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Brompheniramine and Chlorpheniramine Pharmacokinetics Following Single‐Dose Oral Administration in Children Aged 2 to 17 Years
Author(s) -
Pathirana Sudam,
Jayawardena Shyamalie,
Meeves Suzanne,
Thompson Gary A.
Publication year - 2018
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/jcph.1037
Subject(s) - pharmacokinetics , dosing , nomogram , age groups , pharmacodynamics , medicine , sedation , body weight , pharmacology , demography , sociology
Two pediatric studies characterized brompheniramine and chlorpheniramine pharmacokinetics in a total of 72 subjects, aged 2 to 17 years. A single age‐/weight‐based oral dose, ranging from 1 to 4 mg, was administered with 2 to 6 oz of water at least 2 hours after a light breakfast. Plasma samples were obtained before and for 72 hours after dosing and analyzed using high‐pressure liquid chromatography–tandem mass spectrometry. Pharmacokinetic parameters were estimated using noncompartmental methods; relationships with age were assessed using linear regression. Results indicated that for brompheniramine and chlorpheniramine, C max was similar across age groups, although it tended to occur earlier in the youngest group. AUC was ∼15% to 30% higher in the oldest age group. As expected, CL o and V z /F increased with age; however, following allometric scaling, no age‐related differences existed. Because the increase with age for both parameters was similar, no age‐related differences in t 1/2,z existed (∼15 hours). Overall, the single doses were well tolerated. Sedation was the most common reported AE and appeared to be more prevalent in the 2‐ to 5‐year‐old group. Overall, these results indicate that an age/weight dosing nomogram using a 4‐fold range of doses achieves similar C max and AUC.