Estazolam
- CAS No.
- 29975-16-4
- Chemical Name:
- Estazolam
- Synonyms
- ProSom;8-CHLORO-6-PHENYL-4H-[1,2,4]-TRIAZOLO[4,3-A][1,4]BENZODIAZEPINE;Cannoc;D 40TA;d-40ta;u33737;Nemurel;Julodin;Esilgan;Eurodin
- CBNumber:
- CB9247411
- Molecular Formula:
- C16H11ClN4
- Molecular Weight:
- 294.74
- MDL Number:
- MFCD00867537
- MOL File:
- 29975-16-4.mol
| 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) |
| EWG's Food Scores | 1 |
| FDA UNII | 36S3EQV54C |
| ATC code | N05CD04 |
| IARC | 3 (Vol. 66) 1996 |
| NIST Chemistry Reference | Estazolam(29975-16-4) |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |    GHS02,GHS06,GHS08 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Danger | |||||||||
| Hazard statements | H225-H301+H311+H331-H370 | |||||||||
| Precautionary statements | P210-P260-P280-P301+P310-P311 | |||||||||
| 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) | |||||||||
| NFPA 704 |
|
Estazolam Chemical Properties,Uses,Production
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
