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Benzonatate is a reversible voltage-gated sodium channel blocker.1 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.2 Formulations containing benzonatate have been used as antitussive agents for the treatment of coughs.
WARNING This product is not for human or veterinary use.
1. Benzonatate inhibition of voltage-
2. Effects of peripheral airway response on the cough reflex (author’s transl). Nihon Yakurigaku Zasshi. 76(8), 709-716 (1980).