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Primaquine

Prediction of the CYP2D6 enzymatic activity based on investigating of the CYP2D6 genotypes around the vivax malaria patients in Yunnan Province, China

December 17, 2021 - 21:18 -- Open Access
Author(s): 
Ying Dong, Herong Huang, Yan Deng, Yanchun Xu, Mengni Chen, Yan Liu and Canglin Zhang
Reference: 
Malaria Journal 2021 20:448, 25 November 2021

In recent years, the incidence rate of vivax malaria recurrence still had 3.1% in Yunnan Province population after eradication therapy using primaquine (PQ). In order to understand the specific failure reasons for preventing vivax malaria relapses, a preliminary exploration on the CYP2D6 enzyme activity was carried out in the vivax malaria patients in Yunnan Province population by analysing mutational polymorphism in the coding region of CYP2D6 gene.

Not Open Access | Drug-derived surface-active ionic liquids: a cost-effective way to expressively increase blood-stage antimalarial activity of primaquine

December 14, 2021 - 20:24 -- NOT Open Access
Author(s): 
Silva AT, Oliveira IS, Gomes P, et al.
Reference: 
ChemMedChem. 2021 Dec 9

Inspired by previous disclosure of room-temperature ionic liquids derived from primaquine and cinnamic acids, which displayed slightly enhanced blood-stage activity compared to the parent drug, we have now combined this emblematic antimalarial with natural fatty acids.

Primaquine for Plasmodium vivax radical cure: What we do not know and why it matters

October 30, 2021 - 13:10 -- Open Access
Author(s): 
Popovici J, Tebben K, Witkowski B, Serre D
Reference: 
Int J Parasitol Drugs Drug Resist. 2021 Apr;15:36-42

Plasmodium vivax radical cure requires the administration of a blood schizonticide for killing blood-stage parasites and the addition of a drug able to kill hypnozoites, the dormant parasite stages residing in the liver of infected patients.

Safety monitoring experience of single-low dose primaquine co-administered with artemether–lumefantrine among providers and patients in routine healthcare practice: a qualitative study in Eastern Tanzania

October 23, 2021 - 18:05 -- Open Access
Author(s): 
Dominic Mosha, Mwaka A. Kakolwa, Muhidin K. Mahende, Honorati Masanja, Salim Abdulla, Chris Drakeley, Roland Gosling and Joyce Wamoyi
Reference: 
Malaria Journal 2021 20:392, 9 October 2021

Primaquine is a gametocytocidal drug recommended by the World Health Organization (WHO) in a single-low dose combined with artemisinin-based combination therapy (ACT) for the treatment and prevention of Plasmodium falciparum malaria transmission. Safety monitoring concerns and the lack of a universal validated and approved primaquine pharmacovigilance tool is a challenge for a national rollout in many countries. This study aimed to explore the acceptance, reliability and perceived effectiveness of the primaquine roll out monitoring pharmacovigilance tool (PROMPT).

NOT Open Access | Combination of transdermal patches and solid microneedles for improved transdermal delivery of primaquine

October 20, 2021 - 20:05 -- NOT Open Access
Author(s): 
Ananda PWR, Elim D, Zaman HS, Muslimin W, Tunggeng MGR, Permana AD
Reference: 
Int J Pharm. 2021 Oct 16;609:121204

Malaria caused by various types of Plasmodium has become a global health problem. One of the drugs used as the first line of malaria therapy is primaquine (PMQ). PMQ is generally administered through the oral route. However, the use of PMQ orally could potentially cause some side effects and undergo the first-pass metabolism in the liver, reducing its effectiveness. Therefore, it is necessary to develop another drug administration route to avoid this effect. In this study, for the first time, PMQ was formulated into a transdermal patch for transdermal delivery, combined with solid microneedles, Dermaroller®. Following several optimizations, HPMC and glycerin were used as the main polymer and plasticizer, respectively.

