Identification

Name
Ondansetron
Accession Number
DB00904  (APRD00481)
Type
Small Molecule
Groups
Approved
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. [PubChem]

Structure
Thumb
Synonyms
Not Available
Product Ingredients
IngredientUNIICASInChI Key
Ondansetron hydrochloride2999F27MAD99614-01-4MKBLHFILKIKSQM-UHFFFAOYSA-N
Ondansetron hydrochloride dihydrateNMH84OZK2B103639-04-9VRSLTNZJOUZKLX-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act OndansetronTablet8 mgOralActavis Pharma Company2009-06-29Not applicableCanada
Act OndansetronTablet4 mgOralActavis Pharma Company2009-06-29Not applicableCanada
OndansetronSolution4 mgOralAa Pharma Inc2008-03-04Not applicableCanada
OndansetronTablet8 mgOralMeliapharm Inc2011-04-082014-06-25Canada
OndansetronTablet8 mgOralSanis Health Inc2014-03-18Not applicableCanada
OndansetronTablet4 mgOralSanis Health Inc2014-03-18Not applicableCanada
OndansetronTablet8 mgOralPro Doc Limitee2009-06-25Not applicableCanada
OndansetronTablet4 mgOralMeliapharm Inc2011-04-082014-06-25Canada
OndansetronInjection, solution32 mg/50mLIntravenousBaxter Laboratories2006-12-272012-07-25Us
Ondansetron HydrochlorideTablet, film coated24 mg/1OralMylan Pharmaceuticals Inc.2008-01-242008-01-24Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ag-ondansetronTablet8 mgOralAngita Pharma Inc.Not applicableNot applicableCanada
Ag-ondansetronTablet4 mgOralAngita Pharma Inc.Not applicableNot applicableCanada
Apo-ondansetronTablet4 mgOralApotex Corporation2006-11-16Not applicableCanada
Apo-ondansetronTablet8 mgOralApotex Corporation2006-11-16Not applicableCanada
Ava-ondansetronTablet8 mgOralAvanstra Inc2011-08-182016-09-02Canada
Bio-ondansetronTablet8 mgOralBiomed PharmaNot applicableNot applicableCanada
Bio-ondansetronTablet4 mgOralBiomed PharmaNot applicableNot applicableCanada
Ccp-ondansetronTablet4 mgOralCellchem Pharmaceuticals Inc.2017-07-24Not applicableCanada
Ccp-ondansetronTablet8 mgOralCellchem Pharmaceuticals Inc.2017-07-24Not applicableCanada
Dom-ondansetronTablet8 mgOralDominion Pharmacal2008-04-17Not applicableCanada
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
OndansetronOndansetron (8 mg/1)Tablet, orally disintegratingOralRemedy Repack2015-02-262015-12-30Us
International/Other Brands
Zofran odt / Zophren
Categories
UNII
4AF302ESOS
CAS number
99614-02-5
Weight
Average: 293.363
Monoisotopic: 293.152812245
Chemical Formula
C18H19N3O
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

Pharmacology

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.

Associated Conditions
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. The serontonin 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. 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-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.

Mechanism of action

Ondansetron is a selective serotonin 5-HT3 receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 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.

TargetActionsOrganism
A5-hydroxytryptamine receptor 3A
antagonist
Human
U5-hydroxytryptamine receptor 4
agonist
Human
UMu-type opioid receptor
other/unknown
Human
U5-hydroxytryptamine receptor 1A
other/unknown
Human
U5-hydroxytryptamine receptor 1B
other/unknown
Human
Absorption

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

Volume of distribution
Not Available
Protein binding

70%-76% (Plasma protein binding)

Metabolism

Hepatic

Route of elimination
Not Available
Half life

5.7 hours

Clearance
  • 0.38 L/h/kg [Normal Adult Volunteers (19-40 yrs)]
  • 0.32 L/h/kg [Normal Adult Volunteers (61-74 yrs)]
  • 0.26 L/h/kg [Normal Adult Volunteers (>=75 yrs)]
Toxicity

Low blood pressure and fainting, sudden blindness, severe constipation

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
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
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Ondansetron.
(S)-WarfarinThe risk or severity of adverse effects can be increased when Ondansetron is combined with (S)-Warfarin.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when Ondansetron is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of serotonin syndrome can be increased when Ondansetron is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of serotonin syndrome can be increased when Ondansetron is combined with 3,4-Methylenedioxyamphetamine.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Ondansetron.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of serotonin syndrome can be increased when Ondansetron is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Ondansetron.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Ondansetron is combined with 4-Methoxyamphetamine.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Ondansetron.
Food Interactions
  • Take without regard to meals.

