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药品详细

Benzonatate(苯佐那酯)

化学结构式图
中文名
苯佐那酯
英文名
Benzonatate
分子式
C30H53NO11
化学名
2,5,8,11,14,17,20,23,26-nonaoxaoctacosan-28-yl 4-(butylamino)benzoate
分子量
Average: 603.7419
Monoisotopic: 603.361861543
CAS号
104-31-4
ATC分类
R05D 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Benzonatate is a non-narcotic oral antitussive (cough suppressant) drug which works by anesthetizing the tissues of the lungs and pleura responsible for the cough reflex. It is chemically related to other ester anesthetics such as procaine. It has an anesthetic (numbing) action similar to that of benzocaine and “numbs” the stretch sensors in the lungs. It is the stretching of these sensors with breathing that causes the cough. It was approved by the FDA in 1958.

生产厂家
  • Banner pharmacaps inc
  • Forest laboratories inc
  • Kv pharmaceutical co
  • Mikart inc
  • Orit laboratories llc
  • Sun pharmaceutical industries inc
  • The pharma network llc
  • Zydus pharmaceuticals usa inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Cohen V, Jellinek SP, Stansfield L, Truong H, Baseluos C, Marshall JP: Cardiac arrest with residual blindness after overdose of tessalon® (benzonatate) perles. J Emerg Med. 2009 Nov 4. Pubmed
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
  • Aliphatic and Aryl Amines
  • Ethers
  • Benzene and Derivatives
  • Aromatic compounds
  • Benzoyl Derivatives
  • Anilines
适应症
药理
Indication For the symptomatic relief of cough. Has also been applied locally in the oral cavity in adults by releasing the drug from the liquid-filled capsules to provide oropharyngeal anesthesia for conscious intubation.
Pharmacodynamics Benzonatate, a non-narcotic antitussive agent chemically related to tetracaine and other ester-type local anesthetics, is used to suppress cough associated with both acute and chronic respiratory conditions. The drug acts peripherally by anesthetizing the stretch receptors located in the respiratory passages, lungs, and pleura through the dampening of their activity, which reduces the cough reflex.
Mechanism of action Benzonatate acts peripherally, anesthetizing the stretch receptors of vagal afferent fibers in the alveoli of the lungs, bronchi, and pleura. Since these receptors are responsible for mediating the cough reflex, anesthetizing these receptors result in the inhibiton of cough production. Benzonatate also suppresses transmission of the cough reflex at the level of the medulla where the afferent impulse is transmitted to the motor nerves. When applied locally, Benzonatate binds within the intracellular portion of voltage-gated sodium channels, decreasing the rate of membrane depolarization and increasing the threshold for electrical excitability.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Benzonatate is hydrolyzed to para-aminobenzoic acid (PABA) by plasma esterases
Route of elimination Not Available
Half life 3-8 hours
Clearance Not Available
Toxicity Restlessness, tremors, seizures and unconsciousness.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State liquid
Experimental Properties
Property Value Source
water solubility Soluble in most organic solvents except aliphatic hydrocarbons Not Available
logP 2.45 HANSCH,C ET AL. (1995)
Predicted Properties
Property Value Source
water solubility 1.59e-03 g/l ALOGPS
logP 2.09 ALOGPS
logP 2.35 ChemAxon
logS -5.6 ALOGPS
pKa (strongest basic) 3.47 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 11 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 121.4 ChemAxon
rotatable bond count 33 ChemAxon
refractivity 161.54 ChemAxon
polarizability 67.87 ChemAxon
药物相互作用
食物相互作用
  • Take without regard to meals.

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