Ondansetron

Identification

Summary

Ondansetron is a serotonin 5-HT3 receptor antagonist used to prevent nausea and vomiting in cancer chemotherapy and postoperatively.

Brand Names

Zofran, Zuplenz

Generic Name

Ondansetron

DrugBank Accession Number

DB00904

Background

A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.

Having been developed in the 1980s by GlaxoSmithKline and approved by the US FDA since January 1991, ondansetron has demonstrated a long history of use and efficacy. Commonly formulated as oral tablets, orally disintegrating tablets (ODT), and injections, and available as generic products as well, ondansetron continues to see contemporary innovations in its formulation and use, including the development of orally soluble films that are both discreet in administration and less of a burden in comparison to having patients attempt to swallow pills during emesis.⁷

The FDA withdrew its approval for the use of all intravenous drug products containing more than 16 mg of ondansetron hydrochloride in a single dose, due to a high risk of QT prolongation.^8,9

Type

Small Molecule

Groups

Approved, Withdrawn

Structure

3D

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Similar Structures

Structure for Ondansetron (DB00904)

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Weight

Average: 293.363
Monoisotopic: 293.152812245

Chemical Formula

C₁₈H₁₉N₃O

Synonyms

• Ondansetron

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Pharmacology

Indication

In the adult patient population: i) orally administered ondansetron tablets and orally disintegrating tablets (ODT) are indicated for: - the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy, including high dose (ie. greater than or equal to 50 mg/m2) cisplatin therapy, and radiotherapy, and - the prevention and treatment of postoperative nausea and vomiting

ii) intravenously administered ondansetron injection formulations are indicated for: - the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy, including high dose (ie. greater than or equal to 50 mg/m2) cisplatin therapy, and - the prevention and treatment of postoperative nausea and vomiting

In the pediatric (4-18 years of age) patient population: i) ondansetron was effective and well tolerated when given to children 4-12 years of age for the treatment of post-chemotherapy induced nausea and vomiting, ii) ondansetron tablets, ondansetron ODT, ondansetron injection are not indicated for the treatment of children 3 years of age or younger, iii) ondansetron tablets, ondansetron ODT, ondansetron injection are not indicated for use in any age group of the pediatric population for the treatment of post-radiotherapy induced nausea and vomiting, and iV) ondansetron tablets, ondansetron ODT, ondansetron injection are not indicated for use in any age group of the pediatric population for the treatment of postoperative nausea and vomiting

In the geriatric (>65 years of age) patient population: i) efficacy and tolerance of ondansetron were similar to that observed in younger adults for the treatment of post-chemotherapy and radiotherapy-induced nausea and vomiting, and ii) clinical experience in the use of ondansetron in the prevention and treatment of postoperative nausea and vomiting is limited and is not indicated for use in the geriatric patient population

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Prophylaxis of	Chemotherapy-induced nausea and vomiting		••••••••••••
Prophylaxis of	Chemotherapy-induced nausea and vomiting		••••••••••••
Treatment of	Cholestatic pruritus		••• •••••
Prophylaxis of	Post-operative nausea and vomiting		••••••••••••
Treatment of	Uremic pruritus		••• •••••

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Contraindications & Blackbox Warnings

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Pharmacodynamics

Ondansetron is a highly specific and selective serotonin 5-HT₃ receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors ^Label, ^3,4. The serotonin 5-HT₃ receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema ^Label, ^3,4. The temporal relationship between the emetogenic action of emetogenic drugs and the release of serotonin, as well as the efficacy of antiemetic agents, suggest that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract ^Label, ^3,4. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT₃ receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting ^Label, ^3,4.

Moreover, the effect of ondansetron on the QTc interval was evaluated in a double-blind, randomized, placebo and positive (moxifloxacin) controlled, crossover study in 58 healthy adult men and women ^11,12. Ondansetron was tested at single doses of 8 mg and 32 mg infused intravenously over 15 minutes ^11,12. At the highest tested dose of 32 mg, prolongation of the Fridericia-corrected QTc interval (QT/RR0.33=QTcF) was observed from 15 min to 4 h after the start of the 15 min infusion, with a maximum mean (upper limit of 90% CI) difference in QTcF from placebo after baseline-correction of 19.6 (21.5) msec at 20 min ^11,12. At the lower tested dose of 8 mg, QTc prolongation was observed from 15 min to 1 h after the start of the 15-minute infusion, with a maximum mean (upper limit of 90% CI) difference in QTcF from placebo after baseline-correction of 5.8 (7.8) msec at 15 min ^11,12. The magnitude of QTc prolongation with ondansetron is expected to be greater if the infusion rate is faster than 15 minutes ^11,12. The 32 mg intravenous dose of ondansetron must not be administered ^11,12. No treatment-related effects on the QRS duration or the PR interval were observed at either the 8 or 32 mg dose ^11,12.

An ECG assessment study has not been performed for orally administered ondansetron ^11,12. On the basis of pharmacokinetic-pharmacodynamic modelling, an 8 mg oral dose of ondansetron is predicted to cause a mean QTcF increase of 0.7 ms (90% CI -2.1, 3.3) at steady-state, assuming a mean maximal plasma concentration of 24.7 ng/mL (95% CI 21.1, 29.0) ^11,12. The magnitude of QTc prolongation at the recommended 5 mg/m2 dose in pediatrics has not been studied, but pharmacokinetic-pharmacodynamic modeling predicts a mean increase of 6.6 ms (90% CI 2.8, 10.7) at maximal plasma concentrations ^11,12.

In healthy subjects, single intravenous doses of 0.15 mg/kg of ondansetron had no effect on esophageal motility, gastric motility, lower esophageal sphincter pressure, or small intestinal transit time ¹⁰. Multiday administration of ondansetron has been shown to slow colonic transit in healthy subjects ¹⁰. Ondansetron has no effect on plasma prolactin concentrations ¹⁰.