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. [PubMed:11919526]
  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 . [PubMed:19758398]
  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. [PubMed:9506240]
  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. [PubMed:15740177]
External Links
Human Metabolome Database
HMDB0005035
KEGG Drug
D00456
KEGG Compound
C07325
PubChem Compound
4595
PubChem Substance
46504819
ChemSpider
4434
BindingDB
85330
ChEBI
7773
ChEMBL
CHEMBL46
Therapeutic Targets Database
DAP000221
PharmGKB
PA450705
IUPHAR
2290
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Ondansetron
ATC Codes
A04AA01 — Ondansetron
AHFS Codes
  • 56:22.20 — 5-HT3 Receptor Antagonists
FDA label
Download (126 KB)
MSDS
Download (53.2 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedSupportive CareNausea / Vomiting1
0CompletedTreatmentDyspnea1
0RecruitingSupportive CareNausea / Vomiting1
1CompletedNot AvailableHealthy Volunteers9
1CompletedBasic ScienceBrain Function / Healthy Adults1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedDiagnosticAlcohol Dependence1
1CompletedOtherChemotherapy-Induced Nausea and Vomiting (CINV) / Nausea and Vomiting, Postoperative1
1CompletedOtherPost-Operative Nausea and Vomiting (PONV)1
1CompletedPreventionChemotherapy-Induced Nausea and Vomiting (CINV) / Healthy Volunteers1
1CompletedTreatmentChemotherapy-Induced Nausea and Vomiting (CINV)3
1CompletedTreatmentConcussion, Brain / Traumatic Brain Injury (TBI)1
1CompletedTreatmentFasting State1
1CompletedTreatmentFed1
1CompletedTreatmentGastroenteritis1
1CompletedTreatmentHealthy Volunteers4
1CompletedTreatmentMultiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL) / Tumors, Solid1
1CompletedTreatmentNausea3
1CompletedTreatmentNausea / Vomiting2
1CompletedTreatmentPost-Operative Nausea and Vomiting (PONV)1
1RecruitingTreatmentTumors, Solid1
1TerminatedNot AvailableSchizophrenic Disorders1
1TerminatedTreatmentChemotherapy-Induced Nausea and Vomiting (CINV)1
1Unknown StatusTreatmentPsychosis Not Otherwise Specified / Schizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder1
1, 2CompletedNot AvailablePost-Operative Nausea and Vomiting (PONV)1
2Active Not RecruitingTreatmentAdvanced Stage Diffuse Large B-Cell Non-Hodgkin's Lymphoma / Non-Hodgkin's Lymphoma (NHL)1
2CompletedPreventionCINV1
2CompletedPreventionChemotherapy-Induced Nausea and Vomiting (CINV)1
2CompletedPreventionNausea / Vomiting1
2CompletedPreventionPost-Operative Nausea and Vomiting (PONV)1
2CompletedSupportive CareAccelerated Phase Chronic Myelogenous Leukemia / Adult Acute Lymphoblastic Leukemia in Remission / Adult Acute Myeloid Leukemia in Remission / Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(15;17)(q22;q12) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Atypical Chronic Myeloid Leukemia, BCR-ABL Negative / Blastic Phase Chronic Myelogenous Leukemia / Chronic Eosinophilic Leukemia (CEL) / Chronic Lymphocytic Leukemia (CLL) - Refractory / Chronic Myelomonocytic Leukemia / Chronic Neutrophilic Leukemia / Chronic Phase Chronic Myelogenous Leukemia / De Novo Myelodysplastic Syndromes / Disseminated Neuroblastoma / Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue / Myelodysplastic/Myeloproliferative Neoplasm, Unclassifiable / Nodal marginal zone B-cell lymphomas / Noncontiguous Stage II Adult Burkitt Lymphoma / Noncontiguous Stage II Adult Diffuse Large Cell Lymphoma / Noncontiguous Stage II Adult Diffuse Mixed Cell Lymphoma / Noncontiguous Stage II Adult Diffuse Small Cleaved Cell Lymphoma / Noncontiguous Stage II Adult Immunoblastic Large Cell Lymphoma / Noncontiguous Stage II Adult Lymphoblastic Lymphoma / Noncontiguous Stage II Grade 1 Follicular Lymphoma / Noncontiguous Stage II Grade 2 Follicular Lymphoma / Noncontiguous Stage II Grade 3 Follicular Lymphoma / Noncontiguous Stage II Mantle Cell Lymphoma / Noncontiguous Stage II Marginal Zone Lymphoma / Noncontiguous