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药品详细

Xylometazoline(丁苄唑啉)

化学结构式图
中文名
丁苄唑啉
英文名
Xylometazoline
分子式
C16H24N2
化学名
2-[(4-tert-butyl-2,6-dimethylphenyl)methyl]-4,5-dihydro-1H-imidazole
分子量
Average: 244.3752
Monoisotopic: 244.193948778
CAS号
526-36-3
ATC分类
S01G 解充血药及抗过敏药;R01A 未知;R01A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A nasal vasoconstricting decongestant drug which acts by binding to the same receptors as adrenaline. It is applied as a spray or as drops into the nose to ease inflammation and congestion of the nasal passageways. It binds alpha-adrenergic receptors to activate the adrenal system which causes systemic vasoconstriction, thereby easing nasal congestion.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, Bonisch H: Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2009 Dec 17. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Cumenes and Derivatives
    • Phenethylamines
    Substructures
    • Imidazolines
    • Carboxylic Acids and Derivatives
    • Benzene and Derivatives
    • Cumenes and Derivatives
    • Imidazoles
    • Phenethylamines
    • Heterocyclic compounds
    • Aromatic compounds
    • Carboxamidines
    • Imines
    适应症
    药理
    Indication It is used for treating nasal congestion and minor inflammation due to allergies or colds.
    Pharmacodynamics Xylometazoline is a direct acting sympathomimetic adrenergic alpha-agonist used to induce systemic vasoconstriction, thereby decreasing nasal congestion. The sympathomimetic action of xylometazoline constricts the smaller arterioles of the nasal passages, producing a prolonged (8-12 hours) decongesting effect.
    Mechanism of action Xylometazoline is a direct acting sympathomimetic drug, which acts on alpha-adrenergic receptors in the arterioles of the nasal mucosa. This activates the adrenal system to yield systemic vasoconstrction. In producing vasoconstriction, the result is a decrease in blood flow in the nasal passages and consequently 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 Not Available
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 132 °C PhysProp
    logP 3.2 Not Available
    Predicted Properties
    Property Value Source
    water solubility 8.93e-03 g/l ALOGPS
    logP 4.68 ALOGPS
    logP 3.78 ChemAxon
    logS -4.4 ALOGPS
    pKa (strongest basic) 10.29 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 2 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 24.39 ChemAxon
    rotatable bond count 3 ChemAxon
    refractivity 77.82 ChemAxon
    polarizability 29.85 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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