The therapeutic index of an H-1-antihistamine depends on several biochemica
l aspects: pharmacokinetics, metabolism, tissue distribution, lack of inter
ference with active transport systems and existence of anti-allergic activi
ties. Although the ideal H-1-antagonist does not yet exist, new approaches
will probably allow the synthesis of more potent and more specific drugs in
the near future. In this paper, we are going to briefly review the present
knowledge about the available H-1-antihistamines.