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药品详细

Prilocaine(丙胺卡因)

化学结构式图
中文名
丙胺卡因
英文名
Prilocaine
分子式
C13H20N2O
化学名
N-(2-methylphenyl)-2-(propylamino)propanamide
分子量
Average: 220.3107
Monoisotopic: 220.157563272
CAS号
721-50-6
ATC分类
N01B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A local anesthetic that is similar pharmacologically to lidocaine. Currently, it is used most often for infiltration anesthesia in dentistry. (From AMA Drug Evaluations Annual, 1992, p165)

生产厂家
    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
    • Acetanilides
    Substructures
    • Aliphatic and Aryl Amines
    • Amino Ketones
    • Benzene and Derivatives
    • Acetanilides
    • Carboxylic Acids and Derivatives
    • Aromatic compounds
    • Carboxamides and Derivatives
    • Anilines
    适应症
    药理
    Indication Used as a local anaesthetic and is often used in dentistry.
    Pharmacodynamics Prilocaine binds to the intracellular surface of sodium channels which blocks the subsequent influx of sodium into the cell. Action potential propagation and never function is, therefore, prevented. This block is reversible and when the drug diffuses away from the cell, sodium channel function is restored and nerve propagation returns.
    Mechanism of action Prilocaine acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding 98%
    Metabolism
    Not Available
    Route of elimination Prilocaine is metabolized in both the liver and the kidney and excreted via the kidney.
    Half life Not Available
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways
    Pathway Name SMPDB ID
    Smp00401 Prilocaine Pathway SMP00401
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 37-38 °C PhysProp
    boiling point 159-162 °C at 1.00E-01 mm Hg PhysProp
    water solubility 541 mg/L Not Available
    logP 2.11 HANSCH,C ET AL. (1995)
    Predicted Properties
    Property Value Source
    water solubility 3.26e-01 g/l ALOGPS
    logP 1.87 ALOGPS
    logP 2.68 ChemAxon
    logS -2.8 ALOGPS
    pKa (strongest acidic) 13.51 ChemAxon
    pKa (strongest basic) 8.82 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 2 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 41.13 ChemAxon
    rotatable bond count 5 ChemAxon
    refractivity 67.86 ChemAxon
    polarizability 25.98 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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