Chemical: Drug
ondansetron

PharmGKB contains no dosing guidelines for this . To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.



Clinical Variants that meet the highest level of criteria, manually curated by PharmGKB, are shown below.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for ondansetron

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA CYP2D6 *1 N/A N/A N/A
No VIP available CA VA CYP2D6 *1xN N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *2 N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *2xN N/A N/A N/A
No VIP available No VIP available VA CYP2D6 *10 N/A N/A N/A
No VIP available CA VA SLC6A4 HTTLPR long form (L allele) N/A N/A N/A
No VIP available CA VA SLC6A4 HTTLPR short form (S allele) N/A N/A N/A
No VIP available No Clinical Annotations available VA
CYP2D6 poor metabolizer N/A N/A N/A
No VIP available No Clinical Annotations available VA
CYP2D6 ultrarapid metabolizer genotype N/A N/A N/A
No VIP available CA VA
rs1042173 NC_000017.10:g.28525011A>C, NC_000017.11:g.30197993A>C, NG_011747.2:g.42944T>G, NM_001045.5:c.*463T>G, XM_005258025.1:c.*463T>G, rs17825889, rs60303970
A > C
SNP
No VIP available CA VA
rs1045642 NC_000007.13:g.87138645A>G, NC_000007.14:g.87509329A>G, NG_011513.1:g.208920T>C, NM_000927.4:c.3435T>C, NP_000918.2:p.Ile1145=, rs10239679, rs11568726, rs117328163, rs17210003, rs2229108, rs386513066, rs60023214, rs9690664
A > G
SNP
I1145I
VIP No Clinical Annotations available No Variant Annotations available
rs12208357 NC_000006.11:g.160543148C>T, NC_000006.12:g.160122116C>T, NM_003057.2:c.181C>T, NM_153187.1:c.181C>T, NP_003048.1:p.Arg61Cys, NP_694857.1:p.Arg61Cys, XM_005267102.1:c.181C>T, XM_005267102.3:c.181C>T, XM_005267103.1:c.181C>T, XM_005267105.1:c.-485C>T, XM_005267105.3:c.-485C>T, XM_006715552.1:c.181C>T, XM_011536074.1:c.-895C>T, XP_005267159.1:p.Arg61Cys, XP_005267160.1:p.Arg61Cys, XP_006715615.1:p.Arg61Cys, rs56982873
C > T
SNP
R61C
No VIP available CA VA
rs2032582 NC_000007.13:g.87160618A>C, NC_000007.13:g.87160618A>T, NC_000007.14:g.87531302A>C, NC_000007.14:g.87531302A>T, NG_011513.1:g.186947T>A, NG_011513.1:g.186947T>G, NM_000927.4:c.2677T>A, NM_000927.4:c.2677T>G, NP_000918.2:p.Ser893Ala, NP_000918.2:p.Ser893Thr, rs10228331, rs2229106, rs386553610, rs57135550, rs9641018
A > C
SNP
S893A
VIP No Clinical Annotations available No Variant Annotations available
rs34059508 NC_000006.11:g.160575837G>A, NC_000006.12:g.160154805G>A, NM_003057.2:c.1393G>A, NM_153187.1:c.1386-1170G>A, NP_003048.1:p.Gly465Arg, XM_005267102.1:c.1393G>A, XM_005267102.3:c.1393G>A, XM_005267103.1:c.1393G>A, XM_005267104.1:c.817G>A, XM_005267104.3:c.817G>A, XM_005267105.1:c.817G>A, XM_005267105.3:c.817G>A, XM_006715552.1:c.1386-3711G>A, XM_011536074.1:c.817G>A, XP_005267159.1:p.Gly465Arg, XP_005267160.1:p.Gly465Arg, XP_005267161.1:p.Gly273Arg, XP_005267162.1:p.Gly273Arg, XP_011534376.1:p.Gly273Arg, rs45476695, rs57829971
G > A
SNP
G465R
VIP No Clinical Annotations available No Variant Annotations available
rs34130495 NC_000006.11:g.160560824G>A, NC_000006.12:g.160139792G>A, NM_003057.2:c.1201G>A, NM_153187.1:c.1201G>A, NP_003048.1:p.Gly401Ser, NP_694857.1:p.Gly401Ser, XM_005267102.1:c.1201G>A, XM_005267102.3:c.1201G>A, XM_005267103.1:c.1201G>A, XM_005267104.1:c.625G>A, XM_005267104.3:c.625G>A, XM_005267105.1:c.625G>A, XM_005267105.3:c.625G>A, XM_006715552.1:c.1201G>A, XM_011536074.1:c.625G>A, XP_005267159.1:p.Gly401Ser, XP_005267160.1:p.Gly401Ser, XP_005267161.1:p.Gly209Ser, XP_005267162.1:p.Gly209Ser, XP_006715615.1:p.Gly401Ser, XP_011534376.1:p.Gly209Ser, rs45512393
G > A
SNP
G401S
VIP No Clinical Annotations available No Variant Annotations available
rs72552763 NC_000006.11:g.160560883_160560885delGAT, NC_000006.12:g.160139851_160139853delGAT, NM_003057.2:c.1260_1262delGAT, NM_153187.1:c.1260_1262delGAT, NP_003048.1:p.Met420del, NP_694857.1:p.Met420del, XM_005267102.1:c.1260_1262delGAT, XM_005267102.3:c.1260_1262delGAT, XM_005267103.1:c.1260_1262delGAT, XM_005267104.1:c.684_686delGAT, XM_005267104.3:c.684_686delGAT, XM_005267105.1:c.684_686delGAT, XM_005267105.3:c.684_686delGAT, XM_006715552.1:c.1260_1262delGAT, XM_011536074.1:c.684_686delGAT, XP_005267159.1:p.Met420del, XP_005267160.1:p.Met420del, XP_005267161.1:p.Met228del, XP_005267162.1:p.Met228del, XP_006715615.1:p.Met420del, XP_011534376.1:p.Met228del
GAT > -
indel
rs776746 NC_000007.13:g.99270539C>T, NC_000007.14:g.99672916T>C, NG_007938.1:g.12083G=, NG_007938.1:g.12083G>A, NM_000777.4:c.219-237A>G, NM_000777.4:c.219-237G>A, NM_001190484.2:c.219-237A>G, NM_001190484.2:c.219-237G>A, NM_001291829.1:c.-253-1A>G, NM_001291829.1:c.-253-1G>A, NM_001291830.1:c.189-237A>G, NM_001291830.1:c.189-237G>A, NR_033807.2:n.717-1A>G, NR_033807.2:n.717-1G>A, NR_033808.1:n.689-1G>A, NR_033809.1:n.581-237G>A, NR_033810.1:n.689-1G>A, NR_033811.1:n.321-1G>A, NR_033812.1:n.321-1G>A, XM_005250169.1:c.189-237G>A, XM_005250170.1:c.-357-1G>A, XM_005250171.1:c.-253-1G>A, XM_005250172.1:c.-254G>A, XM_005250173.1:c.-331-237G>A, XM_005250198.1:c.806-4288C>T, XM_006715859.2:c.219-237A>G, XM_011515843.1:c.-254A>G, XM_011515844.1:c.-229-237A>G, XM_011515845.1:c.-463-1A>G, XM_011515846.1:c.-331-237A>G, XM_011515847.1:c.-571-1A>G, XR_927383.1:n.344-237A>G, XR_927402.1:n.1466+48736T>C, rs10361242, rs11266830, rs386613022, rs58244770
C > T
SNP
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
Trade Names
  • Apo-ondansetron
  • Novo-ondansetron
  • PHL-ondansetron
  • PMS-ondansetron
  • Ratio-ondansetron
  • Sandoz ondansetron
  • Zofran
  • Zofran ODT
  • Zophren
  • Zudan
Brand Mixture Names

