Astemizole

Astemizole is a long-acting, non-sedating second-generation antihistamine of the piperidine class. It acts primarily as a selective antagonist at histamine H1 receptor, suppressing the formation of edema, flare, and pruritus caused by histaminic activity in allergic conditions. Astemizole does not significantly cross the blood-brain barrier at normal doses and therefore causes minimal central nervous system depression or sedation. It was originally developed by Janssen Pharmaceutica in 1977 for the treatment of allergies, hives (urticaria), and other allergic inflammatory conditions. The drug was withdrawn from global markets in 1999 due to its potential to cause serious cardiac arrhythmias (notably QT prolongation and torsades de pointes), especially when taken with CYP inhibitors or grapefruit juice[1][2][3][4][6]. Astemizole has also been shown to inhibit certain potassium channels (notably hERG/Kv11.1) and has been researched for additional mechanisms such as functional inhibition of acid sphingomyelinase (FIASMA) and disruption of PRC2 complex formation[4][6].

Brand names

Hismanal