Stimulating Effects of H1-Antagonists

Eef   L.   Theunissen; Annemiek      Vermeeren; Eric   F.P.M.   Vuurman; Johannes   G.   Ramaekers

doi:10.2174/138161206777698800

Abstract

Whereas antihistamines are generally known for their sedative side effects, this review shows that several studies also found mild stimulating effects on performance for the H1-antagonists terfenadine, ebastine, fexofenadine and desloratadine. These stimulating effects were mostly demonstrated in tasks involving high levels of attention, e.g. divided attention tasks, vigilance tasks and driving tasks. The stimulating effects of these antihistamines were often dependent of the given dose; however the relation was not always linear. The mechanism responsible for the stimulating effects of these four antihistamines is still unclear, though it is hypothesized that it involves other neurotransmitters like dopamine and GABA, or that it acts through the H3 histamine receptor. Further research is needed to clarify the ambiguous role of histamine in processes of arousal. In addition, it would be useful to determine whether terfenadine, ebastine, fexofenadine and desloratadine can return allergic patients performance back to their preclinical level.

Keywords: Antihistamine, attention, desloratadine, dopamine, ebastine, fexofenadine, GABA, H3 receptor, performance, stimulant