Urinary Excretion of Chlorpheniramine and Its Metabolites in Children

Simons, Keith J.; Simons, F. Estelle R.; Luciuk, George H.; Frith, Evelyn M.

doi:10.1002/jps.2600730505

Cited by 14 publications

(2 citation statements)

References 11 publications

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“…However, other investigators have reported achiral chlorpheniramine t 1/2 values ranging from 12 to 43 h. 6,7 Variation in chlorpheniramine t 1/2 has been attributed to variable renal elimination, which is dependent upon urinary pH and flow rate. [8][9][10][11] We therefore designed this study to minimize variation in urinary pH and flow rate by controlling diet, fluid intake, and physical activity. As a result of these controls, urinary recovery of achiral chlorpheniramine was approximately 7% of the dose, and very reproducible between subjects, as well as periods, given the lack of a ranitidine treatment effect.…”

Section: Discussionmentioning

confidence: 99%

“…8 Urinary excretion is dependent upon both urine pH and urine flow rate, declining from 26.5% at pH 5 to 0.3% at pH 8. [9][10][11] This study was carried out to determine the effect of ranitidine on serum concentrations and urinary excretion of (S)-(+)-and (R)-(-)-chlorpheniramine following administration of racemic chlorpheniramine. It also provided an opportunity to better characterize the pharmacokinetics of chlorpheniramine enantiomers.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Stereoselective Pharmacokinetics of Chlorpheniramine and the Effect of Ranitidine

Koch

O’Connor-Semmes

Davis

et al. 1998

Journal of Pharmaceutical Sciences

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This single-dose, randomized, crossover study was carried out to investigate the potential effect of ranitidine on the pharmacokinetics of chlorpheniramine. The study also afforded an opportunity to add to the limited data currently available on the stereoselective pharmacokinetics of chlorpheniramine. Healthy subjects received a single oral 4 mg dose of racemic chlorpheniramine on two separate occasions: alone, and on day 6 of dosing with ranitidine 75 mg b.i.d. for 8 days. Serum concentrations and urinary recovery of (S)-(+)- and (R)-(-)-chlorpheniramine were unaffected by administration of ranitidine, indicating no pharmacokinetic drug-drug interaction. The observed chlorpheniramine pharmacokinetic data were consistent with previous data and indicated approximately 2.5-fold higher serum concentrations of the (S)-(+) enantiomer. Previously reported high variability in chlorpheniramine pharmacokinetics was greatly reduced by well-controlled food and fluid intake.

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