药品详细

Bromazepam(溴西泮)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

溴西泮

英文名

Bromazepam

分子式

C₁₄H₁₀BrN₃O

化学名

7-bromo-5-(pyridin-2-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one

分子量

Average: 316.153
Monoisotopic: 315.000724604

CAS号

1812-30-2

ATC分类

N05B 未知

药物类型

small molecule

阶段

illicit, approved

商品名

同义名

基本介绍

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. It is a intermediate-acting benzodiazepines.

生产厂家

封装厂家

United States Pharmacopeial Convention Inc.

参考

Synthesis Reference

Not Available

General Reference

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

剂型

规格

化合物类型

Type	small molecule

Classes

Benzodiazepines
Lactams

Substructures

Benzodiazepines
Amino Ketones
Pyridines and Derivatives
Benzene and Derivatives
Carboxylic Acids and Derivatives
Aryl Halides
Heterocyclic compounds
Aromatic compounds
Carboxamides and Derivatives
Diazepines
Lactams
Imines
Anilines
Halobenzenes

适应症

药理

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.
Pharmacodynamics	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.
Mechanism of action	Bromazepam binds to the GABA receptor GABA_A, causing a conformational change and increasing inhibitory effects of GABA. Other neurotransmitters are not influenced.
Absorption	Bioavailability is 84% following oral administration. The time to peak plasma level is 1 - 4 hours. Bromazepam is generally well absorbed after oral administration.
Volume of distribution	1.56 L/kg
Protein binding	70%
Metabolism	Hepatically, via oxidative pathways (via an enzyme belonging to the Cytochrome P450 family of enzymes). One of the main metabolites is 3-hydroxybromazepam. It is pharmacologically active and the half life is similar to that of the parent compound.
Route of elimination	Urine (69%), as metabolites
Half life	10-20 hours
Clearance	0.82 mL/min/kg.
Toxicity	Not Available
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
logP	2.05	SANGSTER (1994)

Predicted Properties

Property	Value	Source
water solubility	3.99e-02 g/l	ALOGPS
logP	2.09	ALOGPS
logP	2.54	ChemAxon
logS	-3.9	ALOGPS
pKa (strongest acidic)	12.24	ChemAxon
pKa (strongest basic)	2.68	ChemAxon
physiological charge	0	ChemAxon
hydrogen acceptor count	3	ChemAxon
hydrogen donor count	1	ChemAxon
polar surface area	54.35	ChemAxon
rotatable bond count	1	ChemAxon
refractivity	76.99	ChemAxon
polarizability	28.11	ChemAxon

药物相互作用

Drug	Interaction
Aminophylline	Aminophylline may decrease the therapeutic effect of bromazepam. Monitor for changes in the therapeutic effects of bromazepam if aminophylline is initiated, discontinued or dose changed.
Atazanavir	Atazanavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if atazanavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
Cimetidine	Co-administration with cimetidine will cause a reduction in bromazepam clearance and increases half-life.
Clarithromycin	Clarithromycin, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if clarithromycin is initiated, discontinued or dose changed. Dosage adjustments may be required.
Clozapine	Bromazepam may increase the adverse effects of clozapine. Consider alternate therapy or a reduction in the bromazepam dose. Monitor for respiratory depression and hypotension if concomitant therapy is initiated.
Conivaptan	Conivaptan, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if conivaptan is initiated, discontinued or dose changed. Dosage adjustments may be required.
Darunavir	Darunavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if darunavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
Delavirdine	Delavirdine, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if delavirdine is initiated, discontinued or dose changed. Dosage adjustments may be required.
Diltiazem	Diltiazem may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or a reductin in the bromazepam dose. Monitor for changes in the therapeutic and adverse effects of bromazepam if diltiazem is initiated, discontinued or dose changed.
Dyphylline	Dyphylline may decrease the therapeutic effect of bromazepam. Monitor for changes in the therapeutic effects of bromazepam if dyphylline is initiated, discontinued or dose changed.
Erythromycin	Erythromcyin may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if erythromycin is initiated, discontinued or dose changed. Dosage adjustments may be required.
Fluconazole	Fluconazole may increase the serum concentration of bromazepam by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if fluconazole is initiated, discontinued or dose changed.
Fosamprenavir	Fosamprenavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if fosamprenavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
Imatinib	Imatinib, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if imatinib is initiated, discontinued or dose changed. Dosage adjustments may be required.
Indinavir	Indinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if indinavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
Isoniazid	Isoniazid, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if isoniazid is initiated, discontinued or dose changed. Dosage adjustments may be required.
Itraconazole	Itraconazole may increase the serum concentration of bromazepam by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if itraconazole is initiated, discontinued or dose changed.
Ketoconazole	Ketoconazole may increase the serum concentration of bromazepam by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if ketoconazole is initiated, discontinued or dose changed.
Lopinavir	Lopinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if lopinavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
Methotrimeprazine	Concomitant therapy may result in additive CNS depressant effects. The dosage of bromazepam should be decreased by 50% prior to initiating concomitant therapy. Monitor for increased CNS depression.
Nefazodone	Nefazodone, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if nefazodone is initiated, discontinued or dose changed. Dosage adjustments may be required.
Nelfinavir	Nelfinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if nelfinavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
Nicardipine	Nicardipine, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if nicardipine is initiated, discontinued or dose changed. Dosage adjustments may be required.
Posaconazole	Posaconazole may increase the serum concentration of bromazepam by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if posaconazole is initiated, discontinued or dose changed.
Propranolol	Co-administration with propranolol will cause a reduction in bromazepam clearance and increases half-life.
Quinidine	Quinidine, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if quinidine is initiated, discontinued or dose changed. Dosage adjustments may be required.
Rifabutin	Rifabutin may decrease the serum concentration of bromazepam by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if rifabutin is initiated, discontinued or dose changed.
Rifampin	Rifampin may decrease the serum concentration of bromazepam by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if rifampin is initiated, discontinued or dose changed.
Rifapentine	Rifapentine may decrease the serum concentration of bromazepam by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if rifapentine is initiated, discontinued or dose changed.
Ritonavir	Ritonavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if ritonavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
Saquinavir	Saquinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if saquinavir is initiated, discontinued or dose changed. Dosage adjustments may be required.
Telithromycin	Telithromycin, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if telithromycin is initiated, discontinued or dose changed. Dosage adjustments may be required.
Theophylline	Theophylline may decrease the therapeutic effect of bromazepam. Monitor for changes in the therapeutic effects of bromazepam if theophylline is initiated, discontinued or dose changed.
Tipranavir	Tipranavir may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if tipranavir is initiated, discontinued or dose changed.
Triprolidine	The CNS depressants, Triprolidine and Bromazepam, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Verapamil	Verapamil may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or a reductin in the bromazepam dose. Monitor for changes in the therapeutic and adverse effects of bromazepam if verapamil is initiated, discontinued or dose changed.
Voriconazole	Voriconazole may increase the serum concentration of bromazepam by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bromazepam if voriconazole is initiated, discontinued or dose changed.

食物相互作用

Not Available

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