Estazolam Chemical Properties

Melting point:

228-229°

Boiling point:

448.04°C (rough estimate)

Density 

1.2294 (rough estimate)

refractive index 

1.6110 (estimate)

Flash point:

11 °C

storage temp. 

2-8°C

solubility 

DMF: 30 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 20 mg/ml; Ethanol: 10 mg/ml

form 

A crystalline solid

pka

pKa 2.84(H2O) (Uncertain)

CAS DataBase Reference

29975-16-4(CAS DataBase Reference)

IARC

3 (Vol. 66) 1996

NIST Chemistry Reference

Estazolam(29975-16-4)

Safety Information

Hazard Codes 

Xi,T,F

Risk Statements 

36/37/38-39/23/24/25-23/24/25-11

Safety Statements 

36/37/39-45-36/37-16-7

RIDADR 

3249

WGK Germany 

3

RTECS 

XZ5473500

HazardClass 

6.1(b)

PackingGroup 

III

HS Code 

2933910000

Toxicity

LD50 orally in male mice, rats and rabbits: 740, 3200, 300 mg/kg (Yokotani)

MSDS

• Language:English Provider:8-Chloro-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
• Language:English Provider:SigmaAldrich

Estazolam Usage And Synthesis

Description

Estazolam, sold under the brand name Prosom among others, is a tranquilizer medication of the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring . It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. 

Pharmacology

Estazolam is classed as a "triazolo" benzodiazepine drug.Estazolam exerts its therapeutic effects via its benzodiazepines receptor agonist properties.Estazolam at high doses decreases histamine turnover via its action at the benzodiazepine-GABA receptor complex in mouse brains.

Adverse reactions

Common adverse reactions such as drowsiness, drowsiness, dizziness, fatigue, unsteady gait, etc., increasing the dose may occasionally cause adverse reactions such as headache, ataxia, motor dysfunction, slurred speech, respiratory depression, tremor, etc. Long-term use can lead to memory loss Adverse reactions such as decline, weight gain, cognitive impairment, loss of libido, etc. In addition, long-term use of estazolam can cause down-regulation of benzodiazepine receptors in the central nervous system, which can lead to tolerance and dependence, and sudden withdrawal can cause Headache, insomnia, depression, nervousness, restlessness, irritability, anxiety, tremor, tachycardia and other withdrawal symptoms, namely drug addiction, are the most serious adverse reactions of long-term use of estazolam.

Originator

Eurodin,Takeda,Japan,1975

Uses

A benzodiazepine derivative possessing anxiolytic, anticonvulsant, and muscle relaxant properties. It is commonly prescribed to treat short-term insomnia. Controlled Substance.

Definition

ChEBI: A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term ma agement of insomnia.

Manufacturing Process

A mixture of 5.74 grams (0.020 mol) of 7-chloro-1,3-dihydro-5-phenyl-2H- 1,4-benzodiazepine-2-thione, 3.6 grams (0.060 mol) of formic acid hydrazide and 200 ml of 1-butanol was refluxed for 3.75 hours with a slow stream of nitrogen bubbling through the mixture. The mixture was concentrated, the residue was suspended in water and the suspension was filtered. The filter cake consisted principally of unchanged starting material. The filtrate was concentrated, ethyl acetate and Skellysolve B hexanes being added during the concentration, giving crude product (2.54 grams), MP 220.5° to 225°C. Recrystallization of this material from ethyl acetate-Skellysolve B hexanes gave 8-chloro-6-phenyl-4H-s-triazolo[4,3-a] [1,4]benzodiazepine, MP 228° to 229°C.

brand name

Prosom (Abbott).

Therapeutic Function

Hypnotic, Sedative

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