Premium
Divided‐dose kinetics of mefloquine in man.
Author(s) -
Franssen G.,
Rouveix B.,
Lebras J.,
Bauchet J.,
Verdier F.,
Michon C.,
Bricaire F.
Publication year - 1989
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1989.tb05413.x
Subject(s) - mefloquine , pharmacology , kinetics , medicine , malaria , chloroquine , immunology , physics , quantum mechanics
The kinetics of mefloquine was investigated following oral divided‐ doses in 10 healthy Caucasian volunteers. They received 500 or 750 mg followed by 500 mg 8 h later. Unchanged mefloquine (M) and its carboxylic acid metabolite (MM) were measured in whole blood and plasma for 50 days by h.p.l.c. Maximum blood and plasma M concentrations of 1872 +/‐ 362 ng ml‐1 (mean +/‐ s.d.) and 1900 +/‐ 434 ng ml‐1, respectively, were found within 6‐10 h after the second dose. The terminal plasma elimination half‐life was 20.1 +/‐ 3.7 days (mean +/‐ s.d.) and the oral clearance was 22.3 +/‐ 6.7 ml h‐1 kg‐1 (mean +/‐ s.d.). Plasma concentrations of MM exceeded those of M by 2‐3 fold within 2 days. The whole blood concentration of MM was lower than that in plasma but also exceeded the whole blood concentration of M.