Mechanism of action

Ondansetron is a selective antagonist of the serotonin receptor subtype, 5-HT3 ^10,11,12.

Cytotoxic chemotherapy and radiotherapy are associated with the release of serotonin (5-HT) from enterochromaffin cells of the small intestine, presumably initiating a vomiting reflex through stimulation of 5-HT3 receptors located on vagal afferents ^10,11,12. Ondansetron may block the initiation of this reflex. Activation of vagal afferents may also cause a central release of serotonin from the chemoreceptor trigger zone of the area postrema, located on the floor of the fourth ventricle ^10,11,12. Thus, the antiemetic effect of ondansetron is probably due to the selective antagonism of 5-HT3 receptors on neurons located in either the peripheral or central nervous systems, or both ^10,11,12.

Although the mechanisms of action of ondansetron in treating postoperative nausea and vomiting and cytotoxic induced nausea and vomiting may share similar pathways, the role of ondansetron in opiate-induced emesis has not yet been formally established ^11,12.

Target	Actions	Organism
A5-hydroxytryptamine receptor 3A	antagonist	Humans
U5-hydroxytryptamine receptor 4	agonist	Humans
UMu-type opioid receptor	other/unknown	Humans
U5-hydroxytryptamine receptor 1A	other/unknown	Humans
U5-hydroxytryptamine receptor 1B	other/unknown	Humans

Absorption

Ondansetron is absorbed from the gastrointestinal tract and undergoes some limited first-pass metabolism ¹⁰. Mean bioavailability in healthy subjects, following administration of a single 8-mg tablet, was recorded as being approximately 56% to 60% ^10,11,12. Bioavailability is also slightly enhanced by the presence of food ¹⁰.

Ondansetron systemic exposure does not increase proportionately to dose ¹⁰. The AUC from a 16-mg tablet was 24% greater than predicted from an 8-mg tablet dose ¹⁰. This may reflect some reduction of first-pass metabolism at higher oral doses ¹⁰.

Volume of distribution

The volume of distribution of ondansetron has been recorded as being approximately 160L ⁵.

Protein binding

The plasma protein binding associated with ondansetron was documented as approximately 73% ^11,12.

Metabolism

In vitro metabolism studies have shown that ondansetron is a substrate for human hepatic cytochrome P450 enzymes, including CYP1A2, CYP2D6 and CYP3A4 ^10,11,12. In terms of overall ondansetron turnover, CYP3A4 played the predominant role ^10,11,12. Because of the multiplicity of metabolic enzymes capable of metabolizing ondansetron, it is likely that inhibition or loss of one enzyme (e.g. CYP2D6 enzyme deficiency) will be compensated by others and may result in little change in overall rates of ondansetron clearance ^10,11,12.

Following oral or IV administration, ondansetron is extensively metabolised and excreted in the urine and faeces ^10,11,12. In humans, less than 10% of the dose is excreted unchanged in the urine ^10,11,12. The major urinary metabolites are glucuronide conjugates (45%), sulphate conjugates (20%) and hydroxylation products (10%) ^10,11,12. The primary metabolic pathway is subsequently hydroxylation on the indole ring followed by subsequent glucuronide or sulfate conjugation ^10,11,12. Although some nonconjugated metabolites have pharmacologic activity, these are not found in plasma at concentrations likely to significantly contribute to the biological activity of ondansetron ^10,11,12.

Hover over products below to view reaction partners

• Ondansetron
  • 6-OH-ondansetron
  • 7-OH-ondansetron
  • 8-OH-ondansetron

Route of elimination

Following oral or IV administration, ondansetron is extensively metabolised and excreted in the urine and faeces ^11,12.

Half-life

The half-life of ondansetron after either an 8 mg oral dose or intravenous dose was approximately 3-4 hours and could be extended to 6-8 hours in the elderly ^11,12.

Clearance

The clearance values determined for ondansetron in various patient age groups were recorded as approximately 0.38 L/h/kg in normal adult volunteers aged 19-40 yrs, 0.32 L/h/kg in normal adult volunteers aged 61-74 yrs, 0.26 L/h/kg in normal adult volunteers aged >=75 yrs ^Label.

Adverse Effects

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Toxicity

At present, there is little information concerning overdosage with ondansetron ^10,11,12. Nevertheless, there have been certain cases of somewhat idiosyncratic adverse effects associated with particular dosages of ondansetron used ^10,11,12.

“Sudden blindness” (amaurosis) of 2 to 3 minutes duration plus severe constipation occurred in one patient that was administered 72 mg of ondansetron intravenously as a single dose ^10,11,12. Hypotension (and faintness) occurred in another patient that took 48 mg of oral ondansetron ^10,11,12. Following infusion of 32 mg over only a 4-minute period, a vasovagal episode with transient second-degree heart block was observed ^10,11,12. Neuromuscular abnormalities, autonomic instability, somnolence, and a brief generalized tonic-clonic seizure (which resolved after a dose of benzodiazepine) were observed in a 12-month-old infant who ingested seven or eight 8-mg ondansetron tablets (approximately forty times the recommended 0.1-0.15 mg/kg dose for a pediatric patient) ^10,11,12. In all instances, however, the events resolved completely ^10,11,12.

The safety of ondansetron for use in human pregnancy has not been established ^11,12. Ondansetron is not teratogenic in animals ^11,12. However, as animal studies are not always predictive of human response, the use of ondansetron in pregnancy is not recommended ^11,12.

Ondansetron is excreted in the milk of lactating rats ^11,12. It is not known if it is excreted in human milk, however, nursing is not recommended during treatment with ondansetron ^11,12.

Insufficient information is available to provide dosage recommendations for children 3 years of age or younger ^11,12.

