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Description
Cetirizine is a bioactive carboxylated metabolite of hydroxyzine that acts as a selective histamine H1 receptor antagonist (pKi = 8). As a second generation antihistamine, it is non-sedating due to low lipophilicity, which prevents blood-brain barrier transit. Cetirizine is a racemic mixture composed of equal amounts of two enantiomers, R-levocetirizine and S-dextrocetirizine, with pharmacological activity residing primarily in the (R)-isomer. Cetirizine has also been shown to inhibit eosinophil chemotaxis and leukotriene B4 release independent from H1 antagonism.
