Details of the Drug

General Information of Drug (ID: DM0Q8MZ)

Drug Name
Trimethadione
Synonyms
Absentol; Absetil; Convenixa; Convexina; Edion; Epidione; Epidone; Epixal; Etydion; Minoaleuiatin; Minoaleviatin; Petidion; Petidon; Petilep; Petimalin; Pitmal; Ptimal; Tioxanona; Tredione; Tricione; Tridilona; Tridion; Tridione; Tridone; Trilidona; Trimedal; Trimedone; Trimetadiona; Trimetadione; Trimethadion; Trimethadionum; Trimethdione; Trimethin; Trimethinum; Trimetin; Trioksal; Trioxanona; Triozanona; Tromedone; Troxidone; Abbott Brand of Trimethadione; Trimetadione [DCIT]; A 2297; Mino-Aleviatin; Neo-Absentol; Tridione (TN); Trimetadiona [INN-Spanish]; Trimethadione [INN:JAN]; Trimethadionum [INN-Latin]; Trimethadione (JP15/INN); 3,3,5-Trimethyl-2,4-diketooxazolidine; 3,5,5,-Trimethyloxazolidine-2,4-dione; 3,5,5-TRIMETHYL-OXAZOLIDINE-2,4-DIONE; 3,5,5-Trimethyl-1,3-oxazolidine-2,4-dione; 3,5,5-Trimethyl-2,4-oxazolidinedione; 3,5,5-Trojmetylooksazolidyno-2,4-dion; 3,5,5-Trojmetylooksazolidyno-2,4-dion [Polish]
Indication
Disease Entry ICD 11 Status REF
Absence epilepsy N.A. Approved [1]
Epilepsy 8A60-8A68 Approved [2]
Pancreatic cancer 2C10 Approved [2]
Therapeutic Class
Anticonvulsants
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 143.14
Logarithm of the Partition Coefficient (xlogp) 0.3
Rotatable Bond Count (rotbonds) 0
Hydrogen Bond Donor Count (hbonddonor) 0
Hydrogen Bond Acceptor Count (hbondacc) 3
ADMET Property
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 279.43982 micromolar/kg/day [3]
Chemical Identifiers
Formula
C6H9NO3
IUPAC Name
3,5,5-trimethyl-1,3-oxazolidine-2,4-dione
Canonical SMILES
CC1(C(=O)N(C(=O)O1)C)C
InChI
InChI=1S/C6H9NO3/c1-6(2)4(8)7(3)5(9)10-6/h1-3H3
InChIKey
IRYJRGCIQBGHIV-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
5576
ChEBI ID
CHEBI:9727
CAS Number
127-48-0
DrugBank ID
DB00347
TTD ID
D0U4VT
INTEDE ID
DR1647
ACDINA ID
D00705
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Voltage-gated calcium channel alpha Cav3.1 (CACNA1G) TT729IR CAC1G_HUMAN Blocker [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [5]
Cytochrome P450 2E1 (CYP2E1) DEVDYN7 CP2E1_HUMAN Substrate [5]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Substrate [5]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Substrate [6]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [7]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Absence epilepsy
ICD Disease Classification
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Voltage-gated calcium channel alpha Cav3.1 (CACNA1G) DTT CACNA1G 3.88E-01 -0.06 -0.18
Voltage-gated calcium channel alpha Cav3.1 (CACNA1G) DTT CACNA1G 9.84E-01 -0.01 -0.03
Cytochrome P450 2E1 (CYP2E1) DME CYP2E1 4.20E-02 -1.71E-01 -3.15E-01
Cytochrome P450 2E1 (CYP2E1) DME CYP2E1 3.07E-01 -2.23E-02 -1.46E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 1.94E-01 -1.03E-01 -3.08E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 7.37E-02 9.49E-02 8.07E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.39E-01 1.54E-02 4.74E-02
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 4.64E-02 -8.21E-02 -7.11E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 8.99E-01 -6.93E-03 -1.36E-02
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 9.21E-01 7.31E-03 6.10E-02
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 4.66E-01 4.25E-02 1.20E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 4.75E-01 5.15E-02 3.64E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Trimethadione (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Levomilnacipran DMV26S8 Moderate Antagonize the effect of Trimethadione when combined with Levomilnacipran. Chronic pain [MG30] [8]
Olopatadine DMKMWQG Moderate Additive CNS depression effects by the combination of Trimethadione and Olopatadine. Conjunctiva disorder [9A60] [9]
Ethanol DMDRQZU Moderate Additive CNS depression effects by the combination of Trimethadione and Ethanol. Cystitis [GC00] [9]
Sertraline DM0FB1J Moderate Antagonize the effect of Trimethadione when combined with Sertraline. Depression [6A70-6A7Z] [8]
Fluoxetine DM3PD2C Moderate Antagonize the effect of Trimethadione when combined with Fluoxetine. Depression [6A70-6A7Z] [8]
Vilazodone DM4LECQ Moderate Antagonize the effect of Trimethadione when combined with Vilazodone. Depression [6A70-6A7Z] [8]
Paroxetine DM5PVQE Moderate Antagonize the effect of Trimethadione when combined with Paroxetine. Depression [6A70-6A7Z] [8]
Vortioxetine DM6F1PU Moderate Antagonize the effect of Trimethadione when combined with Vortioxetine. Depression [6A70-6A7Z] [8]
Duloxetine DM9BI7M Moderate Antagonize the effect of Trimethadione when combined with Duloxetine. Depression [6A70-6A7Z] [8]
Milnacipran DMBFE74 Moderate Antagonize the effect of Trimethadione when combined with Milnacipran. Depression [6A70-6A7Z] [8]
Escitalopram DMFK9HG Moderate Antagonize the effect of Trimethadione when combined with Escitalopram. Depression [6A70-6A7Z] [8]
