PubMed · 1671721
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M E Solin. Nonsedating antihistamines.. https://pubmed.ncbi.nlm.nih.gov/1671721/
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Drug therapy for allergic rhinitis is used either to prevent symptoms from occurring by short-circuiting the reaction and thus inhibiting the production of chemical mediators or to control symptoms after the target organs have been stimulated by these mediators. Antihistamines, the mainstay treatment of allergic rhinitis, are H1-receptor antagonists that bind competitively to histamine receptors. The older, classic antihistamines are effective in treating the symptoms of allergic rhinitis, but most are sedating because they cross the blood-brain barrier. They also have anticholinergic activity, which further restricts their use. The new, nonsedating antihistamines have overcome most of these limitations, and because they are long-acting, they require fewer daily dosages. Many still under development are quite potent and may be used for indications other than allergic rhinitis. Decongestants, sympathomimetic amines, are available both orally and topically as either short- or long-acting preparations. Topical decongestants should be used only for a short time to prevent rebound and ensuring overusage. These drugs interact with numerous antihypertensive medications and tricyclic antidepressants. Often combined with antihistamines, decongestants help offset their sedative effect.
Antihistamines are effective therapy for histamine-mediated conditions, including seasonal and perennial allergic rhinitis and chronic urticaria. Until recently, all antihistamines produced some degree of drowsiness, as well as anticholinergic side effects. Several nonsedating antihistamines have been developed. Two of these antihistamines--terfenadine and astemizole--are commercially available. The lack of central nervous system effects is attributed to the inability of these drugs to penetrate the blood-brain barrier. They also have no appreciable binding to cholinergic receptors. Clinical trials have demonstrated that the newer agents are as effective as classic antihistamines and that they have no greater incidence of central nervous system or anticholinergic side effects than placebo.