This MedLibrary.org supplementary page on Brotizolam is provided directly from the open source Wikipedia as a service to our readers. Please see the note below on authorship of this content, as well as the Wikipedia usage guidelines. To search for other content from our encyclopedia supplement, please use the form below:
Related Sponsors
 |
|
 |
|
|
Brotizolam
|
|
| Systematic (IUPAC) name | |
| 2-Bromo-4-(2-chlorphenyl)-9-methyl-6H-
thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)benzodiazepine |
|
| Identifiers | |
| CAS number | |
| ATC code | N05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C15H10BrClN4S |
| Mol. mass | 393.7 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 48-95% |
| Metabolism | Hepatic |
| Half life | 4.4 hours (range, 2.6–6.9 h) |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status | |
| Routes | Oral |
Brotizolam (marketed under brand name Lendormin) is a drug which is thienobenzodiazepine (a benzodiazepine derivative). It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties, and is considered to be similar in effect to short-acting benzodiazepines such as triazolam. It is used in the short term treatment of insomnia although due to its short half life it is considered to have relatively high abuse potential and so would not be a first-line treatment. Brotizolam is a potent drug with a dosage of 0.5 or 1.0 milligrams, but is rapidly eliminated with an average half life of 4.4 hours (range 3.6 - 7.9 hours).
Brotizolam is not approved for sale in the UK, United States or Canada. It is approved for sale in Portugal and Italy.
Contents |
Pharmacology
Brotizolam induces impairment of motor function and has hypnotic properties.[1] Brotizolam increases the slow wave light sleep (SWLS) in a dose-dependent manner whilst suppressing deep sleep stages. Less time is spent in stages 3 and 4 which are the deep sleep stages when benzodiazepines such as brotizolam are used. Benzodiazepines are therefore not good hypnotics in the treatment of insomnia. The suppression of deep sleep stages by benzodiazepines may be especially problematic to the elderly as they naturally spend less time in the deep sleep stage.[2]
Indications
Insomnia. Brotizolam is prescribed for the short term treatment, 2 - 4 weeks only of severe insomnia. Insomnia can be described as a difficulty falling asleep, frequent awakening, early awakenings or a combination of each. Brotizolam is a short-intermediate acting benzodiazepine and is sometimes used in patients who have difficulty in maintaining sleep or getting to sleep. Hypnotics should only be used on a short term basis or in those with chronic insomnia on an occasional basis.[3]
See also
Notes
- ^ Yasui M; Kato A, Kanemasa T, Murata S, Nishitomi K, Koike K, Tai N, Shinohara S, Tokomura M, Horiuchi M, Abe K. (Jun 2005). "[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes]" 25 (3): 143–51. PMID 16045197.
- ^ Noguchi H; Kitazumi K, Mori M, Shiba T. (Mar 2004). "Electroencephalographic properties of zaleplon, a non-benzodiazepine sedative/hypnotic, in rats." (pdf). J Pharmacol Sci. 94 (3): 246–51. doi:. PMID 15037809.
- ^ Rickels K. (1986). "The clinical use of hypnotics: indications for use and the need for a variety of hypnotics.". Acta Psychiatrica Scandinavica Suppl. 332: 132–41. doi:. PMID 2883820.
References
- Greenblatt DJ, Locniskar A, Shader RI. Pilot pharmacokinetic study of brotizolam, a thienodiazepine hypnotic, using electron-capture gas-liquid chromatography. Sleep. 1983;6(1):72-6. PMID 6844800.
- Langley MS, Clissold SP. Brotizolam. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy as an hypnotic. Drugs. 1988 Feb;35(2):104-22.
- Bechtel WD. Pharmacokinetics and metabolism of brotizolam in humans. British Journal of Clinical Pharmacology. 1983;16 Suppl 2:279S-283S.
- Jochemsen R. Pharmacokinetics of brotizolam in healthy subjects following intravenous and oral administration. British Journal of Clinical Pharmacology. 1983;16 Suppl 2:285S-290S.
External links
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||
 |
This pharmacology-related article is a stub. You can help Wikipedia by expanding it. |
Wikipedia content modification information:
- This page was last modified on 27 June 2008, at 20:01.
Wikipedia Authorship and Review
Wikipedia content provided here is not reviewed directly by MedLibrary.org. Wikipedia content is authored by an open community of volunteers and is not produced by or in any way affiliated with MedLibrary.org.
Wikipedia Usage Guidelines
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article on "Brotizolam".
The URL for this specific entry is:
All Wikipedia text is available under the terms of the GNU Free Documentation License. (See Copyrights for details). Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc.