Efficacy, safety and pharmacokinetics of levocetirizine in allergic children aged 1-2 years

Purpose This was a pilot study to assess the efficacy, safety and pharmacokinetics of levocetirizine in children aged 1–2 years treated for recurrent cough associated with other allergic symptoms. Methods This was a 90 day, open-label, non-controlled study of levocetirizine oral drops, 0.125 mg/kg twice daily in 15 children aged 1-2 years. Cough symptom scores were recorded daily. Serial plasma samples were obtained until 12 h after the first dose, 3-6 days and 90 days of treatment. Histamine-induced wheal and flare reactions were recorded before initiation of therapy, and on days 3–6 and 90. Study visits took place every month. Results The study population included 11 M and 4 F children, aged 1.1 - 2.1 years and weighing 9 - 15 kg. Mean weekly cough score decreased over time. Median wheal and flare inhibition at 12 h post-dose was almost 100%. Safety and tolerability were good. Eleven full PK profiles were available on day 1. Cmax and AUC were similar to those in adults receiving 5 mg daily, however the elimination half-life of 4 h, was 2-fold shorter. Steady-state trough concentrations were within the expected range. Conclusion The observations indicate that levocetirizine has good efficacy and safety profile that needs to be confirmed. The exposure in children was similar to adults and demonstrates that the current dosing regimen is appropriate for further studies in children aged 1 to 2 years. Clinical Pharmacology & Therapeutics (2004) 75, P46–P46; doi: 10.1016/j.clpt.2003.11.174