Details of the Drug

General Information of Drug (ID: DMY4D87)

Drug Name

Quazepam

Synonyms

Cetrane; Doral; Dormalin; Oniria; Prosedar; Quazapam; Quazepamum; Quazium; Selepam; Sch 16134; Doral (TN); Dormalin (TN); Quazepamum [INN-Latin]; Sch-161; Sch-16134; Quazepam (JAN/USP); Quazepam [USAN:BAN:INN]; Quazepam (JAN/USP/INN); 7-Chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2H-1,4-benzodiazepine-2-thione; 7-Chloro-5-(o-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2H-1,4-benzodiazepine-2-thione; 7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepine-2-thione

Indication

Disease Entry	ICD 11	Status	REF
Insomnia	7A00-7A0Z	Approved	[1]
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Therapeutic Class

Hypnotics and Sedatives

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

386.8

Logarithm of the Partition Coefficient (xlogp)

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [2]
Bioavailability: The bioavailability of drug is 29-35% []
Half-life: The concentration or amount of drug in body reduced by one-half in 39 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 0.554 micromolar/kg/day [4]

Chemical Identifiers

Formula: C17H11ClF4N2S
IUPAC Name: 7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepine-2-thione
Canonical SMILES: C1C(=S)N(C2=C(C=C(C=C2)Cl)C(=N1)C3=CC=CC=C3F)CC(F)(F)F
InChI: InChI=1S/C17H11ClF4N2S/c18-10-5-6-14-12(7-10)16(11-3-1-2-4-13(11)19)23-8-15(25)24(14)9-17(20,21)22/h1-7H,8-9H2
InChIKey: IKMPWMZBZSAONZ-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 4999
ChEBI ID: CHEBI:8694
CAS Number: 36735-22-5
DrugBank ID: DB01589
TTD ID: D03NPH
INTEDE ID: DR1374
ACDINA ID: D00574

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]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Substrate	[6]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Substrate	[6]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Substrate	[7]

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Molecular Interaction Atlas (MIA)

MIA Detail

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 Quazepam (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Oliceridine	DM6MDCF	Major	Additive CNS depression effects by the combination of Quazepam and Oliceridine.	Acute pain [MG31]	[8]
Troleandomycin	DMUZNIG	Moderate	Decreased metabolism of Quazepam caused by Troleandomycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[9]
Osilodrostat	DMIJC9X	Moderate	Decreased metabolism of Quazepam caused by Osilodrostat mediated inhibition of CYP450 enzyme.	Cushing syndrome [5A70]	[10]
MK-8228	DMOB58Q	Moderate	Increased metabolism of Quazepam caused by MK-8228 mediated induction of CYP450 enzyme.	Cytomegaloviral disease [1D82]	[11]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Quazepam and Esketamine.	Depression [6A70-6A7Z]	[12]
SODIUM CITRATE	DMHPD2Y	Minor	Altered absorption of Quazepam due to GI dynamics variation caused by SODIUM CITRATE.	Discovery agent [N.A.]	[13]
Cenobamate	DM8KLU9	Moderate	Decreased metabolism of Quazepam caused by Cenobamate mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[14]
Etravirine	DMGV8QU	Moderate	Increased metabolism of Quazepam caused by Etravirine mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[15]
Dabrafenib	DMX6OE3	Moderate	Increased metabolism of Quazepam caused by Dabrafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[16]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Quazepam and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[17]
Lasmiditan	DMXLVDT	Moderate	Additive CNS depression effects by the combination of Quazepam and Lasmiditan.	Migraine [8A80]	[18]
Flibanserin	DM70DTN	Moderate	Additive CNS depression effects by the combination of Quazepam and Flibanserin.	Mood disorder [6A60-6E23]	[19]
Fedratinib	DM4ZBK6	Moderate	Decreased metabolism of Quazepam caused by Fedratinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[16]
Nilotinib	DM7HXWT	Moderate	Decreased metabolism of Quazepam caused by Nilotinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[20]
Teduglutide	DMYOAKS	Moderate	Altered absorption of Quazepam caused by Teduglutide.	Neonatal malabsorption syndrome [KB89]	[21]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Quazepam caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[22]
Lefamulin	DME6G97	Moderate	Decreased metabolism of Quazepam caused by Lefamulin mediated inhibition of CYP450 enzyme.	Pneumonia [CA40]	[23]
Lonafarnib	DMGM2Z6	Moderate	Decreased metabolism of Quazepam caused by Lonafarnib mediated inhibition of CYP450 enzyme.	Premature ageing appearance [LD2B]	[24]
Temsirolimus	DMS104F	Moderate	Increased plasma concentrations of Quazepam and Temsirolimus due to competitive inhibition of the same metabolic pathway.	Renal cell carcinoma [2C90]	[25]
Larotrectinib	DM26CQR	Moderate	Decreased metabolism of Quazepam caused by Larotrectinib mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[12]
Armodafinil	DMGB035	Minor	Increased metabolism of Quazepam caused by Armodafinil mediated induction of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[26]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Quazepam caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[27]
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⏷ Show the Full List of 22 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
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
Magnesium stearate	E00208	11177	lubricant
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
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Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Quazepam 15 mg tablet	15 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page 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: 7288).
2	BDDCS applied to over 900 drugs
3	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
4	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
5	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
6	Interaction between grapefruit juice and hypnotic drugs: comparison of triazolam and quazepam. Eur J Clin Pharmacol. 2006 Mar;62(3):209-15.
7	In vitro metabolism of quazepam in human liver and intestine and assessment of drug interactions. Xenobiotica. 2004 Nov-Dec;34(11-12):1001-11.
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.".
9	Amsden GW "Macrolides versus azalides: a drug interaction update." Ann Pharmacother 29 (1995): 906-17. [PMID: 8547740]
10	Product Information. Isturisa (osilodrostat). Recordati Rare Diseases Inc, Lebanon, NJ.
11	Product Information. Prevymis (letermovir). Merck & Company Inc, Whitehouse Station, NJ.
12	Cerner Multum, Inc. "Australian Product Information.".
13	Chun AH, Carrigan PJ, Hoffman DJ, Kershner RP, Stuart JD "Effect of antacids on absorption of clorazepate." Clin Pharmacol Ther 22 (1977): 329-35. [PMID: 19188]
14	Product Information. Xcopri (cenobamate). SK Life Science, Inc., Paramus, NJ.
15	Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ.
16	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
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	Product Information. Tasigna (nilotinib). Novartis Pharmaceuticals, East Hanover, NJ.
21	Product Information. Gattex (teduglutide). NPS Pharmaceuticals, Bedminster, NJ.
22	Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
23	Product Information. Fycompa (perampanel). Eisai Inc, Teaneck, NJ.
24	Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
25	Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL.
26	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]
27	Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.