Stage II Small Lymphocytic Lymphoma / Poor Prognosis Metastatic Gestational Trophoblastic Tumor / Previously Treated Myelodysplastic Syndromes / Primary Myelofibrosis / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Adult Acute Myeloid Leukemia / Recurrent Adult Burkitt Lymphoma / Recurrent Adult Diffuse Large Cell Lymphoma / Recurrent Adult Diffuse Mixed Cell Lymphoma / Recurrent Adult Diffuse Small Cleaved Cell Lymphoma / Recurrent Adult Hodgkin's Lymphoma / Recurrent Adult Immunoblastic Large Cell Lymphoma / Recurrent Adult Lymphoblastic Lymphoma / Recurrent Childhood Large Cell Lymphoma / Recurrent Childhood Lymphoblastic Lymphoma / Recurrent Childhood Small Noncleaved Cell Lymphoma / Recurrent Cutaneous T-Cell Non-Hodgkin Lymphoma / Recurrent Grade 1 Follicular Lymphoma / Recurrent Grade 2 Follicular Lymphoma / Recurrent Grade 3 Follicular Lymphoma / Recurrent Malignant Testicular Germ Cell Tumor / Recurrent Mantle Cell Lymphoma / Recurrent Marginal Zone Lymphoma / Recurrent Mycosis Fungoides/Sezary Syndrome / Recurrent Neuroblastoma / Recurrent Ovarian Epithelial Cancer / Recurrent Ovarian Germ Cell Tumor / Recurrent Small Lymphocytic Lymphoma / Recurrent/Refractory Childhood Hodgkin Lymphoma / Refractory Hairy Cell Leukemia / Relapsing Chronic Myelogenous Leukemia / Secondary Acute Myeloid Leukemia (Secondary AML, sAML) / Secondary Myelodysplastic Syndromes / Splenic Marginal Zone Lymphoma / Stage I Multiple Myeloma / Stage II Multiple Myeloma / Stage II Ovarian Epithelial Cancer / Stage III Adult Burkitt Lymphoma / Stage III Adult Diffuse Large Cell Lymphoma / Stage III Adult Diffuse Mixed Cell Lymphoma / Stage III Adult Diffuse Small Cleaved Cell Lymphoma / Stage III Adult Hodgkin Lymphoma / Stage III Adult Immunoblastic Large Cell Lymphoma / Stage III Adult Lymphoblastic Lymphoma / Stage III Chronic Lymphocytic Leukemia / Stage III Grade 1 Follicular Lymphoma / Stage III Grade 2 Follicular Lymphoma / Stage III Grade 3 Follicular Lymphoma / Stage III Malignant Testicular Germ Cell Tumor / Stage III Mantle Cell Lymphoma / Stage III Marginal Zone Lymphoma / Stage III Multiple Myeloma / Stage III Ovarian Epithelial Cancer / Stage III Small Lymphocytic Lymphoma / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Adult Burkitt Lymphoma / Stage IV Adult Diffuse Large Cell Lymphoma / Stage IV Adult Diffuse Mixed Cell Lymphoma / Stage IV Adult Diffuse Small Cleaved Cell Lymphoma / Stage IV Adult Hodgkin Lymphoma / Stage IV Adult Immunoblastic Large Cell Lymphoma / Stage IV Adult Lymphoblastic Lymphoma / Stage IV Breast Cancer / Stage IV Chronic Lymphocytic Leukemia / Stage IV Grade 1 Follicular Lymphoma / Stage IV Grade 2 Follicular Lymphoma / Stage IV Grade 3 Follicular Lymphoma / Stage IV Mantle Cell Lymphoma / Stage IV Marginal Zone Lymphoma / Stage IV Ovarian Epithelial Cancer / Stage IV Small Lymphocytic Lymphoma1
2CompletedSupportive CareAcute Myelogenous Leukaemia (AML) / Chemotherapy-Induced Nausea and Vomiting (CINV)1
2CompletedSupportive CareNausea and vomiting / Unspecified Adult Solid Tumor, Protocol Specific1
2CompletedSupportive CareNausea / Vomiting1
2CompletedTreatmentAcute Myelogenous Leukaemia (AML) / Chronic Chronic myelogenous leukemia / Hematologic Diseases / Myelodysplastic Syndrome1
2CompletedTreatmentAlcohol Abuse / Alcohol Dependence1
2CompletedTreatmentAlcohol Dependence3
2CompletedTreatmentAmphetamine-Related Disorders1
2CompletedTreatmentCardiac Output1
2CompletedTreatmentChemotherapy-Induced Nausea and Vomiting (CINV)2
2CompletedTreatmentChemotherapy-Induced / Nausea and vomiting1
2CompletedTreatmentCocaine-Related Disorders / Drug Administration Schedule1
2CompletedTreatmentDependence, Cocaine / Methamphetamine Dependence1
2CompletedTreatmentGliomas / Nausea / Vomiting1
2CompletedTreatmentNausea and Vomiting, Postoperative / Post-Operative Nausea and Vomiting (PONV)1
2CompletedTreatmentNausea and vomiting1
2CompletedTreatmentNausea / Vomiting1
