The pharmacokinetics and electrocardiographic effects of chloroquine in healthy subjects.
Chloroquine prophylaxis was administered to 3 healthy male volunteers at 100 mg base/day for 25 days, followed by the curative dose at 25 mg base/kg for 3 days. Subjects attained effective chloroquine (mean = 50 micrograms/l) and desethylchloroquine (mean = 17 micrograms/l) concentrations by the 3rd week of prophylaxis, underlining the need to start chloroquine prophylaxis two weeks before travel. On the second day of the treatment period, hourly electrocardiographic monitoring showed a diminution of the T wave and prolongation of the QTc interval, manifesting cumulatively during the 3 days' curative dose, but with no cardiac symptoms. A dose-dependent cumulative effect of chloroquine was demonstrated with higher blood concentrations during the treatment period. Electrocardiographic readings spontaneously normalized after the treatment period as drug concentrations diminished progressively.
Bustos
M D
MD
Département des Maladies Infectieuses, Parasitaires, Tropicales et Santé Publique-INSERM U 313, Groupe Hospitalier Pitié-Salpêtrière, Paris, France.
Gay
F
F
Diquet
B
B
Thomare
P
P
Warot
D
D
D000328:Adult; D002738:Chloroquine / Q000009:adverse effects / Q000031:analogs & derivatives / Q000097:blood / Q000493:pharmacokinetics* / Q000494:pharmacology*; D004562:Electrocardiography / Q000187:drug effects*; D005500:Follow-Up Studies; D006321:Heart / Q000187:drug effects*; D006801:Humans; D008297:Male
D002738:Chloroquine; C007278:desethylchloroquine