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药品详细

Ajmaline(阿义马林)

化学结构式图
中文名
阿义马林
英文名
Ajmaline
分子式
C20H26N2O2
化学名
(1R,9R,10S,12R,13S,14R,16S,18R)-13-ethyl-8-methyl-8,15-diazahexacyclo[14.2.1.0^{1,9}.0^{2,7}.0^{10,15}.0^{12,17}]nonadeca-2,4,6-triene-14,18-diol
分子量
Average: 326.4326
Monoisotopic: 326.199428086
CAS号
4360-12-7
ATC分类
C01B 未知;C01B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

An alkaloid found in the root of Rauwolfia serpentina, among other plant sources. It is a class Ia antiarrhythmic agent that apparently acts by changing the shape and threshold of cardiac action potentials. Ajmaline produces potent sodium channel blocking effects and a very short half-life which makes it a very useful drug for acute intravenous treatments. The drug has been very popular in some countries for the treatment of atrial fibrillation in patients with the Wolff–Parkinson–White syndrome and in well tolerated monomorphic ventricular tachycardias. It has also been used for many years as a drug to challenge the conduction system of the heart in cases of bundle branch block and syncope. In these cases, abnormal prolongation of the HV interval has been taken as a proof for infrahisian conduction defects tributary for permanent pacemaker implantation.

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    参考
    Synthesis Reference Not Available
    General Reference
    1. Brugada J, Brugada P, Brugada R: The ajmaline challenge in Brugada syndrome: a useful tool or misleading information? Eur Heart J. 2003 Jun;24(12):1085-6. Pubmed
    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 use as an antiarrhythmic agent.
    Pharmacodynamics Ajmaline is a class 1A antiarrhythmic agent. By interfering with the sodium channels, this drug allows for improvement in abnormal rhythms of the heart
    Mechanism of action The class I antiarrhythmic agents interfere with the sodium channel. A class IA agent lengthens the action potential (right shift) which brings about improvement in abnormal heart rhythms. This drug in particular has a high affinity for the Nav 1.5 sodium channel.
    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 206 °C PhysProp
    water solubility 490 mg/L (at 30 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
    logP 1.81 HANSCH,C ET AL. (1995)
    logS -2.82 ADME Research, USCD
    Predicted Properties
    Property Value Source
    water solubility 4.09e+00 g/l ALOGPS
    logP 1.72 ALOGPS
    logP 1.85 ChemAxon
    logS -1.9 ALOGPS
    pKa (strongest acidic) 13.28 ChemAxon
    pKa (strongest basic) 7.2 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 46.94 ChemAxon
    rotatable bond count 1 ChemAxon
    refractivity 92.57 ChemAxon
    polarizability 36.75 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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