2CompletedTreatmentPost-Operative Nausea and Vomiting (PONV)3
2CompletedTreatmentPost-Operative Nausea / Post-Operative Vomiting1
2CompletedTreatmentPostoperative pain1
2CompletedTreatmentPsychosis Not Otherwise Specified / Schizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder1
2CompletedTreatmentTobacco Use Disorders1
2Not Yet RecruitingTreatmentChemotherapy-Induced Nausea and Vomiting (CINV)1
2RecruitingPreventionDrug withdrawal syndrome neonatal / Narcotic Addiction1
2RecruitingSupportive CareChemo-radiation Induced Nausea and Vomiting1
2RecruitingSupportive CareSarcomas1
2RecruitingTreatmentAlcohol Use Disorder (AUD)1
2RecruitingTreatmentChemotherapy-Induced Nausea and Vomiting (CINV) / Head Neck Cancer / Vomiting1
2RecruitingTreatmentChemotherapy-Induced Nausea and Vomiting (CINV) / Nausea / Vomiting1
2TerminatedSupportive CareNausea / Unspecified Childhood Solid Tumor, Protocol Specific / Vomiting1
2TerminatedTreatmentAlcohol Abuse / Alcohol Dependence1
2TerminatedTreatmentMalignant Neoplasm of Pancreas1
2TerminatedTreatmentObsessive Compulsive Disorder (OCD)1
2Unknown StatusTreatmentAlcohol Dependence1
2Unknown StatusTreatmentCancer, Breast1
2Unknown StatusTreatmentDependence, Cocaine1
2WithdrawnSupportive CareAdverse Effects / Mycobacterium avium complex infection1
2WithdrawnSupportive CareMalignant Gliomas1
2, 3Not Yet RecruitingPreventionOndansetron / Shivering1
2, 3Not Yet RecruitingTreatmentAlcohol Dependence1
2, 3RecruitingPreventionAntiemetics / Antineoplastic Agents / Neoplasms, Breast / Quality of Life1
2, 3RecruitingTreatmentGastroenteritis1
2, 3Unknown StatusPreventionArterial Hypotension / Pregnancy1
3Active Not RecruitingTreatmentCancer of the Cervix1
3CompletedNot AvailableBioavailability1
3CompletedPreventionChemotherapy-Induced Nausea and Vomiting (CINV)6
3CompletedPreventionChemotherapy-Induced Nausea and Vomiting (CINV) / Nausea / Vomiting1
3CompletedPreventionPost-Operative Nausea and Vomiting (PONV)4
3CompletedPreventionRadiotherapy Induced Nausea and Vomiting1
3CompletedPreventionVomiting1
3CompletedSupportive CareChemotherapy-Induced Nausea and Vomiting (CINV) / Nausea and vomiting1
3CompletedSupportive CareChronic Myeloproliferative Disorders / Leukemias / Malignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm / Myelodysplastic Syndromes / Nausea and vomiting / Precancerous Conditions / Small Intestine Cancer / Unspecified Adult Solid Tumor, Protocol Specific / Unspecified Childhood Solid Tumor, Protocol Specific1
3CompletedSupportive CareMalignancies1
3CompletedSupportive CareNausea and vomiting / Unspecified Adult Solid Tumor, Protocol Specific1
3CompletedTreatmentAcute Gastroenteritis / Gastroenteritis / Vomiting1
3CompletedTreatmentAlcohol Dependence2
3CompletedTreatmentAnaesthesia therapy1
3CompletedTreatmentBioavailability1
3CompletedTreatmentChemotherapy-Induced Nausea and Vomiting (CINV)1
3CompletedTreatmentChemotherapy-Induced Nausea and Vomiting (CINV) / Nausea / Vomiting1
3CompletedTreatmentInteraction Between Antiemetic Drugs and Paracetamol1
3CompletedTreatmentPain NOS1
3CompletedTreatmentPost-Operative Nausea and Vomiting (PONV)1
3CompletedTreatmentSchizophrenic Disorders1
3Not Yet RecruitingTreatmentAcute Gastroenteritis / Vomiting1
3RecruitingPreventionAdjunct to general anesthesia therapy / Anaesthesia therapy / Analgesics / Analgesics, Opioid / Dexmedetomidine / Gabapentin / Ketamine / Lidocaine / Narcotics / Obstructive Sleep Apnea of Child / Oximetry, Pulse / Pathologic Processes / Physiologic Effects of Drugs / Postoperative Complications / Respiratory Depression / Sleep Disordered Breathing (SDB) / Tonsillectomy1
3RecruitingPreventionChemotherapy Induced Vomiting / Leukemia Acute Myeloid Leukemia (AML)1
3RecruitingPreventionChildhood Cancers / Nausea / Vomiting1
3RecruitingSupportive CareBreast - Female1
3RecruitingSupportive CareChemotherapy-Induced Nausea and Vomiting (CINV)1