NOT Open Access | Improved Liver Delivery of Primaquine by Phospholipid-Free Small Unilamellar Vesicles with Reduced Hemolytic Toxicity

September 23, 2021 - 08:51 -- NOT Open Access
Author(s): 
Al Fayez N, Böttger R, Rouhollahi E, Cullis PR, Witzigmann D, Li SD
Reference: 
Mol Pharm. 2021 Sep 21

Hemolytic toxicity caused by primaquine (PQ) is a high-risk condition that hampers the wide use of PQ to treat liver-stage malaria. This study demonstrated that phospholipid-free small unilamellar vesicles (PFSUVs) composed of Tween80 and cholesterol could encapsulate and deliver PQ to the hepatocytes with reduced exposure to the red blood cells (RBCs). Nonionic surfactant (Tween80) and cholesterol-forming SUVs with a mean diameter of 50 nm were fabricated for delivering PQ. Drug release/retention, drug uptake by RBCs, pharmacokinetics, and liver uptake of PFSUVs-PQ were evaluated in in vitro and in vivo models in comparison to free drugs.

Development of weight and age-based dosing of daily primaquine for radical cure of vivax malaria

September 14, 2021 - 14:19 -- Open Access
Author(s): 
Walter Robert Taylor, Richard M. Hoglund, Mavuto Mukaka, et al.
Reference: 
Malaria Journal 2021 20:366 9 September 2021

In many endemic areas, Plasmodium vivax malaria is predominantly a disease of young adults and children. International recommendations for radical cure recommend fixed target doses of 0.25 or 0.5 mg/kg/day of primaquine for 14 days in glucose-6-phosphate dehydrogenase normal patients of all ages. However, for many anti-malarial drugs, including primaquine, there is evidence that children have lower exposures than adults for the same weight-adjusted dose. The aim of the study was to develop 14-day weight-based and age-based primaquine regimens against high-frequency relapsing tropical P. vivax.

Dynamics of G6PD activity in patients receiving weekly primaquine for therapy of Plasmodium vivax malaria

September 14, 2021 - 14:07 -- Open Access
Author(s): 
Taylor WRJ, Kim S, Kheng S, Muth S, Tor P, Christophel E, Mukaka M, Kerleguer A, Luzzatto L, Baird JK, Menard D
Reference: 
PLoS Negl Trop Dis. 2021 Sep 8;15(9):e0009690

Acute Plasmodium vivax malaria is associated with haemolysis, bone marrow suppression, reticulocytopenia, and post-treatment reticulocytosis leading to haemoglobin recovery. Little is known how malaria affects glucose-6-phosphate dehydrogenase (G6PD) activity and whether changes in activity when patients present may lead qualitative tests, like the fluorescent spot test (FST), to misdiagnose G6PD deficient (G6PDd) patients as G6PD normal (G6PDn). Giving primaquine or tafenoquine to such patients could result in severe haemolysis.

NOT Open Access | Preliminary studies on drug delivery of polymeric primaquine microparticles using the liver high uptake effect based on size of particles to improve malaria treatment

September 8, 2021 - 15:54 -- NOT Open Access
Author(s): 
da Silva de Barros AO, Portilho FL, Santos-Oliveira R, et al.
Reference: 
Mater Sci Eng C Mater Biol Appl. 2021 Sep;128:112275

Malaria is the most common parasitic disease around the world, especially in tropical and sub-tropical regions. This parasitic disease can have a rapid and severe evolution. It is transmitted by female anopheline mosquitoes. There is no reliable vaccine or diagnostic test against malaria; instead, Artesunate is used for the treatment of severe malaria and Artemisinin is used for uncomplicated falciparum malaria.

Increased primaquine total dose prevents Plasmodium vivax relapses in patients with impaired CYP2D6 activity: report of three cases

August 18, 2021 - 16:20 -- Open Access
Author(s): 
Anielle de Pina-Costa, Ana Carolina Rios Silvino, Edwiges Motta dos Santos, Renata Saraiva Pedro, José Moreira, Gabriela Liseth Umana, Ana Danielle Tavares da Silva, Otília Helena Lupi da Rosa Santos, Karina Medeiros de Deus Henriques, Cláudio Tadeu Daniel-Ribeiro, Patrícia Brasil, Tais Nobrega Sousa and André M. Siqueira
Reference: 
Malaria Journal 2021 20:341, 14 August 2021

The relapsing nature of Plasmodium vivax infection is a major barrier to its control and elimination. Factors such as adequate dosing, adherence, drug quality, and pharmacogenetics can impact the effectiveness of radical cure of P. vivax and need to be adequately evaluated. CYP2D6 pathway mediates the activation of primaquine (primaquine) into an active metabolite(s) in hepatocytes, and impaired activity has been linked to a higher risk of relapse.

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