Pathways

Not Available

Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Interacting Gene/Enzyme	Allele name	Genotype(s)	Defining Change(s)	Type(s)	Description	Details
Cytochrome P450 2D6	CYP2D6*1xN,	Not Available	Gene duplication.	Effect Directly Studied	Patients with this genotype in CYP2D6 are ultrarapid metabolizers with an increased risk of poor therapeutic response and vomiting when treated with ondansteron.	Details
Cytochrome P450 2D6	CYP2D6*2xN	Not Available	Gene duplication.	Effect Directly Studied	Patients with this genotype in CYP2D6 are ultrarapid metabolizers with an increased risk of poor therapeutic response and vomiting when treated with ondansteron.	Details
Cytochrome P450 2D6	CYP2D6*1XN	Not Available	Normal allele duplicated.	ADR Inferred	Ultra-rapid drug metabolizer. Risk of toxicity, alternative drug recommended.	Details
Cytochrome P450 2D6	CYP2D6*2XN	Not Available	2850C>T / 4180G>C  … show all	ADR Inferred	Ultra-rapid drug metabolizer. Risk of toxicity, alternative drug recommended.	Details
Cytochrome P450 2D6	CYP2D6*1XN	Not Available	Normal allele duplicated.	Effect Inferred	Poor response	Details

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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1,2-Benzodiazepine	The risk or severity of CNS depression can be increased when Ondansetron is combined with 1,2-Benzodiazepine.
Abametapir	The serum concentration of Ondansetron can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Ondansetron can be increased when combined with Abatacept.
Abiraterone	The serum concentration of Ondansetron can be increased when it is combined with Abiraterone.
Abrocitinib	The metabolism of Abrocitinib can be decreased when combined with Ondansetron.

Food Interactions

• Take with or without food. The absorption is unaffected by food.

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Ondansetron hydrochloride	2999F27MAD	99614-01-4	MKBLHFILKIKSQM-UHFFFAOYSA-N
Ondansetron hydrochloride dihydrate	NMH84OZK2B	103639-04-9	VRSLTNZJOUZKLX-UHFFFAOYSA-N

Product Images

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International/Other Brands

Zophren

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Athena-ondansetron ODT	Tablet, orally disintegrating	8 mg	Oral	Athena Pharmaceutiques Sas	2015-11-23	Not applicable
Athena-ondansetron ODT	Tablet, orally disintegrating	4 mg	Oral	Athena Pharmaceutiques Sas	2015-11-23	Not applicable
Ondansetron	Tablet	4 mg	Oral	Sanis Health Inc	2014-03-18	Not applicable
Ondansetron	Tablet	4 mg	Oral	Pro Doc Limitee	Not applicable	Not applicable
Ondansetron	Injection, solution	32 mg/50mL	Intravenous	Baxter Laboratories	2006-12-27	2012-07-25

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Accel-ondansetron	Tablet	4 mg	Oral	Accel Pharma Inc	2019-09-19	Not applicable
Accel-ondansetron	Tablet	8 mg	Oral	Accel Pharma Inc	2019-09-19	Not applicable
Accel-ondansetron ODT	Tablet, orally disintegrating	8 mg	Oral	Accel Pharma Inc	2023-12-19	Not applicable
Accel-ondansetron ODT	Tablet, orally disintegrating	4 mg	Oral	Accel Pharma Inc	2023-12-19	Not applicable
Ag-ondansetron	Tablet	8 mg	Oral	Angita Pharma Inc.	Not applicable	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
Mpm Pak	Ondansetron (8 mg/1) + Ibuprofen (800 mg/1) + Mifepristone (200 mg/1) + Misoprostol (200 ug/1)	Kit; Tablet; Tablet, orally disintegrating	Oral	Nucare Pharmaceuticals,inc.	2023-02-24	Not applicable
Mpm Pak	Ondansetron (8 mg/1) + Ibuprofen (800 mg/1) + Mifepristone (200 mg/1) + Misoprostol (200 ug/1)	Kit; Tablet; Tablet, orally disintegrating	Oral	Nucare Pharmaceuticals,inc.	2023-06-14	Not applicable
Mpm Pak	Ondansetron (8 mg/1) + Ibuprofen (800 mg/1) + Mifepristone (200 mg/1) + Misoprostol (200 ug/1)	Kit; Tablet; Tablet, orally disintegrating	Oral	Nucare Pharmaceuticals,inc.	2023-02-24	Not applicable

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
MKO Melt	Ondansetron hydrochloride dihydrate (2 mg/1) + Ketamine hydrochloride (25 mg/1) + Midazolam (3 mg/1)	Troche	Sublingual	Imprimis Njof, Llc	2018-12-01	2019-03-04
MKO Melt Dose Pack	Ondansetron hydrochloride (2 mg/1) + Ketamine hydrochloride (25 mg/1) + Midazolam (3 mg/1)	Troche	Sublingual	Imprimis Njof, Llc	2019-03-04	Not applicable
Ondansetron	Ondansetron (8 mg/1)	Tablet, orally disintegrating	Oral	Remedy Repack	2015-02-26	2015-12-30
Sumansetron	Ondansetron hydrochloride dihydrate (4 mg/1) + Sumatriptan succinate (50 mg/1)	Kit; Tablet; Tablet, film coated	Oral	PureTek Corporation	2021-01-01	Not applicable
ZOPHRALEN 8 MG/4ML IV AMPUL	Ondansetron (8 mg/4ml)	Injection, solution	Intravenous	DEM İLAÇ SAN. VE TİC. A.Ş.	2018-12-25	Not applicable

Categories

ATC Codes

A04AA01 — Ondansetron

• A04AA — Serotonin (5HT3) antagonists
• A04A — ANTIEMETICS AND ANTINAUSEANTS
• A04 — ANTIEMETICS AND ANTINAUSEANTS
• A — ALIMENTARY TRACT AND METABOLISM

