Details of the Drug

General Information of Drug (ID: DM08E9O)

Drug Name
Diazepam
Synonyms
diazepam; Valium; 439-14-5; Diazemuls; Ansiolisina; Sibazon; Relanium; Faustan; Apaurin; Stesolid; Seduxen; Methyldiazepinone; Valitran; Tranqdyn; Seduksen; Relaminal; Quiatril; Quetinil; Dipezona; Diazetard; Diazepan; Calmpose; Tranimul; Tensopam; Serenack; Paranten; Kiatrium; Domalium; Condition; Bialzepam; Ansiolin; Unisedil; Stesolin; Serenamin; Ruhsitus; Renborin; Quievita; Tranquirit; Serenzin; Neurolytril; Liberetas; Diacepan; Ceregulart; Calmocitene; Bensedin; Atensine; Apozepam; Umbrium; Sonacon; Sedipam; Levium; Diapam; Atilen; Assival; Amiprol; Diazepam (intranasal, epilepsy)
Indication
Disease Entry ICD 11 Status REF
Epilepsy 8A60-8A68 Approved [1], [2]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 284.74
Topological Polar Surface Area (xlogp) 3
Rotatable Bond Count (rotbonds) 1
Hydrogen Bond Donor Count (hbonddonor) 0
Hydrogen Bond Acceptor Count (hbondacc) 2
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [3]
Bioavailability
99% of drug becomes completely available to its intended biological destination(s) [4]
Clearance
The drug present in the plasma can be removed from the body at the rate of 0.38 mL/min/kg [5]
Elimination
0.5% of drug is excreted from urine in the unchanged form [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 42 hours [5]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 2.00784 micromolar/kg/day [6]
Unbound Fraction
The unbound fraction of drug in plasma is 0.023% [5]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 1 L/kg [5]
Water Solubility
The ability of drug to dissolve in water is measured as 0.057 mg/mL [3]
Chemical Identifiers
Formula
C16H13ClN2O
IUPAC Name
7-chloro-1-methyl-5-phenyl-3H-1,4-benzodiazepin-2-one
Canonical SMILES
CN1C(=O)CN=C(C2=C1C=CC(=C2)Cl)C3=CC=CC=C3
InChI
InChI=1S/C16H13ClN2O/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11/h2-9H,10H2,1H3
InChIKey
AAOVKJBEBIDNHE-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
3016
ChEBI ID
CHEBI:49575
CAS Number
439-14-5
DrugBank ID
DB00829
TTD ID
D07JVL
VARIDT ID
DR00999
INTEDE ID
DR0480
ACDINA ID
D00190

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Translocator protein (TSPO) TTPTXIN TSPO_HUMAN Agonist [7], [8]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [9]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [10]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Substrate [11]
Mephenytoin 4-hydroxylase (CYP2C19)
Main DME 		DEGTFWK CP2CJ_HUMAN Substrate [12]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [13]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [14]
Cytochrome P450 2B6 (CYP2B6) DEPKLMQ CP2B6_HUMAN Substrate [15]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [16]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [17]
Prostaglandin G/H synthase 1 (COX-1) DE073H6 PGH1_HUMAN Substrate [18]
Cytochrome P450 2C18 (CYP2C18) DEZMWRE CP2CI_HUMAN Substrate [19]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Diazepam
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Stiripentol DMMSDOY Moderate Decreased metabolism of Diazepam caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [94]
Fosphenytoin DMOX3LB Moderate Increased metabolism of Diazepam caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [95]
Coadministration of a Drug Treating the Disease Different from Diazepam (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Sodium bicarbonate DMMU6BJ Minor Altered absorption of Diazepam due to GI dynamics variation caused by Sodium bicarbonate. Acidosis [5C73] [96]
Oliceridine DM6MDCF Major Additive CNS depression effects by the combination of Diazepam and Oliceridine. Acute pain [MG31] [97]
Emapalumab DMZG5WL Moderate Altered metabolism of Diazepam due to Emapalumab alters the formation of CYP450 enzymes. Adaptive immunity immunodeficiency [4A01] [98]
Siltuximab DMGEATB Moderate Altered metabolism of Diazepam due to Siltuximab alters the formation of CYP450 enzymes. Anemia [3A00-3A9Z] [98]
Dronedarone DMA8FS5 Moderate Decreased clearance of Diazepam due to the transporter inhibition by Dronedarone. Angina pectoris [BA40] [99]
Posaconazole DMUL5EW Moderate Decreased metabolism of Diazepam caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [100]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Diazepam caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [101]
Clarithromycin DM4M1SG Moderate Decreased metabolism of Diazepam caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [102]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Diazepam caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [102]
