Banner
targets (6) enzymes (6)
for drugs
Identification
Name Thioridazine
Accession Number DB00679 (APRD00596)
Type small molecule
Groups approved
Description

A phenothiazine antipsychotic used in the management of psychoses, including schizophrenia, and in the control of severely disturbed or agitated behavior. It has little antiemetic activity. Thioridazine has a higher incidence of antimuscarinic effects, but a lower incidence of extrapyramidal symptoms, than chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p618)
Structure Thumb
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms
Thioridazin
Thioridazine Chloride
Thioridazine Hcl
Thioridazine Hydrochloride
Thoridazine Hydrochloride
Salts Not Available
Brand names
Name Company
Aldazine
Mallorol
Malloryl
Meleril
Mellaril
Mellaril Hydrochloride
Mellaril-S
Mellarit
Mellerets
Mellerette
Melleretten
Melleril
Metlaril
Novoridazine
Orsanil
Ridazin
Ridazine
Sonapax
Sonapax Hydrochloride
Stalleril
Thioridazine Hcl Intensol
Thioridazine, Prolongatum
Tioridazin
First Prev Next Last
Brand mixtures Not Available
Categories
  • Antipsychotics
  • Dopamine Antagonists
  • Phenothiazines
  • Antipsychotic Agents
CAS number 50-52-2
Weight Average: 370.575
Monoisotopic: 370.153740222
Chemical Formula C21H26N2S2
InChI Key InChIKey=KLBQZWRITKRQQV-UHFFFAOYSA-N
InChI
InChI=1S/C21H26N2S2/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(24-2)15-19(21)23/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3
Plain Text
IUPAC Name
10-[2-(1-methylpiperidin-2-yl)ethyl]-2-(methylsulfanyl)-10H-phenothiazine
SMILES
CSC1=CC2=C(SC3=CC=CC=C3N2CCC2CCCCN2C)C=C1
Plain Text
Mass Spec show (8.15 KB)
Taxonomy
Kingdom Organic
Classes
  • Phenothiazines
Substructures
  • Ethers
  • Phenothiazines
  • Aliphatic and Aryl Amines
  • Thiazines
  • Benzene and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • Anilines
  • Piperidines
Pharmacology
Indication For the treatment of schizophrenia and generalized anxiety disorder.
Pharmacodynamics Thioridazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Thioridazine has not been shown effective in the management of behaviorial complications in patients with mental retardation.
Mechanism of action Thioridazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; blocks alpha-adrenergic effect, depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.
Absorption 60%
Volume of distribution Not Available
Protein binding 95%
Metabolism Hepatic
Route of elimination Not Available
Half life 21-25 hours
Clearance Not Available
Toxicity LD50=956-1034 mg/kg (Orally in rats); Agitation, blurred vision, coma, confusion, constipation, difficulty breathing, dilated or constricted pupils, diminished flow of urine, dry mouth, dry skin, excessively high or low body temperature, extremely low blood pressure, fluid in the lungs, heart abnormalities, inability to urinate, intestinal blockage, nasal congestion, restlessness, sedation, seizures, shock
Affected organisms
  • Humans and other mammals
Pathways Not Available
Pharmacoeconomics
Manufacturers
  • Novartis pharmaceuticals corp
  • Actavis mid atlantic llc
  • Alpharma us pharmaceuticals division
  • Hi tech pharmacal co inc
  • Pharmaceutical assoc inc div beach products
  • Sandoz inc
  • Teva pharmaceuticals usa
  • Wockhardt eu operations (swiss) ag
  • Roxane laboratories inc
  • Ivax pharmaceuticals inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • Superpharm corp
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • West ward pharmaceutical corp
Packagers
Dosage forms
Form Route Strength
Solution Oral
Suspension Oral
Tablet Oral
Prices
Unit description Cost Unit
Thioridazine hcl powder 11.16 USD g
Thioridazine HCl 200 mg tablet 1.14 USD tablet
Thioridazine HCl 150 mg tablet 1.01 USD tablet
Thioridazine HCl 100 mg tablet 0.69 USD tablet
Thioridazine 100 mg tablet 0.67 USD tablet
Thioridazine HCl 50 mg tablet 0.61 USD tablet
Thioridazine 50 mg tablet 0.58 USD tablet
Thioridazine HCl 25 mg tablet 0.49 USD tablet
Thioridazine 25 mg tablet 0.47 USD tablet
Thioridazine HCl 15 mg tablet 0.45 USD tablet
Thioridazine HCl 10 mg tablet 0.35 USD tablet
Thioridazine 10 mg tablet 0.33 USD tablet
First Prev Next Last
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents Not Available
Properties
State solid
Experimental Properties
Property Value Source
melting point 73 °C PhysProp
boiling point 230 °C at 2.00E-02 mm Hg PhysProp
water solubility 0.0336 mg/L Not Available
logP 5.90 HANSCH,C ET AL. (1995)
pKa 9.5 EL TAYAR,N ET AL. (1985)
Predicted Properties
Property Value Source
water solubility 8.55e-04 g/l ALOGPS
logP 5.93 ALOGPS
logP 5.47 ChemAxon
logS -5.6 ALOGPS
pKa (strongest basic) 8.93 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 6.48 ChemAxon
rotatable bond count 4 ChemAxon
refractivity 113.52 ChemAxon
polarizability 43.26 ChemAxon
References
Synthesis Reference Not Available
General Reference Not Available
External Links
Resource Link
KEGG Drug D00373 Link_out
PubChem Compound 5452 Link_out
PubChem Substance 46509070 Link_out
ChemSpider 5253 Link_out
ChEBI 9566 Link_out
ChEMBL 9566 Link_out
Therapeutic Targets Database DAP000476 Link_out
PharmGKB PA451666 Link_out
IUPHAR 100 Link_out
Guide to Pharmacology 100 Link_out
Drug Product Database 360244 Link_out
RxList http://www.rxlist.com/cgi/generic3/thioridazine.htm Link_out
Drugs.com http://www.drugs.com/cdi/thioridazine.html Link_out
Wikipedia http://en.wikipedia.org/wiki/Thioridazine Link_out
ATC Codes
  • N05AC02
AHFS Codes Not Available
PDB Entries Not Available
FDA label Not Available
MSDS show (44.7 KB)
Interactions
Drug Interactions
Drug Interaction
Amiodarone Increased risk of cardiotoxicity and arrhythmias
Amitriptyline Increased risk of cardiotoxicity and arrhythmias
Amphetamine Decreased anorexic effect, may increase psychotic symptoms
Artemether Additive QTc-prolongation may occur. Concomitant therapy is contraindicated.
Asenapine Thioridazine is a CYP2D6 substrate in which concomitant therapy with asenapine will increase serum levels of thioridazine. Consider alternative therapy.
