Drugs-Forum  
Home Wiki Studies Forum Groups Blog Video Images News Chat
Go Back   Drugs Forum > Wiki Articles > Drug Articles
Mark Forums Read
Register Tags

Notices

Drug Articles Articles about drugs

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


[top]The latest Brotizolam threads

  Article / Page Starter Last Post Comments Views
Egyaddict
27-09-2016 18:01
by donedrone Go to last post
12 413
everio
25-09-2016 17:46
by everio Go to last post
0 60
mickeyd23
25-09-2016 06:51
by lilyofthevalley Go to last post
1 135
Kalios
24-09-2016 22:59
by Kalios Go to last post
0 84
xMeTaL HeAdx
24-09-2016 15:38
by xMeTaL HeAdx Go to last post
5 283
Egyaddict
24-09-2016 08:27
by Jkapel0417 Go to last post
19 918
immortal agony
23-09-2016 22:44
by malsat Go to last post
14 1,087
soulraver132
23-09-2016 02:17
by staples Go to last post
77 136,484
spidermark
21-09-2016 16:32
by Egyaddict Go to last post
1 133
Jkapel0417
21-09-2016 06:01
by Jkapel0417 Go to last post
2 179



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, 18,987 Views

Share this on:
Page Tools


Posting Rules
You may not create new articles
You may not edit articles
You may not protect articles

You may not post comments
You may not post attachments
You may not edit your comments

BB code is On
Smilies are On
[IMG] code is On
HTML code is Off

Sitelinks: Information:

All times are GMT +1. The time now is 04:26.


Copyright: SIN Foundation 2003 - 2014, All rights reserved