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効能
鎮咳薬
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説明
Benzonatate is a reversible voltage-gated sodium channel blocker. It blocks Nav1.7 currents in a concentration- and voltage-dependent manner (IC50s = 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 Nav1.3 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.
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使用
Antitussive
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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.
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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.
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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.