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https://www.readbyqxmd.com/read/28782390/treatment-of-pneumocystis-jirovecii-pneumonia-in-hiv-infected-patients-a-review
#1
Yu-Shan Huang, Jen-Jia Yang, Nan-Yao Lee, Guan-Jhou Chen, Wen-Chien Ko, Hsin-Yun Sun, Chien-Ching Hung
Pneumocystis pneumonia is a potentially life-threatening pulmonary infection that occurs in immunocompromised individuals and HIV-infected patients with a low CD4 cell count. Trimethoprim-sulfamethoxazole has been used as the first-line agent for treatment, but mutations within dihydropteroate synthase gene render potential resistance to sulfamide. Despite advances of combination antiretroviral therapy (cART), Pneumocystis pneumonia continues to occur in HIV-infected patients with late presentation for cART or virological and immunological failure after receiving cART...
August 5, 2017: Expert Review of Anti-infective Therapy
https://www.readbyqxmd.com/read/28756612/clinical-pharmacokinetics-of-systemically-administered-antileishmanial-drugs
#2
REVIEW
Anke E Kip, Jan H M Schellens, Jos H Beijnen, Thomas P C Dorlo
This review describes the pharmacokinetic properties of the systemically administered antileishmanial drugs pentavalent antimony, paromomycin, pentamidine, miltefosine and amphotericin B (AMB), including their absorption, distribution, metabolism and excretion and potential drug-drug interactions. This overview provides an understanding of their clinical pharmacokinetics, which could assist in rationalising and optimising treatment regimens, especially in combining multiple antileishmanial drugs in an attempt to increase efficacy and shorten treatment duration...
July 29, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28711067/pa-6-inhibits-inward-rectifier-currents-carried-by-v93i-and-d172n-gain-of-function-kir2-1-channels-but-increases-channel-protein-expression
#3
Yuan Ji, Marlieke G Veldhuis, Jantien Zandvoort, Fee L Romunde, Marien J C Houtman, Karen Duran, Gijs van Haaften, Eva-Maria Zangerl-Plessl, Hiroki Takanari, Anna Stary-Weinzinger, Marcel A G van der Heyden
BACKGROUND: The inward rectifier potassium current IK1 contributes to a stable resting membrane potential and phase 3 repolarization of the cardiac action potential. KCNJ2 gain-of-function mutations V93I and D172N associate with increased IK1, short QT syndrome type 3 and congenital atrial fibrillation. Pentamidine-Analogue 6 (PA-6) is an efficient (IC50 = 14 nM with inside-out patch clamp methodology) and specific IK1 inhibitor that interacts with the cytoplasmic pore region of the KIR2...
July 15, 2017: Journal of Biomedical Science
https://www.readbyqxmd.com/read/28685254/kh-tfmdi-a-novel-sirtuin-inhibitor-alters-the-cytoskeleton-and-mitochondrial-metabolism-promoting-cell-death-in-leishmania-amazonensis
#4
Brunno Renato Farias Verçoza, Joseane Lima Prado Godinho, Sara Teixeira de Macedo-Silva, Kilian Huber, Franz Bracher, Wanderley de Souza, Juliany Cola Fernandes Rodrigues
Treatment of leishmaniasis involves the use of antimonials, miltefosine, amphotericin B or pentamidine. However, the side effects of these drugs and the reports of drug-resistant parasites demonstrate the need for new treatments that are safer and more efficacious. Histone deacetylase inhibitors are a new class of compounds with potential to treat leishmaniasis. Herein, we evaluated the effects of KH-TFMDI, a novel histone deacetylase inhibitor, on Leishmania amazonensis promastigotes and intracellular amastigotes...
July 6, 2017: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/28623239/-ccug-n-rna-toxicity-in-a-drosophila-model-for-myotonic-dystrophy-type-2-dm2-activates-apoptosis
#5
Vildan Betul Yenigun, Mario Sirito, Alla Amcheslavky, Tomek Czernuszewicz, Jordi Colonques-Bellmunt, Irma García-Alcover, Marzena Wojciechowska, Clare Bolduc, Zhihong Chen, Arturo López Castel, Ralf Krahe, Andreas Bergmann
The myotonic dystrophies are prototypic toxic RNA gain-of-function diseases. Myotonic dystrophy type 1 (DM1) and type 2 (DM2) are caused by different unstable, noncoding microsatellite repeat expansions -- (CTG)DM1 in DMPK and (CCTG)DM2 in CNBP Although transcription of mutant repeats into (CUG)DM1 or (CCUG)DM2 appears to be necessary and sufficient to cause disease, their pathomechanisms remain incompletely understood. To study the mechanisms of (CCUG)DM2 toxicity and develop a convenient model for drug screening, we generated a transgenic DM2 model in the fruit fly Drosophila melanogaster with (CCUG)n repeats of variable length (n=16 and 106)...
