药品详细
Nebivolol(奈必洛尔)
化学结构式图
中文名
奈必洛尔
英文名
Nebivolol
分子式
C22H25F2NO4
化学名
1-(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)-2-{[2-(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)-2-hydroxyethyl]amino}ethan-1-ol
分子量
Average: 405.435
Monoisotopic: 405.175164703
Monoisotopic: 405.175164703
CAS号
99200-09-6
ATC分类
C07A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
Nebivolol is a highly cardioselective vasodilatory beta1 receptor blocker used in treatment of hypertension. In most countries, this medication is available only by prescription. [Wikipedia]
生产厂家
- Forest laboratories inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference |
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剂型
规格
化合物类型
| Type | small molecule |
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| Substructures |
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适应症
药理
| Indication | For the treatment of essential hypertension. | ||||||
| Pharmacodynamics | Nebivolol is a competitive and highly selective beta-1 receptor antagonist with mild vasodilating properties, possibly due to an interaction with the L-arginine/nitric oxide pathway. In preclinical studies, nebivolol has been shown to induce endothelium-dependent arterial relaxation in a dose dependent manner, by stimulation of the release of endothelial nitric oxide. Nitric oxide acts to relax vascular smooth muscle cells and inhibits platelet aggregation and adhesion. | ||||||
| Mechanism of action | Nebivolol is a selective β1-receptor antagonist. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Nebivolol blocks these receptors which reverses the effects of epinephrine, lowering the heart rate and blood pressure. In addition, beta blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. At high enough concentrations, this drug may also bind beta 2 receptors. | ||||||
| Absorption | The absorption of nebivolol is rapid and not affected by food. | ||||||
| Volume of distribution | Not Available | ||||||
| Protein binding | 98% | ||||||
| Metabolism |
Hepatic (CYP2D6-mediated)
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| Route of elimination | Not Available | ||||||
| Half life | 10 hours | ||||||
| Clearance | Not Available | ||||||
| Toxicity | The most common signs and symptoms associated with nebivolol overdosage are bradycardia and hypotension. Other important adverse events reported with nebivolol overdose include cardiac failure, dizziness, hypoglycemia, fatigue and vomiting. Other adverse events associated with β-blocker overdose include bronchospasm and heart block. The largest known ingestion of nebivolol worldwide involved a patient who ingested up to 500 mg of nebivolol along with several 100 mg tablets of acetylsalicylic acid in a suicide attempt. The patient experienced hyperhydrosis, pallor, depressed level of consciousness, hypokinesia, hypotension, sinus bradycardia, hypoglycemia, hypokalemia, respiratory failure and vomiting. The patient recovered. | ||||||
| Affected organisms |
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||||||||
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties | Not Available | ||||||||||||||||||||||||||||||||||||||||||
| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Terazosin | Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Treprostinil | Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. |
食物相互作用
Not Available
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