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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
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
  1. : Effect of metoprolol CR/XL in chronic heart failure: Metoprolol CR/XL Randomised Intervention Trial in Congestive Heart Failure (MERIT-HF) Lancet. 1999 Jun 12;353(9169):2001-7. Pubmed
剂型
Form Route Strength
Liquid Intravenous
Solution Intravenous
Tablet Oral
Tablet, extended release Oral
规格
Unit description Cost Unit
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
  • Phenols and Derivatives
  • Ethers
  • Anisoles
  • Phenyl Esters
Substructures
  • Hydroxy Compounds
  • Aliphatic and Aryl Amines
  • Phenols and Derivatives
  • Ethers
  • Benzene and Derivatives
  • Amino Alcohols
  • Aromatic compounds
  • Anisoles
  • Alcohols and Polyols
  • Phenyl Esters
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

Enzyme Metabolite Reaction Km Vmax
Cytochrome P450 2D6 alpha-Hydroxymetoprolol hydroxylation 70 0.039
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
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00302 Metoprolol Pathway SMP00302
理化性质
Properties
State solid
Melting point 120 oC (tartarate salt)
Experimental Properties
Property Value Source
water solubility 16.9 mg/mL PhysProp
logP 1.6 PhysProp
Caco2 permeability -4.59 [ADME Research, USCD] BiGG
Predicted Properties
Property Value Source
water solubility 4.02e-01 g/l ALOGPS
logP 1.80 ALOGPS
logP 1.76 ChemAxon Molconvert
logS -2.82 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 4 ChemAxon Molconvert
hydrogen donor count 2 ChemAxon Molconvert
polar surface area 50.72 ChemAxon Molconvert
rotatable bond count 9 ChemAxon Molconvert
refractivity 76.70 ChemAxon Molconvert
polarizability 31.90 ChemAxon Molconvert
药物相互作用
Drug Interaction
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.

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