Details of the Drug

General Information of Drug (ID: DMPFWO6)

Drug Name
Halazepam
Synonyms
Halazepamum; Pacinone; Paxipam; Sch 12041; Schering 12041; Alapryl (TN); Halazepamum [INN-Latin]; Pacinone (TN); Paxipam (TN); Sch-12041; Halazepam (USAN/INN); Halazepam [USAN:BAN:INN]; 7-Chloro-1,3-dihydro-5-phenyl-1-(2,2,2-trifluoroethyl)-2H-1,4-benzodiazepin-2-one; 7-Chloro-5-phenyl-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one; 7-chloro-5-phenyl-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepin-2-one; 7=Chlor-5-phenyl-1-(2,2,2-trifluorethyl)-1H-1,4-benzodiazepin-2(3H)-on
Indication
Disease Entry ICD 11 Status REF
Anxiety disorder 6B00-6B0Z Approved [1]
Therapeutic Class
Antianxiety Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 352.7
Logarithm of the Partition Coefficient (xlogp) 4
Rotatable Bond Count (rotbonds) 2
Hydrogen Bond Donor Count (hbonddonor) 0
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
Metabolism
The drug is metabolized via the hepatic []
Chemical Identifiers
Formula
C17H12ClF3N2O
IUPAC Name
7-chloro-5-phenyl-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepin-2-one
Canonical SMILES
C1C(=O)N(C2=C(C=C(C=C2)Cl)C(=N1)C3=CC=CC=C3)CC(F)(F)F
InChI
InChI=1S/C17H12ClF3N2O/c18-12-6-7-14-13(8-12)16(11-4-2-1-3-5-11)22-9-15(24)23(14)10-17(19,20)21/h1-8H,9-10H2
InChIKey
WYCLKVQLVUQKNZ-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
31640
ChEBI ID
CHEBI:5603
CAS Number
23092-17-3
DrugBank ID
DB00801
TTD ID
D0Z9VB

