The pharmacological profile of a specific, safe, effective and non-sedative anti-allergic, astemizole.

In the compound 48/80 lethality test in rats, which is based on the specific activation of mast cells, astemizole was selected as a potent, long-acting and orally very effective inhibitor of anaphylactoid shock. In comparison to other histamine-H1 antagonists astemizole was also a very effective inhibitor of allergic reactions in rats and dogs and remarkably free of non-specific interactions with other biological amines and normal body functions. In numerous tests no evidence of central activity was found and toxicity studies have shown astemizole to be a very safe drug despite of its long duration of action. A daily dose of 10 mg of astemizole was found clinically free of side-effects and more effective than conventional antihistamine treatment.