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
