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Primaquine

The integrity and stability of specimens under different storage conditions for glucose-6-phosphate dehydrogenase deficiency screening using WST-8

May 5, 2021 - 08:56 -- Open Access
Author(s): 
Chamchoy K, Praoparotai A, Pakparnich P, Sudsumrit S, Swangsri T, Chamnanchanunt S, Songdej D, Imwong M, Boonyuen U
Reference: 
Acta Trop. 2021 May;217:105864

Accurate measurement of glucose-6-phosphate dehydrogenase (G6PD) activity is critical for malaria treatment as misclassification of G6PD deficiency could cause serious harm to patients. G6PD activity should be assessed in blood samples on the day of collection. Otherwise, specimens should be stored under suitable conditions to prevent loss of G6PD activity.

Glucose-6-phosphate dehydrogenase mutations in malaria endemic area of Thailand by multiplexed high‐resolution melting curve analysis

April 21, 2021 - 15:07 -- Open Access
Author(s): 
Usa Boonyuen, Duantida Songdej, Mallika Imwong, et al.
Reference: 
Malaria Journal 2021 20:194, 20 April 2021

Glucose-6-phosphate dehydrogenase (G6PD) deficiency, the most common enzymopathy in humans, is prevalent in tropical and subtropical areas where malaria is endemic. Anti-malarial drugs, such as primaquine and tafenoquine, can cause haemolysis in G6PD-deficient individuals. Hence, G6PD testing is recommended before radical treatment against vivax malaria. Phenotypic assays have been widely used for screening G6PD deficiency, but in heterozygous females, the random lyonization causes difficulty in interpreting the results. Over 200 G6PD variants have been identified, which form genotypes associated with differences in the degree of G6PD deficiency and vulnerability to haemolysis. This study aimed to assess the frequency of G6PD mutations using a newly developed molecular genotyping test.

NOT Open Access | Synthesis and biological evaluation of benzhydryl-based antiplasmodial agents possessing Plasmodium falciparum chloroquine resistance transporter (PfCRT) inhibitory activity

April 6, 2021 - 14:20 -- NOT Open Access
Author(s): 
Relitti N, Federico S, Pozzetti L, Campiani G, et al.
Reference: 
Eur J Med Chem. 2021 Apr 5;215:113227

Due to the surge in resistance to common therapies, malaria remains a significant concern to human health worldwide. In chloroquine (CQ)-resistant (CQ-R) strains of Plasmodium falciparum, CQ and related drugs are effluxed from the parasite's digestive vacuole (DV). This process is mediated by mutant isoforms of a protein called CQ resistance transporter (PfCRT). CQ-R strains can be partially re-sensitized to CQ by verapamil (VP), primaquine (PQ) and other compounds, and this has been shown to be due to the ability of these molecules to inhibit drug transport via PfCRT.

Rolling out the radical cure for vivax malaria in Asia: a qualitative study among policy makers and stakeholders

March 24, 2021 - 14:50 -- Open Access
Author(s): 
Bipin Adhikari, Ghulam Rhahim Awab and Lorenz von Seidlein
Reference: 
Malaria Journal 2021 20:164, 23 March 2021

Wide-spread implementation of treatment regimens for the radical cure of vivax malaria is hindered by a range of factors. This has resulted in an increase in the relative proportion of vivax malaria and is an important obstacle in the achievement of global malaria elimination by 2030. The main objective of this study was to explore the current policies guiding the treatment plans on vivax malaria, and the factors affecting the implementation of radical cure in South/South East Asian and Asian Pacific countries.

Plasmodium vivax infection with exflagellated microgametes in peripheral blood smears

March 23, 2021 - 14:34 -- Open Access
Author(s): 
Li THS, Lee ACH, Wong WS, Yip YL
Reference: 
Int J Infect Dis. 2021 Mar 18:S1201-9712(21)00267-8

A 42-year-old man with travel history to Qatar and India was admitted for feverish sensation, headache and epigastric discomfort. Peripheral blood smears showed intraerythrocytic parasites compatible with Plasmodium vivax [Fig. 1 (a) and (b)].

Primaquine plus clindamycin as a promising salvage therapy for Pneumocystis jirovecii pneumonia: A retrospective analysis in Japanese patients

March 17, 2021 - 09:12 -- Open Access
Author(s): 
Koga M, Suganuma A, Kikuchi T, Yoshimura Y, Shoji K, Kobayashi I, Takezaki S, Kato Y, Kimura M, Maruyama H
Reference: 
J Infect Chemother. 2021 Mar 13:S1341-321X(21)00070-2

Treatment of intractable Pneumocystis jirovecii pneumonia (PCP) patients with primaquine (PQ) in combination with clindamycin (CLDM) was conducted by the Research Group on Chemotherapy of Tropical Diseases (RG-CTD), as a kind of compassionate use. Primaquine was not nationally licensed at the time but imported by RG-CTD for the use in a clinical research to investigate safety and efficacy in malaria treatment.

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
Author(s): 
de Souza Pereira C, Costa Quadros H, Navarro M, et al.
Reference: 
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
Author(s): 
Nguyen TT, Nguyen XX, Gryseels C, et al.
Reference: 
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
Author(s): 
Boechat N, Carvalho RCC, Ferreira MLG, Coutinho JP, Sa PM, Seito LN, Rosas EC, Krettli AU, Bastos MM, Pinheiro LCS
Reference: 
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
Author(s): 
Paramjot Mehan, Ashish Garg, Kumar Ajay, Neeraj Mishra
Reference: 
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.

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