Lapatinib DM3BH1Y Moderate Decreased clearance of Diazepam due to the transporter inhibition by Lapatinib. Breast cancer [2C60-2C6Y] [103]
Alpelisib DMEXMYK Moderate Increased metabolism of Diazepam caused by Alpelisib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [104]
Dihydrocodeine DMB0FWL Major Additive CNS depression effects by the combination of Diazepam and Dihydrocodeine. Chronic pain [MG30] [105]
Remifentanil DMZTXCH Major Additive CNS depression effects by the combination of Diazepam and Remifentanil. Corneal disease [9A76-9A78] [97]
Mifepristone DMGZQEF Moderate Decreased metabolism of Diazepam caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [106]
Ivacaftor DMZC1HS Moderate Decreased clearance of Diazepam due to the transporter inhibition by Ivacaftor. Cystic fibrosis [CA25] [107]
Ethanol DMDRQZU Moderate Additive CNS depression effects by the combination of Diazepam and Ethanol. Cystitis [GC00] [108]
MK-8228 DMOB58Q Moderate Decreased metabolism of Diazepam caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [109]
Esketamine DMVU687 Moderate Additive CNS depression effects by the combination of Diazepam and Esketamine. Depression [6A70-6A7Z] [106]
SODIUM CITRATE DMHPD2Y Minor Altered absorption of Diazepam due to GI dynamics variation caused by SODIUM CITRATE. Discovery agent [N.A.] [96]
Itraconazole DMCR1MV Moderate Decreased metabolism of Diazepam caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [100]
Miconazole DMPMYE8 Moderate Decreased metabolism of Diazepam caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [100]
Ketoconazole DMPZI3Q Moderate Decreased metabolism of Diazepam caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [100]
Bumetanide DMRV7H0 Moderate Additive hypotensive effects by the combination of Diazepam and Bumetanide. Heart failure [BD10-BD1Z] [110]
Boceprevir DMBSHMF Moderate Decreased metabolism of Diazepam caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [111]
Telaprevir DMMRV29 Moderate Decreased metabolism of Diazepam caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [112]
Isoniazid DM5JVS3 Moderate Decreased metabolism of Diazepam caused by Isoniazid mediated inhibition of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [113]
Rifampin DMA8J1G Minor Increased metabolism of Diazepam caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [114]
Rifapentine DMCHV4I Moderate Increased metabolism of Diazepam caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [115]
Fosamprenavir DM4W9B3 Moderate Decreased metabolism of Diazepam caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [116]
Cobicistat DM6L4H2 Moderate Decreased clearance of Diazepam due to the transporter inhibition by Cobicistat. Human immunodeficiency virus disease [1C60-1C62] [117]
Etravirine DMGV8QU Moderate Decreased metabolism of Diazepam caused by Etravirine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [118]
Didanosine DMI2QPE Minor Altered absorption of Diazepam due to GI dynamics variation caused by Didanosine. Human immunodeficiency virus disease [1C60-1C62] [96]
Darunavir DMN3GCH Moderate Decreased metabolism of Diazepam caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [119]
Conivaptan DM1V329 Moderate Decreased metabolism of Diazepam caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [120]
Probenecid DMMFWOJ Minor Decreased metabolism of Diazepam caused by Probenecid. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [121]
Crizotinib DM4F29C Moderate Decreased metabolism of Diazepam caused by Crizotinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [122]
Brigatinib DM7W94S Moderate Increased metabolism of Diazepam caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [123]
PF-06463922 DMKM7EW Moderate Increased metabolism of Diazepam caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [106]
Idelalisib DM602WT Moderate Decreased metabolism of Diazepam caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [124]
Vemurafenib DM62UG5 Moderate Decreased metabolism of Diazepam caused by Vemurafenib mediated inhibition of CYP450 enzyme. Melanoma [2C30] [106]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Diazepam caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [98]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Diazepam and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [125]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Diazepam and Lasmiditan. Migraine [8A80] [126]
Exjade DMHPRWG Moderate Decreased metabolism of Diazepam caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [127]
