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NOT Open Access | A Novel Hybrid of Chloroquine and Primaquine Linked by Gold(I): Multitarget and Multiphase Antiplasmodial Agent

February 25, 2021 - 08:21 -- NOT Open Access
de Souza Pereira C, Costa Quadros H, Navarro M, et al.
ChemMedChem. 2021 Feb 17;16(4):662-678

Plasmodium parasites kill 435 000 people around the world every year due to unavailable vaccines, a limited arsenal of antimalarial drugs, delayed treatment, and the reduced clinical effectiveness of current practices caused by drug resistance. Therefore, there is an urgent need to discover and develop new antiplasmodial candidates. In this work, we present a novel strategy to develop a multitarget metallic hybrid antimalarial agent with possible dual efficacy in both sexual and asexual erythrocytic stages.

Diagnostic Practices and Treatment for P. vivax in the InterEthnic Therapeutic Encounter of South-Central Vietnam: A Mixed-Methods Study

January 6, 2021 - 13:13 -- Open Access
Nguyen TT, Nguyen XX, Gryseels C, et al.
Pathogens. 2020 Dec 31;10(1):E26

Malaria elimination in the Greater Mekong Sub-Region is challenged by a rising proportion of malaria attributable to P. vivax. Primaquine (PQ) is effective in eliminating the parasite's dormant liver stages and can prevent relapsing infections, but it induces severe haemolysis in patients with Glucose-6-Phosphate Dehydrogenase (G6PD) deficiency, highlighting the importance of testing enzyme activity prior to treatment.

NOT Open Access | Antimalarial and anti-inflammatory activities of new chloroquine and primaquine hybrids: Targeting the blockade of malaria parasite transmission

December 16, 2020 - 10:03 -- NOT Open Access
Boechat N, Carvalho RCC, Ferreira MLG, Coutinho JP, Sa PM, Seito LN, Rosas EC, Krettli AU, Bastos MM, Pinheiro LCS
Bioorg Med Chem. 2020 Dec 15;28(24):115832

Malaria is a disease that requires new drugs not only to fight Plasmodium but also to reduce symptoms of infection such as fever and inflammation. A series of 21 hybrid compounds were designed from chloroquine (CQ) and primaquine (PQ) linked to the pharmacophoric group present in phenylacetic anti-inflammatory drugs. These compounds were designed to have dual activity: namely, to be capable of killing Plasmodium and still act on the inflammatory process caused by malaria infection.

NOT Open Access | Ligand Decorated Primaquine loaded Nanocarriers for Liver Targeting for Triggered Antimalarial Activity

December 3, 2020 - 12:56 -- NOT Open Access
Paramjot Mehan, Ashish Garg, Kumar Ajay, Neeraj Mishra
Curr Mol Pharmacol. 2020 Nov 25

The aim of the current research to formulate a nano delivery system for effective delivery of primaquine for liver targeting to achieve the potential antimalarial activity. An objective of current development is to formulate a lactobionic acid conjugated polyphosphazene based nanodelivery of primaquine for liver targeting to distinguish antimalarial activity.

Evaluation of a single screen and treat strategy to detect asymptomatic malaria among pregnant women from selected health facilities in Lindi region, Tanzania

December 2, 2020 - 09:45 -- Open Access
Chonge Kitojo, Frank Chacky, Emmanuel S. Kigadye, Joseph P. Mugasa, Abdallah Lusasi, Ally Mohamed, Patrick Walker, Erik J. Reaves, Julie R. Gutman & Deus S. Ishengoma
Malar J 19, 438 (2020)

In areas of high transmission, malaria in pregnancy (MiP) primarily causes asymptomatic infections; these infections nonetheless increase the risk of adverse maternal and fetal outcomes. In 2014, Tanzania initiated a single screening and treatment (SST) strategy for all pregnant women at their first antenatal care (ANC) visit using malaria rapid diagnostic tests (RDT) for surveillance purposes. However, there is paucity of data on the effectiveness of SST in the prevention of MiP. The objective of this study was to estimate the number of asymptomatic infections among pregnant women detected by SST, which would have been missed in the absence of the policy.

