Tìm theo
Benzonatate
Các tên gọi khác (11 ) :
  • 2-[2-[2-[2-[2-[2-[2-[2-(2-Methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl 4-butylaminobenzoate
  • 2,5,8,11,14,17,20,23,26-Nonaoxaoctacosan-28-yl P-(butylamino)benzoate
  • 3,6,9,12,15,18,21,24,27-Nonaoxaoctacosyl 4-butylaminobenzoate
  • 4-(Butylamino)benzoic acid 3,6,9,12,15,18,21,24,27-nonaoxaoctacos-1-yl ester
  • Benzonatat
  • Benzonatate
  • Benzonatato
  • Benzonatatum
  • Benzononatine
  • Nonaethyleneglycol monomethyl ether P-N-butylaminobenzoate
  • P-Butylaminobenzoic acid omega-O-methylnonaethyleneglycol ester
antitussive agents
Thuốc Gốc
Small Molecule
CAS: 104-31-4
ATC: R05DB01
ĐG : Accucaps Industries Ltd. , http://www.accucaps.com
CTHH: C30H53NO11
PTK: 603.7419
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
603.7419
Monoisotopic mass
603.361861543
InChI
InChI=1S/C30H53NO11/c1-3-4-9-31-29-7-5-28(6-8-29)30(32)42-27-26-41-25-24-40-23-22-39-21-20-38-19-18-37-17-16-36-15-14-35-13-12-34-11-10-33-2/h5-8,31H,3-4,9-27H2,1-2H3
InChI Key
InChIKey=MAFMQEKGGFWBAB-UHFFFAOYSA-N
IUPAC Name
2,5,8,11,14,17,20,23,26-nonaoxaoctacosan-28-yl 4-(butylamino)benzoate
Traditional IUPAC Name
benzonatate
SMILES
CCCCNC1=CC=C(C=C1)C(=O)OCCOCCOCCOCCOCCOCCOCCOCCOCCOC
Độ hòa tan
Soluble in most organic solvents except aliphatic hydrocarbons
logP
2.45
logS
-5.6
pKa (Strongest Basic)
3.47
PSA
121.4 Å2
Refractivity
161.54 m3·mol-1
Polarizability
67.87 Å3
Rotatable Bond Count
33
H Bond Acceptor Count
11
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
1
Bioavailability
0
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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. 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.
Dược Động Học :

▧ Metabolism :
Benzonatate is hydrolyzed to para-aminobenzoic acid (PABA) by plasma esterases
▧ Half Life :
3-8 hours
Độc Tính : Restlessness, tremors, seizures and unconsciousness.
Chỉ Định : 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.
Liều Lượng & Cách Dùng : Capsule - Oral
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