Brompheniramine and Chlorpheniramine Pharmacokinetics Following Single-Dose Oral Administration in Children Aged 2 to 17 Years

J Clin Pharmacol. 2018 Apr;58(4):494-503. doi: 10.1002/jcph.1037. Epub 2017 Nov 14.


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, Cmax 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, CLo and Vz /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 t1/2,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 Cmax and AUC.

Trial registration: NCT00894634 NCT00837837.

Keywords: brompheniramine; chlorpheniramine; pediatrics; pharmacokinetics.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Adolescent
  • Anti-Allergic Agents / administration & dosage
  • Anti-Allergic Agents / adverse effects
  • Anti-Allergic Agents / pharmacokinetics*
  • Brompheniramine / administration & dosage
  • Brompheniramine / blood
  • Brompheniramine / pharmacokinetics*
  • Child
  • Child, Preschool
  • Chlorpheniramine / administration & dosage
  • Chlorpheniramine / blood
  • Chlorpheniramine / pharmacokinetics*
  • Histamine H1 Antagonists / administration & dosage
  • Histamine H1 Antagonists / blood
  • Histamine H1 Antagonists / pharmacokinetics*
  • Humans


  • Anti-Allergic Agents
  • Histamine H1 Antagonists
  • Chlorpheniramine
  • Brompheniramine

Associated data