Tissue and blood concentrations of chloroquine following chronic administration in the rat

@article{Adelusi1982TissueAB,
  title={Tissue and blood concentrations of chloroquine following chronic administration in the rat},
  author={S. A. Adelusi and L. A. Salako},
  journal={Journal of Pharmacy and Pharmacology},
  year={1982},
  volume={34}
}
  • S. Adelusi, L. Salako
  • Published 1 November 1982
  • Medicine, Biology
  • Journal of Pharmacy and Pharmacology
The antimalarial drug, chloroquine, is extensively distributed in tissue and slowly eliminated such that after a single dose, a plasma half-life of 3-5 days has been found (McChesney & McAuliff 1961; McChesney et al 1967). A peak tissue/plasma concentration ratio greater than 300 is obtained in many tissues and after a single dose the drug can be found in the liver and urine for up to five years (Gaudette & Coatney 1961; Rubin et al 1963; Zvaifler et al 1963). Chronic administration of… 
Clinical Pharmacokinetics and Metabolism of Chloroquine
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The impact of the patient’s physiopathological status and ethnic origin on chloroquine pharmacokinetics is discussed, and limited in vitro studies and preliminary data from clinical experiments and observations point to CYP3A and CYP2D6 as the 2 major isoforms affected by or involved in chlorquine metabolism.
Disposition of amopyroquin in rats and rabbits and in vitro activity against Plasmodium falciparum.
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Effect of Chronic Oral Administration of Chloroquine on the Histology of the Liver in Wistar Rats
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EFFECT OF CHRONIC ORAL ADMINISTRATION OF CHLOROQUINE ON THE WEIGHT OF THE HEART IN WISTAR RATS
TLDR
Though chloroquine may be a widely used antimalarial and antirheumatic drug, its chronic administration may result in cardiotoxicity and it is recommended that the drug be prescribed with caution in patients with cardiac abnormality, such as cardiomyopathy and further studies to corroborate this observation should be carried.
Modulation of enzyme activities following the coadministration of potassium bromate and chloroquine in selected tissues and serum of albino rats
TLDR
It could be inferred from the results therefore that the intrinsic properties of chemical substances could be modulated or modified intracellularly when in interaction with other compounds and even with the cell system.
Role of lysosomes in hepatic accumulation of chloroquine.
TLDR
At therapeutic free concentrations (120-360 nM in rheumatoid arthritis), the accumulation ratio for chloroquine in viable isolated rat hepatocytes is of the same order of magnitude as in vivo hepatic uptake in the rat, and this suggests that hepatic accumulation of CQ is a consequence of ion trapping in the acidic interior of lysosomes.
Population pharmacokinetics and pharmacodynamics of chloroquine in a Plasmodium vivax volunteer infection study
TLDR
The PK/PD relationship of chloroquine and its major metabolite, desethylchloroquine, in a P. vivax volunteer infection study is characterized using a semimechanistic population PK/ PD modeling and can be used to optimize dosing scenarios and to identify optimal dosing regimens for chlorquine where resistance to chloroquines is increasing.
Estimation of Drug Accumulation in Repeated-Dose Tissue Distribution Studies
The present study used the published data to examine the relationship between accumulation factor (predicted value) and accumulation ratio (observed value) of a compound as a ratio of tissue
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Introduction Chloroquine (7-chloro-4- (4-diethylamino1-methylbutylamino) quinoline (Fig 1) was originally developed as an antimalarial agent. In recent years it has been found to be beneficial in a
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