General Information of Drug (ID: DMETYK5)

Drug Name
Triazolam
Synonyms
Clorazolam; Halcion; Hypnostat; Novidorm; Novodorm; Songar; Triazolamum; Trilam; Apo Triazo; Apotex Brand of Triazolam; Gen Triazolam; Genpharm Brand of Triazolam; Gerard Brand of Triazolam; Pfizer Brand of Triazolam; Triazolam Pfizer Brand; TGAR01H; U 33030; Alti-Triazolam; Apo-Triazo; Gen-Triazolam; Halcion (TN); Halcion (triazolam); Hypam (TN); Novo-Triolam; Triazolamum [INN-Latin]; Trilam (TN); U 33,030; U-33030; U33,030; Apo-Triazo (TN); U-33,030; Triazolam (JAN/USP/INN); Triazolam [USAN:BAN:INN:JAN]; 8-Chloro-6-(2-chlorophenyl)-1-methyl-4H-(1,2,4)triazolo(4,3-a)(1,4)benzodiazepine; 8-Chloro-6-(2-chlorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine; 8-Chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo(4,3-a)(1,4)benzodiazepine; 8-Chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine; 8-Chloro-6-[2-chlorophenyl]-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
Indication
Disease Entry ICD 11 Status REF
Insomnia 7A00-7A0Z Approved [1]
Therapeutic Class
Hypnotics and Sedatives
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 343.2
Logarithm of the Partition Coefficient (xlogp) 2.4
Rotatable Bond Count (rotbonds) 1
Hydrogen Bond Donor Count (hbonddonor) 0
Hydrogen Bond Acceptor Count (hbondacc) 3
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [2]
Bioavailability
The bioavailability of drug is 44% []
Clearance
The drug present in the plasma can be removed from the body at the rate of 3 mL/min/kg [3]
Elimination
2% of drug is excreted from urine in the unchanged form [2]
Half-life
The concentration or amount of drug in body reduced by one-half in 1.5 - 5.5 hours [3]
Metabolism
The drug is metabolized via the hepatic []
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.0208 micromolar/kg/day [4]
Unbound Fraction
The unbound fraction of drug in plasma is 0.1% [3]
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 0.58 L/kg [3]
Water Solubility
The ability of drug to dissolve in water is measured as 0.045 mg/mL [2]
Chemical Identifiers
Formula
C17H12Cl2N4
IUPAC Name
8-chloro-6-(2-chlorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
Canonical SMILES
CC1=NN=C2N1C3=C(C=C(C=C3)Cl)C(=NC2)C4=CC=CC=C4Cl
InChI
InChI=1S/C17H12Cl2N4/c1-10-21-22-16-9-20-17(12-4-2-3-5-14(12)19)13-8-11(18)6-7-15(13)23(10)16/h2-8H,9H2,1H3
InChIKey
JOFWLTCLBGQGBO-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
5556
ChEBI ID
CHEBI:9674
CAS Number
28911-01-5
DrugBank ID
DB00897
TTD ID
D0U3LS
VARIDT ID
DR00865
INTEDE ID
DR1637
ACDINA ID
D00701

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Translocator protein (TSPO) TTPTXIN TSPO_HUMAN Modulator [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [6]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [6]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Substrate [7]
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 Disease Different from Triazolam (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Sodium bicarbonate DMMU6BJ Minor Altered absorption of Triazolam due to GI dynamics variation caused by Sodium bicarbonate. Acidosis [5C73] [8]
Ivosidenib DM8S6T7 Moderate Increased metabolism of Triazolam caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [9]
Arn-509 DMT81LZ Moderate Increased metabolism of Triazolam caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [10]
Oliceridine DM6MDCF Major Additive CNS depression effects by the combination of Triazolam and Oliceridine. Acute pain [MG31] [11]
Emapalumab DMZG5WL Moderate Altered metabolism of Triazolam due to Emapalumab alters the formation of CYP450 enzymes. Adaptive immunity immunodeficiency [4A01] [10]
Siltuximab DMGEATB Moderate Altered metabolism of Triazolam due to Siltuximab alters the formation of CYP450 enzymes. Anemia [3A00-3A9Z] [10]
Dronedarone DMA8FS5 Moderate Decreased metabolism of Triazolam caused by Dronedarone mediated inhibition of CYP450 enzyme. Angina pectoris [BA40] [12]
Posaconazole DMUL5EW Major Decreased metabolism of Triazolam caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [13]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Triazolam caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [14]
Clarithromycin DM4M1SG Moderate Decreased metabolism of Triazolam caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [13]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Triazolam caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [15]
Telithromycin DMZ4P3A Major Decreased metabolism of Triazolam caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [16]
Erdafitinib DMI782S Moderate Increased metabolism of Triazolam caused by Erdafitinib mediated induction of CYP450 enzyme. Bladder cancer [2C94] [17]
Lapatinib DM3BH1Y Moderate Decreased metabolism of Triazolam caused by Lapatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [18]
Tucatinib DMBESUA Major Decreased metabolism of Triazolam caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [19]
Palbociclib DMD7L94 Moderate Decreased metabolism of Triazolam caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [20]
