Identification

Name
Trimethadione
Accession Number
DB00347  (APRD00315)
Type
Small Molecule
Groups
Approved
Description

An 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
  • Trimethadion
  • Triméthadione
  • Trimethadionum
  • Trimethinum
  • Troxidone
External IDs
A 2297 / J2.519D / NSC-15799 / NSC-169503
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
TridioneTablet, chewable150 mg/1OralAbbvie1946-01-25Not applicableUs
International/Other Brands
Minoale (Dainippon Sumitomo) / Tridione
Categories
UNII
R7GV3H6FQ4
CAS number
127-48-0
Weight
Average: 143.1406
Monoisotopic: 143.058243159
Chemical Formula
C6H9NO3
InChI Key
IRYJRGCIQBGHIV-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

Indication

Used in the control of absence (petit mal) seizures that are refractory to treatment with other medications.

Structured Indications
Pharmacodynamics

Paramethadione 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 action

Dione 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.

TargetActionsOrganism
AVoltage-dependent T-type calcium channel subunit alpha-1G
inhibitor
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding

90%

Metabolism
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity

Symptoms of overdose include clumsiness or unsteadiness, coma, dizziness (severe), drowsiness (severe), nausea (severe), and problems with vision.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not 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
BoceprevirThe metabolism of Trimethadione can be decreased when combined with Boceprevir.Approved, Withdrawn
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
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
CrisaboroleThe metabolism of Trimethadione can be decreased when combined with Crisaborole.Approved
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
DihydroergotamineThe metabolism of Trimethadione can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Trimethadione can be decreased when combined with Diltiazem.Approved
DosulepinThe metabolism of Trimethadione can be decreased when combined with Dosulepin.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 metabolism of Trimethadione can be decreased when 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 metabolism of Trimethadione can be decreased when combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Trimethadione can be decreased when combined with Esomeprazole.Approved, Investigational
EtravirineThe metabolism of Trimethadione can be decreased when 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
LobeglitazoneThe metabolism of Trimethadione can be decreased when combined with Lobeglitazone.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
ManidipineThe metabolism of Trimethadione can be decreased when combined with Manidipine.Approved, Investigational
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, Investigational
MidostaurinThe metabolism of Trimethadione can be decreased when combined with Midostaurin.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 metabolism of Trimethadione can be decreased when combined with Modafinil.Approved, Investigational
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.Investigational, 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, Withdrawn
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
TopiroxostatThe metabolism of Trimethadione can be decreased when combined with Topiroxostat.Approved, Investigational
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
ZucapsaicinThe metabolism of Trimethadione can be decreased when combined with Zucapsaicin.Approved
Food Interactions
Not Available

References

General References
Not Available
External Links
Human Metabolome Database
HMDB14491
KEGG Drug
D00392
PubChem Compound
5576
PubChem Substance
46504478
ChemSpider
5374
BindingDB
50019167
ChEBI
9727
ChEMBL
CHEMBL695
Therapeutic Targets Database
DAP001265
PharmGKB
PA164744924
Drugs.com
Drugs.com Drug Page
Wikipedia
Trimethadione
ATC Codes
N03AC02 — Trimethadione

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
  • Abbott laboratories pharmaceutical products div
Packagers
Dosage forms
FormRouteStrength
Tablet, chewableOral150 mg/1
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)46 °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 FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Download (7.69 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - EI-BGC-MSsplash10-0a4l-8900000000-43db0866b0f6797cbff6
GC-MS Spectrum - CI-BGC-MSsplash10-0006-1900000000-5560efcfc7260e1dcfef
Mass Spectrum (Electron Ionization)MSsplash10-0006-9200000000-46082deb9c636fb8f625
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

Taxonomy

Description
This compound belongs to the class of organic compounds known as oxazolidinediones. These are compounds containing an oxazolidine ring which bears two ketones.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Azolidines
Sub Class
Oxazolidines
Direct Parent
Oxazolidinediones
Alternative Parents
Dicarboximides / Carbamate esters / Organic carbonic acids and derivatives / Oxacyclic compounds / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
Substituents
Oxazolidinedione / Dicarboximide / Carbamic acid ester / Carbonic acid derivative / Oxacycle / Azacycle / Carboxylic acid derivative / Hydrocarbon derivative / Organopnictogen compound / Organic oxygen compound
Molecular Framework
Aliphatic heteromonocyclic compounds
External Descriptors
Not 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, hor...
Gene Name
CACNA1G
Uniprot ID
O43497
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1G
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 ...
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]
  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 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. 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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
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 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. 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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
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]

Drug created on June 13, 2005 07:24 / Updated on November 07, 2017 01:36