Summary
The pharmacokinetics of orally administered mefloquine were determined in six healthy male subjects and in six ulcer patients before and after a 3-day course of cimetidine (400 mg morning and evening). Peak plasma concentrations Cmax and AUC0−∞ were similarly and significantly (P<0.05) increased after cimetidine pretreatement in both healthy subjects and peptic ulcer patients Cmax was increased by 42.4% and 20.5% while AUC0−∞ was increased by 37.5% in healthy and peptic ulcer subjects respectively. The values of t1/2ab absorption and t1/2β elimination, totall crearance CLT/F and volume of distribution were altered to varying levels after cimetidine treatment but the changes were not statistically significant in both healthy and peptic ulcer subjects.
The established long t1/2β and this apparent interaction between mefloquine and cimetidine which resulted in increased mefloquine plasma concentration might be of clinical significant in patients with neurological/psychiatric history.
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Kolawole, J.A., Mustapha, A., Abudu-Aguye, I. et al. Mefloquine pharmacokinetics in healthy subjects and in peptic ulcer patients after cimetidine administration. Eur. J. Drug Metab. Pharacokinet. 25, 165–170 (2000). https://doi.org/10.1007/BF03192309
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DOI: https://doi.org/10.1007/BF03192309