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Identification
NameTrimethadione
Accession NumberDB00347  (APRD00315)
TypeSmall Molecule
GroupsApproved
DescriptionAn anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378)
Structure
Thumb
Synonyms
Tridione
Trimethadion
Triméthadione
Trimethadionum
Trimethinum
Troxidone
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
TridioneTablet, chewable150 mg/1OralAbb Vie Inc.1946-01-25Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
MinoaleDainippon Sumitomo
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIR7GV3H6FQ4
CAS number127-48-0
WeightAverage: 143.1406
Monoisotopic: 143.058243159
Chemical FormulaC6H9NO3
InChI KeyIRYJRGCIQBGHIV-UHFFFAOYSA-N
InChI
InChI=1S/C6H9NO3/c1-6(2)4(8)7(3)5(9)10-6/h1-3H3
IUPAC Name
trimethyl-1,3-oxazolidine-2,4-dione
SMILES
CN1C(=O)OC(C)(C)C1=O
Pharmacology
IndicationUsed in the control of absence (petit mal) seizures that are refractory to treatment with other medications.
Structured Indications
PharmacodynamicsParamethadione and trimethadione are anticonvulsants indicated in the control of absence (petit mal) seizures that are refractory to treatment with other medications. Dione anticonvulsants are used in the treatment of epilepsy. They act on the central nervous system (CNS) to reduce the number of seizures.
Mechanism of actionDione anticonvulsants reduce T-type calcium currents in thalamic neurons, including thalamic relay neurons. It does so via the inhibition of voltage dependent T-type calcium channels. This raises the threshold for repetitive activity in the thalamus, and inhibits corticothalamic transmission. Thus, the abnormal thalamocortical rhythmicity, which is thought to underlie the 3-Hz spike-and-wave discharge seen on electroencephalogram(EEG) with absence seizures, is dampened.
TargetKindPharmacological actionActionsOrganismUniProt ID
Voltage-dependent T-type calcium channel subunit alpha-1GProteinyes
inhibitor
HumanO43497 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein binding90%
Metabolism
SubstrateEnzymesProduct
Trimethadione
dimethadioneDetails
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicitySymptoms of overdose include clumsiness or unsteadiness, coma, dizziness (severe), drowsiness (severe), nausea (severe), and problems with vision.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Trimethadione can be increased when it is combined with Abiraterone.Approved
AmiodaroneThe metabolism of Trimethadione can be decreased when combined with Amiodarone.Approved, Investigational
AprepitantThe serum concentration of Trimethadione can be increased when it is combined with Aprepitant.Approved, Investigational
ArmodafinilThe metabolism of Trimethadione can be decreased when combined with Armodafinil.Approved, Investigational
AtazanavirThe metabolism of Trimethadione can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Trimethadione can be decreased when combined with Atomoxetine.Approved
BexaroteneThe serum concentration of Trimethadione can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe metabolism of Trimethadione can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Trimethadione can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Trimethadione can be decreased when it is combined with Bosentan.Approved, Investigational
CapecitabineThe metabolism of Trimethadione can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Trimethadione can be increased when combined with Carbamazepine.Approved, Investigational
CelecoxibThe metabolism of Trimethadione can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Trimethadione can be increased when it is combined with Ceritinib.Approved
ChloramphenicolThe metabolism of Trimethadione can be decreased when combined with Chloramphenicol.Approved, Vet Approved
CholecalciferolThe metabolism of Trimethadione can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Trimethadione can be decreased when combined with Cimetidine.Approved
CitalopramThe metabolism of Trimethadione can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Trimethadione can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Trimethadione can be decreased when combined with Clemastine.Approved
ClopidogrelThe metabolism of Trimethadione can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Trimethadione can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Trimethadione can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Trimethadione can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Trimethadione can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Trimethadione can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Trimethadione can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Trimethadione can be decreased when it is combined with Dabrafenib.Approved
DarunavirThe metabolism of Trimethadione can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Trimethadione can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Trimethadione can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Trimethadione can be decreased when combined with Delavirdine.Approved
DexamethasoneThe serum concentration of Trimethadione can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DihydroergotamineThe metabolism of Trimethadione can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Trimethadione can be decreased when combined with Diltiazem.Approved
DisulfiramThe metabolism of Trimethadione can be decreased when combined with Disulfiram.Approved
DoxycyclineThe metabolism of Trimethadione can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Trimethadione can be decreased when combined with Dronedarone.Approved
