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[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

Brotizolam is 2-Bromo-4-(2-chlorphenyl)-9-methyl-6H thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)benzodiazepine. It has the chemical formula C15H10BRCLN4S and the molecular weight 393.7.

[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]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

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Contributors: Alfa, NeuroChi
Created by NeuroChi , 19-11-2010 at 09:34
Last edited by NeuroChi , 06-12-2010 at 00:29
Last comment by Jatelka on 18-12-2010 at 07:17
2 Comments, 10,926 Views

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