A small window into the status of malaria in North Korea: estimation of imported malaria incidence of the visitors

November 25, 2020 - 12:13 -- Open Access
Sung J, Cheong HK, Lim AY, Kim JH
Epidemiol Health. 2020 Nov 21:e2020068

This study aimed to hypothesize on the trend in malaria incidence in North Korea using malaria incidence among South Korean visitors to North Korea.

The risk of adverse clinical outcomes following treatment of Plasmodium vivax malaria with and without primaquine in Papua, Indonesia

November 12, 2020 - 15:44 -- Open Access
Thriemer K, Poespoprodjo JR, Kenangalem E, Douglas NM, Sugiarto P, Anstey NM, Simpson JA, Price RN
PLoS Negl Trop Dis. 2020 Nov 11;14(11):e0008838

The widespread use of primaquine (PQ) radical cure for P. vivax, is constrained by concerns over its safety. We used routinely collected patient data to compare the overall morbidity and mortality in patients treated with and without PQ without prior testing of Glucose-6-Phosphate-Dehydrogenase (G6PD) deficiency in Papua, Indonesia, where there is a low prevalence of G6PD deficiency. Records were collated from patients older than 1 year, with P. vivax infection, who were treated with an artemisinin combination therapy (ACT).

Absence of gender influence on the pharmacokinetics of chloroquine combined with primaquine in malaria vivax patients

November 7, 2020 - 12:25 -- Open Access
Vieira MVDF, Mello AGCN, Sena LWP, Vieira JLF
Rev Inst Med Trop Sao Paulo. 2020 Oct 30;62:e83

Chloroquine is the first-line therapy against the asexual stages of Plasmodium vivax . There is a high variation of chloroquine plasma levels after therapeutic doses, which can lead to inadequate exposure to the drug. The gender influence was low regarding the disposition of the drug, which is relevant as there are significant physiological variations between male and female patients.

Chloroquine Potentiates Primaquine Activity Against Active and Latent Hepatic Plasmodia Ex vivo: Potentials and Pitfalls

October 21, 2020 - 09:26 -- Open Access
Dembélé L, Franetich JF, Snounou G, et al.
Antimicrob Agents Chemother. 2020 Oct 19:AAC.01416-20

8-aminoquinoline compounds have long been the only therapeutic agents against latent hepatic malaria parasites. These have poor activity against the blood stage plasmodia causing acute malaria and must be used in conjunction with partner blood schizontocidal agents. We examined the impacts of one such agent, chloroquine, upon the activity of primaquine, an 8-aminoquinoline, against hepatic stages of Plasmodium cynomolgi, Plasmodium yoelii, Plasmodium berghei, and Plasmodium falciparum within several ex vivo systems: primary hepatocytes of Macaca fascicularis; primary human hepatocytes; and stably transformed human hepatocarcinoma cell line HepG2.

Mass radical treatment of a group of foreign workers to mitigate the risk of re-establishment of malaria in Sri Lanka

September 29, 2020 - 13:02 -- Open Access
Manonath M. Marasinghe, Vissundara M. Karunasena, Arundika S. Seneratne, Hema D. B. Herath, Deepika Fernando, Rajitha Wickremasinghe, Kamini N. Mendis and Dewanee Ranaweera
Malaria Journal 2020 19:346, 25 September 2020

Following malaria elimination, Sri Lanka was free from indigenous transmission for six consecutive years, until the first introduced case was reported in December 2018. The source of transmission (index case) was a member of a group of 32 migrant workers from India and the location of transmission was their residence reporting a high prevalence of the primary vector for malaria. Despite extensive vector control the situation was highly susceptible to onward transmission if another of the group developed malaria. Therefore, Mass Radical Treatment (MRT) of the group of workers for Plasmodium vivax malaria was undertaken to mitigate this risk.


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