Synthesis of 3-hydroxy desloratadine, the hydroxyl metabolite of loratadine
ABSTRACT:
Allergic rhinitis (AR) is an IgE-mediated disease that can
impact the quality of life and work of affected individuals. Antihistamines
were introduced more than 50 years ago for the treatment of AR. They can be
classified into three groups. First-generation antihistamines such as
promethazine and ketotifen are clinically effective, but they have a considerably
limited use by their sedative and anticholinergic effects. Second-generation
antihistamines such as cetirizine, loratadine1 and mizolastine have
significantly fewer sedative and anticholinergic effects than first-generation.
New generation antihistamines include fexofenadine, levocetirizine,
desloratadine2 and rupatadine. While many of these agents were largely devoid
of CNS (central nervous system) side effects, their tendency for drug-drug
interactions (e.g., terfenadine and astemizole) resulted in an increase
incidence of cardiotoxicity. Furthermore, some of the second-generation H1
antagonists exhibited weak anti-inflammatory properties and had no effect on
nasal congestion. These observations emphasized the need for newer
anti-allergic agents with a potent and long lasting activity, low liability to
enter into the brain and lacking cardiotoxic potential.
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