Academic literature on the topic 'Antimalarial drug Piperaquine (PQ)'

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Journal articles on the topic "Antimalarial drug Piperaquine (PQ)"

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Moore, Brioni R., Kenneth F. Ilett, Madhu Page-Sharp, Jeffrey D. Jago, and Kevin T. Batty. "Piperaquine Pharmacodynamics and Parasite Viability in a Murine Malaria Model." Antimicrobial Agents and Chemotherapy 53, no. 7 (2009): 2707–13. http://dx.doi.org/10.1128/aac.00056-09.

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ABSTRACT Piperaquine (PQ) is an important partner drug in antimalarial combination treatments, but the long half-life of PQ raises concerns about drug resistance. Our aim was to investigate the extended antimalarial effect of PQ in a study of drug efficacy, reinoculation outcomes, and parasite viability after the administration of a single dose of PQ in the murine malaria model. Initially, male Swiss mice were inoculated with Plasmodium berghei and at 64 h after parasite inoculation were given PQ phosphate at 90 mg/kg of body weight intraperitoneally. Parasite viability, drug efficacy, reinocu
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Moore, Brioni R., Kevin T. Batty, Christopher Andrzejewski, Jeffrey D. Jago, Madhu Page-Sharp, and Kenneth F. Ilett. "Pharmacokinetics and Pharmacodynamics of Piperaquine in a Murine Malaria Model." Antimicrobial Agents and Chemotherapy 52, no. 1 (2007): 306–11. http://dx.doi.org/10.1128/aac.00878-07.

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ABSTRACT Piperaquine (PQ) is an important partner in antimalarial treatment strategies. However, there is a paucity of detailed preclinical and pharmacokinetic data to link PQ serum concentrations and toxicity or efficacy. The aim of this study was to investigate the pharmacokinetics and pharmacodynamics of PQ in a murine malaria treatment model. The study comprised three arms. (i) PQ pharmacokinetic parameters were determined in healthy and malaria-infected mice (90 mg/kg PQ phosphate [PQP]). (ii) For determination of single-dose pharmacodynamics, Swiss mice were inoculated with Plasmodium be
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Sim, Ing-Kye, Timothy M. E. Davis, and Kenneth F. Ilett. "Effects of a High-Fat Meal on the Relative Oral Bioavailability of Piperaquine." Antimicrobial Agents and Chemotherapy 49, no. 6 (2005): 2407–11. http://dx.doi.org/10.1128/aac.49.6.2407-2411.2005.

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ABSTRACT Piperaquine (PQ) is an antimalarial drug whose high lipid solubility suggests that its absorption can be increased by a high-fat meal. We examined the pharmacokinetics of PQ phosphate (500 mg given orally) in the fasting state and after a high-fat meal in eight healthy Caucasian volunteers (randomized crossover). Plasma PQ concentration-time profiles were analyzed by using noncompartmental pharmacokinetic analysis. In the fed state, the geometric mean C max increased by 213%, from 21.0 to 65.8 μg/liter (P < 0.001). The time of C max was not significantly different between the fasti
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Nsobya, Samuel L., Moses Kiggundu, Sarah Nanyunja, Moses Joloba, Bryan Greenhouse, and Philip J. Rosenthal. "In Vitro Sensitivities of Plasmodium falciparum to Different Antimalarial Drugs in Uganda." Antimicrobial Agents and Chemotherapy 54, no. 3 (2010): 1200–1206. http://dx.doi.org/10.1128/aac.01412-09.

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ABSTRACT The control of malaria is challenged by resistance of Plasmodium falciparum to multiple drugs. New combination regimens are now advocated for the treatment of uncomplicated falciparum malaria, but the extent of resistance to newer agents is incompletely understood. We measured the in vitro sensitivity of P. falciparum parasites cultured from children enrolled in a drug efficacy trial in Kampala, Uganda, from 2006 to 2008. Sensitivities were measured by comparing levels of histidine-rich protein-2 in parasites incubated with different concentrations of drugs with those in untreated con
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Wallender, Erika, Nan Zhang, Melissa Conrad, et al. "Modeling Prevention of Malaria and Selection of Drug Resistance with Different Dosing Schedules of Dihydroartemisinin-Piperaquine Preventive Therapy during Pregnancy in Uganda." Antimicrobial Agents and Chemotherapy 63, no. 2 (2018): e01393-18. http://dx.doi.org/10.1128/aac.01393-18.

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ABSTRACT Dihydroartemisinin-piperaquine (DHA-PQ) is under study for intermittent preventive treatment during pregnancy (IPTp), but it may accelerate selection for drug resistance. Understanding the relationships between piperaquine concentration, prevention of parasitemia, and selection for decreased drug sensitivity can inform control policies and optimization of DHA-PQ dosing. Piperaquine concentrations, measures of parasitemia, and Plasmodium falciparum genotypes associated with decreased aminoquinoline sensitivity in Africa (pfmdr1 86Y, pfcrt 76T) were obtained from pregnant Ugandan women
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Zhang, Liyuan, Zhaohua Liu, Yunrui Zhang, Yuewu Xie, and Jie Xing. "Metabolism is not a Major Contributor to the Toxicity of Piperaquine, a Long-acting Antimalarial Agent in Artemisinin-based Combination Therapy." Current Drug Metabolism 22, no. 10 (2021): 824–34. http://dx.doi.org/10.2174/1389200222666210928124943.