Drug Categories

• Anti-Anxiety Agents
• Antidepressive Agents
• Antiemetic Serotonin 5-HT3 Receptor Antagonists
• Antiemetics
• Antiemetics and Antinauseants
• Carbazoles
• Central Nervous System Agents
• Central Nervous System Depressants
• Cytochrome P-450 CYP1A2 Inhibitors
• Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
• Cytochrome P-450 CYP1A2 Substrates
• Cytochrome P-450 CYP2C9 Substrates
• Cytochrome P-450 CYP2D6 Substrates
• Cytochrome P-450 CYP2E1 Substrates
• Cytochrome P-450 CYP3A Substrates
• Cytochrome P-450 CYP3A4 Substrates
• Cytochrome P-450 CYP3A5 Substrates
• Cytochrome P-450 CYP3A7 Substrates
• Cytochrome P-450 Enzyme Inhibitors
• Cytochrome P-450 Substrates
• Heterocyclic Compounds, Fused-Ring
• Imidazoles
• Indoles
• Moderate Risk QTc-Prolonging Agents
• Peripheral Nervous System Agents
• Psychotropic Drugs
• QTc Prolonging Agents
• Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
• Serotonin 3 Receptor Antagonists
• Serotonin 5-HT3 Receptor Antagonists
• Serotonin Agents
• Serotonin Receptor Antagonists

Chemical TaxonomyProvided by Classyfire

Description

This compound belongs to the class of organic compounds known as carbazoles. These are compounds containing a three ring system containing a pyrrole ring fused on either side to a benzene ring.

Kingdom

Organic compounds

Super Class

Organoheterocyclic compounds

Class

Indoles and derivatives

Sub Class

Carbazoles

Direct Parent

Carbazoles

Alternative Parents

N-alkylindoles / Indoles / Aryl alkyl ketones / N-substituted imidazoles / N-methylpyrroles / Benzenoids / Vinylogous amides / Heteroaromatic compounds / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives

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Substituents

Aromatic heteropolycyclic compound / Aryl alkyl ketone / Aryl ketone / Azacycle / Azole / Benzenoid / Carbazole / Heteroaromatic compound / Hydrocarbon derivative / Imidazole / Indole / Ketone / N-alkylindole / N-methylpyrrole / N-substituted imidazole / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Pyrrole / Substituted pyrrole / Vinylogous amide

show 14 more

Molecular Framework

Aromatic heteropolycyclic compounds

External Descriptors

carbazoles (CHEBI:7773)

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

4AF302ESOS

CAS number

99614-02-5

InChI Key

FELGMEQIXOGIFQ-UHFFFAOYSA-N

InChI

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

IUPAC Name

9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-2,3,4,9-tetrahydro-1H-carbazol-4-one

SMILES

CN1C2=C(C3=CC=CC=C13)C(=O)C(CN1C=CN=C1C)CC2

References

Synthesis Reference

Peter Bod, Kalman Harsanyi, Ferenc Trischler, Eva Fekecs, Attila Csehi, Bela Hegedus, Eva Mersich nee Donat, Gyorgyi Szabo nee Komlosi, Erika Horvath nee Sziki, "Process for preparing ondansetron." U.S. Patent US5478949, issued September, 1990.

US5478949

General References

1. Ramsook C, Sahagun-Carreon I, Kozinetz CA, Moro-Sutherland D: A randomized clinical trial comparing oral ondansetron with placebo in children with vomiting from acute gastroenteritis. Ann Emerg Med. 2002 Apr;39(4):397-403. [Article]
2. Yilmaz HL, Yildizdas RD, Sertdemir Y: Clinical trial: oral ondansetron for reducing vomiting secondary to acute gastroenteritis in children--a double-blind randomized study. Aliment Pharmacol Ther. 2010 Jan;31(1):82-91. doi: 10.1111/j.1365-2036.2009.04145.x. Epub . [Article]
3. Gregory RE, Ettinger DS: 5-HT3 receptor antagonists for the prevention of chemotherapy-induced nausea and vomiting. A comparison of their pharmacology and clinical efficacy. Drugs. 1998 Feb;55(2):173-89. [Article]
4. Gan TJ: Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same? CNS Drugs. 2005;19(3):225-38. [Article]
5. Roila F, Del Favero A: Ondansetron clinical pharmacokinetics. Clin Pharmacokinet. 1995 Aug;29(2):95-109. doi: 10.2165/00003088-199529020-00004. [Article]
6. Electronic Medicines Compendium: Zofran (ondansetron hydrochloride dihydrate) Tablets 4mg and 8mg Monograph [Link]
7. Midatech’s Commercial Launch of Zuplenz® (Ondansetron) Oral Soluble Film to Prevent Post-Operative, Chemotherapy and Radiation-Induced Nausea and Vomiting in US: Press Release [Link]
8. Federal Register: Determination That Ondansetron (Ondansetron Hydrochloride) Injection, USP in PL 2408 Plastic Container, 32 Milligrams in 50 Milliliters, Was Withdrawn From Sale for Reasons of Safety or Effectiveness [Link]
9. Code of Federal Regulations 216.24: Drug products withdrawn or removed from the market for reasons of safety or effectiveness. [Link]
10. Ondansetron FDA 2016 Label [File]
11. Zofran Canadian Product Information [File]
12. Sandoz Ondansetron Canadian Product Information [File]

External Links

Human Metabolome Database

HMDB0005035

KEGG Drug

D00456

KEGG Compound

C07325

PubChem Compound

4595

PubChem Substance

46504819

ChemSpider

4434

BindingDB

85330

RxNav

26225

ChEBI

7773

ChEMBL

CHEMBL46

Therapeutic Targets Database

DAP000221

PharmGKB

PA450705

Guide to Pharmacology

GtP Drug Page

PDBe Ligand

S87

RxList

RxList Drug Page

Drugs.com

Drugs.com Drug Page

PDRhealth

PDRhealth Drug Page

Wikipedia

Ondansetron

PDB Entries

6w1m

FDA label

Download (126 KB)

