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Approved, Withdrawn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
Weight
Average: 293.363
Monoisotopic: 293.152812245
Chemical Formula
C18H19N3O
Synonyms
  • Ondansetron

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 TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Prophylaxis ofChemotherapy-induced nausea and vomiting••••••••••••
Prophylaxis ofChemotherapy-induced nausea and vomiting••••••••••••
Treatment ofCholestatic pruritus••• •••••
Prophylaxis ofPost-operative nausea and vomiting••••••••••••
Treatment ofUremic pruritus••• •••••
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.

TargetActionsOrganism
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.

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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/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Cytochrome P450 2D6CYP2D6*1xN,Not AvailableGene duplication.Effect Directly StudiedPatients 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 2D6CYP2D6*2xNNot AvailableGene duplication.Effect Directly StudiedPatients 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 2D6CYP2D6*1XNNot AvailableNormal allele duplicated.ADR InferredUltra-rapid drug metabolizer. Risk of toxicity, alternative drug recommended.Details
Cytochrome P450 2D6CYP2D6*2XNNot Available2850C>T / 4180G>C  … show all ADR InferredUltra-rapid drug metabolizer. Risk of toxicity, alternative drug recommended.Details
Cytochrome P450 2D6CYP2D6*1XNNot AvailableNormal allele duplicated.Effect InferredPoor responseDetails

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.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Ondansetron is combined with 1,2-Benzodiazepine.
AbametapirThe serum concentration of Ondansetron can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Ondansetron can be increased when combined with Abatacept.
AbirateroneThe serum concentration of Ondansetron can be increased when it is combined with Abiraterone.
AbrocitinibThe 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
IngredientUNIICASInChI Key
Ondansetron hydrochloride2999F27MAD99614-01-4MKBLHFILKIKSQM-UHFFFAOYSA-N
Ondansetron hydrochloride dihydrateNMH84OZK2B103639-04-9VRSLTNZJOUZKLX-UHFFFAOYSA-N
Product Images
International/Other Brands
Zophren
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Athena-ondansetron ODTTablet, orally disintegrating8 mgOralAthena Pharmaceutiques Sas2015-11-23Not applicableCanada flag
Athena-ondansetron ODTTablet, orally disintegrating4 mgOralAthena Pharmaceutiques Sas2015-11-23Not applicableCanada flag
OndansetronTablet4 mgOralSanis Health Inc2014-03-18Not applicableCanada flag
OndansetronTablet4 mgOralPro Doc LimiteeNot applicableNot applicableCanada flag
OndansetronInjection, solution32 mg/50mLIntravenousBaxter Laboratories2006-12-272012-07-25US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Accel-ondansetronTablet4 mgOralAccel Pharma Inc2019-09-19Not applicableCanada flag
Accel-ondansetronTablet8 mgOralAccel Pharma Inc2019-09-19Not applicableCanada flag
Accel-ondansetron ODTTablet, orally disintegrating8 mgOralAccel Pharma Inc2023-12-19Not applicableCanada flag
Accel-ondansetron ODTTablet, orally disintegrating4 mgOralAccel Pharma Inc2023-12-19Not applicableCanada flag
Ag-ondansetronTablet8 mgOralAngita Pharma Inc.Not applicableNot applicableCanada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Mpm PakOndansetron (8 mg/1) + Ibuprofen (800 mg/1) + Mifepristone (200 mg/1) + Misoprostol (200 ug/1)Kit; Tablet; Tablet, orally disintegratingOralNucare Pharmaceuticals,inc.2023-02-24Not applicableUS flag
Mpm PakOndansetron (8 mg/1) + Ibuprofen (800 mg/1) + Mifepristone (200 mg/1) + Misoprostol (200 ug/1)Kit; Tablet; Tablet, orally disintegratingOralNucare Pharmaceuticals,inc.2023-06-14Not applicableUS flag
Mpm PakOndansetron (8 mg/1) + Ibuprofen (800 mg/1) + Mifepristone (200 mg/1) + Misoprostol (200 ug/1)Kit; Tablet; Tablet, orally disintegratingOralNucare Pharmaceuticals,inc.2023-02-24Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
MKO MeltOndansetron hydrochloride dihydrate (2 mg/1) + Ketamine hydrochloride (25 mg/1) + Midazolam (3 mg/1)TrocheSublingualImprimis Njof, Llc2018-12-012019-03-04US flag
MKO Melt Dose PackOndansetron hydrochloride (2 mg/1) + Ketamine hydrochloride (25 mg/1) + Midazolam (3 mg/1)TrocheSublingualImprimis Njof, Llc2019-03-04Not applicableUS flag
OndansetronOndansetron (8 mg/1)Tablet, orally disintegratingOralRemedy Repack2015-02-262015-12-30US flag
SumansetronOndansetron hydrochloride dihydrate (4 mg/1) + Sumatriptan succinate (50 mg/1)Kit; Tablet; Tablet, film coatedOralPureTek Corporation2021-01-01Not applicableUS flag
ZOPHRALEN 8 MG/4ML IV AMPULOndansetron (8 mg/4ml)Injection, solutionIntravenousDEM İLAÇ SAN. VE TİC. A.Ş.2018-12-25Not applicableTurkey flag

