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The unbound or free fraction of levocetirizine has been reported to be 8%. [1] The true volume of distribution of cetirizine is unknown but is estimated to be 0.3 to 0.45 L/kg. [3] [1] Cetirizine poorly and slowly crosses the blood–brain barrier, which is thought to be due to its chemical properties and its activity as a P-glycoprotein substrate.
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