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chloroquine

Quantifying and preventing Plasmodium vivax recurrences in primaquine-untreated pregnant women: An observational and modeling study in Brazil

August 4, 2020 - 15:35 -- Open Access
Author(s): 
Corder RM, de Lima ACP, Khoury DS, Docken SS, Davenport MP, Ferreira MU
Reference: 
PLoS Negl Trop Dis 14(7): e0008526

Each year, 4.3 million pregnant women are exposed to malaria risk in Latin America and the Caribbean. Plasmodium vivax causes 76% of the regional malaria burden and appears to be less affected than P. falciparum by current elimination efforts. This is in part due to the parasite's ability to stay dormant in the liver and originate relapses within months after a single mosquito inoculation. Primaquine (PQ) is routinely combined with chloroquine (CQ) or other schizontocidal drugs to supress P. vivax relapses and reduce the risk of late blood-stage recrudescences of parasites with low-grade CQ resistance.

Increasing Malaria Parasite Clearance Time after Chloroquine Therapy, South Korea, 2000-2016

August 4, 2020 - 15:29 -- Open Access
Author(s): 
Park SY, Park YS, Park Y, Kwak YG, Song JE, Lee KS, Cho SH, Lee SE, Shin HI, Yeom JS
Reference: 
Emerg Infect Dis. 2020 Aug; 26(8):1852-1855

We reviewed the clinical efficacy of chloroquine for Plasmodium vivax malaria, the changing trend of parasite clearance time, and fever clearance time during 2000-2016 in South Korea.

Chloroquine Dosing Recommendations for Pediatric COVID-19 Supported by Modeling and Simulation

August 3, 2020 - 16:06 -- Open Access
Author(s): 
Verscheijden LFM, van der Zanden TM, van Bussel LPM, de Hoop-Sommen M, Russel FGM, Johnson TN, de Wildt SN
Reference: 
Clin Pharmacol Ther. 2020 Aug; 108(2):248-252

As chloroquine (CHQ) is part of the Dutch Centre for Infectious Disease Control coronavirus disease 2019 (COVID-19) experimental treatment guideline, pediatric dosing guidelines are needed. Recent pediatric data suggest that existing World Health Organization (WHO) dosing guidelines for children with malaria are suboptimal. The aim of our study was to establish best-evidence to inform pediatric CHQ doses for children infected with COVID-19. A previously developed physiologically-based pharmacokinetic (PBPK) model for CHQ was used to simulate exposure in adults and children and verified against published pharmacokinetic data.

Building on Surface-Active Ionic Liquids for the Rescuing of the Antimalarial Drug Chloroquine

July 30, 2020 - 14:00 -- Open Access
Author(s): 
Silva AT, Lobo L, Oliveira IS, Gomes J, Teixeira C, Nogueira F, Marques EF, Ferraz R, Gomes P
Reference: 
Int J Mol Sci. 2020 Jul 27;21(15):E5334

Ionic liquids derived from classical antimalarials are emerging as a new approach towards the cost-effective rescuing of those drugs. Herein, we disclose novel surface-active ionic liquids derived from chloroquine and natural fatty acids whose antimalarial activity in vitro was found to be superior to that of the parent drug.

Chloroquine does not inhibit infection of human lung cells with SARS-CoV-2

July 26, 2020 - 13:28 -- Open Access
Author(s): 
Hoffmann M, Mösbauer K, Hofmann-Winkler H, Kaul A, Kleine-Weber H, Krüger N, Gassen NC, Müller MA, Drosten C, Pöhlmann S
Reference: 
Nature. 2020 Jul 22

The COVID-19 pandemic, which is caused by the novel coronavirus SARS-CoV-2, has been associated with more than 470,000 fatal cases worldwide. In order to develop antiviral interventions quickly, drugs used for treatment of unrelated diseases are currently being repurposed to combat COVID-19. Chloroquine is a anti-malaria drug that is frequently employed for COVID-19 treatment since it inhibits SARS-CoV-2 spread in the kidney-derived cell line Vero1-3.

Chloroquine and Hydroxychloroquine in Coronavirus Disease 2019 (COVID-19). Facts, Fiction & the Hype. A Critical Appraisal

July 21, 2020 - 15:23 -- Open Access
Author(s): 
Khuroo MS, Sofi AA, Khuroo M
Reference: 
Int J Antimicrob Agents. 2020 Jul 17:106101

The coronavirus infection (COVID-19) has turned in to a global catastrophe and there is an intense search for effective drug therapy. Of all the potential therapies, chloroquine and hydroxychloroquine have been the focus of tremendous public attention. Both drugs have been used in the treatment and prophylaxis of malaria and long-term use of hydroxychloroquine is the cornerstone in the treatment of several auto-immune disorders.

Insights in chloroquine action: perspectives and implications in Malaria and COVID-19

July 21, 2020 - 12:08 -- Open Access
Author(s): 
Pillat MM, Krüger A, Guimarães LMF, Lameu C, de Souza EE, Wrenger C, Ulrich H
Reference: 
Cytometry A. 2020 Jul 19

Malaria is a threat to human mankind and kills about half a million people every year. On the other hand, COVID‐19 resulted in several hundred thousand deaths since December 2019 and remains without an efficient and safe treatment. The antimalarials chloroquine (CQ) and its analogue, hydroxychloroquine (HCQ), have been tested for COVID‐19 treatment, and several conflicting evidence has been obtained.

Safety, pharmacokinetics, and activity of high-dose ivermectin and chloroquine against the liver-stage of Plasmodium cynomolgi infection in Rhesus Macaques

July 14, 2020 - 15:56 -- Open Access
Author(s): 
Vanachayangkul P, Im-Erbsin R, Kobylinski KC, et al.
Reference: 
Antimicrob Agents Chemother. 2020 Jul 13:AAC.00741-20

Previously, ivermectin (1-10 mg/kg) was shown to inhibit liver-stage development of Plasmodium berghei in orally dosed mice. Here, ivermectin showed inhibition of the in vitro development of Plasmodium cynomolgi schizonts (IC50 = 10.42 μM) and hypnozoites (IC50 = 29.24 μM) in primary macaque hepatocytes when administered in high-dose prophylactically but not when administered in radical cure mode.

NOT Open Access | Concentration-dependent mortality of chloroquine in overdose

July 9, 2020 - 08:43 -- NOT Open Access
Author(s): 
Watson JA, Tarning J, Hoglund RM, Baud FJ, Megarbane B, Clemessy JL, White NJ
Reference: 
Elife. 2020 Jul 8;9:e58631

Hydroxychloroquine and chloroquine are used extensively in malaria and rheumatological conditions, and now in COVID-19 prevention and treatment. Although generally safe they are potentially lethal in overdose. In-vitro data suggest that high concentrations and thus high doses are needed for COVID-19 infections, but as yet there is no convincing evidence of clinical efficacy.

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