Astemizole Increased risk of cardiotoxicity and arrhythmias
Atomoxetine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
Benzphetamine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
Bretylium Increased risk of cardiotoxicity and arrhythmias
Bromocriptine The phenothiazine decreases the effect of bromocriptine
Bupropion Bupropion may increase the effect and toxicity of thioridazine.
Chloroquine Increased risk of cardiotoxicity and arrhythmias
Chlorpromazine Increased risk of cardiotoxicity and arrhythmias
Cisapride Increased risk of cardiotoxicity and arrhythmias
Dexfenfluramine Decreased anorexic effect, may increase psychotic symptoms
Dextroamphetamine Decreased anorexic effect, may increase psychotic symptoms
Diethylpropion Decreased anorexic effect, may increase psychotic symptoms
Diltiazem Increased risk of cardiotoxicity and arrhythmias
Diphenhydramine Increased risk of cardiotoxicity and arrhythmias
Disopyramide Increased risk of cardiotoxicity and arrhythmias
Dofetilide Increased risk of cardiotoxicity and arrhythmias
Donepezil Possible antagonism of action
Doxepin Increased risk of cardiotoxicity and arrhythmias
Duloxetine Increased risk of cardiotoxicity and arrhythmias
Erythromycin Increased risk of cardiotoxicity and arrhythmias
Fenfluramine Decreased anorexic effect, may increase psychotic symptoms
Flecainide Increased risk of cardiotoxicity and arrhythmias
Fluoxetine Increased risk of cardiotoxicity and arrhythmias
Fluvoxamine Increased risk of cardiotoxicity and arrhythmias
Galantamine Possible antagonism of action
Gatifloxacin Increased risk of cardiotoxicity and arrhythmias
Grepafloxacin Increased risk of cardiotoxicity and arrhythmias
Guanethidine Thioridazine may decrease the effect of guanethidine.
Halofantrine Increased risk of cardiotoxicity and arrhythmias
Haloperidol Increased risk of cardiotoxicity and arrhythmias
Imipramine Increased risk of cardiotoxicity and arrhythmias
Josamycin Increased risk of cardiotoxicity and arrhythmias
Levofloxacin Increased risk of cardiotoxicity and arrhythmias
Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Maprotiline Increased risk of cardiotoxicity and arrhythmias
Mazindol Decreased anorexic effect, may increase psychotic symptoms
Methamphetamine Decreased anorexic effect, may increase psychotic symptoms
Metrizamide Increased risk of convulsions
Paroxetine Increased risk of cardiotoxicity and arrhythmias
Penicillin G Increased risk of cardiotoxicity and arrhythmias
Pentamidine Increased risk of cardiotoxicity and arrhythmias
Phendimetrazine Decreased anorexic effect, may increase psychotic symptoms
Phenmetrazine Decreased anorexic effect, may increase psychotic symptoms
Phentermine Decreased anorexic effect, may increase psychotic symptoms
Phenylpropanolamine Decreased anorexic effect, may increase psychotic symptoms
Pimozide Increased risk of cardiotoxicity and arrhythmias
Pindolol Increased risk of cardiotoxicity and arrhythmias
Procainamide Increased risk of cardiotoxicity and arrhythmias
Propafenone Increased risk of cardiotoxicity and arrhythmias.
Propranolol Increased risk of cardiotoxicity and arrhythmias
Quinidine Increased risk of cardiotoxicity and arrhythmias
Quinidine barbiturate Increased risk of cardiotoxicity and arrhythmias
Quinine Increased risk of cardiotoxicity and arrhythmias
Ranolazine Possible additive effect on QT prolongation
Rivastigmine Possible antagonism of action
Sertindole Increased risk of cardiotoxicity and arrhythmias
Sotalol Increased risk of cardiotoxicity and arrhythmias
Sparfloxacin Increased risk of cardiotoxicity and arrhythmias
Spiramycin Increased risk of cardiotoxicity and arrhythmias
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Thioridazine, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.
Tacrolimus May cause additive QTc-prolonging effects. Concomitant therapy is contraindicated.
Tamoxifen Thioridazine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.
Tamsulosin Thioridazine, a CYP2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Thioridazine is initiated, discontinued, or dose changed.
Telithromycin Telithromycin may increase the QTc-prolonging effect of Thioridazine. Concomitant therapy should be avoided.
Terbinafine Terbinafine may increase serum concentrations of Thioridazine. Concomitant therapy is contraindicated.
Terfenadine Increased risk of cardiotoxicity and arrhythmias
Tetrabenazine May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Thiothixene May cause additive QTc-prolonging effects. Concomitant therapy is contraindicated.
Ticlopidine Ticlopidine may decrease the metabolism of Thioridazine. Concomitant therapy is contraindicated.
Toremifene May cause additive QTc-prolonging effects. Concomitant therapy is contraindicated.
Tramadol Thioridazine may decrease the effect of Tramadol by decreasing active metabolite production.
Tranylcypromine Tranylcypromine, a CYP2D6 inhibitor, may decrease the metabolism and clearance of Thioridazine. Concomitant therapy is contraindicated.
Trimethobenzamide Trimethobenzamide and Thioridazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trimipramine May cause additive QTc-prolonging effects. Concomitant therapy is contraindicated.
Triprolidine The antihistamine, Triprolidine, may increase the arrhythmogenic effect of the phenothiazine, Thioridazine. Monitor for symptoms of ventricular arrhythmias. Additive anticholinergic and CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
Trospium Trospium and Thioridazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Vilazodone Thioridazine prescribing information contraindicates the concomitant use of agents that inhibit CYP2D6 isoenzymes. Avoid combination.
Voriconazole Additive QTc prolongation may occur. Concomitant use is contraindicated.
Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
Zuclopenthixol Additive QTc-prolonging effects increases risk of cardiac arrhythmias. Concomitant therapy is contraindicated.
Food Interactions Not Available
Targets

