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https://www.readbyqxmd.com/read/28327785/ultrastructural-alterations-in-schistosoma-mansoni-juvenile-and-adult-male-worms-after-in-vitro-incubation-with-primaquine
#1
Reem Osama A Kamel, Fatma El-Zahraa Anwar Bayaumy
BACKGROUND: Praziquantel has been cited as the only drug for treating schistosomiasis. However, concerns over drug resistance have encouraged the search for novel drug leads. The antimalarial drug primaquine possesses interesting anti-schistosmal properties. OBJECTIVES: This study is the first to document the potential role of primaquine as a schistosomicide and the ultrastructural changes induced by primaquine on juvenile or adult male worms of Schistosoma mansoni...
April 2017: Memórias do Instituto Oswaldo Cruz
https://www.readbyqxmd.com/read/28319724/interactions-between-tafenoquine-and-artemisinin-combination-therapy-partner-drug-in-asexual-and-sexual-stage-plasmodium-falciparum
#2
Karen Kemirembe, Mynthia Cabrera, Liwang Cui
The 8-aminoquinoline tafenoquine (TFQ), a primaquine derivative, is currently in late-stage clinical development for the radical cure of P. vivax. Here drug interactions between TFQ and chloroquine and six artemisinin-combination therapy (ACT) partner drugs in P. falciparum asexual stages and gametocytes were investigated. TFQ was mostly synergistic with the ACT-partner drugs in asexual parasites regardless of genetic backgrounds. However, at fixed ratios of 1:3, 1:1 and 3:1, TFQ only interacted synergistically with naphthoquine, pyronaridine and piperaquine in gametocytes...
March 11, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28289025/age-weight-and-cyp2d6-genotype-are-major-determinants-of-primaquine-pharmacokinetics-in-african-children
#3
Bronner P Gonçalves, Helmi Pett, Alfred B Tiono, Daryl Murry, Sodiomon Sirima, Mikko Niemi, Teun Bousema, Chris Drakeley, Rob Ter Heine
Low dose primaquine is recommended to prevent Plasmodium falciparum malaria transmission in areas threatened by artemisinin resistance and areas aiming for malaria elimination. Community treatment campaigns with artemisinin-based combination therapy in combination with the gametocytocidal primaquine dose target all age groups but no studies thus far have assessed the pharmacokinetics of this gametocytocidal drug in African children. We recruited forty children participating in a primaquine efficacy trial in Burkina Faso to study primaquine pharmacokinetics...
March 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28279180/primaquine-thiazolidinones-block-malaria-transmission-and-development-of-the-liver-exoerythrocytic-forms
#4
Anna Caroline C Aguiar, Flávio Jr B Figueiredo, Patrícia D Neuenfeldt, Tony H Katsuragawa, Bruna B Drawanz, Wilson Cunico, Photini Sinnis, Fidel Zavala, Antoniana U Krettli
BACKGROUND: Primaquine is an anti-malarial used to prevent Plasmodium vivax relapses and malaria transmission. However, PQ metabolites cause haemolysis in patients deficient in the enzyme glucose-6-phosphate dehydrogenase (G6PD). Fifteen PQ-thiazolidinone derivatives, synthesized through one-post reactions from primaquine, arenealdehydes and mercaptoacetic acid, were evaluated in parallel in several biological assays, including ability to block malaria transmission to mosquitoes. RESULTS: All primaquine derivatives (PQ-TZs) exhibited lower cell toxicity than primaquine; none caused haemolysis to normal or G6PD-deficient human erythrocytes in vitro...
March 9, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28264678/passive-case-detection-of-malaria-in-ratanakiri-province-cambodia-to-detect-villages-at-higher-risk-for-malaria
#5
Somony Heng, Lies Durnez, Sokny Mao, Sovannaroth Siv, Sochantha Tho, Vanna Mean, Vincent Sluydts, Marc Coosemans
BACKGROUND: Cambodia reduced malaria incidence by more than 75% between 2000 and 2015, a target of the Millennium Development Goal 6. The Cambodian Government aims to eliminate all forms of malaria by 2025. The country's malaria incidence is highly variable at provincial level, but less is known at village level. This study used passive case detection (PCD) data at village level in Ratanakiri Province from 2010 to 2014 to describe incidence trends and identify high-risk areas of malaria to be primarily targeted towards malaria elimination...
