title: The pharmacokinetics of three multiple dose regimens of chloroquine: implications for malaria chemoprophylaxis.
abstract: 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.
authors.affiliation: Division of Infectious Diseases, Tropical Medicine and AIDS, Academic Medical Center, Amsterdam, The Netherlands.
authors.forename: J C
authors.initials: JC
authors.lastname: Wetsteyn
authors.forename: P J
authors.initials: PJ
authors.lastname: De Vries
authors.forename: B
authors.initials: B
authors.lastname: Oosterhuis
authors.forename: C J
authors.initials: CJ
authors.lastname: Van Boxtel
mesh_terms: D000328:Adult; D000704:Analysis of Variance; D002738:Chloroquine / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D004334:Drug Administration Schedule; D005260:Female; D005500:Follow-Up Studies; D006801:Humans; D008288:Malaria / Q000188:drug therapy*; D008297:Male
chemical_list: D002738:Chloroquine