Premium
Pharmacokinetics and pharmacodynamics of cetirizine in infants and toddlers
Author(s) -
Špičák Václav,
Dab Isidore,
Hulhoven Réginald,
Desager JeanPierre,
Klánová Marie,
Longueville Marc,
Harvengt Carl
Publication year - 1997
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1016/s0009-9236(97)90165-x
Subject(s) - cetirizine , pharmacodynamics , pharmacokinetics , medicine , pharmacology
The pharmacokinetics of the second‐generation H 1 ‐receptor antagonist cetirizine were studied in 15 infants and toddlers (mean ± SD age, 12.3 ± 5.4 months) who were treated with a single 0.25 mg/kg dose of cetirizine solution. The infants and toddlers were hospitalized for recurrent respiratory infections or other hypersensitivity‐related diseases. Blood samples were collected at ½, 1, 1½, 2, 4, 6, 8, 12, and 24 hours, and a 24‐hour urine sample was obtained. A peak plasma level of 390 ± 135 ng/ml was observed after 2.0 ± 1.3 hours. The elimination half‐life was 3.1 ± 1.8 hours, the apparent oral body clearance was 2.13 ± 1.15 ml/min/kg, and the apparent volume of distribution was 0.44 ± 0.19 L/kg. The excretion of unchanged cetirizine in six complete urinary collections was 62.7% ± 13.2% of the administered dose. An additional pharmacodynamic study (inhibition of the histamine‐induced wheal and flare) was performed in 10 of these infants and toddlers, after the intake of 0.25 mg/kg cetirizine twice a day for at least 4 days. A 90% ± 12% inhibition of the wheal and a 87% ± 17% inhibition of the flare were still observed 12 hours after the last intake. The duration of the H 1 ‐inhibition by cetirizine at the cutaneous level is thus longer in infants and toddlers than could be inferred from its pharmacokinetics; the level of inhibition at 12 hours was the same as in older age groups. Clinical Pharmacology & Therapeutics (1997) 61 , 325–330; doi: