ベンゾナテート 化学特性,用途語,生産方法
効能
鎮咳薬
説明
Benzonatate is a reversible voltage-gated sodium channel blocker. It blocks Na
v1.7 currents in a concentration- and voltage-dependent manner (IC
50s = 5.9 and 1.4 μM at holding potentials of -100 and -70 mV, respectively) and inhibits action potential firing in catecholamine A differentiated (CAD) cells. Benzonatate also blocks 80% of Na
v1.3 currents in N1E-115 cells when used at a concentration of 100 μM.
In vivo, benzonatate (0.85 mg/min) reduces the frequency, but has no effect on the amplitude, of the cough reflex in anesthetized dogs. Formulations containing benzonatate have been used as antitussive agents for the treatment of coughs.
来歴
Benzonatate is used to relieve cough. Benzonatate is in a class of medications called antitussives (cough suppressants). It works by reducing the cough reflex in the lungs and air passages. It was first synthesized in 1956 and was introduced as an antitussive in the United States in 1958.
Availability worldwide is limited, with the drug remaining marketed only in the United States and Mexico. In 2023, it was the 122nd most commonly prescribed medication in the United States, with more than 5 million prescriptions. A 2023 systematic review found that there is inadequate evidence to support the effectiveness and safety of benzonatate for cough and highlighted rising safety concerns.
使用
Antitussive
定義
ChEBI: The ester obtained by formal condensation of 4-butylaminobenzoic acid with nonaethylene glycol monomethyl ether. Structurally related to procaine and benzocaine, it has an anaesthetic effect on the stretch sensors in the lungs, and is used as a non-narcoti
cough suppressant.
生物学の機能
Benzonatate (TessaIon) is related to the local anesthetic
tetracaine. It anesthetizes the stretch receptors in
the lungs, thereby reducing coughing.Adverse reactions
include hypersensitivity, sedation, dizziness, and nausea.
作用機序
It is believed that it acts by two mechanisms: selective anesthesia of irritated receptors in
the lungs and simultaneous suppression of the cough center.
ベンゾナテート 上流と下流の製品情報
原材料
準備製品