1. D(2) dopamine receptor

Pharmacological action: yes
Actions: antagonist

This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase

Organism class: human
UniProt ID: P14416 Link_out
Gene: DRD2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Seeman P: Atypical neuroleptics: role of multiple receptors, endogenous dopamine, and receptor linkage. Acta Psychiatr Scand Suppl. 1990;358:14-20. Pubmed
  2. Assie MB, Sleight AJ, Koek W: Biphasic displacement of [3H]YM-09151-2 binding in the rat brain by thioridazine, risperidone and clozapine, but not by other antipsychotics. Eur J Pharmacol. 1993 Jun 24;237(2-3):183-9. Pubmed
  3. Dimpfel W, Spuler M, Wessel K: Different neuroleptics show common dose and time dependent effects in quantitative field potential analysis in freely moving rats. Psychopharmacology (Berl). 1992;107(2-3):195-202. Pubmed
  4. Barth VN, Chernet E, Martin LJ, Need AB, Rash KS, Morin M, Phebus LA: Comparison of rat dopamine D2 receptor occupancy for a series of antipsychotic drugs measured using radiolabeled or nonlabeled raclopride tracer. Life Sci. 2006 May 22;78(26):3007-12. Epub 2006 Jan 24. Pubmed
  5. Carey GJ, Bergman J: Discriminative-stimulus effects of clozapine in squirrel monkeys: comparison with conventional and novel antipsychotic drugs. Psychopharmacology (Berl). 1997 Aug;132(3):261-9. Pubmed

