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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
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms Not Available
Salts Not Available
Brand names
Name Company
Apo-ondansetron
Novo-ondansetron
PHL-ondansetron
PMS-ondansetron
Ratio-ondansetron
Sandoz ondansetron
Zofran
Zofran ODT
Zophren
Zudan
Brand mixtures Not Available
Categories
  • Anti-anxiety Agents
  • Antiemetics
  • Antipsychotics
  • Serotonin Antagonists
  • Antipruritics
  • Antipsychotic Agents
CAS number 99614-02-5
Weight Average: 293.363
Monoisotopic: 293.152812245
Chemical Formula C18H19N3O
InChI Key InChIKey=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
Plain Text
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
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Organic
Classes
  • Carbazoles
  • Tryptamines and Derivatives
Substructures
  • Indoles and Indole Derivatives
  • Carbazoles
  • Pyrroles
  • Benzene and Derivatives
  • Tryptamines and Derivatives
  • Imidazoles
  • Heterocyclic compounds
  • Aromatic compounds
  • Imines
  • Cyanamides
  • Cyclohexenes and Derivatives
  • Ketones
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.
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.
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
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
Dosage forms
Form Route Strength
Liquid Intravenous
Liquid Oral
Solution Intravenous
Tablet Oral
Prices
Unit description Cost Unit
Ondansetron 30 8 mg Dispersible Tablet Box 1158.51 USD box
Zofran ODT 30 4 mg Dispersible Tablet Box 782.26 USD box
Ondansetron 30 4 mg Dispersible Tablet Box 695.53 USD box
Ondansetron hcl powder 177.0 USD g
Ondansetron hcl 24 mg tablet 105.5 USD tablet
Zofran 8 mg tablet 45.16 USD tablet
Zofran odt 8 mg tablet 41.76 USD tablet
Ondansetron hcl 8 mg tablet 40.75 USD tablet
Ondansetron odt 8 mg tablet 37.13 USD tablet
Zofran 4 mg tablet 27.11 USD tablet
Ondansetron hcl 4 mg tablet 25.07 USD tablet
Zofran odt 4 mg tablet 25.07 USD tablet
Zofran 8 mg Tablet 23.02 USD tablet
Zofran Odt 8 mg Disintegrating Tablet 22.49 USD tablet
Ondansetron odt 4 mg tablet 22.3 USD tablet
Zofran 4 mg Tablet 15.09 USD tablet
Zofran Odt 4 mg Disintegrating Tablet 14.74 USD tablet
Zofran 2 mg/ml vial 12.82 USD ml
Zofran 4 mg/2 ml vial 12.82 USD ml
Apo-Ondansetron 8 mg Tablet 12.06 USD tablet
Co Ondansetron 8 mg Tablet 12.06 USD tablet
Jamp-Ondansetron 8 mg Tablet 12.06 USD tablet
Mint-Ondansetron 8 mg Tablet 12.06 USD tablet
Mylan-Ondansetron 8 mg Tablet 12.06 USD tablet
Novo-Ondansetron 8 mg Tablet 12.06 USD tablet
Ondansetron-Odan 8 mg Tablet 12.06 USD tablet
Phl-Ondansetron 8 mg Tablet 12.06 USD tablet
Pms-Ondansetron 8 mg Tablet 12.06 USD tablet
Ran-Ondansetron 8 mg Tablet 12.06 USD tablet
Ratio-Ondansetron 8 mg Tablet 12.06 USD tablet
Sandoz Ondansetron 8 mg Tablet 12.06 USD tablet
Zofran 2 mg/ml 11.12 USD ml
Apo-Ondansetron 4 mg Tablet 7.9 USD tablet
Co Ondansetron 4 mg Tablet 7.9 USD tablet
Jamp-Ondansetron 4 mg Tablet 7.9 USD tablet
Mint-Ondansetron 4 mg Tablet 7.9 USD tablet
Mylan-Ondansetron 4 mg Tablet 7.9 USD tablet
Novo-Ondansetron 4 mg Tablet 7.9 USD tablet
Ondansetron-Odan 4 mg Tablet 7.9 USD tablet
Phl-Ondansetron 4 mg Tablet 7.9 USD tablet
Pms-Ondansetron 4 mg Tablet 7.9 USD tablet
Ran-Ondansetron 4 mg Tablet 7.9 USD tablet
Ratio-Ondansetron 4 mg Tablet 7.9 USD tablet
Sandoz Ondansetron 4 mg Tablet 7.9 USD tablet
Ondansetron (Preservative Free) 2 mg/ml 6.23 USD ml
Ondansetron (Preserved) 2 mg/ml 6.23 USD ml
Ondansetron (Unpreserved) 2 mg/ml 6.23 USD ml
Ondansetron (With Preservative) 2 mg/ml 6.23 USD ml
Ondansetron Omega (Preservative Free) 2 mg/ml 6.23 USD ml
Ondansetron Omega (With Preservative) 2 mg/ml 6.23 USD ml
Ondansetron hcl 4 mg/2 ml vial 3.13 USD ml
Zofran 0.8 mg/ml Solution 2.3 USD ml
Apo-Ondansetron 0.8 mg/ml Solution 1.53 USD ml
Ondansetron 32 mg/50 ml bag 0.86 USD ml
Ondansetron hcl 32 mg/50 ml bg 0.42 USD ml
Ondansetron 40 mg/20 ml vial 0.17 USD ml
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Patents
Country Patent Number Approved Expires (estimated)
United States 5854270 1996-05-20 2016-05-20
United States 5344658 1994-09-06 2011-09-06
Canada 2205600 2000-05-30 2015-11-20
Properties
State solid
Experimental Properties
Property Value Source
logP 2.4 Not Available
Predicted Properties
Property Value Source
water solubility 2.48e-01 g/l ALOGPS
logP 2.56 ALOGPS
logP 2.35 ChemAxon
logS -3.1 ALOGPS
pKa (strongest acidic) 15.39 ChemAxon
pKa (strongest basic) 7.34 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 39.82 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 86.78 ChemAxon
polarizability 33.16 ChemAxon
References
Synthesis Reference Not Available
General Reference
  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
  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. Epub . Pubmed
  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
  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
External Links
Resource Link
KEGG Drug D00456 Link_out
KEGG Compound C07325 Link_out
PubChem Compound 4595 Link_out
PubChem Substance 46504819 Link_out
ChemSpider 4434 Link_out
BindingDB 50000493 Link_out
Therapeutic Targets Database DAP000221 Link_out
PharmGKB PA450705 Link_out
IUPHAR 2290 Link_out
Guide to Pharmacology 2290 Link_out
Drug Product Database 2239372 Link_out
RxList http://www.rxlist.com/cgi/generic/ondansetron.htm Link_out
Drugs.com http://www.drugs.com/cdi/ondansetron.html Link_out
PDRhealth http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/zof1501.shtml Link_out
Wikipedia http://en.wikipedia.org/wiki/Ondansetron Link_out
ATC Codes
  • A04AA01
AHFS Codes
  • 56:22.20
PDB Entries Not Available
FDA label show (126 KB)
MSDS show (53.2 KB)
Interactions
Drug Interactions
Drug Interaction
Asenapine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Pazopanib Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
Telavancin Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Food Interactions
  • Take without regard to meals.
Targets