EfavirenzThe serum concentration of Trimethadione can be decreased when it is combined with Efavirenz.Approved, Investigational
EnzalutamideThe serum concentration of Trimethadione can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Trimethadione can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Trimethadione can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Trimethadione can be decreased when combined with Esomeprazole.Approved, Investigational
EtravirineThe serum concentration of Trimethadione can be decreased when it is combined with Etravirine.Approved
FelodipineThe metabolism of Trimethadione can be decreased when combined with Felodipine.Approved, Investigational
FloxuridineThe metabolism of Trimethadione can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Trimethadione can be decreased when combined with Fluconazole.Approved
FluorouracilThe metabolism of Trimethadione can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Trimethadione can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluvastatinThe metabolism of Trimethadione can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Trimethadione can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Trimethadione can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Trimethadione can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Trimethadione can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Trimethadione can be increased when it is combined with Fusidic Acid.Approved
GemfibrozilThe metabolism of Trimethadione can be decreased when combined with Gemfibrozil.Approved
IdelalisibThe serum concentration of Trimethadione can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Trimethadione can be decreased when combined with Imatinib.Approved
IndinavirThe metabolism of Trimethadione can be decreased when combined with Indinavir.Approved
IrbesartanThe metabolism of Trimethadione can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Trimethadione can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Trimethadione can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Trimethadione can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Trimethadione can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Trimethadione can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Trimethadione can be decreased when combined with Ketoconazole.Approved, Investigational
LapatinibThe metabolism of Trimethadione can be decreased when combined with Lapatinib.Approved, Investigational
LeflunomideThe metabolism of Trimethadione can be decreased when combined with Leflunomide.Approved, Investigational
LopinavirThe metabolism of Trimethadione can be decreased when combined with Lopinavir.Approved
LosartanThe metabolism of Trimethadione can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Trimethadione can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Trimethadione can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Trimethadione can be increased when it is combined with Lumacaftor.Approved
MefloquineThe therapeutic efficacy of Trimethadione can be decreased when used in combination with Mefloquine.Approved
MianserinThe therapeutic efficacy of Trimethadione can be decreased when used in combination with Mianserin.Approved
MifepristoneThe serum concentration of Trimethadione can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Trimethadione can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Trimethadione can be decreased when combined with Moclobemide.Approved
ModafinilThe serum concentration of Trimethadione can be decreased when it is combined with Modafinil.Approved, Investigational
NafcillinThe serum concentration of Trimethadione can be decreased when it is combined with Nafcillin.Approved
NefazodoneThe metabolism of Trimethadione can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Trimethadione can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Trimethadione can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Trimethadione can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Trimethadione can be decreased when combined with Nicardipine.Approved
NicotineThe metabolism of Trimethadione can be decreased when combined with Nicotine.Approved
NilotinibThe metabolism of Trimethadione can be decreased when combined with Nilotinib.Approved, Investigational
OlaparibThe metabolism of Trimethadione can be decreased when combined with Olaparib.Approved
OmeprazoleThe metabolism of Trimethadione can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OrlistatThe serum concentration of Trimethadione can be decreased when it is combined with Orlistat.Approved, Investigational
OsimertinibThe serum concentration of Trimethadione can be increased when it is combined with Osimertinib.Approved
PalbociclibThe serum concentration of Trimethadione can be increased when it is combined with Palbociclib.Approved
PantoprazoleThe metabolism of Trimethadione can be decreased when combined with Pantoprazole.Approved
PentobarbitalThe metabolism of Trimethadione can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe metabolism of Trimethadione can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Trimethadione can be increased when combined with Phenytoin.Approved, Vet Approved
PioglitazoneThe metabolism of Trimethadione can be decreased when combined with Pioglitazone.Approved, Investigational
PosaconazoleThe metabolism of Trimethadione can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Trimethadione can be increased when combined with Primidone.Approved, Vet Approved
PyrimethamineThe metabolism of Trimethadione can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuinineThe metabolism of Trimethadione can be decreased when combined with Quinine.Approved
