药品详细
Bretylium(溴苄胺)
化学结构式图
中文名
溴苄胺
英文名
Bretylium
分子式
C11H17BrN
化学名
[(2-bromophenyl)methyl](ethyl)dimethylazanium
分子量
Average: 243.163
Monoisotopic: 242.054437196
Monoisotopic: 242.054437196
CAS号
59-41-6
ATC分类
C01B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
Bretylium blocks the release of noradrenaline from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation. The primary mode of action for bretylium is thought to be inhibition of voltage-gated K(+) channels. Recent evidence has shown that bretylium may also inhibit the Na,K-ATPase by binding to the extracellular K-site.
生产厂家
- Abbott laboratories pharmaceutical products div
- Abraxis pharmaceutical products
- Astrazeneca lp
- B braun medical inc
- Baxter healthcare corp
- Baxter healthcare corp anesthesia and critical care
- Hospira inc
- International medication system
- Luitpold pharmaceuticals inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
药理
| Indication | For use in the prophylaxis and therapy of ventricular fibrillation. Also used in the treatment of life-threatening ventricular arrhythmias, such as ventricular tachycardia, that have failed to respond to adequate doses of a first-line antiarrhythmic agent, such as lidocaine. |
| Pharmacodynamics | Bretylium is a bromobenzyl quaternary ammonium compound which selectively accumulates in sympathetic ganglia and their postganglionic adrenergic neurons where it inhibits norepinephrine release by depressing adrenergic nerve terminal excitability. Bretylium also suppresses ventricular fibrillation and ventricular arrhythmias. |
| Mechanism of action | Bretylium inhibits norepinephrine release by depressing adrenergic nerve terminal excitability. The mechanisms of the antifibrillatory and antiarrhythmic actions of bretylium are not established. In efforts to define these mechanisms, the following electrophysiologic actions of bretylium have been demonstrated in animal experiments: increase in ventricular fibrillation threshold, increase in action potential duration and effective refractory period without changes in heart rate, little effect on the rate of rise or amplitude of the cardiac action potential (Phase 0) or in resting membrane potential (Phase 4) in normal myocardium, decrease in the disparity in action potential duration between normal and infarcted regions, and increase in impulse formation and spontaneous firing rate of pacemaker tissue as well as increase ventricular conduction velocity. |
| Absorption | Not Available |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism |
No metabolites have been identified following administration in man and laboratory animals.
|
| Route of elimination | Not Available |
| Half life | The terminal half-life in four normal volunteers averaged 7.8±0.6 hours (range 6.9-8.1). During hemodialysis, this patient's arterial and venous bretylium concentrations declined rapidly, resulting in a half-life of 13 hours. |
| Clearance | Not Available |
| Toxicity | Oral, mouse: LD50 = 400 mg/kg. In the presence of life-threatening arrhythmias, underdosing with bretylium probably presents a greater risk to the patient than potential overdosage. However, one case of accidental overdose has been reported in which a rapidly injected intravenous bolus of 30 mg/kg was given instead of an intended 10 mg/kg dose during an episode of ventricular tachycardia. Marked hypertension resulted, followed by protracted refractory hypotension. The patient expired 18 hours later in asystole, complicated by renal failure and aspiration pneumonitis. Bretylium serum levels were 8000 ng/mL. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | solid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Cisapride | Increased risk of cardiotoxicity and arrhythmias |
| Clarithromycin | Increased risk of cardiotoxicity and arrhythmias |
| Erythromycin | Increased risk of cardiotoxicity and arryhthmias |
| Gatifloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Grepafloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Levofloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Mesoridazine | Increased risk of cardiotoxicity and arrhythmias |
| Moxifloxacin | Increased risk of cardiotoxicity and arrhythmias |
| Ranolazine | Possible additive effect on QT prolongation |
| Telithromycin | Increased risk of cardiotoxicity and arrhythmias |
| Thioridazine | Increased risk of cardiotoxicity and arrhythmias |
食物相互作用
Not Available
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