药品详细
Metoprolol (美托洛尔 )
化学结构式图
中文名
美托洛尔
英文名
Metoprolol
分子式
Not Available
化学名
{2-hydroxy-3-[4-(2-methoxyethyl)phenoxy]propyl}(propan-2-yl)amine
分子量
Average: 267.3639
Monoisotopic: 267.183443671
Monoisotopic: 267.183443671
CAS号
37350-58-6
ATC分类
C07A 未知;C07A 未知
药物类型
small molecule
阶段
商品名
Beloc;Betaloc;Lopresor;Lopresoretic;Lopressor;Lopressor HCT;Metroprolol;Prelis;Selo-Zok;Seloken;Selopral;Toprol;Toprol XL;Toprol-XL;
同义名
Metoprolol succinate;Metoprolol Tartrate;
基本介绍
A selective adrenergic beta-1-blocking agent with no stimulatory action. It's binding to plasma albumin is weaker than alprenolol and it may be useful in angina pectoris, hypertension, or cardiac arrhythmias. [PubChem]
生产厂家
- Apothecon inc div bristol myers squibb
- Astrazeneca lp
- Aurobindo pharma ltd
- Bedford laboratories
- Caraco pharmaceutical laboratories ltd
- Hikma farmaceutica (portugal) sa
- Hospira inc
- Ipca laboratories ltd
- Kv pharmaceutical co
- Luitpold pharmaceuticals inc
- Mutual pharmaceutical co inc
- Mylan pharmaceuticals inc
- Novartis pharmaceuticals corp
- Purepac pharmaceutical co
- Sagent strides llc
- Sandoz canada inc
- Sandoz inc
- Solco healthcare us llc
- Teva pharmaceuticals usa
- Teva pharmaceuticals usa inc
- Watson laboratories inc
- Watson laboratories inc florida
- Wockhardt ltd
封装厂家
参考
Synthesis Reference | Not Available |
General Reference |
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剂型
Form | Route | Strength |
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Liquid | Intravenous | |
Solution | Intravenous | |
Tablet | Oral | |
Tablet, extended release | Oral |
规格
Unit description | Cost | Unit |
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Metoprolol tartrate powder | 5.51 USD | g |
Lopressor 5 mg/5 ml ampul | 3.85 USD | ml |
Lopressor hct 100-25 tablet | 3.21 USD | tablet |
Toprol XL 200 mg 24 Hour tablet | 3.08 USD | tablet |
Lopressor HCT 100-50 mg tablet | 3.06 USD | tablet |
Toprol xl 200 mg tablet | 2.96 USD | tablet |
Lopressor hct 100-50 tablet | 2.82 USD | tablet |
Lopressor 100 mg tablet | 2.75 USD | tablet |
Metoprolol Succinate 200 mg 24 Hour tablet | 2.62 USD | tablet |
Metoprolol succ er 200 mg tablet | 2.29 USD | tablet |
Lopressor HCT 100-25 mg tablet | 2.21 USD | tablet |
Lopressor HCT 50-25 mg tablet | 2.14 USD | tablet |
Lopressor hct 50-25 tablet | 2.06 USD | tablet |
Toprol XL 100 mg 24 Hour tablet | 1.93 USD | tablet |
Toprol xl 100 mg tablet | 1.86 USD | tablet |
Lopressor 50 mg tablet | 1.81 USD | tablet |
Metoprolol Succinate 100 mg 24 Hour tablet | 1.53 USD | tablet |
Metoprolol succ er 100 mg tablet | 1.44 USD | tablet |
Toprol XL 25 mg 24 Hour tablet | 1.43 USD | tablet |
Toprol XL 50 mg 24 Hour tablet | 1.43 USD | tablet |
Lopresor 1 mg/ml | 1.29 USD | ml |
Toprol xl 25 mg tablet | 1.24 USD | tablet |
Toprol xl 50 mg tablet | 1.24 USD | tablet |
Metoprolol Succinate 25 mg 24 Hour tablet | 1.17 USD | tablet |
Metoprolol Succinate 50 mg 24 Hour tablet | 1.13 USD | tablet |
Metoprolol succ er 50 mg tablet | 0.9 USD | tablet |
Metoprolol succ er 25 mg tablet | 0.87 USD | tablet |
Metoprolol tartrate 100 mg tablet | 0.8 USD | tablet |
Toprol xl 100 mg tablet sa | 0.8 USD | tablet |
Lopresor 100 mg Tablet | 0.61 USD | tablet |
Lopresor Sr 200 mg Sustained-Release Tablet | 0.61 USD | tablet |
Metoprolol tartrate 50 mg tablet | 0.56 USD | tablet |
Metoprolol tartrate 25 mg tablet | 0.34 USD | tablet |
