Bromazepam
Structural formula | |||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
![]() |
|||||||||||||||||||
General | |||||||||||||||||||
Non-proprietary name | Bromazepam | ||||||||||||||||||
other names |
7-Bromo-5-pyridin-2-yl-1,3-dihydrobenzo [ e ] [1,4] diazepin-2-one ( IUPAC ) |
||||||||||||||||||
Molecular formula | C 14 H 10 BrN 3 O | ||||||||||||||||||
External identifiers / databases | |||||||||||||||||||
|
|||||||||||||||||||
Drug information | |||||||||||||||||||
ATC code | |||||||||||||||||||
Drug class | |||||||||||||||||||
properties | |||||||||||||||||||
Molar mass | 316.15 g · mol -1 | ||||||||||||||||||
Physical state |
firmly |
||||||||||||||||||
Melting point |
237–239 ° C (decomposition) |
||||||||||||||||||
safety instructions | |||||||||||||||||||
|
|||||||||||||||||||
Toxicological data | |||||||||||||||||||
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . |
Bromazepam is a tranquilizer from the group of benzodiazepines , which is characterized by an anxiolytic effect and is used in medicine to treat acute anxiety, as a sedative or sleep aid. The effect is based on a binding to GABA receptors in the brain (GABA = gamma-aminobutyric acid , a neurotransmitter ). Bromazepam was introduced to the German market in 1977.
Pharmacokinetics
After oral ingestion of bromazepam, maximum plasma concentrations are reached within two hours. The biological half-life is between 10 and 20 hours. On average, only 2.3% of the dose is excreted unchanged in the urine. The two major metabolites excreted in the urine and accounting for 27% and 40% of the administered dose, respectively, are 3-hydroxybromazepam and 2- (2-amino-5-bromo-3-hydroxybenzoyl) pyridine. Due to rapid glucuronization, no clinically relevant concentration of 3-hydroxybromazepam is reached. The benzoylpyridine metabolite is inactive. The equivalent dose to 10 mg diazepam is 6 mg.
Side effects
Typical side effects of sedative drugs are tiredness, difficulty concentrating, inability to drive, dizziness and nausea. In older patients, a paradoxical (opposing) effect with excitement (fear, aggressiveness, agitated state of confusion) can occur, which must never be answered by increasing the dose.
Bromazepam is one of the most frequently prescribed anxiety relievers (anxiolytics) and tranquilizers (sedatives) and has a high (psychological and physical) potential for dependence . This applies to all benzodiazepines. After two to four weeks of regular use, even in the therapeutic dose range, physical and psychological withdrawal symptoms can be expected if the drug is stopped abruptly. The symptoms are identical to those that were originally intended to be combated with the preparation: restlessness, fear, sleep disorders. They do not yet prove dependency, but can keep long-term use going and thus be the first step towards low-dose dependence. After prolonged use, abrupt withdrawal can lead to cerebral seizures and extremely agitated states.
Use with minors
As with other benzodiazepines, bromazepam should only be administered to children and adolescents after careful consideration of the risk-benefit ratio. If the doctor considers bromazepam treatment to be indicated, the dose should be adjusted based on the child's lower body weight.
Use during pregnancy and breastfeeding
Bromazepam should not be used during pregnancy unless clearly necessary and unless a safer alternative is available. If the drug is prescribed to a woman of childbearing potential, she should be advised to notify her doctor if she is planning or suspecting pregnancy so that treatment can be stopped, as benzodiazepines can be excreted in breast milk. Therefore, breastfeeding women should not use bromazepam either.
Trade names
Bromazanil (D), Gityl (D), Lexostad (D), Lexotanil (D, A, CH) (withdrawn from the market in 2016, no longer available), Bromazepam OPT (D), Normoc (D), various generics (D, A)
Individual evidence
- ↑ Entry on Bromazepam. In: Römpp Online . Georg Thieme Verlag, accessed on November 10, 2014.
- ↑ a b c d data sheet bromazepam from Sigma-Aldrich , accessed on November 7, 2016 ( PDF ).
- ↑ epsy.de: Psychopharmaka Zeittafel .
- ^ A b Christian Haasen, Rüdiger Holzbach: Ordinance of Benzodiazepines ( Memento of April 15, 2010 in the Internet Archive ), In: Hamburger Ärzteblatt, June 2009, pages 12-14. (PDF; 7.8 MB)
- ^ Specialist information of the Swiss Medicines Compendium: Lexotanil; Status: April 2009.
- ↑ Guideline of the German Medical Association for dealing with drugs with addiction potential. In: bundesaerztekammer.de. Retrieved May 11, 2017 .
- ↑ a b Technical information of the Swiss Medicines Compendium: Lexotanil; Status: October 2006.