Levocetirizine is indicated for the relief of symptoms associated with allergic rhinitis (seasonal and perennial) in adults and children 6 years of age and older.
Mode of Action:
Levocetirizine, the active enantiomer of cetirizine, is an anti-histamine; its principal effects are mediated via selective inhibition of H1 receptors. The antihistaminic activity of levocetirizine has been documented in a variety of animal and human models. In vitro binding studies revealed that levocetirizine has an affinity for the human H1-receptor 2-fold higher than that of cetirizine (Ki = 3 nmol/L vs. 6 nmol/L, respectively). This increased affinity has unknown clinical relevance.
Levocetirizine is poorly metabolized and mostly excreted. This is favourable as it is unlikely to be modified by drugs administered concomitantly.
Grant JA, Riethuisen JM, Moulaert B, DeVos C: A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjects. Ann Allergy Asthma Immunol. 2002 Feb;88(2):190-7. [PubMed:11868924]
Ferrer M: Pharmacokinetic evaluation of levocetirizine. Expert Opin Drug Metab Toxicol. 2011 Aug;7(8):1035-47. doi: 10.1517/17425255.2011.590131. Epub 2011 Jun 4. [PubMed:21639816 ]
Devillier P, Roche N, Faisy C: Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review. Clin Pharmacokinet. 2008;47(4):217-30. [PubMed:18336052 ]
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