The new H1-receptor antagonists such as astemizole, cetirizine, loratadine, levocabastine, ketotifen, and azelastine have diverse pharmacokinetics, pharmacodynamics, and potency. Astemizole, for example, is the most long-acting of the new drugs and is not suitable for sporadic use. Cetirizine, the carboxylic acid metabolite of hydroxyzine, unlike other H1-receptor antagonists, is minimally metabolized in the body and is primarily excreted in unchanged form in the urine. Levocabastine is the most potent of the new drugs and can be applied topically to the conjunctivae or to the nasal mucosa for relief of allergic rhinoconjunctivitis. Ketotifen and azelastine have well-described antiallergic effects in addition of their antihistaminic effects. None of the new H1-receptor antagonists is any more effective in relieving nasal congestion than the first-generation H1-receptor antagonists are. Most, but not all, of the new H1-receptor antagonists lack anticholinergic effects and are relatively nonsedating.
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