1. 5-hydroxytryptamine 3 receptor

Pharmacological action: yes
Actions: antagonist

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-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel

Organism class: human
UniProt ID: P46098 Link_out
Gene: HTR3A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  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
  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
  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
  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 spinal receptor involvement in acute pain in humans. Anesth Analg. 2002 Jun;94(6):1553-7, table of contents. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  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
  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
  9. Dimitrov DH: Effect of Ondansetron, a 5-HT Receptor Antagonist, on Fatigue in 2 Veterans With Hepatitis C. Prim Care Companion J Clin Psychiatry. 2009;11(6):366-7. Pubmed
  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
  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
  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
  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

2. 5-hydroxytryptamine 4 receptor

Pharmacological action: unknown
Actions: agonist

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 is mediated by G proteins that stimulate adenylate cyclase

Organism class: human
UniProt ID: Q13639 Link_out
Gene: HTR4 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

3. Mu-type opioid receptor

Pharmacological action: unknown
Actions: other/unknown

Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Receptor for beta-endorphin

Organism class: human
UniProt ID: P35372 Link_out
Gene: OPRM1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

4. 5-hydroxytryptamine 1A receptor

Pharmacological action: unknown
Actions: other/unknown

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 is mediated by G proteins that inhibit adenylate cyclase activity

Organism class: human
UniProt ID: P08908 Link_out
Gene: HTR1A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

5. 5-hydroxytryptamine 1B receptor

Pharmacological action: unknown
Actions: other/unknown

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 is mediated by G proteins that inhibit adenylate cyclase activity

Organism class: human
UniProt ID: P28222 Link_out
Gene: HTR1B Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
Enzymes

1. Cytochrome P450 3A4

Actions: substrate

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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4- hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. The enzyme also hydroxylates etoposide

UniProt ID: P08684 Link_out
Gene: CYP3A4
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  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. Epub 2009 Nov 24. Pubmed

2. Cytochrome P450 1A2

Actions: substrate, inhibitor

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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N3-demethylation. Also acts in the metabolism of aflatoxin B1 and acetaminophen

UniProt ID: P05177 Link_out
Gene: CYP1A2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  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. Epub 2009 Nov 24. Pubmed

3. Cytochrome P450 2D6

Actions: substrate, inhibitor

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 antidepressants

UniProt ID: P10635 Link_out
Gene: CYP2D6 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. 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
  3. 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. Epub 2009 Nov 24. Pubmed

4. Cytochrome P450 3A5

Actions: substrate

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 unrelated compounds, including steroids, fatty acids, and xenobiotics

UniProt ID: P20815 Link_out
Gene: CYP3A5 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

5. Cytochrome P450 3A7

Actions: substrate

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 unrelated compounds, including steroids, fatty acids, and xenobiotics

UniProt ID: P24462 Link_out
Gene: CYP3A7 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

6. Cytochrome P450 2C9

Actions: substrate

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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S- warfarin, diclofenac, phenytoin, tolbutamide and losartan

UniProt ID: P11712 Link_out
Gene: CYP2C9
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Epub 2009 Nov 24. Pubmed

7. Cytochrome P450 2E1

Actions: substrate

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 or carcinogenic forms

UniProt ID: P05181 Link_out
Gene: CYP2E1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. Epub 2009 Nov 24. Pubmed
Comments
Drug created on June 13, 2005 07:24 / Updated on February 08, 2013 16:19