药品详细
Propranolol(普萘洛尔)
化学结构式图
中文名
普萘洛尔
英文名
Propranolol
分子式
C16H21NO2
化学名
[2-hydroxy-3-(naphthalen-1-yloxy)propyl](propan-2-yl)amine
分子量
Average: 259.3434
Monoisotopic: 259.157228921
Monoisotopic: 259.157228921
CAS号
525-66-6
ATC分类
C07A 未知
药物类型
small molecule
阶段
approved
商品名
Angilol;Apsolol;Avlocardyl;Bedranol;Beprane;Berkolol;Beta-Neg;Beta-Propranolol;Beta-Tablinen;Beta-Timelets;Betachron;Betalong;Cardinol;Caridolol;Corpendol;Deralin;Dociton;Duranol;Efektolol;Elbrol;Etalong;Euprovasin;Frekven;Inderal;Inderal La;Inderide;Indobloc;Innopran XL;Intermigran;Kemi S;Migrastat;Obsidan;Oposim;Prano-Puren;Propanix;Prophylux;Propranolol Hcl Intensol;Propranur;Proprasylyt;Pylapron;Rapynogen;Reducor;Reducor Line;Sagittol;Servanolol;Sloprolol;Sumial;Tesnol;
同义名
Dl-Propranolol Hydrochloride;Propanalol;Propanolol;Propranalol;propranolol;Propranolol Hcl;Propranolol Hydrochloride;R,S-Propranolol Hydrochloride;
基本介绍
A widely used non-cardioselective beta-adrenergic antagonist. Propranolol is used in the treatment or prevention of many disorders including acute myocardial infarction, arrhythmias, angina pectoris, hypertension, hypertensive emergencies, hyperthyroidism, migraine, pheochromocytoma, menopause, and anxiety. [PubChem]
生产厂家
- Actavis elizabeth llc
- Akrimax pharmaceuticals llc
- App pharmaceuticals llc
- Baxter healthcare corp anesthesia critical care
- Bedford laboratories div ben venue laboratories inc
- Clonmel healthcare ltd
- Duramed pharmaceuticals inc sub barr laboratories inc
- Glaxosmithkline llc
- Hikma farmaceutica (portugal) sa
- Interpharm inc
- Inwood laboratories inc sub forest laboratories inc
- Ipca laboratories ltd
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Lederle laboratories div american cyanamid co
- Morton grove pharmaceuticals inc
- Mutual pharmaceutical co inc
- Mylan pharmaceuticals inc
- Northstar healthcare holdings ltd
- Par pharmaceutical
- Par pharmaceutical inc
- Pliva inc
- Purepac pharmaceutical co
- Roxane laboratories inc
- Sandoz canada inc
- Sandoz inc
- Schering corp sub schering plough corp
- Smith and nephew solopak div smith and nephew
- Solopak medical products inc
- Superpharm corp
- Teva pharmaceuticals usa inc
- Upsher smith laboratories inc
- Vintage pharmaceuticals
- Warner chilcott div warner lambert co
- Warner chilcott inc
- Watson laboratories inc
- Wyeth ayerst laboratories
封装厂家
- Actavis Group
- Advanced Pharmaceutical Services Inc.
- Akrimax Pharmaceuticals
- Amerisource Health Services Corp.
- Apotheca Inc.
- APP Pharmaceuticals
- A-S Medication Solutions LLC
- Barr Pharmaceuticals
- Baxter International Inc.
- Bedford Labs
- Ben Venue Laboratories Inc.
- Bryant Ranch Prepack
- Cardinal Health
- Caremark LLC
- Comprehensive Consultant Services Inc.
- Dept Health Central Pharmacy
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Eurand Pharmaceuticals Inc.
- General Injectables and Vaccines Inc.
- GlaxoSmithKline Inc.
- Group Health Cooperative
- H and H Laboratories
- H.J. Harkins Co. Inc.
- Heartland Repack Services LLC
- Heritage Pharmaceuticals
- Hikma Pharmaceuticals
- Ipca Laboratories Ltd.
- Ivax Pharmaceuticals
- Kaiser Foundation Hospital
- Lake Erie Medical and Surgical Supply
- Liberty Pharmaceuticals
- Major Pharmaceuticals
- Medisca Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Northstar Rx LLC
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- Par Pharmaceuticals
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmacy Service Center
- Pharmedix
- Physicians Total Care Inc.
- Piramal Healthcare
- Pliva Inc.
- Preferred Pharmaceuticals Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Qualitest
- Rebel Distributors Corp.
- Remedy Repack
- Resource Optimization and Innovation LLC
- Rouses Point Pharmaceuticals LLC
- Roxane Labs
- Sandhills Packaging Inc.