Dihydrocodeine DMB0FWL Major Additive CNS depression effects by the combination of Triazolam and Dihydrocodeine. Chronic pain [MG30] [21]
Remifentanil DMZTXCH Major Additive CNS depression effects by the combination of Triazolam and Remifentanil. Corneal disease [9A76-9A78] [11]
Lumacaftor DMCLWDJ Major Increased metabolism of Triazolam caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [13]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Triazolam caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [22]
Ethanol DMDRQZU Moderate Additive CNS depression effects by the combination of Triazolam and Ethanol. Cystitis [GC00] [23]
Nefazodone DM4ZS8M Major Decreased metabolism of Triazolam caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [24]
Esketamine DMVU687 Moderate Additive CNS depression effects by the combination of Triazolam and Esketamine. Depression [6A70-6A7Z] [13]
SODIUM CITRATE DMHPD2Y Minor Altered absorption of Triazolam due to GI dynamics variation caused by SODIUM CITRATE. Discovery agent [N.A.] [8]
Cenobamate DM8KLU9 Moderate Increased metabolism of Triazolam caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [25]
Fosphenytoin DMOX3LB Moderate Increased metabolism of Triazolam caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [26]
Tazemetostat DMWP1BH Moderate Increased metabolism of Triazolam caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [27]
Itraconazole DMCR1MV Major Decreased metabolism of Triazolam caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [19]
Miconazole DMPMYE8 Moderate Decreased metabolism of Triazolam caused by Miconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [19]
Ketoconazole DMPZI3Q Major Decreased metabolism of Triazolam caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [19]
Boceprevir DMBSHMF Major Decreased metabolism of Triazolam caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [28]
Simeprevir DMLUA9D Moderate Decreased metabolism of Triazolam caused by Simeprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [29]
Telaprevir DMMRV29 Major Decreased metabolism of Triazolam caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [28]
Isoniazid DM5JVS3 Moderate Decreased metabolism of Triazolam caused by Isoniazid mediated inhibition of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [30]
Rifampin DMA8J1G Minor Increased metabolism of Triazolam caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [31]
Rifapentine DMCHV4I Moderate Increased metabolism of Triazolam caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [32]
Fosamprenavir DM4W9B3 Major Decreased metabolism of Triazolam caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [33]
Cobicistat DM6L4H2 Major Decreased metabolism of Triazolam caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [19]
Saquinavir DMG814N Major Decreased metabolism of Triazolam caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [33]
Etravirine DMGV8QU Moderate Increased metabolism of Triazolam caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [34]
Didanosine DMI2QPE Minor Altered absorption of Triazolam due to GI dynamics variation caused by Didanosine. Human immunodeficiency virus disease [1C60-1C62] [8]
Darunavir DMN3GCH Major Decreased metabolism of Triazolam caused by Darunavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [33]
Atazanavir DMSYRBX Major Decreased metabolism of Triazolam caused by Atazanavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [33]
Probenecid DMMFWOJ Minor Decreased metabolism of Triazolam caused by Probenecid. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [35]
Lesinurad DMUR64T Moderate Increased metabolism of Triazolam caused by Lesinurad mediated induction of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [36]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Triazolam caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [37]
Crizotinib DM4F29C Moderate Decreased metabolism of Triazolam caused by Crizotinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [38]
Brigatinib DM7W94S Moderate Increased metabolism of Triazolam caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [39]
Ceritinib DMB920Z Major Decreased metabolism of Triazolam caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [19]
PF-06463922 DMKM7EW Moderate Increased metabolism of Triazolam caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [40]
Osimertinib DMRJLAT Moderate Increased metabolism of Triazolam caused by Osimertinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [10]
Selpercatinib DMZR15V Moderate Decreased metabolism of Triazolam caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [10]
Idelalisib DM602WT Major Decreased metabolism of Triazolam caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [19]
IPI-145 DMWA24P Moderate Decreased metabolism of Triazolam caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [41]
LGX818 DMNQXV8 Moderate Increased metabolism of Triazolam caused by LGX818 mediated induction of CYP450 enzyme. Melanoma [2C30] [42]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Triazolam and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [43]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Triazolam and Lasmiditan. Migraine [8A80] [44]
