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药品详细

Proparacaine(丙美卡因)

化学结构式图
中文名
丙美卡因
英文名
Proparacaine
分子式
C16H26N2O3
化学名
2-(diethylamino)ethyl 3-amino-4-propoxybenzoate
分子量
Average: 294.3892
Monoisotopic: 294.194342708
CAS号
499-67-2
ATC分类
S01H 局部麻醉药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Proparacaine is a topical anesthetic drug of the amino ester group. It is available as its hydrochloride salt in ophthalmic solutions at a concentration of 0.5%. [Wikipedia]

生产厂家
  • Alcon laboratories inc
  • Allergan pharmaceutical
  • Apothecon inc div bristol myers squibb
  • Bausch and lomb pharmaceuticals inc
  • Optopics laboratories corp
  • Pharmafair inc
  • Sola barnes hind
  • Taylor pharmacal co
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
  • Aminobenzoates
Substructures
  • Aminobenzoates
  • Carboxylic Acids and Derivatives
  • Benzyl Alcohols and Derivatives
  • Acetates
  • Benzoates
  • Phenols and Derivatives
  • Aliphatic and Aryl Amines
  • Ethers
  • Benzene and Derivatives
  • Aromatic compounds
  • Anisoles
  • Benzoyl Derivatives
  • Phenyl Esters
  • Anilines
适应症
药理
Indication Used as a local (ophthalmic) anesthetic.
Pharmacodynamics Proparacaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action. More specifically, proparacaine appears to bind or antagonize the function of voltage gated sodium channels.
Mechanism of action The exact mechanism whereby proparacaine and other local anesthetics influence the permeability of the cell membrane is unknown; however, several studies indicate that local anesthetics may limit sodium ion permeability through the lipid layer of the nerve cell membrane. Proparacaine may alter epithelial sodium channels through interaction with channel protein residues. This limitation prevents the fundamental change necessary for the generation of the action potential.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Plasma
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00403 Proparacaine Pathway SMP00403
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 182-183.3 °C Not Available
water solubility Soluble Not Available
logP 2.5 Not Available
pKa 3.2 Not Available
Predicted Properties
Property Value Source
water solubility 1.39e+00 g/l ALOGPS
logP 2.97 ALOGPS
logP 2.6 ChemAxon
logS -2.3 ALOGPS
pKa (strongest basic) 8.96 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 4 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 64.79 ChemAxon
rotatable bond count 10 ChemAxon
refractivity 86.04 ChemAxon
polarizability 34 ChemAxon
药物相互作用
食物相互作用
Not Available

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