terfenadine

Terfenadine is a peripherally selective antihistamine that was formerly used for the treatment of allergic conditions such as seasonal and perennial allergic rhinitis, chronic urticaria (hives), and other histamine-mediated disorders. It acts as a reversible antagonist at the histamine H1 receptor in various tissues including the gastrointestinal tract, uterus, large blood vessels, and bronchial muscle. Terfenadine is a prodrug that is extensively metabolized in the liver to its active metabolite fexofenadine by cytochrome P450 3A4. Unlike many first-generation antihistamines, it does not readily cross the blood-brain barrier and thus has minimal central nervous system depressant effects. However, terfenadine itself can cause serious cardiac arrhythmias (notably QT interval prolongation and torsades de pointes) especially when taken with CYP3A4 inhibitors or in overdose situations; this led to its withdrawal from markets worldwide in the late 1990s[1][2][3][10].

Brand names

SeldaneTriludanTeldane

Other names

terfenadineSeldaneTriludanTeldane