388	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8591723/ \| https://pubmed.ncbi.nlm.nih.gov/20201779/ \|https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf	yes	likely (co-administration study) Comment: inducers or inhibitors of CYP2D6 may change the clearance and, hence, the half-life of ondansetron Sources: https://pubmed.ncbi.nlm.nih.gov/8591723/ \| https://pubmed.ncbi.nlm.nih.gov/20201779/ \|https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/8591723/ \| https://pubmed.ncbi.nlm.nih.gov/20201779/ \|https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf	yes	yes (co-administration study) Comment: In patients treated with potent inducers of CYP3A4 (i.e., phenytoin, carbamazepine, and rifampin), the clearance of ondansetron was significantly increased and ondansetron blood concentrations were decreased. However, on the basis of available data, no dosage adjustment for ZOFRAN is recommended for patients on these drugs. Sources: https://pubmed.ncbi.nlm.nih.gov/8591723/ \| https://pubmed.ncbi.nlm.nih.gov/20201779/ \|https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020103s035_020605s019_020781s019lbl.pdf

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://pubmed.ncbi.nlm.nih.gov/11046096/

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY34510	https://www.001chemical.com/chem/116002-70-1
001 Chemical	DY34512	https://www.001chemical.com/chem/103639-04-9
001 Chemical	DY583739	https://www.001chemical.com/chem/99614-01-4
001 Chemical	NO16446	https://www.001chemical.com/chem/99614-02-5
AA Blocks	AA0065H0	http://www.aablocks.com/goods/Goods/detail?id=AA0065H0
Aaron Chemicals	AR00668S	http://www.aaronchem.com/99614-02-5
abcr GmbH	AB439962	http://www.abcr.com/shop/en/AB439962
AbMole Bioscience	M3211	http://www.abmole.com/products/ondansetron.html
Achemo Scientific Limited	AC-14570	http://www.achemo.com/search/?Keyword= 99614-02-5
Achemtek	0104-023952	http://www.achemtek.com/99614-02-5
Acorn PharmaTech	ACN-049703	http://www.acornpharmatech.com/
AEchem Scientific Corp., USA	AE1-012226	http://www.aechemsc.com/info_products/AE1-012226.php
AHH Chemical co.,ltd	API-1222	http://www.ahhchemical.com/product/API-1222.html
AK Scientific, Inc. (AKSCI)	I544	http://www.aksci.com/item_detail.php?cat=I544
Angene	AGN-PC-0W9MM0	http://www.angenechemical.com/productshow/AGN-PC-0W9MM0.html
ApexBio Technology	A5166	http://www.apexbt.com/ondansetron-hcl.html
Ark Pharm	AK-29654	http://www.arkpharminc.com/products/99614-02-5.html
AstaTech, Inc.	34628	http://www.astatechinc.com/CPSResult.php?CRNO=35772
Aurora Fine Chemicals LLC	K02.257.922	http://online.aurorafinechemicals.com/info?ID=K02.257.922
Aurum Pharmatech LLC	S-2116	http://www.Aurumpharmatech.com/Product/ProductDetails/S_2116
AvaChem Scientific	1530B	http://www.avachem.com/productSearch.asp?1530B
BioChemPartner	BCP28911	http://www.biochempartner.com/99614-02-5-BCP28911
BioCrick	BCC5043	http://www.biocrick.com/Ondansetron-BCC5043.html
BLD Pharm	BD23373	http://www.bldpharm.com/products/99614-02-5.html
Boerchem	BC220610	http://www.boerchem.com/?product_37310.html
Chem Scene	CS-2393	http://www.chemscene.com/99614-02-5.html
Chemenu	CM110039	http://www.chemenu.com/products/CM110039
ChemMol	49401168	http://www.chemmol.com/chemmol/49401168.html
ChemMol	99179435	http://www.chemmol.com/chemmol/99179435.html
ChemReagents	80015792	http://www.chemreagents.com/Product/Product.asp?ProductID=80015792
Chemspace	CSSB00000692966	https://chem-space.com/CSSB00000692966
Clearsynth	CS-O-00286	https://www.clearsynth.com/en/CSO00286.html
CSNpharm	CSN13137	https://www.csnpharm.com/products/ondansetron.html
Enamine	Z1741971217	https://www.enaminestore.com/catalog/Z1741971217
eNovation Chemicals	D544001	http://www.enovationchem.com/productDetails.asp?productID=D544001
Finetech	FT-0631004	http://www.finetechnology-ind.com/prod/detail/pub/99614-02-5.html
Glentham Life Sciences	GP8457	http://www.glentham.com/products/product/GP8457/
Hairui	HR129742	http://www.hairuichem.com/en/product/116002-70-1.html
Hairui	HR129931	http://www.hairuichem.com/en/product/99614-02-5.html
Hefei Hirisun Pharmatech Co., Ltd	HR011780	http://www.hirisunpharm.com/99614-02-5.html
iChemical	EBD25456	http://www.ichemical.com/products/99614-02-5.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
Lab Network	LN00221208	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00221208
LGC Standards	LGCFOR0252.09	https://www.lgcstandards.com/US/en/p/LGCFOR0252.09
LGC Standards	MM0252.09	https://www.lgcstandards.com/US/en/p/MM0252.09
Matrix Scientific	118975	https://www.matrixscientific.com/118975.html
mcule	MCULE-9438746800	https://mcule.com/MCULE-9438746800/
MedChem Express	HY-B0002B	https://www.medchemexpress.com/Ondansetron.html
Molcore	CS16446	https://www.molcore.com/product/99614-02-5
Molcore	MC34510	https://www.molcore.com/product/116002-70-1
Molcore	MC34512	https://www.molcore.com/product/103639-04-9
Molcore	MC583739	https://www.molcore.com/product/99614-01-4
MuseChem	A000623	https://www.musechem.com/product/A000623.html
MuseChem	M017775	https://www.musechem.com/product/M017775.html
Oakwood	47250	http://www.oakwoodchemical.com/ProductsList.aspx?CategoryID=-2&txtSearch=41112&ExtHyperLink=1
OChem	8322	http://www.ocheminc.com/index.php?act=psearch&pid=39O049
Selleck Chemicals	S1996	http://www.selleckchem.com/products/ondansetron-zofran.html
Vesino Industrial Co Ltd	VA11441	http://www.vsnchem.com/goto/product/22764/
Vitas-M Laboratory	BBL010304	http://www.request.vitasmlab.biz/index.php?option=com_search_stk&Itemid=22&stk=BBL010304&?utm_source=pubchem&utm_medium=p_search_link&utm_campaign=pubchem_search&utm_content=pubchem_slink
VladaChem	VL273950-1G	https://www.vladachem.com/product.php?products=99614-02-5
Yuhao Chemical	LT7279	http://www.chemyuhao.com/99614-02-5.html