- Sandoz
- Southwood Pharmaceuticals
- Stat Rx Usa
- Tya Pharmaceuticals
- UDL Laboratories
- United Research Laboratories Inc.
- Upsher Smith Laboratories
- Vangard Labs Inc.
- Watson Pharmaceuticals
- West-Ward Pharmaceuticals
- Wyeth Pharmaceuticals
参考
Synthesis Reference | Not Available |
General Reference |
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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 the prophylaxis of migraine. | ||||||||||||
Pharmacodynamics | Propranolol, the prototype of the beta-adrenergic receptor antagonists, is a competitive, nonselective beta-blocker similar to nadolol without intrinsic sympathomimetic activity. Propanolol is a racemic compound; the l-isomer is responsible for adrenergic blocking activity. | ||||||||||||
Mechanism of action | Propranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. | ||||||||||||
Absorption | Propranolol is almost completely absorbed from the GI tract; however, plasma concentrations attained are quite variable among individuals. | ||||||||||||
Volume of distribution |
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Protein binding | More than 90% | ||||||||||||
Metabolism |
Hepatic
Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.
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Route of elimination | Propranolol is extensively metabolized with most metabolites appearing in the urine. | ||||||||||||
Half life | 4 hours | ||||||||||||
Clearance | Not Available | ||||||||||||
Toxicity | Symptoms of overdose include bradycardia, cardiac failure, hypotension, and brochospasm. LD50=565 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 | ||||||||||||||||||||||||||||||||||||||||||
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, propranolol, may decrease symptoms of hypoglycemia. |
Aminophylline | Antagonism of action and increased effect of theophylline |
Bromazepam | Co-administration with propranolol will cause a reduction in bromazepam clearance and increases half-life. |
Chlorpromazine | Increased effect of both drugs |
Chlorpropamide | The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. |
Cimetidine | Cimetidine may increase the serum concentration of propranolol by decreasing its metabolism. |
Citalopram | The SSRI, citalopram, may increase the bradycardic effect of the beta-blocker, propranolol. |
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, propranolol, may increase the toxicity of disopyramide. |
Dronedarone | Propranolol is a CYP2D6 substrate and because dronedarone inhibits this enzyme, will increase propranolol exposure 1.3-fold. Lower dose of metoprolol. |
Dyphylline | Antagonism of action and increased effect of theophylline |
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, propranolol. |
Fenoterol | Antagonism |
Fluoxetine | The SSRI, fluoxetine, may increase the bradycardic effect of the beta-blocker, propranolol. |
Formoterol | Antagonism |
Gliclazide | The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. |
Glipizide | The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. |
Glisoxepide | The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. |
Glyburide | The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. |
Glycodiazine | The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. |
Haloperidol | Increased effect of both drugs |
Hydralazine | Increased effect of both drugs |
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 Glargine | The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. |
Isoproterenol | Antagonism |
Lidocaine | The beta-blocker, propranolol, may increase the effect and toxicity of lidocaine. |
Maprotiline | Propranolol increases the serum levels of cisapride |
Mesoridazine | Increased risk of cardiotoxicity and arrhythmias |
Methyldopa | Possible hypertensive crisis |
Methysergide | Ischemia with risk of gangrene |
Orciprenaline | Antagonism |
Oxtriphylline | Antagonism of action and increased effect of theophylline |
Paroxetine | The SSRI, paroxetine, may increase the bradycardic effect of the beta-blocker, propranolol. |
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 the beta-blocker, propranolol. |
Repaglinide | The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. |
Rifampin | Rifampin may decrease the serum concentration of propranolol by increasing its metabolism. |
Rizatriptan | Propranolol increases the effect and toxicity of rizatriptan |
Salbutamol | Antagonism |
Salmeterol | Antagonism |
Sertraline | The SSRI, sertraline, may increase the bradycardic effect of the beta-blocker, propranolol. |
Terazosin | Increased risk of hypotension. Initiate concomitant therapy cautiously. |
Terbinafine | Terbinafine may reduce the metabolism and clearance of Propranolol. Consider alternate therapy or monitor for therapeutic/adverse effects of Propranolol if Terbinafine is initiated, discontinued or dose changed. |
Terbutaline | Antagonism |
Theophylline | Antagonism of action and increased effect of theophylline |
Thioridazine | Increased risk of cardiotoxicity and arrhythmias |
Tolazamide | The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. |
Tolbutamide | The beta-blocker, propranolol, may decrease symptoms of hypoglycemia. |
Topotecan | The p-glycoprotein inhibitor, Propranolol, may increase the bioavailability of oral Topotecan. A clinically significant effect is also expected with IV Topotecan. Concomitant therapy should be avoided. |
Verapamil | Increased effect of both drugs |
食物相互作用
- Avoid alcohol.
- Avoid natural licorice.
- Take with food.