Apo-Metoprolol Sr 200 mg Sustained-Release Tablet | 0.34 USD | tablet |
Lopresor Sr 100 mg Sustained-Release Tablet | 0.34 USD | tablet |
Sandoz Metoprolol Sr 200 mg Sustained-Release Tablet | 0.34 USD | tablet |
Lopresor 50 mg Tablet | 0.3 USD | tablet |
Apo-Metoprolol (Type L) 100 mg Tablet | 0.23 USD | tablet |
Apo-Metoprolol 100 mg Tablet | 0.23 USD | tablet |
Mylan-Metoprolol (Type L) 100 mg Tablet | 0.23 USD | tablet |
Novo-Metoprol (Fc) 100 mg Tablet | 0.23 USD | tablet |
Novo-Metoprol 100 mg Tablet | 0.23 USD | tablet |
Nu-Metop 100 mg Tablet | 0.23 USD | tablet |
Pms-Metoprolol-L 100 mg Tablet | 0.23 USD | tablet |
Sandoz Metoprolol (Type L) 100 mg Tablet | 0.23 USD | tablet |
Apo-Metoprolol Sr 100 mg Sustained-Release Tablet | 0.19 USD | tablet |
Sandoz Metoprolol Sr 100 mg Sustained-Release Tablet | 0.19 USD | tablet |
Apo-Metoprolol (Type L) 50 mg Tablet | 0.13 USD | tablet |
Apo-Metoprolol 50 mg Tablet | 0.13 USD | tablet |
Mylan-Metoprolol (Type L) 50 mg Tablet | 0.13 USD | tablet |
Novo-Metoprol (Fc) 50 mg Tablet | 0.13 USD | tablet |
Novo-Metoprol 50 mg Tablet | 0.13 USD | tablet |
Nu-Metop 50 mg Tablet | 0.13 USD | tablet |
Pms-Metoprolol-L 50 mg Tablet | 0.13 USD | tablet |
Sandoz Metoprolol (Type L) 50 mg Tablet | 0.13 USD | tablet |
Apo-Metoprolol 25 mg Tablet | 0.07 USD | tablet |
Pms-Metoprolol-L 25 mg Tablet | 0.07 USD | tablet |
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 the treatment of hypertension and angina pectoris. | ||||||||||
Pharmacodynamics | Metoprolol, a competitive, beta1-selective (cardioselective) adrenergic antagonist, is similar to atenolol in its moderate lipid solubility, lack of intrinsic sympathomimetic activity (ISA), and weak membrane stabilizing activity (MSA). | ||||||||||
Mechanism of action | Metoprolol competes with adrenergic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart. Beta(1)-receptor blockade results in a decrease in heart rate, cardiac output, and blood pressure. | ||||||||||
Absorption | Rapid and complete, 50% | ||||||||||
Volume of distribution | Not Available | ||||||||||
Protein binding | 12% | ||||||||||
Metabolism |
Primarily hepatic
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Route of elimination | Less than 5% of an oral dose of metoprolol is recovered unchanged in the urine; the rest is excreted by the kidneys as metabolites that appear to have no beta-blocking activity. | ||||||||||
Half life | 3-7 hours | ||||||||||
Clearance | Not Available | ||||||||||
Toxicity | LD50=5500 mg/kg (orally in rats), toxic effects include bradycardia, hypotension, bronchospasm, and cardiac failure. LD50=2090 mg/kg (orally in mice) | ||||||||||
Affected organisms |
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Pathways |
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理化性质
Properties | |||||||||||||||||||||||||||||||||||||
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State | solid | ||||||||||||||||||||||||||||||||||||
Melting point | 120 oC (tartarate salt) | ||||||||||||||||||||||||||||||||||||
Experimental Properties |
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Predicted Properties |
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药物相互作用
Drug | Interaction |
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Acetohexamide | The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. |
