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Brotizolam

Brotizolam is a sedative, hypnotic drug which is a benzodiazepine analog that possesses anxiolytic, anticonvulsant, hypnotic, sedative, and skeletal muscle relaxant properties, and is considered to be similar in effect to short-acting benzodiazepines.It is commonly used in the treatment of severe, debilitating insomnia, and has an average half life in the body for up to four and a half hours. Dangers are related to CNS (cental nervous system) depression, and include ataxia, headache, dizziness, fatigue, slurred speech, and others. Common side effects are similar to those of other hypnotic benzodiazepines.

Contents




[top]Introduction to Brotizolam



[top]Using Brotizolam

[top]Ways of administration

[top]Effects of Brotizolam

[top]Combinations with Brotizolam

[top]Different Uses for Brotizolam



[top]Pharmacology of Brotizolam


LD50 (mg/kg) [1]:
Mice : >10000 orally, 920 intraperitoneally
Rat : >10000 orally, 1000 intraperitoneally

[top]Pharmacokinetics


Bioavailability after an oral dose is approximately 70%. Time to peak plasma concentrations is 1 hour. It is 90% bound to plasma proteins. It is metabolized by the liver to N-desmethyl-brotizolam (terminal half-life 4-19.5 hours), and others. Elimination half-life is 5.6 hours (range: 2.6 to 6.9 hours, but up to 13 hours in patients with liver failure). 22.5% of the dose is excreted by the kidneys, and excretion in bile also occurs. Brotizolam is also excreted in breast milk (in animal studies) and has been demonstrated to cross the placenta.

[top]Indications


The short-term treatment of insomnia. The usual therapeutic dose is 0.25-0.5mg at night (0.125mg is recommended as the starting dose in elderly or debilitated patients). The dose should also be reduced in liver and renal failure.

Pharmacokinetics and metabolism of brotizolam in humans (1983)

Kinetic and dynamic interaction of brotizolam and ethanol (1986)


[top]Chemistry of Brotizolam


Systematic (IUPAC) name:2-Bromo-4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
Synonyms:2-bromo-4-(o-chlorophenyl)-9-methyl-6H-thieno[3,2-f]-s-triazolo[4,3-a][1,4]diazepine, 8-bromo-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo[3,4-c]thieno[2,3-e]-1,4-diazepine, WE-941-BS, Lendorm, Lendormin, Mederantil, Nimbisan, Sintonal
Molecular Formula:C15H10BrClN4S
Molar mass:393.69 g/mol
CAS Registry Number:57801-81-7
Melting Point:212-214C
Boiling Point:no data
Flash Point:no data
Solubility:no data
Additionnal data:none
Notes:Aspect : colorless crystals; crystallized from ethanol
[1]


[top]The dangers of Brotizolam

[top]Contraindications

Hypersensitivity, severe respiratory and liver disease, closed angle-glaucoma, pregnancy and lactation.

[top]Adverse Effects


In post marketing studies up to 50% of people experienced transient adverse effects, which were more likely at higher doses. Very common (greater than 25%) were somnolence, confusion and ataxia. Common (up to 25%) were headache, depression, slurred speech, poor concentration, changes in libido, GI upset and hypersalivation. Uncommon (1-9%): Jaundice, dermatitis/urticaria, low blood counts, psychosis and paradoxical excitation. Rarely (less than 1%): Hypo/Hypertension, bradycardian and tachycardia.

As with all benzodiazepines a physical tolerance develops with as little as 14 days of continuous use. Brotizolam should not be discontinued suddenly.


[top]Producing Brotizolam



[top]Forms of Brotizolam

[top]Appearance



[top]Legal status of Brotizolam

[top]United Nations

[top]USA

[top]EU

[top]Other Countries



[top]History of Brotizolam



[top]More Brotizolam Sections


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Contributors: gonzochef, John_bob, Alfa, NeuroChi
Created by NeuroChi, 19-11-2010 at 09:34
Last edited by gonzochef, 31-10-2015 at 18:15
Last comment by Jatelka on 18-12-2010 at 07:17
2 Comments, 17,998 Views

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