PharmGKB Accession Id

PA450705

Type(s):

Drug

Description

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.

Source: Drug Bank

Indication

For the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy, postoperation, and radiation. Also used for the treatment of postoperative nausea and vomiting.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Ondansetron is a selective serotonin 5-HT 3 receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT 3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT 3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.

Source: Drug Bank

Pharmacology

Ondansetron is a highly specific and selective serotonin 5-HT 3 receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. The serontonin 5-HT 3 receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. 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. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT 3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.

Source: Drug Bank

Food Interaction

Take without regard to meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic

Source: Drug Bank

Protein Binding

70%-76% (Plasma protein binding)

Source: Drug Bank

Absorption

Ondansetron is well absorbed after oral administration and undergoes limited first-pass metabolism.

Source: Drug Bank

Half-Life

5.7 hours

Source: Drug Bank

Toxicity

Low blood pressure and fainting, sudden blindness, severe constipation

Source: Drug Bank

Chemical Properties

Chemical Formula

C18H19N3O

Source: Drug Bank

Isomeric SMILES

Cc1nccn1CC2CCc3c(c4ccccc4n3C)C2=O

Source: OpenEye

Canonical SMILES

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

Source: Drug Bank

Average Molecular Weight

293.363

Source: Drug Bank

Monoisotopic Molecular Weight

293.152812245

Source: Drug Bank

SMILES

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

Source: Drug Bank

InChI String

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

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
HTR1A (source: Drug Bank)
HTR1B (source: Drug Bank)
HTR3A (source: Drug Bank)
HTR4 (source: Drug Bank)
HTR6 (source: Drug Bank)
OPRM1 (source: Drug Bank)
No related drugs are available.

