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A review on possible modes of actions of Chloroquine/ Hydroxychloroquine: Repurposing against SAR-COV-2 (COVID 19) pandemic

May 26, 2020 - 07:53 -- Open Access
Tripathy S, Dassarma B, Roy S, Chabalala H, Matsabisa MG
Int J Antimicrob Agents. 2020 May 22:106028

The chloroquine (CQ) and its analogue hydroxychloroquine (HCQ) have been used as frontline drugs for treatment and prophylaxis against all types of human malaria worldwide. Since late December 2019, humans have been under threat due to an outbreak of a novel coronavirus (SARS-CoV-2) disease (COVID-19; previously known as 2019-nCoV), since its first reported cases in Wuhan, China [1].

Hydroxychloroquine or chloroquine with or without a macrolide for treatment of COVID-19: a multinational registry analysis

May 26, 2020 - 07:51 -- Open Access
Mehra MR, Desai SS, Ruschitzka F, Patel AN
Lancet. 2020 May 22:S0140-6736(20)31180-6

Hydroxychloroquine or chloroquine, often in combination with a second-generation macrolide, are being widely used for treatment of COVID-19, despite no conclusive evidence of their benefit. Although generally safe when used for approved indications such as autoimmune disease or malaria, the safety and benefit of these treatment regimens are poorly evaluated in COVID-19.

Population pharmacokinetics and pharmacodynamics of chloroquine in a Plasmodium vivax volunteer infection study

May 19, 2020 - 15:01 -- Open Access
Abd-Rahman AN, Marquart L, Gobeau N, Kümmel A, Simpson JA, Chalon S, Möhrle JJ, McCarthy JS
Clin Pharmacol Ther. 2020 May 16

Chloroquine has been used for the treatment of malaria for more than 70 years; however, chloroquine pharmacokinetic (PK) and pharmacodynamic (PD) profile in Plasmodium vivax malaria is poorly understood. The objective of this study was to describe the PKPD relationship of chloroquine and its major metabolite, desethylchloroquine, in a P. vivax volunteer infection study.

NOT Open Access | Speed of action and stage specificity of Bencha-loga-wichian, a Thai traditional antipyretic formulation, against Plasmodium falciparum and the chloroquine-potentiating activity of its active compounds, tiliacorinine and yanangcorinine

May 6, 2020 - 15:03 -- NOT Open Access
Nutmakul T, Pattanapanyasat K, Soonthornchareonnon N, Shiomi K, Mori M, Prathanturarug S
J Ethnopharmacol. 2020 Apr 30:112909

Bencha-loga-wichian (BLW), a Thai traditional antipyretic formulation, has been reported to have promising antiplasmodial activity, and it was previously revealed that tiliacorinine and yanangcorinine, isolated from Tiliacora triandra, were the active compounds. However, the mechanisms of action of BLW have not been investigated. In addition, these active compounds are bisbenzylisoquinoline alkaloids, many compounds of which have been reported to potentiate the efficacy of chloroquine.

Experimentally engineered mutations in a ubiquitin hydrolase, UBP-1, modulate in vivo susceptibility to artemisinin and chloroquine in Plasmodium berghei

April 29, 2020 - 09:05 -- Open Access
Simwela NV, Hughes KR, Roberts AB, Rennie MT, Barrett MP, Waters AP
Antimicrob Agents Chemother. 2020 Apr 27. pii: AAC.02484-19

As resistance to artemisinins (current frontline drugs in malaria treatment) emerges in south East Asia, there is an urgent need to identify the genetic determinants and understand the molecular mechanisms underpinning such resistance. Such insights could lead to prospective interventions to contain resistance and prevent the eventual spread to other malaria endemic regions. Artemisinin reduced susceptibility in South East Asia (SEA) has been primarily linked to mutations in P. falciparum Kelch-13, which is currently widely recognised as a molecular marker of artemisinin resistance.

Chloroquine and Hydroxychloroquine for the Prevention or Treatment of Novel Coronavirus Disease (COVID-19) in Africa: Caution for Inappropriate Off-Label Use in Healthcare Settings

April 27, 2020 - 12:50 -- Open Access
Abena PM, Decloedt EH, Nachega JB, et al.
Am J Trop Med Hyg. 2020 Apr 22

The novel severe acute respiratory syndrome-coronavirus-2 pandemic has spread to Africa, where nearly all countries have reported laboratory-confirmed cases of novel coronavirus disease (COVID-19). Although there are ongoing clinical trials of repurposed and investigational antiviral and immune-based therapies, there are as yet no scientifically proven, clinically effective pharmacological treatments for COVID-19.

Neuropsychiatric adverse events of chloroquine: a real-world pharmacovigilance study using the FDA Adverse Event Reporting System (FAERS) database

April 27, 2020 - 12:46 -- Open Access
Sato K, Mano T, Iwata A, Toda T
Biosci Trends. 2020 Apr 22

In late March and early April 2020, the antimalarial drug, chloroquine, has been approved as an emergency treatment for the coronavirus disease 2019 (COVID-19) in the United States and in Europe. Although infrequent, neuropsychiatric symptoms have been reported in patients who received chloroquine for the treatment of malaria or autoimmune diseases.

Chloroquine dosing recommendations for pediatric COVID-19 supported by modeling and simulation

April 23, 2020 - 14:30 -- Open Access
Verscheijden LFM, van der Zanden TM, van Bussel LPM, de Hoop-Sommen M, Russel FGM, Johnson TN, de Wildt SN
Clin Pharmacol Ther. 2020 Apr 22

As chloroquine (CHQ) is part of the Dutch Centre for Infectious Disease Control COVID‐19 experimental treatment guideline, pediatric dosing guidelines are needed. Recent pediatric data suggest that existing 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.

Chloroquine for SARS-CoV-2: Implications of Its Unique Pharmacokinetic and Safety Properties

April 20, 2020 - 09:43 -- Open Access
Smit C, Peeters MYM, van den Anker JN, Knibbe CAJ
Clin Pharmacokinet. 2020 Apr 18

Since in vitro studies and a preliminary clinical report suggested the efficacy of chloroquine for COVID-19-associated pneumonia, there is increasing interest in this old antimalarial drug. In this article, we discuss the pharmacokinetics and safety of chloroquine that should be considered in light of use in SARS-CoV-2 infections. Chloroquine is well absorbed and distributes extensively resulting in a large volume of distribution with an apparent and terminal half-life of 1.6 days and 2 weeks, respectively.

G6PD and chloroquine: selecting the treatment against SARS-CoV-2

April 14, 2020 - 14:40 -- Open Access
Kassi EN, Papavassiliou KA, Papavassiliou AG
J Cell Mol Med. 2020 Apr 12

In light of the severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2 or COVID‐19) pandemic and the possible widespread use of chloroquine (a member of the drug class 4‐aminoquinoline primarily used to prevent and treat malaria and amebiasis) and its derivatives (e.g. hydroxychloroquine, a metabolite of chloroquine),1 a safety issue is addressed, concerning the selection of patients suitable to receive it.


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