MSDS

Download (53.2 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Basic Science	Motility Disorder of Intestine / Ondansetron / Small Bowel Water	1
4	Completed	Health Services Research	Laparoscopic Cholecystectomy	1
4	Completed	Other	Abdominal Pain / Diarrhea / Eosinophilic Gastroenteritis / Hematochezia / Inflammatory Bowel Diseases (IBD) / Weight Loss	1
4	Completed	Prevention	Bone Fractures / Morphine Adverse Reaction / Post Operative Nausea and Vomiting (PONV) / Pruritus / Satisfaction, Personal	1
4	Completed	Prevention	Breast Neoplasms / Nausea / Vomiting	1

Pharmacoeconomics

Manufacturers

• Par pharmaceutical
• Aurobindo pharma ltd
• Barr laboratories inc
• Glenmark generics ltd
• Kv pharmaceutical co
• Mylan pharmaceuticals inc
• Par pharmaceutical inc
• Sandoz inc
• Sun pharmaceutical industries ltd
• Teva pharmaceuticals usa inc
• Glaxosmithkline
• Akorn strides llc
• Apotex inc
• App pharmaceuticals llc
• Baxter healthcare corp anesthesia and critical care
• Bedford laboratories div ben venue laboratories inc
• Emcure pharmaceuticals ltd
• Gland pharma ltd
• Hikma farmaceutica (portugal) sa
• Hospira inc
• Lannett holdings inc
• Luitpold pharmaceuticals inc
• Pharmaforce inc
• Pliva hrvatska doo
• Sandoz canada inc
• Spectrum pharmaceuticals
• Wockhardt ltd
• Bedford laboratories
• Claris lifesciences ltd
• Teva parenteral medicines inc
• Baxter healthcare corp
• Apotex inc richmond hill
• Taro pharmaceuticals ireland ltd
• Roxane laboratories inc
• Taro pharmaceutical industries ltd
• Dr reddys laboratories ltd
• Natco pharma ltd
• West ward pharmaceutical corp

Packagers

• Aceto Pharma Inc.
• Actavis Group
• Aidarex Pharmacuticals LLC
• Akorn Inc.
• Amerigen Pharmaceuticals Inc.
• Apotex Inc.
• Apotheca Inc.
• APP Pharmaceuticals
• A-S Medication Solutions LLC
• Ascend Laboratories LLC
• Atlantic Biologicals Corporation
• Aurobindo Pharma Ltd.
• Baxter International Inc.
• Bedford Labs
• Ben Venue Laboratories Inc.
• Cardinal Health
• Catalent Pharma Solutions
• Claris Lifesciences Inc.
• Cura Pharmaceutical Co. Inc.
• Dispensing Solutions
• Diversified Healthcare Services Inc.
• Doctor Reddys Laboratories Ltd.
• Emcure Pharmaceuticals Ltd.
• Ethex Corp.
• GlaxoSmithKline Inc.
• Glenmark Generics Ltd.
• Greenstone LLC
• Hikma Pharmaceuticals
• Hospira Inc.
• Kaiser Foundation Hospital
• Kali Laboratories Inc.
• Lake Erie Medical and Surgical Supply
• Lannett Co. Inc.
• Murfreesboro Pharmaceutical Nursing Supply
• Mylan
• Natco Pharma Ltd.
• Northstar Rx LLC
• Nucare Pharmaceuticals Inc.
• PD-Rx Pharmaceuticals Inc.
• Penn Labs
• Pfizer Inc.
• Physicians Total Care Inc.
• Pliva Inc.
• Preferred Pharmaceuticals Inc.
• Professional Co.
• Ranbaxy Laboratories
• Rebel Distributors Corp.
• Redpharm Drug
• Roxane Labs
• Sagent Pharmaceuticals
• Sandoz
• Southwood Pharmaceuticals
• Stat Rx Usa
• Strides Arcolab Limited
• Sun Pharmaceutical Industries Ltd.
• Taro Pharmaceuticals USA
• Teva Pharmaceutical Industries Ltd.
• UDL Laboratories
• Watson Pharmaceuticals
• West-Ward Pharmaceuticals
• Wockhardt Ltd.

