Ambroxol (hydrochloride)

Ambroxol is an expectorant and active metabolite of bromhexine.¹ It decreases short-circuit currents in electrically stimulated isolated canine tracheal epithelial cells when applied submucosally (IC₅₀ = 60 nM).² It inhibits the voltage-gated sodium channel Na_v1.2 in isolated dorsal root neurons (IC₅₀ = 110 µM for the rat channel).³ Ambroxol (100 µM) decreases IL-13-induced production of mucin 5AC (MUC5AC) in primary human airway epithelial cells and inhibits IL-13-induced decreases in the mucociliary transport rate of endogenous particles in the same cells.⁴ Ambroxol increases phenol red secretion, a marker of expectorant activity, in mice when administered at doses of 30, 60, or 120 mg/kg.⁵ Formulations containing ambroxol have been used in the treatment of acute or chronic respiratory conditions.

WARNING This product is not for human or veterinary use.

1. Malerba, M., and Ragnoli, B. Ambroxol in the 21^st century: Pharmacological and clinical update. Expert Opin. Drug Metab. Toxicol. 4(8), 1119-1129 (2008).

2. Tamaoki, J., Chiyotani, A., Yamauchi, F., et al. Ambroxol inhibits Na⁺ absorption by canine airway epithelial cells in culture. J. Pharm. Pharmacol. 43(12), 841-843 (1991).

3. Weiser, T. Comparison of the effects of four Na⁺ channel analgesics on TTX-resistant Na⁺ currents in rat sensory neurons and recombinant Na_v1.2 channels. Neurosci. Lett. 395(3), 179-184 (2006).

4. Seagrave, J., Albrecht, H.H., Hill, D.B., et al. Effects of guaifenesin, N-acetylcysteine, and ambroxol on MUC5AC and mucociliary transport in primary differentiated human tracheal-bronchial cells. Respir. Res. 13(1), 98 (2012).

5. Menezes, P.M.N., Brito, M.C., Sousa de Sá, P.G., et al. Analytical and pharmacological validation of the quantification of phenol red in a mouse model: An optimized method to evaluate expectorant drugs. J. Pharmacol. Toxicol. Methods 98, 106586 (2019).