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.
Niemegeers
C J
CJ
Awouters
F
F
Janssen
P A
PA
D000707:Anaphylaxis / Q000517:prevention & control; D000818:Animals; D016589:Astemizole; D001562:Benzimidazoles / Q000494:pharmacology* / Q000633:toxicity; D006634:Histamine H1 Antagonists / Q000494:pharmacology*; D006967:Hypersensitivity / Q000188:drug therapy*; D010276:Parasympatholytics / Q000494:pharmacology; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D051381:Rats; D003189:p-Methoxy-N-methylphenethylamine / Q000494:pharmacology
D001562:Benzimidazoles; D006634:Histamine H1 Antagonists; D010276:Parasympatholytics; D003189:p-Methoxy-N-methylphenethylamine; D016589:Astemizole