PMID: 9647356Jul 1, 1998Paper

Effect of experimental diabetes mellitus and arthritis on the pharmacokinetics of hydroxychloroquine enantiomers in rats

Pharmaceutical Research
J EmamiF Jamali

Abstract

To study the effect of experimental diabetes and arthritis on the pharmacokinetics of hydroxychloroquine (HCQ) enantiomers in rats. The pharmacokinetic studies were carried out following administration of 40 mg/kg of racemic HCQ to diabetic, insulin-treated diabetic, adjuvant arthritic and control rats. Renal (70% and 62% for R- and S-HCQ, respectively) and non-renal clearance (100% and 145% for R- and S-HCQ, respectively) of HCQ enantiomers were significantly increased in diabetic rats. Diabetes-induced alterations in the disposition of HCQ were reversed by insulin treatment. In arthritic rats, systemic clearance (CL) of HCQ enantiomers was significantly reduced (1.05 +/- 0.15 and 1.3 +/- 0.19 l/h/kg for R- and S-HCQ, respectively) compared to controls (1.69 +/- 0.32 and 1.93 +/- 0.34 l/h/kg for R- and S-HCQ, respectively). The fraction unbound of the R- and S-HCQ were 49.4% and 50.5% lower in platelet rich plasma of arthritic rats compared to healthy rats. Increased blood concentrations of HCQ enantiomers in arthritic rats were significantly related to the degree of inflammation. Diabetes significantly increased the CL of both R- and S-HCQ by increasing renal and non-renal clearance. Arthritis caused a significant decrease in...Continue Reading

Citations

Apr 6, 2005·The Journal of Pharmacy and Pharmacology·N LealE Suarez
Oct 20, 2006·Journal of Clinical Pharmacology·Josiane Cristófani PoggiMarina Lemos dos Reis
Aug 6, 2008·European Journal of Clinical Pharmacology·Elaine Christine Dantas MoisésSérgio Pereira da Cunha
Apr 30, 2013·Biopharmaceutics & Drug Disposition·Forugh SanaeeFakhreddin Jamali
Dec 20, 2002·Canadian Journal of Physiology and Pharmacology·Adriana RochaVera Lucia Lanchote
Sep 25, 2004·Chirality·Giuliano Rodrigo BarissaVera Lucia Lanchote
Jan 4, 2017·British Journal of Clinical Pharmacology·Gabriela Campos de Oliveira FilgueiraRicardo Carvalho Cavalli
Dec 6, 2020·The Journal of Pharmacology and Experimental Therapeutics·Xin Liu, William J Jusko
Jun 22, 2017·Biochemical Pharmacology·Chun-Han LinChun-Jung Lin

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