Background: Levocetirizine is the R-enantiomer of cetirizine dihydrochloride with pharmacodynamically and pharmacokinetically favourable characteristics.
Objective: To review the evidence that levocetirizine is an effective therapy for allergic disease.
Methodology: Relevant articles in English or with English abstracts were identified from systematic PubMed searches.
Results: Levocetirizine has high bioavailability, high affinity for and occupancy of the H1 receptor, rapid onset of action, limited distribution and minimal hepatic metabolism. Clinical trials indicate that it is safe and effective for the treatment of allergic rhinitis and chronic idiopathic urticaria in adults and children with a minimal number of untoward effects. It is also becoming clearer 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. Furthermore, there appears to be a growing trend for the use of levocetirizine as long-term therapy in addition to it being used as a treatment for the immediate short-term manifestations of allergic disease.
Conclusion: Levocetirizine is an effective and safe treatment for use in adults and children with allergic disease.