Chlorpropamide | The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. |
Cimetidine | Cimetidine may increase the serum concentration of metoprolol by decreasing its metabolism. |
Citalopram | The SSRI, citalopram, may increase the bradycardic effect of the beta-blocker, metoprolol. |
Clonidine | Increased hypertension when clonidine stopped |
Dihydroergotamine | Ischemia with risk of gangrene |
Dihydroergotoxine | Ischemia with risk of gangrene |
Diltiazem | Increased risk of bradycardia |
Disopyramide | The beta-blocker, metoprolol, may increase adverse effects of disopyramide. |
Epinephrine | Hypertension, then bradycardia |
Ergonovine | Ischemia with risk of gangrene |
Ergotamine | Ischemia with risk of gangrene |
Escitalopram | The SSRI, escitalopram, may increase the bradycardic effect of the beta-blocker, metoprolol. |
Fenoterol | Antagonism |
Fluoxetine | The SSRI, fluoxetine, may increase the bradycardic effect of the beta-blocker, metoprolol. |
Formoterol | Antagonism |
Glibenclamide | The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. |
Gliclazide | The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. |
Glipizide | The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. |
Glisoxepide | The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. |
Glycodiazine | The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. |
Hydralazine | Increased effect of both drugs |
Ibuprofen | Risk of inhibition of renal prostaglandins |
Indomethacin | Risk of inhibition of renal prostaglandins |
Insulin | The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. |
Insulin Glargine | The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. |
Isoproterenol | Antagonism |
Lidocaine | The beta-blocker, metoprolol, may increase the effect and toxicity of lidocaine |
Methysergide | Ischemia with risk of gangrene |
Orciprenaline | Antagonism |
Paroxetine | The SSRI increases the effect of the beta-blocker |
Phenobarbital | The barbiturate decreases the effect of the metabolized beta-blocker |
Pipobroman | Antagonism |
Pirbuterol | Antagonism |
Piroxicam | Risk of inhibition of renal prostaglandins |
Prazosin | Risk of hypotension at the beginning of therapy |
Primidone | The barbiturate decreases the effect of metabolized beta-blocker |
Procaterol | Antagonism |
Propafenone | Propafenone may increase the effect of beta-blocker, metoprolol. |
Repaglinide | The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. |
Rifampin | Rifampin may decrease the serum concentration of metoprolol by increasing its metabolism. |
Salbutamol | Antagonism |
Salmeterol | Antagonism |
Sertraline | The SSRI increases the effect of the beta-blocker |
Telithromycin | Telithromycin may possibly increase metoprolol effect |
Terazosin | Increased risk of hypotension. Initiate concomitant therapy cautiously. |
Terbinafine | Terbinafine may reduce the metabolism and clearance of Metoprolol. Consider alternate therapy or monitor for therapeutic/adverse effects of Metoprolol if Terbinafine is initiated, discontinued or dose changed. |
Terbutaline | Antagonism |
Tolazamide | The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. |
Tolbutamide | The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia. |
Treprostinil | Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. |
Verapamil | Increased effect of both drugs |
食物相互作用
- Avoid alcohol.
- Avoid natural licorice.
- Take with food.