Categories

ATC Codes
A04AA01 — Ondansetron
Drug Categories
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
show 3 more
Substituents
Aromatic heteropolycyclic compound / Aryl alkyl ketone / Aryl ketone / Azacycle / Azole / Benzenoid / Carbazole / Heteroaromatic compound / Hydrocarbon derivative / Imidazole
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]
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

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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
FormRouteStrength
SolutionOral4 mg / 5 mL
Tablet, orally disintegratingOral4 mg
Tablet, orally disintegratingOral8 mg
SolutionIntravenous8 mg
Injection, solutionParenteral4 MG
Injection, solutionParenteral8 MG
SolutionIntramuscular; Intravenous9.96 mg
TabletOral
SolutionIntramuscular; Intravenous4 mg
SolutionParenteral4.988 mg
Tablet, coatedOral8 mg
SolutionIntravenous4.00 mg
SolutionParenteral8.000 mg
InjectionParenteral
SolutionIntravenous8.000 mg
Solution2.00 mg
TabletOral4.988 mg
Injection, solution4 mg/2ml
Injection, solution8 mg/4ml
TrocheSublingual
SolutionParenteral8 mg
Kit; tablet; tablet, orally disintegratingOral
TabletOral8.0 mg
Tablet, film coatedOral9.977 MG
InjectionIntramuscular; Intravenous
SolutionIntravenous9.997 mg
SolutionIntravenous8.00 mg
SolutionIntramuscular2.000 mg
SolutionIntravenous4 mg
Injection
SolutionIntramuscular; Intravenous2 mg
TabletOral800000 mg
SyrupOral
SolutionIntravenous4 mg/2ml
SolutionIntravenous8 mg/4ml
InjectionIntravenous2 mg/1mL
Injection, solutionIntramuscular2 mg/1mL
Injection, solutionIntramuscular; Intravenous2 mg/1mL
Injection, solutionIntramuscular; Intravenous4 mg/2mL
Injection, solutionIntravenous2 mg/1mL
SolutionOral4 mg/5mL
TabletOral24 mg/1
TabletOral4 mg/1
TabletOral8 mg/1
Tablet, film coatedOral24 mg/1
Tablet, orally disintegratingOral4 mg/1
Tablet, orally disintegratingOral8 mg/1
InjectionParenteral4 MG/2ML
InjectionParenteral8 MG/4ML
Injection, solution4 mg
Injection, solution8 mg
InjectionParenteral4 MG
InjectionParenteral8 MG
Injection, solutionParenteral2 MG/ML
Injection, solutionParenteral0.08 MG/ML
Injection, solutionParenteral0.16 MG/ML
Injection, solutionIntramuscular; Intravenous2.000 mg/mL
SolutionParenteral0.16 MG/ML
Tablet, orally disintegratingOral
Injection, solutionParenteral4 MG/2ML
Injection, solutionParenteral8 MG/4ML
Injection, solution2 MG/ML
Tablet, coatedOral4 mg/31
Injection2 mg/ml
InjectionIntramuscular; Intravenous2 mg/1mL
SolutionIntramuscular; Intravenous2 mg/1mL
SolutionIntravenous2 mg/1mL
Tablet, film coatedOral16 mg/1
Tablet, film coatedOral4 mg/1
Tablet, film coatedOral8 mg/1
Injection, solutionIntravenous32 mg/50mL
TabletOral4.99 MG
TabletOral9.98 MG
Tablet, film coatedOral4.99 MG
Tablet, film coatedOral9.98 MG
Tablet, film coatedOral10 MG
Tablet, film coatedOral5 MG
SolutionIntravenous2 mg / mL
SolutionIntravenous2.00 mg / mL
SolutionIntravenous4 mg / 2 mL
SolutionIntravenous8 mg / 4 mL
SolutionParenteral0.08 mg/ml
Solution
Injection, solutionIntravenous2 mg/ml
SolutionIntravenous2 mg
Injection, solutionIntramuscular; Intravenous2 mg/ml
Injection, solutionIntravenous4 MG/2ML
Injection, solutionIntravenous8 MG/4ML
Injection, solution
Injection, solutionParenteral
SolutionIntramuscular; Intravenous
Tablet, solubleOral
Tablet, solubleOral8 MG
InjectionIntravenous2 mg/ml
Tablet, coatedOral4 mg
SolutionIntramuscular; Intravenous8 mg
InjectionIntramuscular; Intravenous2 mg/mL
Film, solubleOral4 mg
Film, solubleOral8 mg
SolutionParenteral
SolutionIntravenous9.960 mg
Kit; tablet; tablet, film coatedOral
Tablet, film coatedOral
Solution2 mg/ml
TabletOral8.000 mg
TabletOral8 mg
InjectionIntravenous32 mg/50mL
Injection, solutionParenteral40 MG/20ML
SuppositoryRectal16 MG
SyrupOral4 MG/5ML
TabletOral10.000 mg
