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Quazepam

Quazepam structure

CAS No:
36735-22-5
Formula:
C17H11ClF4N2S
Chemical Name:
Quazepam
Synonyms:
2H-1,4-Benzodiazepine-2-thione,7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-;7-Chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2H-1,4-benzodiazepine-2-thione;7-Chloro-1-(2,2,2-trifluoroethyl)-1,3-dihydro-5-(o-fluorophenyl)-2H-1,4-benzodiazepine-2-thione;7-Chloro-1-(2,2,2-trifluoroethyl)-1,3-dihydro-5-(2-fluorophenyl)-2H-1,4-benzodiazepine-2-thione;Quazepam;Sch 16134;Oniria;Selepam;Prosedar;Dormalin;Quazium;Doral;NSC 309702
Categories:
Active Pharmaceutical Ingredients > Nervous System Drugs

Description

Solid

Quazepam is a benzodiazepine.|Quazepam is a DEA Schedule IV controlled substance. Substances in the DEA Schedule IV have a low potential for abuse relative to substances in Schedule III.|Quazepam is a drug which is a benzodiazepine derivative. It induces impairment of motor function and has hypnotic properties. Quazepam is used to treat insomnia.|Quazepam is a Benzodiazepine.|Quazepam is an orally available benzodiazepine used to treat insomnia. As with most benzodiazepines, quazepam therapy has not been associated with serum aminotransferase or alkaline phosphatase elevations, and clinically apparent liver injury from quazepam has not been reported and must be very rare, if it occurs at all.|Quazepam is a synthetic benzodiazepine derivative with anxiolytic, sedative and hypnotic properties. Quazepam and its major metabolite 2-oxoquazepam potentiate gamma-aminobutyric acid (GABA) activity by binding to the benzodiazepine-1 recognition site (BZ-1) within the GABA-A receptor, located in the limbic, neocortical and mesencephalic reticular system. This increases the frequency of GABA-activated chloride channel opening events, allowing the flow of chloride ions into the neuron leading to membrane hyperpolarization and decreased neuronal excitability.

Quazepam Basic Attributes

Molecular Weight：

386.8

Exact Mass：

386.79

EC Number：

253-179-4

UNII：

JF8V0828ZI

DEA Code Number：

2881

NSC Number：

309702

DSSTox ID：

DTXSID60190193

NCI Thesaurus Code：

C47699

ATC Code：

N - Nervous system

HScode：

2933996500

Characteristics

PSA：

47.69000

XLogP3：

4.06

Appearance：

Solid

Density：

1.4±0.1 g/cm3

Melting Point：

137.5-139 °C

Boiling Point：

429.9±55.0 °C at 760 mmHg

Flash Point：

213.8±31.5 °C

Refractive Index：

1.595

Water Solubility：

2.31e-03 g/L

Toxicity：

LD50 in mice (mg/kg): >1370 i.v., >5000 orally (Orgini); LD50 in male, female mice, rats (mg/kg): 845, 921, 3072, 2749 i.p. (Black)

Collision Cross Section：

174.9 Å² [M+H]+ [CCS Type: TW, Method: Major Mix IMS/Tof Calibration Kit (Waters)]

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

3249

Toxicity

Hepatotoxicity：

Quazepam, like other benzodiazepines, is rarely associated with serum ALT elevations, and clinically apparent liver injury from quazepam is extremely rare, if it occurs at all. There have been no case reports of symptomatic, acute liver injury from quazepam, but it has not been available for very long. Cases of clinically apparent liver injury have been reported with other benzodiazepines including alprazolam, chlordiazepoxide, clonazepam, diazepam, flurazepam and triazolam. The clinical pattern of acute liver injury from benzodiazepines is typically cholestatic and mild-to-moderate in severity with a latency of 1 to 6 months. Fever and rash are uncommon as is autoantibody formation.

Drug Information

Drug Indication：

Used to treat insomnia.

LiverTox Summary：

Quazepam is an orally available benzodiazepine used to treat insomnia. As with most benzodiazepines, quazepam therapy has not been associated with serum aminotransferase or alkaline phosphatase elevations, and clinically apparent liver injury from quazepam has not been reported and must be very rare, if it occurs at all.

Drug Classes：

Sedatives and Hypnotics

Pharmacology：

Quazepam is a benzodiazepine derivative. The main pharmacological action of quazepam is the enhancement of the neurotransmitter GABA at the GABA_A receptor.

MeSH：

Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety. (See all compounds classified as Hypnotics and Sedatives.)

Absorption：

Bioavailability is 29-35% following oral administration.

Metabolism/Metabolites：

Hepatic.|Quazepam has known human metabolites that include 2-oxoquazepam.

Biological Half-Life：

39 hours

MeSH Entry Terms：

Doral

DEA Controlled Substances：

Quazepam|Doral|2881|Schedule IV - Substances in the DEA Schedule IV have a low potential for abuse relative to substances in Schedule III.|No

Quazepam Use and Manufacturing

Uses

Selepam is a benzodiazepine derivative drug and is known to bind nonspecifically to benzodiazepine receptors, which affects muscle relaxation, anticonvulsant activty, motor coordination and memory. Selepam is known to induce motor impairment and exerts hypnotic properties. Selepam is often used for the treatment of insomina.

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:386.8
XLogP3:4
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:2
Exact Mass:386.0267599
Monoisotopic Mass:386.0267599
Topological Polar Surface Area:47.7
Heavy Atom Count:25
Complexity:539
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes