物质信息
ID:1349
名称和标识
IUPAC传统名
bromazepam
商标名
Apo-BromazepamCreosedinLexotanNu-BromazepamUltramidolDurazanilLexaurinLexomilLexotanilSomaliumLexiliumNovo-bromazepamCompediumCompendiumGen-BromazepamLectopamLekotamNormocCalmepam
别名
7-Bromo-5-(2-pyridyl)-3H-1,4-benzodiazepin-2(1H)-oneBromazepamum [inn-latin]Bromazepam7-Bromo-5-(2-pyridyl)-3H-1,4-benzodiaxepin-2(1H)-one
IUPAC标准名
7-bromo-5-(pyridin-2-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one
化合物性质
理化性质
疏水性(logP)
2.05 [SANGSTER (1994)]
描述信息
Drug Groups
illicit; approved
Description
One of the benzodiazepines that is used in the treatment of anxiety disorders. [PubChem] It is a Schedule IV drug in the U.S. and Canada and under the Convention on Psychotropic Substances.
Indication
For the short-term treatment of insomnia, short-term treatment of anxiety or panic attacks, if a benzodiazepine is required, and the alleviation of the symptoms of alcohol- and opiate-withdrawal.
Pharmacology
Bromazepam is a lipophilic, long-acting benzodiazepine and with sedative, hypnotic, anxiolytic and skeletal muscle relaxant properties. It does not possess any antidepressant qualities. Bromazepam shares with other benzodiazepines the risk of abuse, misuse, psychological and/or physical dependence. According to many psychiatric experts Bromazepam has a greater abuse potential than other benzodiazepines because of fast resorption and rapid onset of action.
Affected Organisms
Humans and other mammals
Biotransformation
Hepatically, via oxidative pathways (via an enzyme belonging to the Cytochrome P450 family of enzymes).
Absorption
Bioavailability is 84% following oral administration.
Half Life
10-20 hours
References
•
Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines] Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72.
[Pubmed]
•
Oda M, Kotegawa T, Tsutsumi K, Ohtani Y, Kuwatani K, Nakano S: The effect of itraconazole on the pharmacokinetics and pharmacodynamics of bromazepam in healthy volunteers. Eur J Clin Pharmacol. 2003 Nov;59(8-9):615-9. Epub 2003 Sep 27.
[Pubmed]
•
van Harten J: Overview of the pharmacokinetics of fluvoxamine. Clin Pharmacokinet. 1995;29 Suppl 1:1-9.
[Pubmed]
•
Ochs HR, Greenblatt DJ, Friedman H, Burstein ES, Locniskar A, Harmatz JS, Shader RI: Bromazepam pharmacokinetics: influence of age, gender, oral contraceptives, cimetidine, and propranolol. Clin Pharmacol Ther. 1987 May;41(5):562-70.
[Pubmed]
External Links
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参考文献
• Oda M, Kotegawa T, Tsutsumi K, Ohtani Y, Kuwatani K, Nakano S: The effect of itraconazole on the pharmacokinetics and pharmacodynamics of bromazepam in healthy volunteers. Eur J Clin Pharmacol. 2003 Nov;59(8-9):615-9. Epub 2003 Sep 27. Pubmed
• Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines] Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72. Pubmed
• van Harten J: Overview of the pharmacokinetics of fluvoxamine. Clin Pharmacokinet. 1995;29 Suppl 1:1-9. Pubmed
• Ochs HR, Greenblatt DJ, Friedman H, Burstein ES, Locniskar A, Harmatz JS, Shader RI: Bromazepam pharmacokinetics: influence of age, gender, oral contraceptives, cimetidine, and propranolol. Clin Pharmacol Ther. 1987 May;41(5):562-70. Pubmed