PubMed

Title	Date	PubMed
Cardiorespiratory decompensation following methylprednisolone administration.	1993 Jul-Sep	8217541
Extrapyramidal reaction caused by ondansetron.	1994 Feb	8173151
Adjusting the dose of intravenous ondansetron plus dexamethasone to the emetogenic potential of the chemotherapy regimen.	1995 Aug	7636556
The efficacy of prophylactic ondansetron, droperidol, perphenazine, and metoclopramide in the prevention of nausea and vomiting after major gynecologic surgery.	1995 Jul	7598243
Inhibitory effect of ethanol on the 5-hydroxytryptamine-induced Bezold-Jarisch reflex--involvement of peripheral 5-HT3 receptors.	1995 May 26	7672010
A phase II study of ondansetron as antiemetic prophylaxis in patients receiving high-dose polychemotherapy and stem cell transplantation.	1995 Sep	8520876
Nondepolarizing neuromuscular blockers inhibit the serotonin-type 3A receptor expressed in Xenopus oocytes.	2000 Feb	10648343
Effect of the 5-HT3 receptor antagonist ondansetron on amphetamine-induced hyperactivity and stereotypy in rats.	2000 Jul	10941627
Cloning, expression, and characterization of ferret 5-HT(3) receptor subunit.	2000 Jul 7	10884508
Randomized, double-blind, crossover, placebo-controlled trial of intravenous ondansetron for the prevention of intrathecal chemotherapy-induced vomiting in children.	2001 Dec	11902300
Tropisetron vs ondansetron for prevention of postoperative nausea and vomiting after laparoscopic cholecystectomy: a randomized double-blind, placebo-controlled study.	2002 Jul	12165828
Ondansetron inhibits the analgesic effects of tramadol: a possible 5-HT(3) spinal receptor involvement in acute pain in humans.	2002 Jun	12032025
Ondansetron given in the acute withdrawal from a repeated cocaine sensitization dosing regimen reverses the expression of sensitization and inhibits self-administration.	2002 Oct	12377391
Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.	2003 Feb 27	12593651
Involvement of some 5-HT receptors in methamphetamine-induced locomotor activity in mice.	2004 Jun	15213358
Role of central 5-HT3 receptors in the control of blood pressure in stressed and non-stressed rats.	2004 Nov 26	15518641
Ondansetron, given during the acute cocaine withdrawal, attenuates oral cocaine self-administration.	2004 Oct 25	15496303
Ondansetron amelioration of scopolamine induced cognitive deficits in three-panel runway apparatus in rats.	2004 Sep	15462187
Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same?	2005	15740177
The influence of dexamethasone in the decrease of chemotherapy-induced nausea and vomiting.	2007 Apr-Jun	17600880
Reversal of cocaine-induced behavioral sensitization and associated phosphorylation of the NR2B and GluR1 subunits of the NMDA and AMPA receptors.	2007 Feb	16794574
Interactions between metoclopramide and morphine: enhanced antinociception and motor dysfunction in rats.	2007 Jan-Feb	17201744
Droperidol and ondansetron-induced QT interval prolongation: a clinical drug interaction study.	2008 Aug	18648229
Comparative efficacy of maropitant and selected drugs in preventing emesis induced by centrally or peripherally acting emetogens in dogs.	2008 Dec	19000276
Ondansetron-associated hypokalemia in a 2-year-old with pre-B-cell ALL.	2008 Jan	18176182
Ondansetron given intravenously attenuates arterial blood pressure drop due to spinal anesthesia: a double-blind, placebo-controlled study.	2008 Jul-Aug	18675744
Neonatal extrapyramidal movements. Neonatal withdrawal due to maternal citalopram and ondansetron use.	2008 Mar	18411854
Ondansetron and seizures.	2009 Dec	19490041
Coronary vasospasm and atrial fibrillation associated with ondansetron therapy.	2009 Mar	19261954
Acute anti-emetic withdrawal associated with a hemorrhagic cerebellar arteriovenous malformation.	2010 Aug	20488707
Ondansetron-induced headache in a parturient mimicking postdural puncture headache.	2010 Feb	20043218
Multimodal prevention of pain, nausea and vomiting after breast cancer surgery.	2010 Oct	20935616
Ondansetron-induced migraine-type headache.	2010 Sep	20661681
Single-dose fosaprepitant for the prevention of chemotherapy-induced nausea and vomiting associated with cisplatin therapy: randomized, double-blind study protocol--EASE.	2011 Apr 10	21383291
In vivo assessment of antiemetic drugs and mechanism of lycorine-induced nausea and emesis.	2011 Dec	21626407
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.	2011 Jul 14	21599003
Prophylaxis of radiation-induced nausea and vomiting using 5-hydroxytryptamine-3 serotonin receptor antagonists: a systematic review of randomized trials.	2012 Jan 1	21075553

