Pharmacokinetic Parameters of Quinine in Healthy Subjects and in Patients with Uncomplicated Malaria in Nigeria: Analysis of Data using a Population Approach

Adehin, Ayorinde; Igbinoba, Sharon Iyobor; Soyinka, Julius O.; Onyeji, Cyprian O.; Babalola, Chinedum P.

doi:10.1016/j.curtheres.2019.100567

Cited by 11 publications

(11 citation statements)

References 26 publications

(41 reference statements)

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“…Quinine showed medium antiviral in vitro activity with EC 50 of 10.7 ± 3.0 μM and EC 90 of 38.8 ± 34 μM. A 600 mg single oral dose of quinine sulphate led to blood C max around 3.5 mg/l (around 8.5 μM) [ 60 ]. In rat, after intravenous dose of 10 mg/kg of quinine, the observed concentration lung/blood ratio was 246 [ 61 ].…”

Section: Discussionmentioning

confidence: 99%

Antimalarial drugs inhibit the replication of SARS-CoV-2: An in vitro evaluation

Gendrot

Andréani

Boxberger

et al. 2020

Travel Medicine and Infectious Disease

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In December 2019, a new severe acute respiratory syndrome coronavirus (SARS-CoV-2) causing coronavirus diseases 2019 (COVID-19) emerged in Wuhan, China. African countries see slower dynamic of COVID-19 cases and deaths. One of the assumptions that may explain this later emergence in Africa, and more particularly in malaria endemic areas, would be the use of antimalarial drugs. We investigated the in vitro antiviral activity against SARS-CoV-2 of several antimalarial drugs. Chloroquine (EC 50 = 2.1 μM and EC 90 = 3.8 μM), hydroxychloroquine (EC 50 = 1.5 μM and EC 90 = 3.0 μM), ferroquine (EC 50 = 1.5 μM and EC 90 = 2.4 μM), desethylamodiaquine (EC 50 = 0.52 μM and EC 90 = 1.9 μM), mefloquine (EC 50 = 1.8 μM and EC 90 = 8.1 μM), pyronaridine (EC 50 = 0.72 μM and EC 90 = 0.75 μM) and quinine (EC 50 = 10.7 μM and EC 90 = 38.8 μM) showed in vitro antiviral effective activity with IC 50 and IC 90 compatible with drug oral uptake at doses commonly administered in malaria treatment. The ratio C lung /EC 90 ranged from 5 to 59. Lumefantrine, piperaquine and dihydroartemisinin had IC 50 and IC 90 too high to be compatible with expected plasma concentrations (ratio C max /EC 90 < 0.05). Based on our results, we would expect that countries which commonly use artesunate-amodiaquine or artesunate-mefloquine report fewer cases and deaths than those using artemether-lumefantrine or dihydroartemisinin-piperaquine. It could be necessary now to compare the antimalarial use and the dynamics of COVID-19 country by country to confirm this hypothesis.

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Section: Discussionmentioning

confidence: 99%

Antimalarial drugs inhibit the replication of SARS-CoV-2: An in vitro evaluation

Gendrot

Andréani

Boxberger

et al. 2020

Travel Medicine and Infectious Disease

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“…Quinine, the second-line treatment for severe malaria after artesunate IV, showed medium anti-SARS-CoV-2 in vitro activity with an EC 50 of 10.7 μM and an EC 90 of 38.8 μM [ 130 ]. A 600 mg single oral dose of quinine sulphate led to blood C max around 3.5 mg/l (around 8.5 μM) [ 131 ]. However, after intravenous doses of 10 mg/kg of quinine in rats, the observed concentration of the lung/blood ratio was 246 [ 132 ].…”

Section: Resultsmentioning

confidence: 99%

Drug Repurposing Against SARS-CoV-1, SARS-CoV-2 and MERS-CoV

et al. 2021

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Since the beginning of the COVID-19 pandemic, large in silico screening studies and numerous in vitro studies have assessed the antiviral activity of various drugs on SARS-CoV-2. In the context of health emergency, drug repurposing represents the most relevant strategy because of the reduced time for approval by international medicines agencies, the low cost of development and the well-known toxicity profile of such drugs. Herein, we aim to review drugs with in vitro antiviral activity against SARS-CoV-2, combined with molecular docking data and results from preliminary clinical studies. Finally, when considering all these previous findings, as well as the possibility of oral administration, 11 molecules consisting of nelfinavir, favipiravir, azithromycin, clofoctol, clofazimine, ivermectin, nitazoxanide, amodiaquine, heparin, chloroquine and hydroxychloroquine, show an interesting antiviral activity that could be exploited as possible drug candidates for COVID-19 treatment.

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“…Adherence to quinine was the lowest. Quinine has been used for over 400 years [ 23 ]; it was the first chemical compound that was successfully used to treat an infectious disease [ 24 ] and has undisputedly saved many lives. However, quinine is not recommended as first-line therapy by the PNLP because of its narrow therapeutic window, worse average treatment outcome compared with modern drugs, and complex application, but it still was the most frequently used drug for the management of uncomplicated malaria.…”

Section: Discussionmentioning

confidence: 99%

Determinants of Patients’ Adherence to Malaria Treatment in the Democratic Republic of the Congo

et al. 2022

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(1) Background: Malaria heavily affects the Democratic Republic of the Congo (DRC) despite the use of effective drugs. Poor adherence to malaria treatment may contribute to this problem. (2) Methods: In one rural and one urban health area in each of the 11 former provinces of the DRC, all households with a case of malaria in the 15 days preceding the survey were selected and the patients or caregivers were interviewed. Adherence to malaria treatment was assessed by self-declaration about its completion. Logistic regression was used to assess predictors. (3) Results: 1732 households participated. Quinine was the most used drug; adherence to artesunate–amodiaquine was the lowest and the main reason for treatment discontinuation was adverse reactions. Predictors of adherence were residence in an urban area, university education, catholic religion, and adoption of recommended behaviour towards a malaria case. Adherence was significantly lower for responders who obtained information on antimalarials from Community Health Workers (CHW). (4) Conclusions: Usage of recommended drugs and adherence to malaria treatment need to be promoted, especially in rural areas, and CHW involvement needs to be improved. Awareness messages need to be made accessible and comprehensible to poorly educated populations and churches need to be involved.

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Pharmacokinetic Parameters of Quinine in Healthy Subjects and in Patients with Uncomplicated Malaria in Nigeria: Analysis of Data using a Population Approach

Cited by 11 publications

References 26 publications

Antimalarial drugs inhibit the replication of SARS-CoV-2: An in vitro evaluation

Antimalarial drugs inhibit the replication of SARS-CoV-2: An in vitro evaluation

Drug Repurposing Against SARS-CoV-1, SARS-CoV-2 and MERS-CoV

Determinants of Patients’ Adherence to Malaria Treatment in the Democratic Republic of the Congo

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