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药品详细

Oxymetazoline(羟甲唑啉)

化学结构式图
中文名
羟甲唑啉
英文名
Oxymetazoline
分子式
C16H24N2O
化学名
6-tert-butyl-3-(4,5-dihydro-1H-imidazol-2-ylmethyl)-2,4-dimethylphenol
分子量
Average: 260.3746
Monoisotopic: 260.1888634
CAS号
1491-59-4
ATC分类
R01A 未知;R01A 未知;S01G 解充血药及抗过敏药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251)

生产厂家
  • Johnson and johnson group consumer companies
  • Schering plough healthcare products inc
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Phenols and Derivatives
  • Cumenes and Derivatives
  • Phenethylamines
Substructures
  • Hydroxy Compounds
  • Imidazolines
  • Carboxylic Acids and Derivatives
  • Phenols and Derivatives
  • Benzene and Derivatives
  • Cumenes and Derivatives
  • Imidazoles
  • Phenethylamines
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamidines
  • Imines
  • Phenyl Esters
适应症
药理
Indication For treatment of nasal congestion and redness associated with minor irritations of the eye
Pharmacodynamics Oxymetazoline a adrenergic alpha-agonists, direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion The sympathomimetic action of oxymetazoline constricts the smaller arterioles of the nasal passages, producing a prolonged (up to 12 hours), gentle and decongesting effect. Oxymetazoline elicits relief of conjunctival hyperemia by causing vasoconstriction of superficial conjunctival blood vessels. The drug's action has been demonstrated in acute allergic conjunctivitis and in chemical (chloride) conjunctivitis.
Mechanism of action Oxymetazoline is a direct acting sympathomimetic amine, which acts on alpha-adrenergic receptors in the arterioles of the conjunctiva and nasal mucosa. It produces vasoconstriction, resulting in decreased conjunctival congestion in ophthalmic. In nasal it produces constriction, resulting in decreased blood flow and decreased nasal congestion.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 182 °C PhysProp
logP 3.4 Not Available
Predicted Properties
Property Value Source
water solubility 5.15e-02 g/l ALOGPS
logP 3.7 ALOGPS
logP 3.03 ChemAxon
logS -3.7 ALOGPS
pKa (strongest acidic) 10.91 ChemAxon
pKa (strongest basic) 10.15 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 44.62 ChemAxon
rotatable bond count 3 ChemAxon
refractivity 79.8 ChemAxon
polarizability 30.64 ChemAxon
药物相互作用
Drug Interaction
Tranylcypromine The MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of the alpha1-agonist, Oxymetazoline. Concomitant therapy should be avoided.
食物相互作用
Not Available

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