3RecruitingSupportive CareNeoplasms, Malignant1
3RecruitingTreatmentIrritable Bowel Syndrome (IBS)1
3RecruitingTreatmentSchizoaffective and Schizophreniform Disorders / Schizophrenic Disorders1
3TerminatedPreventionChemotherapy-Induced Nausea and Vomiting (CINV)1
3TerminatedTreatmentGastroenteritis / Vomiting1
3TerminatedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
3Unknown StatusSupportive CareMalignancies1
3WithdrawnSupportive CareChemotherapy-Induced Nausea and Vomiting (CINV) / Malignancies / Nausea and vomiting / Solid Tumor Cancers1
4Active Not RecruitingTreatmentAlcohol Use Disorder (AUD) / Bipolar Disorder (BD) / Dual Diagnosis1
4Active Not RecruitingTreatmentTrigeminal Neuralgia (TN)1
4Active Not RecruitingTreatmentVomiting1
4CompletedPreventionCardiac Repolarization1
4CompletedPreventionCesarean Section / Hemodynamics / Ondansetron / Spinal Anaesthesia1
4CompletedPreventionFractures, Bone / Morphine Adverse Reaction / Nausea and Vomiting, Postoperative / Pruritus / Satisfaction, Personal1
4CompletedPreventionMaternal Hypotension1
4CompletedPreventionNausea / Postoperative Nausea and Vomiting (PONV)1
4CompletedPreventionNausea / Satisfaction / Vomiting1
4CompletedPreventionNausea / Vomiting1
4CompletedPreventionPonv1
4CompletedPreventionPost-Operative Nausea and Vomiting (PONV)8
4CompletedPreventionGallstone formation1
4CompletedTreatmentAnaesthetics Gases, Xenon / Anaesthetics Volatile, Sevoflurane / Depth of Anaesthesia / Post-Operative Nausea and Vomiting (PONV)1
4CompletedTreatmentAnalgesics / Pain, Chronic / Postoperative pain1
4CompletedTreatmentCardiac Output Change Following Ephedrine, Phenylephrine, Norepinephrine, Ondansetron / Cardiac Output, Low1
4CompletedTreatmentChemotherapy-induced Acute or Delayed Nausea and Vomiting (CINV)1
4CompletedTreatmentChlorzoxazone / Postoperative pain1
4CompletedTreatmentDehydration / Gastroenteritis / Severe or persistent diarrhea / Vomiting2
4CompletedTreatmentDrug Overdose1
4CompletedTreatmentElectrocardiogram QTc interval prolonged1
4CompletedTreatmentGall Stone Disease1
4CompletedTreatmentHeadaches1
4CompletedTreatmentIrritable Bowel Syndrome With Diarrhoea1
4CompletedTreatmentNarcotic Use / Nausea / Occasional Constipation / Pain NOS1
4CompletedTreatmentNausea1
4CompletedTreatmentNausea and Vomiting, Postoperative1
4CompletedTreatmentNausea / Vomiting4
4CompletedTreatmentObsessive Compulsive Disorder (OCD)2
4CompletedTreatmentPain NOS1
4CompletedTreatmentPost-Operative Nausea and Vomiting (PONV)1
4CompletedTreatmentPost-Operative Nausea and Vomiting (PONV) / Postoperative Function Level / Postoperative pain1
4CompletedTreatmentPostoperative pain1
4Enrolling by InvitationTreatmentAnesthesia Complication / Hemodynamics Instability / Ileus paralytic / Nausea / Postoperative pain / Vomiting1
4Not Yet RecruitingPreventionPost-Operative Nausea and Vomiting (PONV)1
4RecruitingPreventionAnesthesia, Pediatrics, Surgery1
4RecruitingPreventionArterial Hypotension1
4RecruitingPreventionLaparoscopic Sleeve Gastrectomy / Post-Operative Nausea and Vomiting (PONV)1
4RecruitingPreventionPost-Operative Nausea and Vomiting (PONV)1
4RecruitingPreventionPruritus1
4RecruitingSupportive CareBehaviors / Cognitive Change1
4RecruitingSupportive CareObstructive Sleep Apnea (OSA)1
4RecruitingTreatmentCannabis Use Disorders1
4RecruitingTreatmentGilles de la Tourette's Syndrome / Obsessive Compulsive Disorder (OCD) / Tic Disorders1
4RecruitingTreatmentInguinal Hernias / Postoperative pain1
4RecruitingTreatmentPost-Operative Nausea and Vomiting (PONV)2
4TerminatedTreatmentAbdominal Pain (AP) / Nausea1
4TerminatedTreatmentTumors1
4Unknown StatusNot AvailableDependence, Cocaine1
4WithdrawnTreatmentMalignant Childhood Neoplasm1
Not AvailableActive Not RecruitingNot AvailableAAT Deficiency / AATD / Alpha-1 Antitrypsin Deficiency / Fibrosis, Liver1
Not AvailableActive Not RecruitingTreatmentNausea / Vomiting1
Not AvailableActive Not RecruitingTreatmentOpiate withdrawal symptoms / Physical Dependence1