SuppositoryRectal
Injection, solutionIntramuscular; Intravenous
Solution4 mg
Injection, solutionIntramuscular; Intravenous8 mg/4ml
Solution8 mg
LiquidIntravenous2 mg / mL
InjectionIntramuscular; Intravenous4 mg/2ml
InjectionIntramuscular; Intravenous8 mg/4ml
TabletOral4 mg / tab
TabletOral8 mg / tab
Tablet, solubleOral4 mg
TabletOral
TabletOral4 mg
FilmOral4 mg/1
FilmOral8 mg/1
Film, solubleOral4 mg/1
Film, solubleOral8 mg/1
Solution2 mg/1ml
Tablet, film coatedOral8 mg
Tablet, film coatedOral4 mg
Injection, solution2 mg/1ml
Prices
Unit descriptionCostUnit
Ondansetron 30 8 mg Dispersible Tablet Box1158.51USD box
Zofran ODT 30 4 mg Dispersible Tablet Box782.26USD box
Ondansetron 30 4 mg Dispersible Tablet Box695.53USD box
Ondansetron hcl powder177.0USD g
Ondansetron hcl 24 mg tablet105.5USD tablet
Zofran 8 mg tablet45.16USD tablet
Zofran odt 8 mg tablet41.76USD tablet
Ondansetron hcl 8 mg tablet40.75USD tablet
Ondansetron odt 8 mg tablet37.13USD tablet
Zofran 4 mg tablet27.11USD tablet
Ondansetron hcl 4 mg tablet25.07USD tablet
Zofran odt 4 mg tablet25.07USD tablet
Zofran 8 mg Tablet23.02USD tablet
Zofran Odt 8 mg Disintegrating Tablet22.49USD tablet
Ondansetron odt 4 mg tablet22.3USD tablet
Zofran 4 mg Tablet15.09USD tablet
Zofran Odt 4 mg Disintegrating Tablet14.74USD tablet
Zofran 2 mg/ml vial12.82USD ml
Zofran 4 mg/2 ml vial12.82USD ml
Apo-Ondansetron 8 mg Tablet12.06USD tablet
Co Ondansetron 8 mg Tablet12.06USD tablet
Jamp-Ondansetron 8 mg Tablet12.06USD tablet
Mint-Ondansetron 8 mg Tablet12.06USD tablet
Mylan-Ondansetron 8 mg Tablet12.06USD tablet
Novo-Ondansetron 8 mg Tablet12.06USD tablet
Ondansetron-Odan 8 mg Tablet12.06USD tablet
Phl-Ondansetron 8 mg Tablet12.06USD tablet
Pms-Ondansetron 8 mg Tablet12.06USD tablet
Ran-Ondansetron 8 mg Tablet12.06USD tablet
Ratio-Ondansetron 8 mg Tablet12.06USD tablet
Sandoz Ondansetron 8 mg Tablet12.06USD tablet
Zofran 2 mg/ml11.12USD ml
Apo-Ondansetron 4 mg Tablet7.9USD tablet
Co Ondansetron 4 mg Tablet7.9USD tablet
Jamp-Ondansetron 4 mg Tablet7.9USD tablet
Mint-Ondansetron 4 mg Tablet7.9USD tablet
Mylan-Ondansetron 4 mg Tablet7.9USD tablet
Novo-Ondansetron 4 mg Tablet7.9USD tablet
Ondansetron-Odan 4 mg Tablet7.9USD tablet
Phl-Ondansetron 4 mg Tablet7.9USD tablet
Pms-Ondansetron 4 mg Tablet7.9USD tablet
Ran-Ondansetron 4 mg Tablet7.9USD tablet
Ratio-Ondansetron 4 mg Tablet7.9USD tablet
Sandoz Ondansetron 4 mg Tablet7.9USD tablet
Ondansetron (Preservative Free) 2 mg/ml6.23USD ml
Ondansetron (Preserved) 2 mg/ml6.23USD ml
Ondansetron (Unpreserved) 2 mg/ml6.23USD ml
Ondansetron (With Preservative) 2 mg/ml6.23USD ml
Ondansetron Omega (Preservative Free) 2 mg/ml6.23USD ml
Ondansetron Omega (With Preservative) 2 mg/ml6.23USD ml
Ondansetron hcl 4 mg/2 ml vial3.13USD ml
Zofran 0.8 mg/ml Solution2.3USD ml
Apo-Ondansetron 0.8 mg/ml Solution1.53USD ml
Ondansetron 32 mg/50 ml bag0.86USD ml
Ondansetron hcl 32 mg/50 ml bg0.42USD ml
Ondansetron 40 mg/20 ml vial0.17USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5344658No1994-09-062011-09-06US flag
CA2205600No2000-05-302015-11-20Canada flag
US5955488Yes1999-09-212016-05-14US flag
US6063802Yes2000-05-162016-05-14US flag
US5854270Yes1998-12-292016-05-20US flag
US9095577No2015-08-042030-07-13US flag
US8580830No2013-11-122029-11-23US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP2.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.248 mg/mLALOGPS
logP2.56ALOGPS
logP2.35Chemaxon
logS-3.1ALOGPS
pKa (Strongest Acidic)16.13Chemaxon
pKa (Strongest Basic)7.34Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count2Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area39.82 Å2Chemaxon
Rotatable Bond Count2Chemaxon
Refractivity86.78 m3·mol-1Chemaxon
Polarizability33.16 Å3Chemaxon
