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The pharmacokinetics of three multiple dose regimens of chloroquine: implications for malaria chemoprophylaxis.
Author(s) -
Wetsteyn JC,
Vries PJ,
Oosterhuis B.,
Boxtel CJ
Publication year - 1995
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.1365-2125.1995.tb05731.x
Subject(s) - chloroquine , pharmacokinetics , volume of distribution , chemoprophylaxis , malaria , proguanil , pharmacology , medicine , half life , immunology
The pharmacokinetics of chloroquine were studied in healthy volunteers who received one of three different multiple‐dose regimens for 3 weeks: once weekly 300 mg, twice weekly 200 mg and once daily 50 mg chloroquine. Plasma concentrations of chloroquine and metabolites were determined by h.p.l.c. with fluorescence detection. The concentration‐ time course was fitted to a multiple‐dose pharmacokinetic model. Volume of distribution, elimination half‐life and clearance were not different for the three regimens, ranging from 250‐302 l kg‐1, 374‐479 h and 0.44‐ 0.58 l h‐1 kg‐1 respectively. After the first week of all dosage regimens, peak and trough concentrations of chloroquine were above 16 micrograms l‐1, sufficiently suppressive for chloroquine‐sensitive P. falciparum strains. These data suggest that once daily chloroquine could be combined with proguanil in a single tablet and should improve compliance when given for malaria chemoprophylaxis.