Dosage Forms

Form	Route	Strength
Solution	Oral	4 mg / 5 mL
Tablet, orally disintegrating	Oral	4 mg
Tablet, orally disintegrating	Oral	8 mg
Solution	Intravenous	8 mg
Injection, solution	Parenteral	4 MG
Injection, solution	Parenteral	8 MG
Solution	Intramuscular; Intravenous	9.96 mg
Tablet	Oral
Solution	Intramuscular; Intravenous	4 mg
Solution	Parenteral	4.988 mg
Tablet, coated	Oral	8 mg
Solution	Intravenous	4.00 mg
Solution	Parenteral	8.000 mg
Injection	Parenteral
Solution	Intravenous	8.000 mg
Solution		2.00 mg
Tablet	Oral	4.988 mg
Injection, solution		4 mg/2ml
Injection, solution		8 mg/4ml
Troche	Sublingual
Solution	Parenteral	8 mg
Kit; tablet; tablet, orally disintegrating	Oral
Tablet	Oral	8.0 mg
Tablet, film coated	Oral	9.977 MG
Injection	Intramuscular; Intravenous
Solution	Intravenous	9.997 mg
Solution	Intravenous	8.00 mg
Solution	Intramuscular	2.000 mg
Solution	Intravenous	4 mg
Injection
Solution	Intramuscular; Intravenous	2 mg
Tablet	Oral	800000 mg
Syrup	Oral
Solution	Intravenous	4 mg/2ml
Solution	Intravenous	8 mg/4ml
Injection	Intravenous	2 mg/1mL
Injection, solution	Intramuscular	2 mg/1mL
Injection, solution	Intramuscular; Intravenous	2 mg/1mL
Injection, solution	Intramuscular; Intravenous	4 mg/2mL
Injection, solution	Intravenous	2 mg/1mL
Solution	Oral	4 mg/5mL
Tablet	Oral	24 mg/1
Tablet	Oral	4 mg/1
Tablet	Oral	8 mg/1
Tablet, film coated	Oral	24 mg/1
Tablet, orally disintegrating	Oral	4 mg/1
Tablet, orally disintegrating	Oral	8 mg/1
Injection	Parenteral	4 MG/2ML
Injection	Parenteral	8 MG/4ML
Injection, solution		4 mg
Injection, solution		8 mg
Injection	Parenteral	4 MG
Injection	Parenteral	8 MG
Injection, solution	Parenteral	2 MG/ML
Injection, solution	Parenteral	0.08 MG/ML
Injection, solution	Parenteral	0.16 MG/ML
Injection, solution	Intramuscular; Intravenous	2.000 mg/mL
Solution	Parenteral	0.16 MG/ML
Tablet, orally disintegrating	Oral
Injection, solution	Parenteral	4 MG/2ML
Injection, solution	Parenteral	8 MG/4ML
Injection, solution		2 MG/ML
Tablet, coated	Oral	4 mg/31
Injection		2 mg/ml
Injection	Intramuscular; Intravenous	2 mg/1mL
Solution	Intramuscular; Intravenous	2 mg/1mL
Solution	Intravenous	2 mg/1mL
Tablet, film coated	Oral	16 mg/1
Tablet, film coated	Oral	4 mg/1
Tablet, film coated	Oral	8 mg/1
Injection, solution	Intravenous	32 mg/50mL
Tablet	Oral	4.99 MG
Tablet	Oral	9.98 MG
Tablet, film coated	Oral	4.99 MG
Tablet, film coated	Oral	9.98 MG
Tablet, film coated	Oral	10 MG
Tablet, film coated	Oral	5 MG
Solution	Intravenous	2 mg / mL
Solution	Intravenous	2.00 mg / mL
Solution	Intravenous	4 mg / 2 mL
Solution	Intravenous	8 mg / 4 mL
Solution	Parenteral	0.08 mg/ml
Solution
Injection, solution	Intravenous	2 mg/ml
Solution	Intravenous	2 mg
Injection, solution	Intramuscular; Intravenous	2 mg/ml
Injection, solution	Intravenous	4 MG/2ML
Injection, solution	Intravenous	8 MG/4ML
Injection, solution
Injection, solution	Parenteral
Solution	Intramuscular; Intravenous
Tablet, soluble	Oral
Tablet, soluble	Oral	8 MG
Injection	Intravenous	2 mg/ml
Tablet, coated	Oral	4 mg
Solution	Intramuscular; Intravenous	8 mg
Injection	Intramuscular; Intravenous	2 mg/mL
Film, soluble	Oral	4 mg
Film, soluble	Oral	8 mg
Solution	Parenteral
Solution	Intravenous	9.960 mg
Kit; tablet; tablet, film coated	Oral
Tablet, film coated	Oral
Solution		2 mg/ml
Tablet	Oral	8.000 mg
Tablet	Oral	8 mg
Injection	Intravenous	32 mg/50mL
Injection, solution	Parenteral	40 MG/20ML
Suppository	Rectal	16 MG
Syrup	Oral	4 MG/5ML
Tablet	Oral	10.000 mg
Suppository	Rectal
Injection, solution	Intramuscular; Intravenous
Solution		4 mg
Injection, solution	Intramuscular; Intravenous	8 mg/4ml
Solution		8 mg
Liquid	Intravenous	2 mg / mL
Injection	Intramuscular; Intravenous	4 mg/2ml
Injection	Intramuscular; Intravenous	8 mg/4ml
Tablet	Oral	4 mg / tab
Tablet	Oral	8 mg / tab
Tablet, soluble	Oral	4 mg
Tablet	Oral
Tablet	Oral	4 mg
Film	Oral	4 mg/1
Film	Oral	8 mg/1
Film, soluble	Oral	4 mg/1
Film, soluble	Oral	8 mg/1
Solution		2 mg/1ml
Tablet, film coated	Oral	8 mg
Tablet, film coated	Oral	4 mg
Injection, solution		2 mg/1ml

