Brotizolam

Drugbox
IUPAC_name = 2-Bromo-4-(2-chlorphenyl)-9-methyl-6H-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)benzodiazepine

---

---

width = 200
CAS_number=57801-81-7
ChemSpiderID = 2357
ATC_prefix=N05
ATC_suffix=CD09
ATC_supplemental=
PubChem=2451
DrugBank=?
C=15 | H=10 | Br=1 | Cl=1 | N=4 | S=1
molecular_weight = 393.7 g/mol
bioavailability= 48-95%
metabolism = Hepatic
elimination_half-life= 4.4 hours (range, 2.6–6.9 h)
excretion = Renal
pregnancy_category = ?
legal_NL = List II
legal_AUS = Category 4
legal_US = Schedule IV
routes_of_administration= 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, Italy and Japan.

Pharmacology

Brotizolam induces impairment of motor function and has hypnotic properties. [cite journal |author=Yasui M |coauthors=Kato A, Kanemasa T, Murata S, Nishitomi K, Koike K, Tai N, Shinohara S, Tokomura M, Horiuchi M, Abe K. |title= [Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes] |volume=25 |issue=3 |pages=143–51 |month=Jun |year=2005 |pmid=16045197 |journal=Nihon Shinkei Seishin Yakurigaku Zasshi ] 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. [cite journal | author = Noguchi H | coauthors = Kitazumi K, Mori M, Shiba T. | year = 2004 | month = Mar | title = Electroencephalographic properties of zaleplon, a non-benzodiazepine sedative/hypnotic, in rats | journal = J Pharmacol Sci. | volume = 94 | issue = 3 | pages = 246–51 | pmid = 15037809 | url = http://www.jstage.jst.go.jp/article/jphs/94/3/246/_pdf | format = pdf | doi = 10.1254/jphs.94.246 ]

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. [cite journal | author = Rickels K. | year = 1986 | title = The clinical use of hypnotics: indications for use and the need for a variety of hypnotics | journal = Acta Psychiatrica Scandinavica Suppl. | volume = 332 | pages = 132–41 | pmid = 2883820 | doi = 10.1111/j.1600-0447.1986.tb08990.x ]

ee also

*Benzodiazepines
*Midazolam
*Triazolam
*Estazolam

Notes

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

* [http://www.inchem.org/documents/pims/pharm/pim919.htm Inchem.org - Brotizolam]