RabeprazoleThe metabolism of Trimethadione can be decreased when combined with Rabeprazole.Approved, Investigational
RanolazineThe metabolism of Trimethadione can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Trimethadione can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Trimethadione can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Trimethadione can be increased when combined with Rifapentine.Approved
RitonavirThe metabolism of Trimethadione can be decreased when combined with Ritonavir.Approved, Investigational
RosiglitazoneThe metabolism of Trimethadione can be decreased when combined with Rosiglitazone.Approved, Investigational
SaquinavirThe metabolism of Trimethadione can be decreased when combined with Saquinavir.Approved, Investigational
SecobarbitalThe metabolism of Trimethadione can be increased when combined with Secobarbital.Approved, Vet Approved
SertralineThe metabolism of Trimethadione can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Trimethadione can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Trimethadione can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Trimethadione can be increased when it is combined with Simeprevir.Approved
SorafenibThe metabolism of Trimethadione can be decreased when combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Trimethadione can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Trimethadione can be increased when it is combined with Stiripentol.Approved
SulfadiazineThe metabolism of Trimethadione can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Trimethadione can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Trimethadione can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TamoxifenThe metabolism of Trimethadione can be decreased when combined with Tamoxifen.Approved
TelaprevirThe metabolism of Trimethadione can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Trimethadione can be decreased when combined with Telithromycin.Approved
TeriflunomideThe metabolism of Trimethadione can be decreased when combined with Teriflunomide.Approved
TicagrelorThe metabolism of Trimethadione can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Trimethadione can be decreased when combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Trimethadione can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Trimethadione can be decreased when combined with Tolbutamide.Approved
TopiramateThe metabolism of Trimethadione can be decreased when combined with Topiramate.Approved
TranylcypromineThe metabolism of Trimethadione can be decreased when combined with Tranylcypromine.Approved
TrimethoprimThe metabolism of Trimethadione can be decreased when combined with Trimethoprim.Approved, Vet Approved
Valproic AcidThe metabolism of Trimethadione can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Trimethadione can be decreased when combined with Valsartan.Approved, Investigational
VenlafaxineThe metabolism of Trimethadione can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Trimethadione can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Trimethadione can be decreased when combined with Voriconazole.Approved, Investigational
ZafirlukastThe metabolism of Trimethadione can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe metabolism of Trimethadione can be decreased when combined with Ziprasidone.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesN03AC02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9954
Blood Brain Barrier+0.9479
Caco-2 permeable+0.5287
P-glycoprotein substrateNon-substrate0.8304
P-glycoprotein inhibitor INon-inhibitor0.6154
P-glycoprotein inhibitor IINon-inhibitor0.8382
Renal organic cation transporterNon-inhibitor0.9503
CYP450 2C9 substrateNon-substrate0.8289
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.5881
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.9694
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9361
Ames testNon AMES toxic0.6493
CarcinogenicityNon-carcinogens0.8515
BiodegradationNot ready biodegradable0.7859
Rat acute toxicity1.8563 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9961
hERG inhibition (predictor II)Non-inhibitor0.9775
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Abbott laboratories pharmaceutical products div
Packagers
Dosage forms
FormRouteStrength
Tablet, chewableOral150 mg/1
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point46 °CPhysProp
water solubility5E+004 mg/LMERCK INDEX (1996)
logP0Not Available
Predicted Properties
PropertyValueSource
Water Solubility212.0 mg/mLALOGPS
logP0.07ALOGPS
logP0.5ChemAxon
logS0.17ALOGPS
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area46.61 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity33.2 m3·mol-1ChemAxon
Polarizability13.59 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (7.69 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
MSMass Spectrum (Electron Ionization)splash10-0006-9200000000-46082deb9c636fb8f625View in MoNA
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as oxazolidinediones. These are compounds containing an oxazolidine ring which bears two ketones.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzolidines
Sub ClassOxazolidines
Direct ParentOxazolidinediones
Alternative Parents
Substituents
  • Oxazolidinedione
  • Tertiary amine
  • Carboxamide group
  • Oxacycle
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aliphatic heteromonocyclic compound
Molecular FrameworkAliphatic heteromonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Scaffold protein binding
Specific Function:
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1G gives rise to T-type calcium currents. T-type calcium channels belong to the "low-v...
