Apparent dose-dependence of chloroquine pharmacokinetics due to limited assay sensitivity and short sampling times
- 39 Downloads
We have shown that apparent nonlinearities in the pharmacokinetics of chloroquine and wide variability in reported kinetic values are possibly artefacts of experimental design. We have used simulated data based on linear equations to demonstrate that chloroquine kinetics may appear to be dose-dependent if samples are collected over a short period or if they are assayed with a method of low sensitivity.
Key wordschloroquine pharmacokinetics dose-dependence exponential equations
Unable to display preview. Download preview PDF.
- 1.Frisk-Holmberg M, Bergkvist Y, Domeij-Nyberg B, Hellström L, Jansson F (1979) Chloroquine serum concentration and side-effects: Evidence for dose-dependent kinetics. Clin Pharmacol Ther 25: 345–350Google Scholar
- 2.Gustafsson LL, Rombo L, Alvan G, Björkman A, Lind M, Walker O (1983) On the question of dose-dependent chloroquine elimination of a single dose. Clin Pharmacol Ther 34: 383–385Google Scholar
- 3.Tulpule A, Krishnaswamy K (1983) Chloroquine kinetics in the undernourished. Eur J Clin Pharmacol 24: 273–276Google Scholar
- 4.Gustafsson LL, Walker O, Alvan G, Beermann B, Estevez F, Gleisner L, Lindström B, Sjöqvist F (1983) Disposition of chloroquine in man after single intravenous and oral doses. Br J Clin Pharmacol 15: 471–479Google Scholar
- 5.Gupta KC, Joshi JV, Desai NK, Sankolli GM, Chowdhary VN, Joshi UM, Chitalange S, Satoskar RS (1984) Kinetics of chloroquine and contraceptive steroids in oral contraceptive users during concurrent chloroquine prophylaxis. Ind J Med Res 80: 658–662Google Scholar
- 6.Frisk-Holmberg M, Bergqvist Y, Termond E, Domeij-Nyberg B (1984) The single dose kinetics of chloroquine and it's major metabolite desethylchloroquine in healthy subjects. Eur J Clin Pharmacol 26: 521–530Google Scholar
- 7.Frisk-Holmberg M, Bergqvist Y, Termond E (1985) Further support for changes in chloroquine disposition and metabolism between a low and a high dose. Eur J Clin Pharmacol 28: 721–722Google Scholar