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 [2]
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 Halazepam (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Sodium bicarbonate DMMU6BJ Minor Altered absorption of Halazepam due to GI dynamics variation caused by Sodium bicarbonate. Acidosis [5C73] [3]
Oliceridine DM6MDCF Major Additive CNS depression effects by the combination of Halazepam and Oliceridine. Acute pain [MG31] [4]
Dalfopristin DM4LTKV Moderate Decreased metabolism of Halazepam caused by Dalfopristin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [5]
Clarithromycin DM4M1SG Moderate Decreased metabolism of Halazepam caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [6]
Dihydrocodeine DMB0FWL Major Additive CNS depression effects by the combination of Halazepam and Dihydrocodeine. Chronic pain [MG30] [4]
Propofol DMB4OLE Moderate Additive cardiorespiratory depression effects by the combination of Halazepam and Propofol. Corneal disease [9A76-9A78] [7]
Alfentanil DMVO0UB Major Additive CNS depression effects by the combination of Halazepam and Alfentanil. Corneal disease [9A76-9A78] [8]
Remifentanil DMZTXCH Major Additive CNS depression effects by the combination of Halazepam and Remifentanil. Corneal disease [9A76-9A78] [8]
Ethanol DMDRQZU Moderate Additive CNS depression effects by the combination of Halazepam and Ethanol. Cystitis [GC00] [9]
Nefazodone DM4ZS8M Moderate Decreased metabolism of Halazepam caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [10]
Esketamine DMVU687 Moderate Additive CNS depression effects by the combination of Halazepam and Esketamine. Depression [6A70-6A7Z] [11]
SODIUM CITRATE DMHPD2Y Minor Altered absorption of Halazepam due to GI dynamics variation caused by SODIUM CITRATE. Discovery agent [N.A.] [3]
Fosphenytoin DMOX3LB Moderate Increased metabolism of Halazepam caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [12]
Isoniazid DM5JVS3 Moderate Decreased metabolism of Halazepam caused by Isoniazid mediated inhibition of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [13]
Rifampin DMA8J1G Minor Increased metabolism of Halazepam caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [14]
Fosamprenavir DM4W9B3 Moderate Decreased metabolism of Halazepam caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [15]
Didanosine DMI2QPE Minor Altered absorption of Halazepam due to GI dynamics variation caused by Didanosine. Human immunodeficiency virus disease [1C60-1C62] [3]
Probenecid DMMFWOJ Minor Decreased metabolism of Halazepam caused by Probenecid. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [16]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Halazepam and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [17]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Halazepam and Lasmiditan. Migraine [8A80] [18]
Flibanserin DM70DTN Moderate Additive CNS depression effects by the combination of Halazepam and Flibanserin. Mood disorder [6A60-6E23] [19]
Thalidomide DM70BU5 Moderate Additive CNS depression effects by the combination of Halazepam and Thalidomide. Multiple myeloma [2A83] [20]
Teduglutide DMYOAKS Moderate Altered absorption of Halazepam caused by Teduglutide. Neonatal malabsorption syndrome [KB89] [21]
Apraclonidine DMO4PVE Moderate Additive CNS depression effects by the combination of Halazepam and Apraclonidine. Optic nerve disorder [9C40] [22]
Oxymorphone DM65AGJ Major Additive CNS depression effects by the combination of Halazepam and Oxymorphone. Pain [MG30-MG3Z] [8]
Levorphanol DMGS80V Major Additive CNS depression effects by the combination of Halazepam and Levorphanol. Pain [MG30-MG3Z] [8]
Nalbuphine DMOSQGU Major Additive CNS depression effects by the combination of Halazepam and Nalbuphine. Pain [MG30-MG3Z] [8]
Buprenorphine DMPRI8G Major Additive CNS depression effects by the combination of Halazepam and Buprenorphine. Pain [MG30-MG3Z] [23]
Hydrocodone DMQ2JO5 Major Additive CNS depression effects by the combination of Halazepam and Hydrocodone. Pain [MG30-MG3Z] [8]
Temsirolimus DMS104F Moderate Increased plasma concentrations of Halazepam and Temsirolimus due to competitive inhibition of the same metabolic pathway. Renal cell carcinoma [2C90] [24]
Fentanyl DM8WAHT Major Additive CNS depression effects by the combination of Halazepam and Fentanyl. Sensation disturbance [MB40] [8]
Armodafinil DMGB035 Minor Increased metabolism of Halazepam caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [25]
Sirolimus DMGW1ID Moderate Increased plasma concentrations of Halazepam and Sirolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [24]
Tacrolimus DMZ7XNQ Moderate Increased plasma concentrations of Halazepam and Tacrolimus due to competitive inhibition of the same metabolic pathway. Transplant rejection [NE84] [24]
Amiodarone DMUTEX3 Minor Potentiate the pharmacologic effects by the combination of Halazepam and Amiodarone. Ventricular tachyarrhythmia [BC71] [26]
⏷ Show the Full List of 35 DDI Information of This Drug

References

1 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: 7195).
2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
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4 US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
5 Product Information. Synercid (dalfopristin-quinupristin) Rhone-Poulenc Rorer, Collegeville, PA.
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8 US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
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15 Product Information. Agenerase (amprenavir). Glaxo Wellcome, Research Triangle Pk, NC.
16 Abernethy DR, Greenblatt DJ, Ameer B, Shader RI "Probenecid impairment of acetaminophen and lorazepam clearance: direct inhibition of ether glucuronide formation." J Pharmacol Exp Ther 234 (1985): 345-9. [PMID: 4020675]
17 Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
18 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
19 Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
20 Warrington SJ, Ankier SI, Turner P "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology 15 (1986): 31-7. [PMID: 3725002]
21 Product Information. Gattex (teduglutide). NPS Pharmaceuticals, Bedminster, NJ.
22 Product Information. Alphagan (brimonidine ophthalmic). Allergan Inc, Irvine, CA.
23 Sekar M, Mimpriss TJ "Buprenorphine, benzodiazepines and prolonged respiratory depression." Anaesthesia 42 (1987): 567-8. [PMID: 3592200]
24 Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL.
25 Doherty MM, Charman WN "The mucosa of the small intestine: how clinically relevant as an organ of drug metabolism?" Clin Pharmacokinet 41 (2002): 235-53. [PMID: 11978143]
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