March 6, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28254294/fabrication-of-highly-sensitive-gold-nanourchins-based-electrochemical-sensor-for-nanomolar-determination-of-primaquine
#6
Neeta Bachheti Thapliyal, Tirivashe Elton Chiwunze, Rajshekhar Karpoormath, Srinivasulu Cherukupalli
A gold nanourchins modified glassy carbon electrode (AuNu/GCE) was developed for the determination of antimalarial drug, primaquine (PQ). The surface of AuNu/GCE was characterized by electrochemical impedance spectroscopy (EIS), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and cyclic voltammetry (CV). EIS results indicated that the electron transfer process at AuNu/GCE was faster as compared to the bare electrode. The SEM and TEM image confirmed the presence and uniform dispersion of gold nanourchins on the GCE surface...
May 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28187990/how-to-contain-artemisinin-and-multidrug-resistant-falciparum-malaria
#7
REVIEW
Arjen M Dondorp, Frank M Smithuis, Charley Woodrow, Lorenz von Seidlein
In the Greater Mekong subregion (GMS), artemisinin resistance is increasingly compounded by partner drug resistance, causing high failure rates of artemisinin combination therapies in some areas. For its containment, an accelerated elimination strategy will be needed. This includes high-quality implementation of conventional malaria control measures: early case management with quality artemisinin combination therapies (avoiding artesunate monotherapies) and single gametocytocidal low dose of primaquine, vector control and surveillance...
February 7, 2017: Trends in Parasitology
https://www.readbyqxmd.com/read/28170391/haemolysis-in-g6pd-heterozygous-females-treated-with-primaquine-for-plasmodium-vivax-malaria-a-nested-cohort-in-a-trial-of-radical-curative-regimens
#8
Cindy S Chu, Germana Bancone, Kerryn A Moore, Htun Htun Win, Niramon Thitipanawan, Christina Po, Nongnud Chowwiwat, Rattanaporn Raksapraidee, Pornpimon Wilairisak, Aung Pyae Phyo, Lily Keereecharoen, Stéphane Proux, Prakaykaew Charunwatthana, François Nosten, Nicholas J White
BACKGROUND: Radical cure of Plasmodium vivax malaria with 8-aminoquinolines (primaquine or tafenoquine) is complicated by haemolysis in individuals with glucose-6-phosphate dehydrogenase (G6PD) deficiency. G6PD heterozygous females, because of individual variation in the pattern of X-chromosome inactivation (Lyonisation) in erythroid cells, may have low G6PD activity in the majority of their erythrocytes, yet are usually reported as G6PD "normal" by current phenotypic screening tests...
February 2017: PLoS Medicine
https://www.readbyqxmd.com/read/28155819/modelling-primaquine-induced-haemolysis-in-g6pd-deficiency
#9
James Watson, Walter Rj Taylor, Didier Menard, Sim Kheng, Nicholas J White
Primaquine is the only drug available to prevent relapse in vivax malaria. The main adverse effect of primaquine is erythrocyte age and dose-dependent acute haemolytic anaemia in individuals with glucose-6-phosphate dehydrogenase deficiency (G6PDd). As testing for G6PDd is often unavailable, this limits the use of primaquine for radical cure. A compartmental model of the dynamics of red blood cell production and destruction was designed to characterise primaquine-induced haemolysis using a holistic Bayesian analysis of all published data and was used to predict a safer alternative to the currently recommended once weekly 0...
February 4, 2017: ELife
https://www.readbyqxmd.com/read/28152025/prevalence-of-g6pd-deficiency-in-selected-populations-from-two-previously-high-malaria-endemic-areas-of-sri-lanka
#10
Sharmini Gunawardena, G M G Kapilananda, Dilhani Samarakoon, Sashika Maddevithana, Sulochana Wijesundera, Lallindra V Goonaratne, Nadira D Karunaweera
Glucose-6-Phosphate Dehydrogenase (G6PD) enzyme deficiency is known to offer protection against malaria and an increased selection of mutant genes in malaria endemic regions is expected. However, anti-malarial drugs such as primaquine can cause haemolytic anaemia in persons with G6PD deficiency. We studied the extent of G6PD deficiency in selected persons attending Teaching Hospitals of Anuradhapura and Kurunegala, two previously high malaria endemic districts in Sri Lanka. A total of 2059 filter-paper blood spots collected between November 2013 and June 2014 were analysed for phenotypic G6PD deficiency using the modified WST-8/1-methoxy PMS method...