Patents

Sample Use Guides

In Vivo Use Guide

To prevent nausea and vomiting associated with cancer chemotherapy the recommended adult oral dosage of ondansetron (ZOFRAN®) is a single 24-mg tablet administered 30 minutes before the start of single-day highly emetogenic chemotherapy; for moderately emetogenic cancer chemotherapy the recommended adult oral dosage is one 8-mg ondansetron (ZOFRAN®) tablet given twice a day (every 12 hours) for 1 to 2 days after completion of chemotherapy: the first dose should be administered 30 minutes before the start of emetogenic chemotherapy, with a subsequent dose 8 hours after the first dose. To prevent nausea and vomiting associated with radiotherapy the recommended adult oral dosage is one 8-mg ondansetron (ZOFRAN®) tablet given 3 times a day; for total body irradiation, one 8-mg ondansetron (ZOFRAN®) tablet should be administered 1 to 2 hours before each fraction of radiotherapy administered each day; for single high-dose fraction radiotherapy to the abdomen, one 8-mg ondansetron (ZOFRAN®) tablet should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for 1 to 2 days after completion of radiotherapy; for daily fractionated radiotherapy to the abdomen, one 8-mg ondansetron (ZOFRAN®) tablet should be administered 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for each day radiotherapy is given. To prevent postoperative nausea and vomiting the recommended adult oral dosage is 16 mg given as two 8-mg ondansetron (ZOFRAN®) tablets 1 hour before induction of anesthesia.

Route of Administration: Oral

In Vitro Use Guide

On the isolated vagus nerve and superior cervical ganglion of the rat, R,S-GR38032F (ondansetron) behaved as a reversible competitive antagonist of 5-HT-induced depolarization with pKB values of 8.61+/-0.08 (n=19) and 8.13+/-0.07 (n=16), respectively. The resolved R- and S-isomers of GR38032F were approximately equipotent as 5-HT antagonists on the rat vagus nerve: the pKB values were 8.95+/-0.05 (n=16) and 8.63+/-0.08 (n=17), respectively. R,S-GR38032F was also an effective antagonist of 5-HT on the rabbit isolated vagus nerve: in this case the pKB value was 9.40+/-0.14 (n=4).

Substance Class	Chemical Created by `admin` on `Mon Mar 31 19:36:59 GMT 2025` Edited by `admin` on `Mon Mar 31 19:36:59 GMT 2025`
Record UNII	4AF302ESOS
Record Status	`Validated (UNII)`
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Type

Language

A04AA01

Preferred Name

English

ONDANSETRON

Official Name

English

ONDANSETRON [MI]

Common Name

English

(±)-2,3-DIHYDRO-9-METHYL-3-((2-METHYLIMIDAZOL-1-YL)METHYL)CARBAZOL-4(1H)-ONE

Systematic Name

English

ONDANSETRON [MART.]

Common Name

English

EUR-1025

Code

English

ondansetron [INN]

Common Name

English

4H-CARBAZOL-4-ONE, 1,2,3,9-TETRAHYDRO-9-METHYL-3-((2-METHYL-1H-IMIDAZOL-1-YL)METHYL)- (±)-

Systematic Name

English

NSC-757870

Code

English

ONDANSETRON [VANDF]

Common Name

English

ONDANSETRON [USP MONOGRAPH]

Common Name

English

ZOFRAN ODT

Brand Name

English

ONDANSETRON [ORANGE BOOK]

Common Name

English

ONDANSETRON [JAN]

Common Name

English

Ondansetron [WHO-DD]

Common Name

English

ONDANSETRON [USP-RS]

Common Name

English

Classification Tree Code System Code

WHO-ESSENTIAL MEDICINES LIST

17.2