Exjade DMHPRWG Moderate Decreased metabolism of Triazolam caused by Exjade mediated inhibition of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [45]
Flibanserin DM70DTN Moderate Additive CNS depression effects by the combination of Triazolam and Flibanserin. Mood disorder [6A60-6E23] [46]
Thalidomide DM70BU5 Moderate Additive CNS depression effects by the combination of Triazolam and Thalidomide. Multiple myeloma [2A83] [47]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Triazolam caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [10]
Nilotinib DM7HXWT Moderate Decreased metabolism of Triazolam caused by Nilotinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [48]
Dasatinib DMJV2EK Moderate Decreased metabolism of Triazolam caused by Dasatinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [49]
Teduglutide DMYOAKS Moderate Altered absorption of Triazolam caused by Teduglutide. Neonatal malabsorption syndrome [KB89] [50]
Entrectinib DMMPTLH Moderate Decreased metabolism of Triazolam caused by Entrectinib mediated inhibition of CYP450 enzyme. Non-small cell lung cancer [2C25] [51]
Levomethadyl Acetate DM06HG5 Major Additive CNS depression effects by the combination of Triazolam and Levomethadyl Acetate. Opioid use disorder [6C43] [21]
Apraclonidine DMO4PVE Moderate Additive CNS depression effects by the combination of Triazolam and Apraclonidine. Optic nerve disorder [9C40] [52]
Olaparib DM8QB1D Moderate Decreased metabolism of Triazolam caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [13]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Triazolam caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [53]
Oxymorphone DM65AGJ Major Additive CNS depression effects by the combination of Triazolam and Oxymorphone. Pain [MG30-MG3Z] [11]
Dezocine DMJDB0Y Major Additive CNS depression effects by the combination of Triazolam and Dezocine. Pain [MG30-MG3Z] [11]
Buprenorphine DMPRI8G Major Additive CNS depression effects by the combination of Triazolam and Buprenorphine. Pain [MG30-MG3Z] [54]
Hydrocodone DMQ2JO5 Major Additive CNS depression effects by the combination of Triazolam and Hydrocodone. Pain [MG30-MG3Z] [11]
Abametapir DM2RX0I Moderate Decreased metabolism of Triazolam caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [55]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Triazolam caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [19]
Enzalutamide DMGL19D Moderate Increased metabolism of Triazolam caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [56]
Ustekinumab DMHTYK3 Moderate Altered metabolism of Triazolam due to Ustekinumab alters the formation of CYP450 enzymes. Psoriasis [EA90] [10]
Temsirolimus DMS104F Moderate Increased plasma concentrations of Triazolam and Temsirolimus due to competitive inhibition of the same metabolic pathway. Renal cell carcinoma [2C90] [57]
Tocilizumab DM7J6OR Moderate Altered metabolism of Triazolam due to Tocilizumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [10]
Canakinumab DM8HLO5 Moderate Altered metabolism of Triazolam due to Canakinumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [10]
Rilonacept DMGLUQS Moderate Altered metabolism of Triazolam due to Rilonacept alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [10]
Golimumab DMHZV7X Moderate Altered metabolism of Triazolam due to Golimumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [10]
Sarilumab DMOGNXY Moderate Altered metabolism of Triazolam due to Sarilumab alters the formation of CYP450 enzymes. Rheumatoid arthritis [FA20] [10]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Triazolam caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [58]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Triazolam caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [10]
Larotrectinib DM26CQR Moderate Decreased metabolism of Triazolam caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [13]
Armodafinil DMGB035 Moderate Increased metabolism of Triazolam caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [59]
LEE011 DMMX75K Moderate Decreased metabolism of Triazolam caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [60]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Triazolam caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [61]
Brilinta DMBR01X Moderate Decreased metabolism of Triazolam caused by Brilinta mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [10]
Amiodarone DMUTEX3 Minor Potentiate the pharmacologic effects by the combination of Triazolam and Amiodarone. Ventricular tachyarrhythmia [BC71] [62]
⏷ Show the Full List of 91 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
Docusate sodium E00563 23673837 Surfactant
FD&C blue no. 1 E00263 19700 Colorant
FD&C blue no. 2 E00446 2723854 Colorant
Sodium benzoate E00432 517055 Antimicrobial preservative; lubricant
Beta-D-lactose E00099 6134 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 7 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Triazolam 0.25 mg tablet 0.25 mg Oral Tablet Oral
Triazolam 0.125 mg tablet 0.125 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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