药品详细

Oxprenolol(氧烯洛尔)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

氧烯洛尔

英文名

Oxprenolol

分子式

C₁₅H₂₃NO₃

化学名

{2-hydroxy-3-[2-(prop-2-en-1-yloxy)phenoxy]propyl}(propan-2-yl)amine

分子量

Average: 265.348
Monoisotopic: 265.167793607

CAS号

6452-71-7

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

A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety. [PubChem]

生产厂家

Novartis pharmaceuticals corp

封装厂家

参考

Synthesis Reference	Not Available
General Reference	McDevitt DG: Comparison of pharmacokinetic properties of beta-adrenoceptor blocking drugs. Eur Heart J. 1987 Dec;8 Suppl M:9-14. Pubmed

剂型

规格

化合物类型

Type	small molecule

Classes

Phenols and Derivatives
Ethers
Catechols
Anisoles
Phenyl Esters

Substructures

Hydroxy Compounds
Alkanes and Alkenes
Aliphatic and Aryl Amines
Phenols and Derivatives
Ethers
Benzene and Derivatives
Amino Alcohols
Catechols
Aromatic compounds
Anisoles
Alcohols and Polyols
Phenyl Esters

适应症

药理

Indication

Used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety.

Pharmacodynamics

Oxprenolol is a non-selective beta blocker with some intrinsic sympathomimetic activity. Oxprenolol is a lipophilic beta blocker which passes the blood-brain barrier more easily than water soluble beta blockers. As such, it is associated with a higher incidence of CNS-related side effects than hydrophilic ligands such as atenolol, sotalol and nadolol. Oxprenolol is an potent beta-blocker and should not be administered to asthmatics because it can cause irreversible airway failure and inflammation.

Mechanism of action

Like other beta-adrenergic antagonists, oxprenolol competes with adrenergic neurotransmitters such as catecholamines for binding at sympathetic receptor sites. Like propranolol and timolol, oxprenolol binds at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting the effects of the catecholamines epinephrine and norepinephrine and decreasing heart rate, cardiac output, and systolic and diastolic blood pressure. It also blocks beta-2 adrenergic receptors located in bronchiole smooth muscle, causing vasoconstriction. By binding beta-2 receptors in the juxtaglomerular apparatus, oxprenolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production. Oxprenolol therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.

Absorption

Oral bioavailability is 20-70%.

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Hepatic.

Route of elimination

Not Available

Half life

1-2 hours

Clearance

Not Available

Toxicity

Symptoms of overdose include abdominal irritation, central nervous system depression, coma, extremely slow heartbeat, heart failure, lethargy, low blood pressure, and wheezing.

Affected organisms

Humans and other mammals

Pathways

Pathway	Name	SMPDB ID
	Oxprenolol Pathway	SMP00304

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
logP	2.10	HANSCH,C ET AL. (1995)
Caco2 permeability	-4.68	ADME Research, USCD

Predicted Properties

Property	Value	Source
water solubility	6.80e-01 g/l	ALOGPS
logP	2.44	ALOGPS
logP	2.17	ChemAxon
logS	-2.6	ALOGPS
pKa (strongest acidic)	14.09	ChemAxon
pKa (strongest basic)	9.67	ChemAxon
physiological charge	1	ChemAxon
hydrogen acceptor count	4	ChemAxon
hydrogen donor count	2	ChemAxon
polar surface area	50.72	ChemAxon
rotatable bond count	9	ChemAxon
refractivity	76	ChemAxon
polarizability	30.31	ChemAxon

药物相互作用

Drug	Interaction
Acetohexamide	The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
Chlorpropamide	The beta-blocker, oxprenolol, 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, oxprenolol, 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, oxprenolol, may decrease symptoms of hypoglycemia.
Glipizide	The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
Glisoxepide	The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
Glyburide	The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
Glycodiazine	The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
Ibuprofen	Risk of inhibition of renal prostaglandins
Indomethacin	Risk of inhibition of renal prostaglandins
Insulin Glargine	The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
Isoproterenol	Antagonism
Lidocaine	The beta-blocker increases the effect and toxicity of lidocaine
Methyldopa	Possible hypertensive crisis
Methysergide	Ischemia with risk of gangrene
Orciprenaline	Antagonism
Pipobroman	Antagonism
Pirbuterol	Antagonism
Piroxicam	Risk of inhibition of renal prostaglandins
Practolol	Antagonism
Prazosin	Risk of hypotension at the beginning of therapy
Repaglinide	The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
Salbutamol	Antagonism
Salmeterol	Antagonism
Terazosin	Increased risk of hypotension. Initiate concomitant therapy cautiously.
Terbutaline	Antagonism
Tolazamide	The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
Tolbutamide	The beta-blocker, oxprenolol, 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 without regard to meals.

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