Not AvailableCompletedNot AvailableHealthy Volunteers2
Not AvailableCompletedNot AvailableNausea and vomiting / Unspecified Adult Solid Tumor, Protocol Specific1
Not AvailableCompletedNot AvailableOndansetron1
Not AvailableCompletedOtherPain NOS1
Not AvailableCompletedPreventionAnesthesia; Adverse Effect, Spinal and Epidural1
Not AvailableCompletedPreventionCesarean Delivery1
Not AvailableCompletedPreventionCesarean Section / Pruritus1
Not AvailableCompletedPreventionLaparoscopic Marsupialization of Renal Cyst1
Not AvailableCompletedPreventionMorphine Adverse Reaction1
Not AvailableCompletedPreventionPost-Operative Nausea and Vomiting (PONV)5
Not AvailableCompletedSupportive CareMale Breast Cancer / Nausea and vomiting / Stage I Breast Carcinoma / Stage II Breast Cancer / Stage IIIA Breast Cancer1
Not AvailableCompletedSupportive CareMalignancies1
Not AvailableCompletedSupportive CareNeoplasms, Malignant1
Not AvailableCompletedTreatmentAbdominal mass1
Not AvailableCompletedTreatmentBenign Paroxysmal Positional Vertigo (BPPV)1
Not AvailableCompletedTreatmentCataracts1
Not AvailableCompletedTreatmentDrug Drug Interaction (DDI)1
Not AvailableCompletedTreatmentHip Fracture Surgery / Post Operative Pain Control1
Not AvailableCompletedTreatmentItching1
Not AvailableCompletedTreatmentMalignant Lymphomas1
Not AvailableCompletedTreatmentMicrovascular Decompression Surgery / Post-Operative Nausea and Vomiting (PONV)1
Not AvailableCompletedTreatmentMyocardial Repolarization1
Not AvailableCompletedTreatmentNeoplasms, Pancreatic1
Not AvailableCompletedTreatmentPost-Operative Nausea and Vomiting (PONV)1
Not AvailableCompletedTreatmentSchizophrenic Disorders1
Not AvailableCompletedTreatmentSedation, Conscious1
Not AvailableCompletedTreatmentSubstance Withdrawal Syndrome1
Not AvailableCompletedTreatmentSubstance-Related Disorders1
Not AvailableCompletedTreatmentVomiting of Pregnancy1
Not AvailableRecruitingNot AvailableAdverse Reaction to Other Drugs and Medicines1
Not AvailableRecruitingDiagnosticNausea1
Not AvailableRecruitingPreventionPost-Operative Nausea and Vomiting (PONV)2
Not AvailableRecruitingSupportive CareCancer, Breast / Post-Operative Nausea and Vomiting (PONV)1
Not AvailableRecruitingSupportive CareInguinal Hernias / Postoperative pain1
Not AvailableRecruitingSupportive CarePostoperative pain / Undescended Testis1
Not AvailableRecruitingTreatmentAdverse Anesthesia Outcome1
Not AvailableRecruitingTreatmentAnaesthesia therapy / Anesthesia Morbidity / Breast Neoplasm Female / Regional Anesthesia / Regional Anesthesia Morbidity1
Not AvailableRecruitingTreatmentDrug-induced Nausea and Vomiting1
Not AvailableRecruitingTreatmentNausea1
Not AvailableRecruitingTreatmentRectal Carcinoma1
Not AvailableTerminatedPreventionArterial Hypotension1
Not AvailableTerminatedTreatmentNausea1
Not AvailableUnknown StatusPreventionArterial Hypotension / Nausea and vomiting / Shivering / Vasopressor1
Not AvailableUnknown StatusPreventionNausea and vomiting1
Not AvailableUnknown StatusSupportive CareNon-Hodgkin's Lymphoma (NHL)1
Not AvailableUnknown StatusTreatmentDependence, Cocaine / Human Immunodeficiency Virus (HIV) Infections1
Not AvailableUnknown StatusTreatmentSedation and Analgesia / Side Effect of Drug1
Not AvailableWithdrawnPreventionPolymorphism, Genetic / Post-Operative Nausea and Vomiting (PONV)1
Not AvailableWithdrawnPreventionPost-Operative Nausea and Vomiting (PONV)1
Not AvailableWithdrawnPreventionRespiratory Complications / Swallowing Disorders1
Not AvailableWithdrawnSupportive CareLeukemias / Lymphoproliferative Disorders / Malignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm / Myelodysplastic Syndromes / Myeloproliferative Disorders / Nausea and vomiting / Tumors, Solid1
Not AvailableWithdrawnTreatmentDehydration / Gastroenteritis1
Not AvailableWithdrawnTreatmentPost Operative Nausea and Vomiting (PONV) / Rescue Emetic Therapy1