2. D(1A) dopamine receptor

Pharmacological action: yes
Actions: antagonist

This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase

Organism class: human
UniProt ID: P21728 Link_out
Gene: DRD1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Hammock RG, Schroeder SR, Levine WR: The effect of clozapine on self-injurious behavior. J Autism Dev Disord. 1995 Dec;25(6):611-26. Pubmed

3. Alpha-1A adrenergic receptor

Pharmacological action: yes
Actions: antagonist

This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins

Organism class: human
UniProt ID: P35348 Link_out
Gene: ADRA1A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Sleight AJ, Koek W, Bigg DC: Binding of antipsychotic drugs at alpha 1A- and alpha 1B-adrenoceptors: risperidone is selective for the alpha 1B-adrenoceptors. Eur J Pharmacol. 1993 Jul 20;238(2-3):407-10. Pubmed
  2. Cahir M, King DJ: Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat. Eur Neuropsychopharmacol. 2005 Mar;15(2):231-4. Pubmed

4. Alpha-1B adrenergic receptor

Pharmacological action: yes
Actions: antagonist

This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system

Organism class: human
UniProt ID: P35368 Link_out
Gene: ADRA1B Link_out
Protein Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Cahir M, King DJ: Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat. Eur Neuropsychopharmacol. 2005 Mar;15(2):231-4. Pubmed

5. 5-hydroxytryptamine 2A 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 mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. This receptor is involved in tracheal smooth muscle contraction, bronchoconstriction, and control of aldosterone production

Organism class: human
UniProt ID: P28223 Link_out
Gene: HTR2A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Andree TH, Mikuni M, Tong CY, Koenig JI, Meltzer HY: Differential effect of subchronic treatment with various neuroleptic agents on serotonin2 receptors in rat cerebral cortex. J Neurochem. 1986 Jan;46(1):191-7. Pubmed
  2. Canton H, Verriele L, Millan MJ: Competitive antagonism of serotonin (5-HT)2C and 5-HT2A receptor-mediated phosphoinositide (PI) turnover by clozapine in the rat: a comparison to other antipsychotics. Neurosci Lett. 1994 Nov 7;181(1-2):65-8. Pubmed
  3. Burki HR: Binding of psychoactive drugs to rat brain amine receptors, measured ex vivo, and their effects on the metabolism of biogenic amines. Naunyn Schmiedebergs Arch Pharmacol. 1986 Mar;332(3):258-66. Pubmed
  4. Costall B, Naylor RJ: Behavioural interactions between 5-hydroxytryptophan, neuroleptic agents and 5-HT receptor antagonists in modifying rodent responding to aversive situations. Br J Pharmacol. 1995 Dec;116(7):2989-99. Pubmed
  5. Morisset S, Sahm UG, Traiffort E, Tardivel-Lacombe J, Arrang JM, Schwartz JC: Atypical neuroleptics enhance histamine turnover in brain via 5-Hydroxytryptamine2A receptor blockade. J Pharmacol Exp Ther. 1999 Feb;288(2):590-6. Pubmed

6. Potassium voltage-gated channel subfamily H member 2

Pharmacological action: unknown
Actions: inhibitor

Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (IKr). Isoform 3 has no channel activity by itself, but modulates channel characteristics when associated with isoform 1

Organism class: human
UniProt ID: Q12809 Link_out
Gene: KCNH2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Milnes JT, Witchel HJ, Leaney JL, Leishman DJ, Hancox JC: hERG K+ channel blockade by the antipsychotic drug thioridazine: An obligatory role for the S6 helix residue F656. Biochem Biophys Res Commun. 2006 Dec 8;351(1):273-80. Epub 2006 Oct 23. Pubmed
Enzymes

1. 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. Otani K, Aoshima T: Pharmacogenetics of classical and new antipsychotic drugs. Ther Drug Monit. 2000 Feb;22(1):118-21. Pubmed
  2. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  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

2. Cytochrome P450 2C19

Actions: substrate

Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine

UniProt ID: P33261 Link_out
Gene: CYP2C19 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

3. 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. 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 2C8

Actions: 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. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme responsible for the metabolism the anti- cancer drug paclitaxel (taxol)

UniProt ID: P10632 Link_out
Gene: CYP2C8
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

5. Cytochrome P450 2C9

Actions: 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. 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

6. Cytochrome P450 2E1

Actions: inhibitor

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