Flibanserin DM70DTN Moderate Additive CNS depression effects by the combination of Diazepam and Flibanserin. Mood disorder [6A60-6E23] [128]
Thalidomide DM70BU5 Moderate Additive CNS depression effects by the combination of Diazepam and Thalidomide. Multiple myeloma [2A83] [129]
Teduglutide DMYOAKS Moderate Altered absorption of Diazepam caused by Teduglutide. Neonatal malabsorption syndrome [KB89] [130]
Levomethadyl Acetate DM06HG5 Major Additive CNS depression effects by the combination of Diazepam and Levomethadyl Acetate. Opioid use disorder [6C43] [105]
Apraclonidine DMO4PVE Moderate Additive CNS depression effects by the combination of Diazepam and Apraclonidine. Optic nerve disorder [9C40] [131]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Diazepam caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [132]
Oxymorphone DM65AGJ Major Additive CNS depression effects by the combination of Diazepam and Oxymorphone. Pain [MG30-MG3Z] [97]
Levorphanol DMGS80V Major Additive CNS depression effects by the combination of Diazepam and Levorphanol. Pain [MG30-MG3Z] [97]
Dezocine DMJDB0Y Major Additive CNS depression effects by the combination of Diazepam and Dezocine. Pain [MG30-MG3Z] [97]
Nalbuphine DMOSQGU Major Additive CNS depression effects by the combination of Diazepam and Nalbuphine. Pain [MG30-MG3Z] [97]
Buprenorphine DMPRI8G Major Additive CNS depression effects by the combination of Diazepam and Buprenorphine. Pain [MG30-MG3Z] [133]
Hydrocodone DMQ2JO5 Major Additive CNS depression effects by the combination of Diazepam and Hydrocodone. Pain [MG30-MG3Z] [97]
Abametapir DM2RX0I Moderate Decreased metabolism of Diazepam caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [134]
Lefamulin DME6G97 Moderate Decreased metabolism of Diazepam caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [135]
Enzalutamide DMGL19D Moderate Increased metabolism of Diazepam caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [136]
Ustekinumab DMHTYK3 Moderate Altered metabolism of Diazepam due to Ustekinumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [98]
Ixekizumab DMXW92T Moderate Altered metabolism of Diazepam due to Ixekizumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [98]
Temsirolimus DMS104F Moderate Increased plasma concentrations of Diazepam and Temsirolimus due to competitive inhibition of the same metabolic pathway. Renal cell carcinoma [2C90] [137]
Tocilizumab DM7J6OR Moderate Altered metabolism of Diazepam due to Tocilizumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [98]
Canakinumab DM8HLO5 Moderate Altered metabolism of Diazepam due to Canakinumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [98]
Rilonacept DMGLUQS Moderate Altered metabolism of Diazepam due to Rilonacept alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [98]
Sarilumab DMOGNXY Moderate Altered metabolism of Diazepam due to Sarilumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [98]
Armodafinil DMGB035 Moderate Decreased metabolism of Diazepam caused by Armodafinil mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [106]
LEE011 DMMX75K Moderate Decreased metabolism of Diazepam caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [138]
Fostamatinib DM6AUHV Moderate Decreased clearance of Diazepam due to the transporter inhibition by Fostamatinib. Thrombocytopenia [3B64] [139]
Sirolimus DMGW1ID Moderate Increased plasma concentrations of Diazepam and Sirolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [137]
Tacrolimus DMZ7XNQ Moderate Increased plasma concentrations of Diazepam and Tacrolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [137]
Amiodarone DMUTEX3 Minor Potentiate the pharmacologic effects by the combination of Diazepam and Amiodarone. Ventricular tachyarrhythmia [BC71] [140]
⏷ Show the Full List of 72 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
FD&C blue no. 1 E00263 19700 Colorant
Quinoline yellow WS E00309 24671 Colorant
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sunset yellow FCF E00255 17730 Colorant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Calcium stearate E00244 15324 lubricant
Carmellose sodium E00625 Not Available Disintegrant
Galactose E00093 6036 Complexing agent; Flavoring agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
⏷ Show the Full List of 11 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Diazepam 10 mg tablet 10 mg Oral Tablet Oral
Diazepam 5 mg tablet 5 mg Oral Tablet Oral
Diazepam 2 mg tablet 2 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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