Gene Name:
CACNA1G
Uniprot ID:
O43497
Molecular Weight:
262468.62 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Shen H, Zhang B, Shin JH, Lei D, Du Y, Gao X, Wang Q, Ohlemiller KK, Piccirillo J, Bao J: Prophylactic and therapeutic functions of T-type calcium blockers against noise-induced hearing loss. Hear Res. 2007 Apr;226(1-2):52-60. Epub 2006 Dec 31. [PubMed:17291698 ]
  4. Barton ME, Eberle EL, Shannon HE: The antihyperalgesic effects of the T-type calcium channel blockers ethosuximide, trimethadione, and mibefradil. Eur J Pharmacol. 2005 Oct 3;521(1-3):79-85. Epub 2005 Sep 19. [PubMed:16171802 ]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

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 or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
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 ]
  2. Tanaka E, Kurata N, Yasuhara H: Involvement of cytochrome P450 2C9, 2E1 and 3A4 in trimethadione N-demethylation in human microsomes. J Clin Pharm Ther. 2003 Dec;28(6):493-6. [PubMed:14651673 ]
  3. Kurata N, Nishimura Y, Iwase M, Fischer NE, Tang BK, Inaba T, Yasuhara H: Trimethadione metabolism by human liver cytochrome P450: evidence for the involvement of CYP2E1. Xenobiotica. 1998 Nov;28(11):1041-7. [PubMed:9879636 ]
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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. Tanaka E, Kurata N, Yasuhara H: Involvement of cytochrome P450 2C9, 2E1 and 3A4 in trimethadione N-demethylation in human microsomes. J Clin Pharm Ther. 2003 Dec;28(6):493-6. [PubMed:14651673 ]
  3. Kurata N, Nishimura Y, Iwase M, Fischer NE, Tang BK, Inaba T, Yasuhara H: Trimethadione metabolism by human liver cytochrome P450: evidence for the involvement of CYP2E1. Xenobiotica. 1998 Nov;28(11):1041-7. [PubMed:9879636 ]
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 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...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 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. Kurata N, Nishimura Y, Iwase M, Fischer NE, Tang BK, Inaba T, Yasuhara H: Trimethadione metabolism by human liver cytochrome P450: evidence for the involvement of CYP2E1. Xenobiotica. 1998 Nov;28(11):1041-7. [PubMed:9879636 ]
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 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, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
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. Tanaka E, Kurata N, Yasuhara H: Involvement of cytochrome P450 2C9, 2E1 and 3A4 in trimethadione N-demethylation in human microsomes. J Clin Pharm Ther. 2003 Dec;28(6):493-6. [PubMed:14651673 ]
  3. Kurata N, Nishimura Y, Iwase M, Fischer NE, Tang BK, Inaba T, Yasuhara H: Trimethadione metabolism by human liver cytochrome P450: evidence for the involvement of CYP2E1. Xenobiotica. 1998 Nov;28(11):1041-7. [PubMed:9879636 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
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.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 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. Kurata N, Nishimura Y, Iwase M, Fischer NE, Tang BK, Inaba T, Yasuhara H: Trimethadione metabolism by human liver cytochrome P450: evidence for the involvement of CYP2E1. Xenobiotica. 1998 Nov;28(11):1041-7. [PubMed:9879636 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23