2017: PloS One
https://www.readbyqxmd.com/read/28121993/a-comparison-of-three-quantitative-methods-to-estimate-g6pd-activity-in-the-chittagong-hill-tracts-bangladesh
#11
Benedikt Ley, Mohammad Shafiul Alam, James J O'Donnell, Mohammad Sharif Hossain, Mohammad Golam Kibria, Nusrat Jahan, Wasif A Khan, Kamala Thriemer, Mark D Chatfield, Ric N Price, Jack S Richards
BACKGROUND: Glucose-6-phosphate-dehydrogenase-deficiency (G6PDd) is a major risk factor for primaquine-induced haemolysis. There is a need for improved point-of-care and laboratory-based G6PD diagnostics to unsure safe use of primaquine. METHODS: G6PD activities of participants in a cross-sectional survey in Bangladesh were assessed using two novel quantitative assays, the modified WST-8 test and the CareStart™ G6PD Biosensor (Access Bio), The results were compared with a gold standard UV spectrophotometry assay (Randox)...
2017: PloS One
https://www.readbyqxmd.com/read/28107969/a-new-paper-based-analytical-device-for-detection-of-glucose-6-phosphate-dehydrogenase-deficiency
#12
Phuritat Kaewarsa, Wanida Laiwattanapaisal, Attakorn Palasuwan, Duangdao Palasuwan
Glucose-6-phosphate dehydrogenase (G6PD) deficiency is a genetic haemolytic disorder. Most persons with G6PD deficiency are asymptomatic, but exposure to oxidant drugs, such as the anti-malarial drug primaquine, may induce haemolysis, which is commonly found in Asian countries. A reliable test is necessary for diagnosing the deficiency to prevent an acute haemolytic crisis. This study proposes a novel quantitative method to detect G6PD deficiency using paper-based analytical devices (G6PDD-PAD). Wax printing was utilized for fabricating circular reaction zone patterns in paper...
March 1, 2017: Talanta
https://www.readbyqxmd.com/read/28103889/heterogeneity-of-g6pd-deficiency-prevalence-in-mozambique-a-school-based-cross-sectional-survey-in-three-different-regions
#13
Beatriz Galatas, Lurdes Mabote, Wilson Simone, Gloria Matambisso, Lidia Nhamussua, María Del Mar Mañú-Pereira, Clara Menéndez, Francisco Saute, Eusebio Macete, Quique Bassat, Pedro Alonso, Pedro Aide
BACKGROUND: Glucose-6-phosphate dehydrogenase (G6PD) deficiency is an X-linked hereditary enzymatic abnormality that affects more than 400 million people worldwide. Most deficient individuals do not manifest any symptoms; however, several precipitant agents-such as fava intake, infections, or several drugs-may trigger acute haemolytic anaemia. Countries should be informed of the prevalence of this enzymatic anomaly within their borders, in order to make safe and appropriate national decisions regarding the use of potentially unsafe drugs for G6PD deficient individuals...
January 19, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28102941/synthesis-of-primaquine-glyco-conjugates-as-potential-tissue-schizontocidal-antimalarial-agents
#14
Chandra S Azad, Mridula Saxena, Arif J Siddiqui, Jyoti Bhardwaj, Sunil K Puri, Guru P Dutta, Nity Anand, Anil K Saxena
Primaquine (PQ) is the only drug used to prevent relapse of malaria due to P. vivax and P. ovale, by eradicating the dormant liver form of the parasite (hypnozoites). The side effects associated with PQ limits is uses in treatment of malaria. To overcome the premature oxidative deamination and to increase the life span of drug in the biological system the novel glyco-conjugates of PQ were synthesized by coupling of primaquine with hexoses in phosphate buffer. The saccharide part of the hybrid molecules thought to be direct the drug to the liver, where hypnozoites resides...
January 19, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28095658/therapeutic-assessment-of-primaquine-for-radical-cure-of-plasmodium-vivax-malaria-at-primary-and-tertiary-care-centres-in-southwestern-india
#15
Rishikesh Kumar, Vasudeva Guddattu, Kavitha Saravu
Acquaintance is scanty on primaquine (PQ) efficacy and Plasmodium vivax recurrence in Udupi district, Karnataka, India. We assessed the efficacy of 14 days PQ regimen (0.25 mg/kg/day) to prevent P. vivax recurrence. Microscopically, aparasitemic adults (≥18 years) after acute vivax malaria on day 28 were re-enrolled into 15 months' long follow-up study. A peripheral blood smear examination was performed with participants at every 1-2 month interval. A nested PCR test was performed to confirm the mono-infection with P...