Prices

Unit description	Cost	Unit
Ondansetron 30 8 mg Dispersible Tablet Box	1158.51USD	box
Zofran ODT 30 4 mg Dispersible Tablet Box	782.26USD	box
Ondansetron 30 4 mg Dispersible Tablet Box	695.53USD	box
Ondansetron hcl powder	177.0USD	g
Ondansetron hcl 24 mg tablet	105.5USD	tablet
Zofran 8 mg tablet	45.16USD	tablet
Zofran odt 8 mg tablet	41.76USD	tablet
Ondansetron hcl 8 mg tablet	40.75USD	tablet
Ondansetron odt 8 mg tablet	37.13USD	tablet
Zofran 4 mg tablet	27.11USD	tablet
Ondansetron hcl 4 mg tablet	25.07USD	tablet
Zofran odt 4 mg tablet	25.07USD	tablet
Zofran 8 mg Tablet	23.02USD	tablet
Zofran Odt 8 mg Disintegrating Tablet	22.49USD	tablet
Ondansetron odt 4 mg tablet	22.3USD	tablet
Zofran 4 mg Tablet	15.09USD	tablet
Zofran Odt 4 mg Disintegrating Tablet	14.74USD	tablet
Zofran 2 mg/ml vial	12.82USD	ml
Zofran 4 mg/2 ml vial	12.82USD	ml
Apo-Ondansetron 8 mg Tablet	12.06USD	tablet
Co Ondansetron 8 mg Tablet	12.06USD	tablet
Jamp-Ondansetron 8 mg Tablet	12.06USD	tablet
Mint-Ondansetron 8 mg Tablet	12.06USD	tablet
Mylan-Ondansetron 8 mg Tablet	12.06USD	tablet
Novo-Ondansetron 8 mg Tablet	12.06USD	tablet
Ondansetron-Odan 8 mg Tablet	12.06USD	tablet
Phl-Ondansetron 8 mg Tablet	12.06USD	tablet
Pms-Ondansetron 8 mg Tablet	12.06USD	tablet
Ran-Ondansetron 8 mg Tablet	12.06USD	tablet
Ratio-Ondansetron 8 mg Tablet	12.06USD	tablet
Sandoz Ondansetron 8 mg Tablet	12.06USD	tablet
Zofran 2 mg/ml	11.12USD	ml
Apo-Ondansetron 4 mg Tablet	7.9USD	tablet
Co Ondansetron 4 mg Tablet	7.9USD	tablet
Jamp-Ondansetron 4 mg Tablet	7.9USD	tablet
Mint-Ondansetron 4 mg Tablet	7.9USD	tablet
Mylan-Ondansetron 4 mg Tablet	7.9USD	tablet
Novo-Ondansetron 4 mg Tablet	7.9USD	tablet
Ondansetron-Odan 4 mg Tablet	7.9USD	tablet
Phl-Ondansetron 4 mg Tablet	7.9USD	tablet
Pms-Ondansetron 4 mg Tablet	7.9USD	tablet
Ran-Ondansetron 4 mg Tablet	7.9USD	tablet
Ratio-Ondansetron 4 mg Tablet	7.9USD	tablet
Sandoz Ondansetron 4 mg Tablet	7.9USD	tablet
Ondansetron (Preservative Free) 2 mg/ml	6.23USD	ml
Ondansetron (Preserved) 2 mg/ml	6.23USD	ml
Ondansetron (Unpreserved) 2 mg/ml	6.23USD	ml
Ondansetron (With Preservative) 2 mg/ml	6.23USD	ml
Ondansetron Omega (Preservative Free) 2 mg/ml	6.23USD	ml
Ondansetron Omega (With Preservative) 2 mg/ml	6.23USD	ml
Ondansetron hcl 4 mg/2 ml vial	3.13USD	ml
Zofran 0.8 mg/ml Solution	2.3USD	ml
Apo-Ondansetron 0.8 mg/ml Solution	1.53USD	ml
Ondansetron 32 mg/50 ml bag	0.86USD	ml
Ondansetron hcl 32 mg/50 ml bg	0.42USD	ml
Ondansetron 40 mg/20 ml vial	0.17USD	ml

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US5344658	No	1994-09-06	2011-09-06
CA2205600	No	2000-05-30	2015-11-20
US5955488	Yes	1999-09-21	2016-05-14
US6063802	Yes	2000-05-16	2016-05-14
US5854270	Yes	1998-12-29	2016-05-20
US9095577	No	2015-08-04	2030-07-13
US8580830	No	2013-11-12	2029-11-23

Properties

State

Solid

Experimental Properties

Property	Value	Source
logP	2.4	Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.248 mg/mL	ALOGPS
logP	2.56	ALOGPS
logP	2.35	Chemaxon
logS	-3.1	ALOGPS
pKa (Strongest Acidic)	16.13	Chemaxon
pKa (Strongest Basic)	7.34	Chemaxon
Physiological Charge	1	Chemaxon
Hydrogen Acceptor Count	2	Chemaxon
Hydrogen Donor Count	0	Chemaxon
Polar Surface Area	39.82 Å2	Chemaxon
Rotatable Bond Count	2	Chemaxon
Refractivity	86.78 m3·mol-1	Chemaxon
Polarizability	33.16 Å3	Chemaxon
Number of Rings	4	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	Yes	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	0.9941
Blood Brain Barrier	+	0.9882
Caco-2 permeable	+	0.8867
P-glycoprotein substrate	Substrate	0.7019
P-glycoprotein inhibitor I	Inhibitor	0.5833
P-glycoprotein inhibitor II	Inhibitor	0.8807
Renal organic cation transporter	Inhibitor	0.7955
CYP450 2C9 substrate	Non-substrate	0.7456
CYP450 2D6 substrate	Substrate	0.8918
CYP450 3A4 substrate	Substrate	0.647
CYP450 1A2 substrate	Inhibitor	0.9107
CYP450 2C9 inhibitor	Non-inhibitor	0.9071
CYP450 2D6 inhibitor	Inhibitor	0.8932
CYP450 2C19 inhibitor	Non-inhibitor	0.9026
CYP450 3A4 inhibitor	Non-inhibitor	0.8309
CYP450 inhibitory promiscuity	High CYP Inhibitory Promiscuity	0.5954
Ames test	Non AMES toxic	0.5463
Carcinogenicity	Non-carcinogens	0.9676
Biodegradation	Not ready biodegradable	0.9884
Rat acute toxicity	2.4555 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.7054
hERG inhibition (predictor II)	Inhibitor	0.7926

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	splash10-00nb-9840000000-3e06f3c6b7dfe3741b9d
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0006-0590000000-1c293e5af06aedfb74e1
LC-MS/MS Spectrum - LC-ESI-QFT , positive	LC-MS/MS	splash10-006x-0790000000-39dfc83ad8c54c21d83d
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-03dl-0690000000-9e5470d5dbf81d3c54d2
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0006-0090000000-f83b00979a2f7b970e96
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-03dl-0190000000-0560b40beb1825c4c377
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-03di-0290000000-40a417b00ddf9f789d9a
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-01qa-3980000000-896d1abbd163f1d033dc
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0gvk-0490000000-a57f5af157112d1dfc95
1H NMR Spectrum	1D NMR	Not Applicable
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable
[1H,13C] 2D NMR Spectrum	2D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å2)	Source type	Source
[M-H]-	181.9766661	predicted	DarkChem Lite v0.1.0
[M-H]-	166.07027	predicted	DeepCCS 1.0 (2019)
[M+H]+	182.0708661	predicted	DarkChem Lite v0.1.0
[M+H]+	168.42827	predicted	DeepCCS 1.0 (2019)
[M+Na]+	181.3861661	predicted	DarkChem Lite v0.1.0
[M+Na]+	174.52142	predicted	DeepCCS 1.0 (2019)

Targets

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Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	0.09	N/A	N/A	A7684
Kd (nM)	0.0794	N/A	N/A	A29189
Kd (nM)	50.12	N/A	N/A	A29189
Kd (nM)	0.398	N/A	N/A	A29189
Ki (nM)	16	N/A	N/A	A29196 / A29197
Ki (nM)	7.6	N/A	N/A	A29198
Ki (nM)	12	N/A	N/A	A27359
Ki (nM)	3.4	N/A	N/A	A29199
Ki (nM)	2.8	N/A	N/A	A7684

Details

Binding Properties1. 5-hydroxytryptamine receptor 3A

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Antagonist

General Function

Voltage-gated potassium channel activity

Specific Function

This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gate...

