The second-generation H1-receptor antagonists terfenadine, astemizole, loratadine, and cetirizine are important first-line drugs for the relief of symptoms in patients with allergic rhinoconjunctivitis or chronic urticaria and may eventually supplant the potentially sedating first-generation H1-receptor antagonists in the treatment of these disorders. Terfenadine, astemizole, loratadine, and cetirizine produce an incidence of central nervous system and anticholinergic adverse effects similar to that produced by placebo. Our ability to use H1-receptor antagonists optimally has been greatly enhanced by recent pharmacokinetic and pharmacodynamic studies of these medications.