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
InjectionIntravenous2 mg/1mL
Injection, solutionIntramuscular2 mg/1mL
Injection, solutionIntramuscular; Intravenous2 mg/1mL
Injection, solutionIntramuscular; Intravenous4 mg/2mL
SolutionOral4 mg/5mL
SolutionOral4 mg
TabletOral24 mg/1
TabletOral4 mg/1
TabletOral8 mg/1
Tablet, orally disintegratingOral4 mg/1
Tablet, orally disintegratingOral8 mg/1
Tablet, coatedOral4 mg/31
InjectionIntramuscular; Intravenous2 mg/1mL
Injection, solutionIntravenous2 mg/1mL
SolutionIntramuscular; Intravenous2 mg/1mL
SolutionIntravenous2 mg/1mL
Tablet, film coatedOral16 mg/1
Tablet, film coatedOral24 mg/1
Tablet, film coatedOral4 mg/1
Tablet, film coatedOral8 mg/1
Injection, solutionIntravenous32 mg/50mL
SolutionIntravenous2 mg
SolutionIntravenous2.00 mg
LiquidIntravenous2 mg
Film, solubleOral4 mg
Film, solubleOral8 mg
TabletOral4 mg
TabletOral8 mg
Tablet, orally disintegratingOral4 mg
Tablet, orally disintegratingOral8 mg
InjectionIntravenous32 mg/50mL
FilmOral4 mg/1
FilmOral8 mg/1
Film, solubleOral4 mg/1
Film, solubleOral8 mg/1
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)
US5344658No1994-09-062011-09-06Us
CA2205600No2000-05-302015-11-20Canada
US5955488Yes1999-09-212016-05-14Us
US6063802Yes2000-05-162016-05-14Us
US5854270Yes1998-12-292016-05-20Us
US9095577No2015-08-042030-07-13Us
US8580830No2013-11-122029-11-23Us

