Abstract
Histamine plays a prominent and diverse role in the pathophysiology of allergic disease and therapeutic intervention is therefore typically focused on blocking the effects of this biogenic amine. A new antihistamine, levocetirizine, is the R-enantiomer of cetirizine dihydrochloride and like its parent compound undergoes minimal hepatic metabolism. Levocetirizine has pharmacodynamically and pharmacokinetically favourable characteristics, including high bioavailability, rapid onset of action, limited distribution and a low degree of metabolism. Clinical trials indicate that it is safe and effective for the treatment of allergic rhinitis and chronic urticaria with a minimal number of untoward effects. Furthermore, several recent studies have demonstrated that, in addition to its being a potent antihistamine, levocetirizine has several anti-inflammatory effects that are observed at clinically relevant concentrations that may enhance its therapeutic benefit.
Keywords: Levocetirizine, antihistamine, allergy, anti-inflammatory
Current Medicinal Chemistry
Title: Levocetirizine: An Update
Volume: 13 Issue: 22
Author(s): Garry M. Walsh
Affiliation:
Keywords: Levocetirizine, antihistamine, allergy, anti-inflammatory
Abstract: Histamine plays a prominent and diverse role in the pathophysiology of allergic disease and therapeutic intervention is therefore typically focused on blocking the effects of this biogenic amine. A new antihistamine, levocetirizine, is the R-enantiomer of cetirizine dihydrochloride and like its parent compound undergoes minimal hepatic metabolism. Levocetirizine has pharmacodynamically and pharmacokinetically favourable characteristics, including high bioavailability, rapid onset of action, limited distribution and a low degree of metabolism. Clinical trials indicate that it is safe and effective for the treatment of allergic rhinitis and chronic urticaria with a minimal number of untoward effects. Furthermore, several recent studies have demonstrated that, in addition to its being a potent antihistamine, levocetirizine has several anti-inflammatory effects that are observed at clinically relevant concentrations that may enhance its therapeutic benefit.
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Cite this article as:
Walsh M. Garry, Levocetirizine: An Update, Current Medicinal Chemistry 2006; 13 (22) . https://dx.doi.org/10.2174/092986706778201594
DOI https://dx.doi.org/10.2174/092986706778201594 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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