Description
Azelastine is a second generation antihistamine that inhibits H1 histamine receptors. Azelastine exhibits anti-allergic, anti-inflammatory, and anti-tussive activities and is clinically used to treat allergic rhinitis. Azelastine activates transient receptor potential vanilloid 1 (TRPV1) channels, inducing desensitization. In mast cells, azelastine inhibits production of TNF-α, IL-6, and IL-8 and suppresses activation of NF-κB. Additionally, this compound decreases capsaicin-induced cough in vivo.
References
Singh U, Bernstein JA, Haar L, et al. Azelastine desensitization of transient receptor potential vanilloid 1: A potential mechanism explaining its therapeutic effect in nonallergic rhinitis. Am J Rhinol Allergy. 2014 May;28(3):215-24. PMID: 24980233.
Horak F, Zieglmayer UP. Azelastine nasal spray for the treatment of allergic and nonallergic rhinitis. Expert Rev Clin Immunol. 2009 Nov;5(6):659-69. PMID: 20477689.
Kempuraj D, Huang M, Kandere-Grzybowska K, et al. Azelastine inhibits secretion of IL-6, TNF-alpha and IL-8 as well as NF-kappaB activation and intracellular calcium ion levels in normal human mast cells. Int Arch Allergy Immunol. 2003 Nov;132(3):231-9. PMID: 14646384.
Ito N, Shioya T, Watanabe A, et al. Mechanism of the antitussive effect of azelastine in guinea pigs. Arzneimittelforschung. 2002;52(6):441-7. PMID: 12109044.