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)15.39ChemAxon
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-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0006-0590000000-1c293e5af06aedfb74e1
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-006x-0790000000-39dfc83ad8c54c21d83d
1H NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable

Taxonomy

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
Carbazole / N-alkylindole / Indole / Aryl ketone / Aryl alkyl ketone / N-methylpyrrole / N-substituted imidazole / Substituted pyrrole / Benzenoid / Imidazole
show 14 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
carbazoles (CHEBI:7773)

Targets

Kind
Protein
Organism
Human
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. [PubMed:10065930]
  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. [PubMed:10517265]
  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. [PubMed:11763467]
  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. [PubMed:11972287]
  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. [PubMed:12032025]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  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. [PubMed:19320280]
  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. [PubMed:8588861]
  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. [PubMed:20098535]
  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. [PubMed:17269994]
  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. [PubMed:11919526]
  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. [PubMed:9506240]
  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. [PubMed:15740177]
Kind
Protein
Organism
Human
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. [PubMed:2164935]
Kind
Protein
Organism
Human
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. [PubMed:2164935]
Kind
Protein
Organism
Human
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. [PubMed:2164935]
Kind
Protein
Organism
Human
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. [PubMed:2164935]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Human
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. 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. [PubMed:16946512]
  3. 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. [PubMed:8591723]
  4. Zofran FDA [File]
Kind
Protein
Organism
Human
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. [PubMed:16192915]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Drug created on June 13, 2005 07:24 / Updated on December 12, 2018 03:40