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Background: Hepatocellular damage has been reported for the antimalarial piperaquine (PQ) in the clinic after cumulative doses. Objectives: The role of metabolism in PQ toxicity was evaluated, and the mechanism mediating PQ hepatotoxicity was investigated. Method: The toxicity of PQ and its major metabolite (PQ N-oxide; M1) in mice was evaluated in terms of serum biochemical parameters. The role of metabolism in PQ toxicity was investigated in mice pretreated with an inhibitor of CYP450 (ABT) and/or FMO enzyme (MMI). The dose-dependent pharmacokinetics of PQ and M1 were studied in mice. Histop
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Cabrera, Mynthia, and Liwang Cui. "In VitroActivities of Primaquine-Schizonticide Combinations on Asexual Blood Stages and Gametocytes of Plasmodium falciparum." Antimicrobial Agents and Chemotherapy 59, no. 12 (2015): 7650–56. http://dx.doi.org/10.1128/aac.01948-15.

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ABSTRACTCurrently, the World Health Organization recommends addition of a 0.25-mg base/kg single dose of primaquine (PQ) to artemisinin combination therapies (ACTs) forPlasmodium falciparummalaria as a gametocytocidal agent for reducing transmission. Here, we investigated the potential interactions of PQ with the long-lasting components of the ACT drugs for eliminating the asexual blood stages and gametocytes ofin vitro-culturedP. falciparumstrains. Using the SYBR green I assay for asexual parasites and a flow cytometry-based assay for gametocytes, we determined the interactions of PQ with the
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Benjamin, John M., Brioni R. Moore, Sam Salman, et al. "Population Pharmacokinetics, Tolerability, and Safety of Dihydroartemisinin-Piperaquine and Sulfadoxine-Pyrimethamine-Piperaquine in Pregnant and Nonpregnant Papua New Guinean Women." Antimicrobial Agents and Chemotherapy 59, no. 7 (2015): 4260–71. http://dx.doi.org/10.1128/aac.00326-15.

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ABSTRACTThe tolerability, safety, and disposition of dihydroartemisinin (DHA) and piperaquine (PQ) were assessed in 32 pregnant (second/third trimester) and 33 nonpregnant Papua New Guinean women randomized to adult treatment courses of DHA-PQ (three daily doses) or sulfadoxine-pyrimethamine (SP)-PQ (three daily PQ doses, single dose of SP). All dose adminstrations were observed, and subjects fasted for 2 h postdose. Plasma PQ was assayed by using high-performance liquid chromatography, and DHA was assessed by using liquid chromatography-mass spectrometry. Compartmental pharmacokinetic models
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Moore, B. R., J. M. Benjamin, S. Salman, et al. "Effect of Coadministered Fat on the Tolerability, Safety, and Pharmacokinetic Properties of Dihydroartemisinin-Piperaquine in Papua New Guinean Children with Uncomplicated Malaria." Antimicrobial Agents and Chemotherapy 58, no. 10 (2014): 5784–94. http://dx.doi.org/10.1128/aac.03314-14.

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ABSTRACTCoadministration of dihydroartemisinin-piperaquine (DHA-PQ) with fat may improve bioavailability and antimalarial efficacy, but it might also increase toxicity. There have been no studies of these potential effects in the pediatric age group. The tolerability, safety, efficacy, and pharmacokinetics of DHA-PQ administered with or without 8.5 g fat were investigated in 30 Papua New Guinean children aged 5 to 10 years diagnosed with uncomplicated falciparum malaria. Three daily 2.5:11.5-mg-base/kg doses were given with water (n= 14, group A) or milk (n= 16, group B), with regular clinical
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Tumwebaze, Patrick, Melissa D. Conrad, Andrew Walakira, et al. "Impact of Antimalarial Treatment and Chemoprevention on the Drug Sensitivity of Malaria Parasites Isolated from Ugandan Children." Antimicrobial Agents and Chemotherapy 59, no. 6 (2015): 3018–30. http://dx.doi.org/10.1128/aac.05141-14.

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ABSTRACTChanging treatment practices may be selecting for changes in the drug sensitivity of malaria parasites. We characterizedex vivodrug sensitivity and parasite polymorphisms associated with sensitivity in 459Plasmodium falciparumsamples obtained from subjects enrolled in two clinical trials in Tororo, Uganda, from 2010 to 2013. Sensitivities to chloroquine and monodesethylamodiaquine varied widely; sensitivities to quinine, dihydroartemisinin, lumefantrine, and piperaquine were generally good. Associations betweenex vivodrug sensitivity and parasite polymorphisms included decreased chloro
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Dissertations / Theses on the topic "Antimalarial drug Piperaquine (PQ)"

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Mohammed, Yousuf Hussain. "The synthesis of the antimalarial compound hydroxypiperaquine (HPQ)." Thesis, Curtin University, 2007. http://hdl.handle.net/20.500.11937/1111.

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Malaria remains one of the most common causes of illness and death in developing countries.1 The development of new drugs to combat the disease is becoming one of the fastest growing research areas. Hydroxypiperaquine (HPQ) is an antimalarial bisquinoline compound related to the emerging antimalarial drug Piperaquine (PQ).2 Various research programs are being conducted internationally in efforts to prepare PQ for possible clinical use in combination with artemisinin derivatives. The hydroxy compound (HPQ) has been described in the Chinese literature but no data exists for this compound within
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