Desvenlafaxine DMHD4PE Moderate Antagonize the effect of Trimethadione when combined with Desvenlafaxine. Depression [6A70-6A7Z] [8]
Esketamine DMVU687 Moderate Additive CNS depression effects by the combination of Trimethadione and Esketamine. Depression [6A70-6A7Z] [10]
Brimonidine DMQLT4N Moderate Additive CNS depression effects by the combination of Trimethadione and Brimonidine. Glaucoma [9C61] [11]
Chloroquine DMSI5CB Moderate Antagonize the effect of Trimethadione when combined with Chloroquine. Malaria [1F40-1F45] [10]
Hydroxychloroquine DMSIVND Moderate Antagonize the effect of Trimethadione when combined with Hydroxychloroquine. Malaria [1F40-1F45] [10]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Trimethadione and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [12]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Trimethadione and Lasmiditan. Migraine [8A80] [13]
Flibanserin DM70DTN Moderate Additive CNS depression effects by the combination of Trimethadione and Flibanserin. Mood disorder [6A60-6E23] [14]
Thalidomide DM70BU5 Moderate Additive CNS depression effects by the combination of Trimethadione and Thalidomide. Multiple myeloma [2A83] [9]
Ocrelizumab DMEZ2KH Moderate Additive immunosuppressive effects by the combination of Trimethadione and Ocrelizumab. Multiple sclerosis [8A40] [15]
Omacetaxine mepesuccinate DMPU2WX Moderate Additive immunosuppressive effects by the combination of Trimethadione and Omacetaxine mepesuccinate. Myeloproliferative neoplasm [2A20] [16]
Apraclonidine DMO4PVE Moderate Additive CNS depression effects by the combination of Trimethadione and Apraclonidine. Optic nerve disorder [9C40] [11]
Dextropropoxyphene DM23HCX Major Additive CNS depression effects by the combination of Trimethadione and Dextropropoxyphene. Pain [MG30-MG3Z] [17]
Buprenorphine DMPRI8G Major Additive CNS depression effects by the combination of Trimethadione and Buprenorphine. Pain [MG30-MG3Z] [18]
Meperidine DMX4GND Moderate Additive CNS depression effects by the combination of Trimethadione and Meperidine. Pain [MG30-MG3Z] [19]
Tizanidine DMR2IQ4 Moderate Additive CNS depression effects by the combination of Trimethadione and Tizanidine. Tonus and reflex abnormality [MB47] [20]
Ganciclovir DM1MBYQ Moderate Additive myelosuppressive effects by the combination of Trimethadione and Ganciclovir. Virus infection [1A24-1D9Z] [10]
Valganciclovir DMS2IUH Moderate Additive myelosuppressive effects by the combination of Trimethadione and Valganciclovir. Virus infection [1A24-1D9Z] [10]
⏷ Show the Full List of 29 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Magnesium trisilicate E00477 5311266 Glidant
Saccharose E00091 5988 Binding agent; Coating agent; Cryoprotectant; Diluent; Flavoring agent; Suspending agent; Viscosity-controlling agent
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Trimethadione 150 mg tablet 150 mg Chewable Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Trimethadione FDA Label
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7316).
3 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
4 Prophylactic and therapeutic functions of T-type calcium blockers against noise-induced hearing loss. Hear Res. 2007 Apr;226(1-2):52-60.
5 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.
6 Evaluation of child/adult pharmacokinetic differences from a database derived from the therapeutic drug literature. Toxicol Sci. 2002 Apr;66(2):185-200.
7 Trimethadione metabolism by human liver cytochrome P450: evidence for the involvement of CYP2E1. Xenobiotica. 1998 Nov;28(11):1041-7.
8 Belcastro V, Costa C, Striano P "Levetiracetam-associated hyponatremia." Seizure 17 (2008): 389-90. [PMID: 18584781]
9 Warrington SJ, Ankier SI, Turner P "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology 15 (1986): 31-7. [PMID: 3725002]
10 Cerner Multum, Inc. "Australian Product Information.".
11 Product Information. Alphagan (brimonidine ophthalmic). Allergan Inc, Irvine, CA.
12 Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
13 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
14 Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
15 Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
16 Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA.
17 Hansen BS, Dam M, Brandt J, et al "Influence of dextropropoxyphene on steady state serum levels and protein binding of three anti-epileptic drugs in man." Acta Neurol Scand 61 (1980): 357-67. [PMID: 6998251]
18 Sekar M, Mimpriss TJ "Buprenorphine, benzodiazepines and prolonged respiratory depression." Anaesthesia 42 (1987): 567-8. [PMID: 3592200]
19 Lambertsen CJ, Wendel H, Longenhagen JB "The separate and combined respiratory effects of chlorpromazine and meperidine in normal men controlled at 46 mm Hg alveolar pCO2." J Pharmacol Exp Ther 131 (1961): 381-93. [PMID: 13758472]
20 Product Information. Zanaflex (tizanidine). Acorda Therapeutics, Hawthorne, NY.