Number of Rings4Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleYesChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9941
Blood Brain Barrier+0.9882
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.7019
P-glycoprotein inhibitor IInhibitor0.5833
P-glycoprotein inhibitor IIInhibitor0.8807
Renal organic cation transporterInhibitor0.7955
CYP450 2C9 substrateNon-substrate0.7456
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.647
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5954
Ames testNon AMES toxic0.5463
CarcinogenicityNon-carcinogens0.9676
BiodegradationNot ready biodegradable0.9884
Rat acute toxicity2.4555 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7054
hERG inhibition (predictor II)Inhibitor0.7926
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-00nb-9840000000-3e06f3c6b7dfe3741b9d
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0006-0590000000-1c293e5af06aedfb74e1
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-006x-0790000000-39dfc83ad8c54c21d83d
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-03dl-0690000000-9e5470d5dbf81d3c54d2
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-0090000000-f83b00979a2f7b970e96
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-03dl-0190000000-0560b40beb1825c4c377
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-03di-0290000000-40a417b00ddf9f789d9a
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-01qa-3980000000-896d1abbd163f1d033dc
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0gvk-0490000000-a57f5af157112d1dfc95
1H NMR Spectrum1D NMRNot Applicable
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[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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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]
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]
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]
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]
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]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Dixon CM, Colthup PV, Serabjit-Singh CJ, Kerr BM, Boehlert CC, Park GR, Tarbit MH: Multiple forms of cytochrome P450 are involved in the metabolism of ondansetron in humans. Drug Metab Dispos. 1995 Nov;23(11):1225-30. [Article]
  2. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Niwa T, Yamamoto S, Saito M, Kobayashi N, Ikeda K, Noda Y, Takagi A: Effects of serotonin-3 receptor antagonists on cytochrome P450 activities in human liver microsomes. Biol Pharm Bull. 2006 Sep;29(9):1931-5. [Article]
  2. Dixon CM, Colthup PV, Serabjit-Singh CJ, Kerr BM, Boehlert CC, Park GR, Tarbit MH: Multiple forms of cytochrome P450 are involved in the metabolism of ondansetron in humans. Drug Metab Dispos. 1995 Nov;23(11):1225-30. [Article]
  3. Zofran FDA [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Janicki PK: Cytochrome P450 2D6 metabolism and 5-hydroxytryptamine type 3 receptor antagonists for postoperative nausea and vomiting. Med Sci Monit. 2005 Oct;11(10):RA322-8. Epub 2005 Sep 26. [Article]
  2. Dixon CM, Colthup PV, Serabjit-Singh CJ, Kerr BM, Boehlert CC, Park GR, Tarbit MH: Multiple forms of cytochrome P450 are involved in the metabolism of ondansetron in humans. Drug Metab Dispos. 1995 Nov;23(11):1225-30. [Article]
  3. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
This enzyme action is supported by data from 1 in vitro study available in the literature.
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Sanwald P, David M, Dow J: Characterization of the cytochrome P450 enzymes involved in the in vitro metabolism of dolasetron. Comparison with other indole-containing 5-HT3 antagonists. Drug Metab Dispos. 1996 May;24(5):602-9. [Article]

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