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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 57801-81-7
ATC code N05CD09
PubChem 2451
DrugBank ?
Chemical data
Formula C15H10BrClN4S 
Mol. mass 393. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Chlorine (ˈklɔriːn from the Greek word 'χλωρóς' ( khlôros, meaning 'pale green' is the Chemical element with Atomic number 17 and Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Sulfur or sulphur (ˈsʌlfɚ see spelling below) is the Chemical element that has the Atomic number 16 The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 7 g/mol
Pharmacokinetic data
Bioavailability 48-95%
Metabolism Hepatic
Half life 4. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The liver is a vital organ in the human body and is present in Vertebrates and some other animals The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity 4 hours (range, 2. 6–6. 9 h)
Excretion Renal
Therapeutic considerations
Pregnancy cat.

?
Legal status

Schedule IV(US)
Routes Oral

Brotizolam (marketed under brand name Lendormin) is a drug which is thienobenzodiazepine (a benzodiazepine derivative). Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The kidneys are complicated organs that have numerous biological roles The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction The Controlled Substances Act ( CSA) was enacted into law by the Congress of the United States as Title II of the Comprehensive Drug Abuse Prevention and Control The United States of America —commonly referred to as the In Pharmacology and Toxicology, a route A thienobenzodiazepine is a Heterocyclic compound containing a Diazepine ring fused to a Thiophene ring and a Benzene ring The benzodiazepines (pronounced, often abbreviated to "benzos") are a class of Psychoactive drugs with varying Hypnotic 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. An anxiolytic is a drug prescribed for the treatment of Symptoms of Anxiety. The anticonvulsants, also called antiepileptic drugs (abbreviated "AEDs" are a diverse group of pharmaceuticals used in the treatment of epileptic A sedative, or more specifically a sedative-hypnotic, is a substance that depresses the Central nervous system (CNS resulting in calmness relaxation sleepiness This article refers to skeletal muscle relaxants For information on Smooth muscle relaxants see Antispasmodic. Triazolam (marketed under brand names Halcion, Novodorm, Songar) is a Benzodiazepine derivative drug 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. Insomnia is a symptom of a sleeping disorder characterized by persistent difficulty falling asleep or staying asleep despite the opportunity 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.

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

  1. ^ Yasui M; Kato A, Kanemasa T, Murata S, Nishitomi K, Koike K, Tai N, Shinohara S, Tokomura M, Horiuchi M, Abe K. The benzodiazepines (pronounced, often abbreviated to "benzos") are a class of Psychoactive drugs with varying Hypnotic Midazolam (marketed under brand names Dormicum, Flormidal, Versed, Hypnovel and Dormonid, pronounced mɪˈdæzəlæm Triazolam (marketed under brand names Halcion, Novodorm, Songar) is a Benzodiazepine derivative drug Estazolam (marketed under the brand names ProSom, Eurodin) is a drug which is a Benzodiazepine derivative. (Jun 2005). "[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes]" 25 (3): 143–51. PMID 16045197.  
  2. ^ 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:10.1254/jphs.94.246. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 15037809.  
  3. ^ Rickels K. (1986). "The clinical use of hypnotics: indications for use and the need for a variety of hypnotics. ". Acta Psychiatrica Scandinavica Suppl. The Acta Psychiatrica Scandinavica is a Scandinavian Peer reviewed Scientific journal containing Original research, Systematic 332: 132–41. doi:10.1111/j.1600-0447.1986.tb08990.x. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 2883820.  

References

External links


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