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
May Prevent
Contraindicated With

Publications related to ondansetron: 22

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Development of Human Membrane Transporters: Drug Disposition and Pharmacogenetics. Clinical pharmacokinetics. 2015. Mooij Miriam G, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Serotonergic gene variation in substance use pharmacotherapy: a systematic review. Pharmacogenomics. 2015. Bauer Isabelle E, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Subjective response as a consideration in the pharmacogenetics of alcoholism treatment. Pharmacogenomics. 2015. Roche Daniel Jo, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association of ABCB1 polymorphisms with the efficacy of ondansetron in chemotherapy-induced nausea and vomiting. Clinical therapeutics. 2014. He Hui, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association of ABCB1, 5-HT3B receptor and CYP2D6 genetic polymorphisms with ondansetron and metoclopramide antiemetic response in Indonesian cancer patients treated with highly emetogenic chemotherapy. Japanese journal of clinical oncology. 2011. Perwitasari Dyah A, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
CYP2D6- and CYP3A-dependent enantioselective plasma concentrations of ondansetron in postanesthesia care. Anesthesia and analgesia. 2011. Stamer Ulrike M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. Journal of medicinal chemistry. 2011. Kido Yasuto, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura M, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pharmacogenetic approach at the serotonin transporter gene as a method of reducing the severity of alcohol drinking. The American journal of psychiatry. 2011. Johnson Bankole A, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Antagonistic effects of ondansetron and tramadol? A randomized placebo and active drug controlled study. The journal of pain : official journal of the American Pain Society. 2010. Rauers Neele I, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Association of ABCB1 polymorphisms with the efficacy of ondansetron for postoperative nausea and vomiting. Anaesthesia. 2010. Choi E M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Effects of OCT1 polymorphisms on the cellular uptake, plasma concentrations and efficacy of the 5-HT(3) antagonists tropisetron and ondansetron. The pharmacogenomics journal. 2010. Tzvetkov M V, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The influence of ondansetron on the analgesic effect of acetaminophen after laparoscopic hysterectomy. Clinical pharmacology and therapeutics. 2010. Jokela R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Machine learning methods and docking for predicting human pregnane X receptor activation. Chemical research in toxicology. 2008. Khandelwal Akash, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica; the fate of foreign compounds in biological systems. 2008. Zhou S-F. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Serotonin type 3 receptor genes: HTR3A, B, C, D, E. Pharmacogenomics. 2008. Niesler Beate, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
The impact of pharmacogenomics on postoperative nausea and vomiting: do CYP2D6 allele copy number and polymorphisms affect the success or failure of ondansetron prophylaxis?. Anesthesiology. 2005. Candiotti Keith A, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Patient-tailored antiemetic treatment with 5-hydroxytryptamine type 3 receptor antagonists according to cytochrome P-450 2D6 genotypes. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2002. Kaiser Rolf, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Multiple forms of cytochrome P450 are involved in the metabolism of ondansetron in humans. Drug metabolism and disposition: the biological fate of chemicals. 1995. Dixon C M, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
The pharmacokinetics of ondansetron after intravenous injection in healthy volunteers phenotyped as poor or extensive metabolisers of debrisoquine. British journal of clinical pharmacology. 1994. Ashforth E I, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The polymorphic cytochrome P-4502D6 is involved in the metabolism of both 5-hydroxytryptamine antagonists, tropisetron and ondansetron. Drug metabolism and disposition: the biological fate of chemicals. 1994. Fischer V, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0338-1762-41
DrugBank:
DB00904
KEGG Compound:
C07325
KEGG Drug:
D00456
PubChem Compound:
4595
PubChem Substance:
194568
46504819
IUPHAR Ligand:
2290
Drugs Product Database (DPD):
2239372
BindingDB:
50000493
ChemSpider:
4434
Therapeutic Targets Database:
DAP000221
FDA Drug Label at DailyMed:
8e66d883-2977-46c3-be24-41eba7a903b3

Clinical Trials

These are trials that mention ondansetron and are related to either pharmacogenetics or pharmacogenomics.

No trials found.

Common Searches

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Sources for PharmGKB drug information: DrugBank, PubChem.