药品详细
Bisoprolol(比索洛尔)
化学结构式图
中文名
比索洛尔
英文名
Bisoprolol
分子式
C18H31NO4
化学名
[2-hydroxy-3-(4-{[2-(propan-2-yloxy)ethoxy]methyl}phenoxy)propyl](propan-2-yl)amine
分子量
Average: 325.443
Monoisotopic: 325.225308485
Monoisotopic: 325.225308485
CAS号
66722-44-9
ATC分类
C07A 未知
药物类型
small molecule
阶段
approved
商品名
Cardicor;Concor;Condyline;Condylox;Detensiel;Emconcor;Emcor;Euradal;Isoten;Monocor;Soloc;Soprol;Zebeta;
同义名
Bisoprolol Fumarate;Bisoprolol fumerate;Bisoprolol Hemifumarate;
基本介绍
Bisoprolol is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension. Bisoprolol is structurally similar to metoprolol, acebutolol and atenolol in that it has two substituents in the para position of the benzene ring. The β1-selectivity of these agents is thought to be due in part to the large substituents in the para position. At lower doses (less than 20 mg daily), bisoprolol selectively blocks cardiac β1-adrenergic receptors with little activity against β2-adrenergic receptors of the lungs and vascular smooth muscle. Receptor selectivity decreases with daily doses of 20 mg or greater. Unlike propranolol and pindolol, bisoprolol does not exhibit membrane-stabilizing or sympathomimetic activity. Bisoprolol possesses a single chiral centre and is administered as a racemic mixture. Only l-bisoprolol exhibits significant β-blocking activity.
生产厂家
- Aurobindo pharma ltd
- Duramed pharmaceuticals inc sub barr laboratories inc
- Mutual pharmaceutical co inc
- Mylan pharmaceuticals inc
- Sandoz inc
- Teva pharmaceuticals usa
- Unichem pharmaceuticals (usa) inc
封装厂家
- Atlantic Biologicals Corporation
- Aurobindo Pharma Ltd.
- Duramed
- Eon Labs
- Greenstone LLC
- Kaiser Foundation Hospital
- Lake Erie Medical and Surgical Supply
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Novopharm Ltd.
- Physicians Total Care Inc.
- Resource Optimization and Innovation LLC
- Teva Pharmaceutical Industries Ltd.
- Unichem Laboratories Ltd.
- Watson Pharmaceuticals
- Wyeth Pharmaceuticals
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
ANTIHYPERTENSIVES 降血压;
药理
| Indication | For management of heart failure, angina pectoris, and mild to moderate hypertension and for secondary prevention of myocardial infarction (MI). | ||||||
| Pharmacodynamics | Bisoprolol is a competitive, cardioselective β1-adrenergic antagonist. Activation of β1-receptors (located mainly in the heart) by epinephrine increases heart rate and the blood pressure causing the heart to consume more oxygen. β1-adrenergic blocking agents such as bisopolol lower the heart rate and blood pressure and may be used to reduce workload on the heart and hence oxygen demands. They are routinely prescribed in patients with ischemic heart disease. In addition, β1-selective blockers prevent the release of renin, a hormone produced by the kidneys causes constriction of blood vessels. Bisoprolol is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane-stabilizing activity. | ||||||
| Mechanism of action | Bisoprolol selectively blocks catecholamine stimulation of β1-adrenergic receptors in the heart and vascular smooth muscle. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. At higher doses (e.g. 20 mg and greater) bisoprolol may competitively block β2-adrenergic receptors in bronchial and vascular smooth muscle causing bronchospasm and vasodilation. | ||||||
| Absorption | Well absorbed. Bioavailability > 80%. Absorption is not affected by food. Peak plasma concentrations occur within 2-4 hours. | ||||||
| Volume of distribution | Not Available | ||||||
| Protein binding | Binding to serum proteins is approximately 30% | ||||||
| Metabolism |
Approximately 50% of the dose is metabolized primarily metabolized by CYP3A4 to inactive metabolites. In vitro studies have shown that bisoprolol is also metabolized by CYP2D6 though this does not appear to be clinically significant. Approximately half the administered dose is excreted in unchanged in urine.
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| Route of elimination | Eliminated equally by renal and non-renal pathways. Approximately 50% of the total orally administered dose is excreted unchanged in urine with the remainder appearing as inactive metabolites. Less than 2% of the dose is excreted in the feces. | ||||||
| Half life | 9-12 hours; prolonged in the elderly and those with decreased renal function | ||||||
| Clearance | Not Available | ||||||
| Toxicity | Oral, mouse: LD50 = 100 mg/kg; Skin, rabbit: LD50 = 200 mg/kg; Skin, rat: LD50 = 500 mg/kg. Symptoms of overdose include congestive heart failure (marked by sudden weight gain, swelling of the legs, feet, and ankles, fatigue, and shortness of breath), difficult or labored breathing, low blood pressure, low blood sugar, and slow heartbeat. | ||||||
| Affected organisms |
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| Pathways |
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||||||||
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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 |
|---|---|
| Acetohexamide | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Chlorpropamide | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Clonidine | Increased hypertension when clonidine stopped |
| Dihydroergotamine | Ischemia with risk of gangrene |
| Dihydroergotoxine | Ischemia with risk of gangrene |
| Disopyramide | The beta-blocker, bisoprolol, may increase the toxicity of disopyramide. |
| Epinephrine | Hypertension, then bradycardia |
| Ergonovine | Ischemia with risk of gangrene |
| Ergotamine | Ischemia with risk of gangrene |
| Fenoterol | Antagonism |
| Formoterol | Antagonism |
| Gliclazide | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Glipizide | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Glisoxepide | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Glyburide | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Glycodiazine | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Ibuprofen | Risk of inhibition of renal prostaglandins |
| Indacaterol | Beta-adrenergic antagonists, especially those that are not cardioselective, may interfere with the effect of indacaterol when administered concurrently. Beta-blockers may exacerbate bronchospasms in patients with COPD. |
| Indomethacin | Risk of inhibition of renal prostaglandins |
| Insulin Aspart | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Insulin Detemir | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Insulin Glargine | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Insulin Glulisine | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Insulin Lispro | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Isoproterenol | Antagonism |
| Lidocaine | The beta-blocker, bisoprolol, may increase the effect and toxicity of lidocaine. |
| Methysergide | Ischemia with risk of gangrene |
| Orciprenaline | Antagonism |
| Pipobroman | Antagonism |
| Pirbuterol | Antagonism |
| Piroxicam | Risk of inhibition of renal prostaglandins |
| Prazosin | Risk of hypotension at the beginning of therapy |
| Procaterol | Antagonism |
| Repaglinide | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Rifampin | Rifampin may decrease the serum concentration of bisprolol by increasing its metabolism. |
| Salbutamol | Antagonism |
| Salmeterol | Antagonism |
| Telithromycin | Telithromycin may reduce clearance of Bisoprolol. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Bisoprolol if Telithromycin is initiated, discontinued or dose changed. |
| Terazosin | Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Terbutaline | Antagonism |
| Tolazamide | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Tolbutamide | The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia. |
| Treprostinil | Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. |
| Verapamil | Increased effect of both drugs |
| Voriconazole | Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of bisoprolol by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of bisoprolol if voriconazole is initiated, discontinued or dose changed. |
食物相互作用
- Take without regard to meals.
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