Analyzing the clinical efficacy and safety of levocetirizine based on its receptor occupancy, intraclass comparison and role in the treatment of CSU: an AROG consensus statement.

Second-generation antihistamines constitute the first step in the therapeutic ladder for managing CSU. Levocetirizine has high bioavailability, a high affinity for and occupancy of the H1 receptor, a rapid onset of action, limited distribution, and minimal hepatic metabolism. It exhibits significant anti-inflammatory effects at clinically relevant concentrations. The marked receptor occupancy translates to better efficacy as compared to similarly dosed SGAH and the lower cost of the molecule makes it an appropriate drug for chronic use. Receptor occupancy should serve as the basis of intra-class head-to-head trials for CSU.