Gene Name

HTR3A

Uniprot ID

P46098

Uniprot Name

5-hydroxytryptamine receptor 3A

Molecular Weight

55279.835 Da

References

1. Artaiz I, Zazpe A, Del Rio J: Characterization of serotonergic mechanisms involved in the behavioural inhibition induced by 5-hydroxytryptophan in a modified light-dark test in mice. Behav Pharmacol. 1998 Mar;9(2):103-12. [Article]
2. Fortuno A, Ballaz S, Del Rio J, Barber A: CCK-mediated response in the activation of 5-HT receptor types in the guinea-pig ileum. J Physiol Biochem. 1999 Jun;55(2):85-92. [Article]
3. Llacer JM, Gallardo V, Delgado R, Parraga J, Martin D, Ruiz MA: X-ray diffraction and electron microscopy in the polymorphism study of ondansetron hydrochloride. Drug Dev Ind Pharm. 2001 Oct;27(9):899-908. [Article]
4. Carvalho F, Macedo D, Bandeira I, Maldonado I, Salles L, Azevedo MF, Rocha MA Jr, Fregoneze JB, De Castro-e-Silva E: Central 5-HT3 receptor stimulation by m-CPBG increases blood glucose in rats. Horm Metab Res. 2002 Feb;34(2):55-61. [Article]
5. Arcioni R, della Rocca M, Romano S, Romano R, Pietropaoli P, Gasparetto A: Ondansetron inhibits the analgesic effects of tramadol: a possible 5-HT(3) spinal receptor involvement in acute pain in humans. Anesth Analg. 2002 Jun;94(6):1553-7, table of contents. [Article]
6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
7. Gallardo Lara V, Gallardo ML, Morales Hernandez ME, Ruiz Martinez MA: Ondansetron: design and development of oral pharmaceutical suspensions. Pharmazie. 2009 Feb;64(2):90-3. [Article]
8. Mohan KC, Ravikumar K: Ondansetron hydrochloride: a competitive serotonin 5-HT3 receptor blocker. Acta Crystallogr C. 1995 Dec 15;51 ( Pt 12):2627-9. [Article]
9. Dimitrov DH: Effect of Ondansetron, a 5-HT(3) receptor antagonist, on fatigue in 2 veterans with hepatitis C. Prim Care Companion J Clin Psychiatry. 2009;11(6):366-7. doi: 10.4088/PCC.08l00755. [Article]
10. Szajewska H, Gieruszczak-Bialek D, Dylag M: Meta-analysis: ondansetron for vomiting in acute gastroenteritis in children. Aliment Pharmacol Ther. 2007 Feb 15;25(4):393-400. [Article]
11. Ramsook C, Sahagun-Carreon I, Kozinetz CA, Moro-Sutherland D: A randomized clinical trial comparing oral ondansetron with placebo in children with vomiting from acute gastroenteritis. Ann Emerg Med. 2002 Apr;39(4):397-403. [Article]
12. Gregory RE, Ettinger DS: 5-HT3 receptor antagonists for the prevention of chemotherapy-induced nausea and vomiting. A comparison of their pharmacology and clinical efficacy. Drugs. 1998 Feb;55(2):173-89. [Article]
13. Gan TJ: Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same? CNS Drugs. 2005;19(3):225-38. [Article]

Details2. 5-hydroxytryptamine receptor 4

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Agonist

General Function

Serotonin receptor activity

Specific Function

This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...

Gene Name

HTR4

Uniprot ID

Q13639

Uniprot Name

5-hydroxytryptamine receptor 4

Molecular Weight

43760.975 Da

References

1. van Wijngaarden I, Tulp MT, Soudijn W: The concept of selectivity in 5-HT receptor research. Eur J Pharmacol. 1990 Jun 12;188(6):301-12. [Article]

Details3. Mu-type opioid receptor

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Other/unknown

General Function

Voltage-gated calcium channel activity

Specific Function

Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...

Gene Name

OPRM1

Uniprot ID

P35372

Uniprot Name

Mu-type opioid receptor

Molecular Weight

44778.855 Da

References

1. van Wijngaarden I, Tulp MT, Soudijn W: The concept of selectivity in 5-HT receptor research. Eur J Pharmacol. 1990 Jun 12;188(6):301-12. [Article]

Details4. 5-hydroxytryptamine receptor 1A

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Other/unknown

General Function

Serotonin receptor activity

Specific Function

G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...

Gene Name

HTR1A

Uniprot ID

P08908

Uniprot Name

5-hydroxytryptamine receptor 1A

Molecular Weight

46106.335 Da

References

1. van Wijngaarden I, Tulp MT, Soudijn W: The concept of selectivity in 5-HT receptor research. Eur J Pharmacol. 1990 Jun 12;188(6):301-12. [Article]

Details5. 5-hydroxytryptamine receptor 1B

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Other/unknown

General Function

Serotonin receptor activity

Specific Function

G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...

Gene Name

HTR1B

Uniprot ID

P28222

Uniprot Name

5-hydroxytryptamine receptor 1B

Molecular Weight

43567.535 Da

References

1. van Wijngaarden I, Tulp MT, Soudijn W: The concept of selectivity in 5-HT receptor research. Eur J Pharmacol. 1990 Jun 12;188(6):301-12. [Article]

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Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55