December 2016: Korean Journal of Parasitology
https://www.readbyqxmd.com/read/28070879/a-review-of-pharmacogenetics-of-antimalarials-and-associated-clinical-implications
#16
REVIEW
Hazem Elewa, Kyle John Wilby
Genetic variability in drug-metabolizing enzymes and drug transporters is known to influence the pharmacokinetics of many drugs. Antimalarial drugs are a class of agents known to utilize metabolic and elimination pathways prone to genetic variation. This paper aims to review the genetic variants affecting antimalarial medications and discuss their clinical implications. Data were identified for the genes coding for the cytochrome P450 (CYP) enzymes: CYP2C8, CYP2C19, CYP2A6, CYP2D6, CYP2B6, and the P-glycoprotein drug transporter...
January 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28025283/costs-and-cost-effectiveness-of-plasmodium-vivax-control
#17
Michael T White, Shunmay Yeung, Edith Patouillard, Richard Cibulskis
The continued success of efforts to reduce the global malaria burden will require sustained funding for interventions specifically targeting Plasmodium vivax The optimal use of limited financial resources necessitates cost and cost-effectiveness analyses of strategies for diagnosing and treating P. vivax and vector control tools. Herein, we review the existing published evidence on the costs and cost-effectiveness of interventions for controlling P. vivax, identifying nine studies focused on diagnosis and treatment and seven studies focused on vector control...
December 28, 2016: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/27993160/erratum-to-an-optimised-age-based-dosing-regimen-for-single-low-dose-primaquine-for-blocking-malaria-transmission-in-cambodia
#18
Rithea Leang, Naw Htee Khu, Mavuto Mukaka, Mark Debackere, Rupam Tripura, Soy Ty Kheang, Say Chy, Neeraj Kak, Philippe Buchy, Arnaud Tarantola, Didier Menard, Arantxa Roca-Felterer, Rick M Fairhurst, Sim Kheng, Sinoun Muth, Song Ngak, Arjen M Dondorp, Nicholas J White, Walter Robert John Taylor
No abstract text is available yet for this article.
December 20, 2016: BMC Medicine
https://www.readbyqxmd.com/read/27940264/lincosamides-chemical-structure-biosynthesis-mechanism-of-action-resistance-and-applications
#19
REVIEW
Jaroslav Spížek, Tomáš Řezanka
Lincomycin and its derivatives are antibiotics exhibiting biological activity against bacteria, especially Gram-positive ones, and also protozoans. Lincomycin and its semi-synthetic chlorinated derivative clindamycin are widely used in clinical practice. Both antibiotics are bacteriostatic, inhibiting protein synthesis in sensitive bacteria; however, at higher concentrations, they may be bactericidal. Clindamycin is usually much more active than lincomycin in the treatment of bacterial infections, in particular those caused by anaerobic species; it can also be used for the treatment of important protozoal diseases, e...
December 7, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27923405/cytochrome-p450-2d-mediated-metabolism-is-not-necessary-for-tafenoquine-and-primaquine-to-eradicate-the-erythrocytic-stages-of-plasmodium-berghei
#20
Erin E Milner, Jonathan Berman, Diana Caridha, Samuel P Dickson, Mark Hickman, Patricia J Lee, Sean R Marcsisin, Lisa T Read, Norma Roncal, Brian A Vesely, Lisa H Xie, Jing Zhang, Ping Zhang, Qigui Li
BACKGROUND: Due to the ability of the 8-aminoquinolines (8AQs) to kill different stages of the malaria parasite, primaquine (PQ) and tafenoquine (TQ) are vital for causal prophylaxis and the eradication of erythrocytic Plasmodium sp. parasites. Recognizing the potential role of cytochrome (CYP) 450 2D6 in the metabolism and subsequent hepatic efficacy of 8-aminoquinolines, studies were designed to explore whether CYP2D-mediated metabolism was related to the ability of single-dose PQ and TQ to eliminate the asexual and sexual erythrocytic stages of Plasmodium berghei...
December 7, 2016: Malaria Journal
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