Chloroquine Phosphate Metabolism and Gender-based Phenotypic Analysis in Healthy Subjects’ Urine Following Oral Administration

Background: Chloroquine, ۴-N-(۷-chloroquinolin-۴-yl)-۱-N,-N-diethylpentane-۱,۴-diamine has promising activity against corona virus disease ۲۰۱۹ (COVID-۱۹) and as such, it is imperative to thoroughly understand and determine the rate at which individual body systems metabolizes the drug. Chloroquine a known antimalarial drug belongs to the chemical class of ۴-aminoquinolines. Objectives: The study aimed to analyze Chloroquine and its metabolite in biological fluids of healthy subjects by simple thin layer chromatography (TLC), which is an efficient, and inexpensive method for quantifying Chloroquine and its metabolites. Methods: A total of ۳۰ healthy volunteers participated in the study by ingesting ۵۰۰ mg of chloroquine, and the results were compared with side effects experienced by these subjects. Two brands of Chloroquine phosphate were used for the analysis and the urine were collected pre and post-drug administration and the intensities of the spots observed were compared with the reference standard stock solution. The same or greater intensity of sample spot indicates poor metabolizer, less intensity when compared to the stock spot indicates intermediate metabolizer while a much lesser intensity indicates an extensive metabolizer. Results: There was a statistically significant difference between the brands of chloroquine used at P<۰.۰۵. ۳۰% of the volunteers were assigned poor metabolizer phenotype, ۵۰% were assigned extensive metabolizer phenotype, and ۲۰% assigned Intermediate metabolizer phenotype based on the intensity of spots observed. The majority of the poor metabolizers were females while the majority of the extensive metabolizers were males. Conclusion: Gender differences plays a vital the role in metabolism, therefore outine implementation of phenotype determination before therapy will therefore greatly improve the goal of therapy and quality of life. implementation of phenotype determination before therapy will, therefore, greatly improve the goal of therapy and quality of life.

Keywords:

Chloroquine , Hydroxychloroquine , Adverse effects , Phenotype