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

Abstract

Background: Chloroquine, 4-N-(7-chloroquinolin-4-yl)-1-N,-N-diethylpentane-1,4-diamine has promising activity against corona virus disease 2019 (COVID-19) 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 4-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 30 healthy volunteers participated in the study by ingesting 500 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<0.05. 30% of the volunteers were assigned poor metabolizer phenotype, 50% were assigned extensive metabolizer phenotype, and 20% 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.

Electrochemical Determination of Chloroquine Phosphate in Real Samples Using a Diresorcinate‐1,10‐phenanthrolinecobalt(II)‐Modified Glassy Carbon Electrode

“…[ 2 , 3 , 4 , 5 ] It has been suggested as a potential anticancer drug, [6] and for treatment of COVID‐19. [ 1 , 7 , 8 ] Several studies suggested that interactions of chloroquine with DNA might underlie the antimalarial activity of CQP. [6] …”

“…This is important to reach at decisions whether malaria developed resistance to this medication and alternative solutions. [ 4 , 7 , 8 ]…”

“…[2][3][4][5] It has been suggested as a potential anticancer drug, [6] and for treatment of COVID-19. [1,7,8] Several studies suggested that interactions of chloroquine with DNA might underlie the antimalarial activity of CQP. [6] Side effects of CQP include cardiac arrest, kidney failure, blindness, heart arrhythmias, and cerebral edema, ophthalmic complications and sudden death.…”

“…This is important to reach at decisions whether malaria developed resistance to this medication and alternative solutions. [4,7,8] Different analytical methods including spectrophotometry, [11,12] spectrofluorometry, [5] LC-MS/MS, [2] HPLC-DAD, [3] HPLC, [13] GC-MS, [14] and capillary electrophoresis [15] are reported for the quantification of CQP in biological fluid samples and pharmaceutical forms. However, these methods show some disadvantages such as extended analysis time, complicated sample preparation steps, required trained manpower, high instrumental and analysis cost, which also contributes to the more significant production of chemical residues.…”

Usefulness of herbal medicines in the prevention and management of coronavirus disease-2019 (COVID-19) and its symptoms: A review

“…Although diarrhea is present in approximately 20-25% of patients infected with MERS-Cov or SARS-Cov, intestinal symptoms have rarely been reported in patients with COVID-19 (Sahin, Erdogan & Agaoglu, 2020) [66] . Various studies have been conducted to identify drug candidates to combat the virus, from natural and synthetic sources, with different individuals metabolizing such drugs in diverse manners as results of their genetic makeup (Bunu et al, 2020) [15] . For the meantime, some persons believe that consuming herbal medicines or medicinal plants that act as immunomodulators can prevent or even cure COVID-19 infection (Nugraha et al, 2020) [57] .…”