Astemizole: a long-acting, nonsedating antihistamine.

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Krstenansky PM, Cluxton RJ Jr

Astemizole: a long-acting, nonsedating antihistamine.

Drug Intell Clin Pharm. 1987 Dec;21(12):947-53.

PubMed ID

2892659 [ View in PubMed

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Abstract

Astemizole is a long-acting, highly selective histamine1-receptor antagonist with minimal central and anticholinergic effects. Comparison studies have shown astemizole to be equal or superior to currently available antihistamines, beclomethasone nasal spray, and cromolyn sodium in relieving allergic symptoms of seasonal and perennial allergic rhinitis. Other uses include treatment of allergic conjunctivitis and chronic urticaria. Astemizole is not as effective for treatment of acute allergic symptoms because of its delayed onset of action. Astemizole and its active metabolite, desmethylastemizole, have long elimination half-lives permitting once-daily dosing. The incidence of sedation is lower than with conventional antihistamines, but increased appetite and weight gain do occur. Astemizole should be useful for both maintenance and prophylactic therapy in patients with chronic allergic conditions who cannot tolerate the sedative or anticholinergic effects of conventional antihistamines.

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Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Astemizole	Histamine H1 receptor	Protein	Humans	Yes	Antagonist	Details