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Showing 1 to 18 of 18 for “"Mefloquine"”.
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Characterisation of Mefloquine accumulation in Plasmodium falciparum
Mefloquine has been in use for over twenty years and still very little is known about its interaction with Plasmodium falciparum. In 1979, Fitch er al carried out the only other published extensive investigation of mefloquine accumulation, but were not able to demonstrate energy dependent uptake. …
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In vitro metabolism studies to inform physiologically-based pharmacokinetic modelling of mefloquine, ritonavir and proguanil
… characteristics of 3 commonly used drugs, namely mefloquine, proguanil and ritonavir, were measured. This was done by measuring the microsomal metabolism of these drugs in human liver microsomes, then determining the fraction of the drug metabolized by CYP (fm,CYP) isoforms and confirming this …
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The Anti Selective Aldol Addition of Ketones to Aldehydes Mediated by N-Amino Cyclic Carbamate Chiral Auxiliaries and Its Use in the Asymmetric Total Synthesis of (+)- and (-)-Mefloquine Hydrochloride
… the asymmetric total synthesis of (+)- and (-)-mefloquine hydrochloride, a potent antimalarial compound. The synthesis is based on an ACC-mediated asymmetric Darzens reaction between an α-chloro ketone and a quinoline-based aldehyde. This novel methodology gives a highly enantioenriched …
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A cost analysis of the treatment of first-line uncomplicated malaria in the Tonga district of Mpumalanga
… co-artemether, halofantrine, amodiaquine, and mefloquine. It was found that sulfadoxinepyrimethamine was 5 times more cost-effective as first line therapy than chloroquine. Of the other modelled drugs, it was recommended that an artesunate combination should be implemented when it becomes …
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The effect of quinoline anti-malarial drugs on the endolysosomal and secretory pathways of plasmodium falciparum strain 3D7, dictyostelium discoideum and mammalian A549 cells
… of chloroquine, amadiaquine, halofantrine, mefloquine and quinine on the endolysosomal systems in Plasmodium falciparum 3D7, Dictyostelium discoideum and A549 pulmonary cancer cells were examined.
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Brain Stimulation Reward is Integrated by A Network of Electrically-Coupled GABA Neurons
… and GJ blockers, including the Cx36 blocker mefloquine, increase the threshold for IC self-stimulation without affecting performance. Thus, electrical coupling between this network of GABA neurons fits the prevailing model for the elusive integrator of BSR.</p>
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Comparative and Epidemiological Genomics of Human Malaria Parasites
… sequences with associated phenotype data on mefloquine, an antimalarial drug. I show that the current outbreak of multidrug resistance in Southeast Asia is accompanied by a hyper-sensitization of the parasite population through the acquisition of a complex genetic architecture of mefloquine …
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Changing Antimalarial Drug Sensitivities in Uganda
… and greater sensitivities to lumefantrine and mefloquine, consistent with DP selection pressure. Compared to results for isolates from 2010-13, sensitivities of 2016 community isolates to chloroquine, amodiaquine, and piperaquine improved (geometric mean IC<sub>50</sub>s 248, 76.9, and 19.1 nM …
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The efficacy and safety of artesunate suppositories in combination with other antimalarials in the treatment of severe malaria in Sudan.
… by doxycycline or pyrimethamine/sulphadoxine or mefloquine resulted in clinical cure rates of 100%, 100% and 96.7% respectively. The combination with either doxycycline or pynmethamine/sulphadoxine is equally effective to that followed by mefloquine in preventing recrudescence. The three …
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Development of novel strategies to combat multidrug resistance mediated by efflux transporters and intracellular bacteria
… antimalarial drugs hydroxychloroquine, quinine, mefloquine and primaquine in an effort to inhibit PfCRT. A quinine dimer, Q2, blocked PfCRT mediated efflux and successfully cleared parasitemia <em>in vivo</em> in a <em>Plasmodium berghei</em>mice model.Efforts to target pathogenic bacteria that …
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Anti-malaria drug treatment in Vietnam
… combination with other antimalarial drugs such mefloquine or other compound (s); which is the best regimen (s); can artemisinin and its derivatives (artesunate or artemether) reduce the mortality in severe malaria and which is the best drug(s); are there important neurotoxic side effects in …
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REGULATION OF ADAPTIVE IMMUNE RESPONSES TO PLASMODIUM CHABAUDI MALARIA INFECTION
… at day 3 post infection with the antimalarial mefloquine (MQ) to reduce immune stimulation early in our system. This early MQ treatment resulted in a great expansion of IFN-γ+ Th1 cells and a great reduction of Th1-like Tfh cells. In conclusion, our studies have provided vital information …
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Bioassay-guided fractionation of Artemisia afra for in vitro antimalarial activity against Plasmodium falciparum
… and resistance to both chloroquine and mefloquine. Their sensitivity against artemisinin was also established. IC₅₀ values obtained for the isolated pure compound against P. falciparum ranged from 0.87 to 2.54μg/ml. The IC₅₀ values obtained for general cytotoxicity of the crude extract …
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Effects of constitutive and acute Connexin 36 deficiency on brain-wide susceptibility to PTZ-induced neuronal hyperactivity
… as acute pharmacological blockade of Cx36 by mefloquine results in increased susceptibility to PTZ-induced neuronal hyperactivity. Together, these results demonstrate a reciprocal relationship between Cx36 and seizure-associated neuronal hyperactivity: Cx36 deficiency contributes …
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The influence of genetic background on drug resistance in the malaria parasite Plasmodium falciparum
… sensitivity to multiple antimalarials, including mefloquine and lumefantrine, popular partner drugs in first-line artemisinin combination therapies. During my PhD, I assessed a panel of parasite lines that had undergone *in vitro* evolution experiments, identifying polymorphisms in a poorly …
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A pharmacokinetic and antimalarial efficacy evaluation of pyridodibemequines and their metabolites
… CQR strains of P. falciparum. 43M1 or 47M1 with mefloquine or lumefantrine displayed in vitro antimalarial synergy in a CQS strain of P. falciparum; however, in a CQR strain, antagonism and additivity were displayed with mefloquine and lumefantrine, respectively. Additionally, 43M1 and 47M1 were …
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Antimalarial Agents: New Mechanisms of Actions for Old and New Drugs
… of action of an established antimalarial drug, Mefloquine (MQ). Dr. Klemba's recently developed amino acid efflux assay was used to determine the effect of MQ and its open-ring analogs on hemoglobin endocytosis and catabolism in P. falciparum-infected erythrocytes. In total 26 MQ analogs were …
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Development of analytical techniques for probing the effects of -haematin inhibiting compounds on the malaria parasite Plasmodium falciparum
… known non-inhibiting haemozoin drugs, including mefloquine, Abstract lumefantrine, pyrimethamine and tetrahydrocannabinol (THC). This higher throughput cellular fractionation assay will significantly increase throughput while also becoming an invaluable technique for probing haemozoin inhibition …