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药品详细

Chloropyramine(氯毗胺)

化学结构式图
中文名
氯毗胺
英文名
Chloropyramine
分子式
C16H20ClN3
化学名
N-[(4-chlorophenyl)methyl]-N-[2-(dimethylamino)ethyl]pyridin-2-amine
分子量
Average: 289.803
Monoisotopic: 289.134575362
CAS号
59-32-5
ATC分类
D04A 未知;R06A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Chloropyramine is a first generation antihistamine drug approved in some Eastern European countries for the treatment of allergic conjunctivitis, allergic rhinitis, bronchial asthma, and other atopic (allergic) conditions. Related indications for clinical use include Quincke’s edema, allergic reactions to insect bites, food and drug allergies, and anaphylactic shock.

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    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 Not Available
    Substructures Not Available
    适应症
    药理
    Indication For the treatment of allergic conjunctivitis, allergic rhinitis, bronchial asthma, and other atopic (allergic) conditions.
    Pharmacodynamics Chloropyramine is known as a competitive reversible H1-receptor antagonist (also known as an H1 inverse agonist), meaning that it exerts its pharmacological action by competing with histamine for the H1 subtype histamine receptor. By blocking the effects of histamine, the drug inhibits the vasodilation, increased vascular permeability, and tissue edema associated with histamine release in the tissue. In addition, chloropyramine has some anticholinergic properties. Chloropyramine's anticholinergic properties and the fact that it can pass through the blood-brain barrier are linked to its clinical side effects: drowsiness, weakness, vertigo, fatigue, dryness in the mouth, constipation, and rarely - visual disturbances and increase of intraocular pressure.
    Mechanism of action Chloropyramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
    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 Oral (LD50): Acute: 142 mg/kg [Rat]. 135 mg/kg [Mouse]. DUST (LC50): Acute: 209 mg/m 2 hours [Rat].
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point < 25 °C PhysProp
    boiling point 154.5 °C at 2.00E-01 mm Hg PhysProp
    water solubility Insoluble MSDS
    Predicted Properties
    Property Value Source
    water solubility 4.41e-01 g/l ALOGPS
    logP 3.79 ALOGPS
    logP 3.81 ChemAxon
    logS -2.8 ALOGPS
    pKa (strongest basic) 8.76 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 3 ChemAxon
    hydrogen donor count 0 ChemAxon
    polar surface area 19.37 ChemAxon
    rotatable bond count 6 ChemAxon
    refractivity 86.08 ChemAxon
    polarizability 32.25 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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