June 16, 2017: Disease Models & Mechanisms
https://www.readbyqxmd.com/read/28622334/sterol-14%C3%AE-demethylase-mutation-leads-to-amphotericin-b-resistance-in-leishmania-mexicana
#6
Roy Mwenechanya, Julie Kovářová, Nicholas J Dickens, Manikhandan Mudaliar, Pawel Herzyk, Isabel M Vincent, Stefan K Weidt, Karl E Burgess, Richard J S Burchmore, Andrew W Pountain, Terry K Smith, Darren J Creek, Dong-Hyun Kim, Galina I Lepesheva, Michael P Barrett
Amphotericin B has emerged as the therapy of choice for use against the leishmaniases. Administration of the drug in its liposomal formulation as a single injection is being promoted in a campaign to bring the leishmaniases under control. Understanding the risks and mechanisms of resistance is therefore of great importance. Here we select amphotericin B-resistant Leishmania mexicana parasites with relative ease. Metabolomic analysis demonstrated that ergosterol, the sterol known to bind the drug, is prevalent in wild-type cells, but diminished in the resistant line, where alternative sterols become prevalent...
June 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28583257/in-vitro-and-in-vivo-comparison-of-two-nebulizers-used-for-inhaled-pentamidine-delivery
#7
Nicolas Audag, Giuseppe Liistro, Dimitri Van der Linden, Françoise Smets, Teresinha Leal, Gregory Reychler
No abstract text is available yet for this article.
June 2, 2017: Archivos de Bronconeumología
https://www.readbyqxmd.com/read/28582438/in-silico-discovery-of-substituted-pyrido-2-3-d-pyrimidines-and-pentamidine-like-compounds-with-biological-activity-in-myotonic-dystrophy-models
#8
Àlex L González, Piotr Konieczny, Beatriz Llamusi, Estefanía Delgado-Pinar, José I Borrell, Jordi Teixidó, Enrique García-España, Manuel Pérez-Alonso, Roger Estrada-Tejedor, Rubén Artero
Myotonic dystrophy type 1 (DM1) is a rare multisystemic disorder associated with an expansion of CUG repeats in mutant DMPK (dystrophia myotonica protein kinase) transcripts; the main effect of these expansions is the induction of pre-mRNA splicing defects by sequestering muscleblind-like family proteins (e.g. MBNL1). Disruption of the CUG repeats and the MBNL1 protein complex has been established as the best therapeutic approach for DM1, hence two main strategies have been proposed: targeted degradation of mutant DMPK transcripts and the development of CUG-binding molecules that prevent MBNL1 sequestration...
2017: PloS One
https://www.readbyqxmd.com/read/28542844/the-inward-rectifier-current-inhibitor-pa-6-terminates-atrial-fibrillation-and-does-not-cause-ventricular-arrhythmias-in-goat-and-dog-models
#9
Yuan Ji, Rosanne Varkevisser, Dragan Opacic, Alexandre Bossu, Marion Kuiper, Jet D M Beekman, Sihyung Yang, Azinwi Phina Khan, Dobromir Dobrev, Niels Voigt, Michael Zhuo Wang, Sander Verheule, Marc A Vos, Marcel A G van der Heyden
BACKGROUND AND PURPOSE: The density of the inward rectifier current (IK1 ) increases in atrial fibrillation (AF), shortening effective refractory period and thus promoting atrial re-entry. The synthetic compound pentamidine analogue 6 (PA-6) is a selective and potent IK1 inhibitor. We tested PA-6 for anti-AF efficacy and potential proarrhythmia, using established models in large animals. EXPERIMENTAL APPROACH: PA-6 was applied i.v. in anaesthetized goats with rapid pacing-induced AF and anaesthetized dogs with chronic atrio-ventricular (AV) block...
August 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28506844/proarrhythmic-risk-assessment-using-conventional-and-new-in%C3%A2-vitro-assays
#10
Sonia Goineau, Vincent Castagné
Drug-induced QT prolongation is a major safety issue in the drug discovery process. This study was conducted to assess the electrophysiological responses of four substances using established preclinical assays usually used in regulatory studies (hERG channel or Purkinje fiber action potential) and a new assay (human-induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs)-field potential). After acute exposure, moxifloxacin and dofetilide concentration-dependently decreased IKr amplitude (IC50 values: 102 μM and 40 nM, respectively) and lengthened action potential (100 μM moxifloxacin: +23% and 10 nM dofetilide: +18%) and field potential (300 μM moxifloxacin: +76% and 10 nM dofetilide: +38%) durations...
May 12, 2017: Regulatory Toxicology and Pharmacology: RTP
https://www.readbyqxmd.com/read/28470665/pentamidine-blocks-hepatotoxic-injury-in-mice
#11
Enpeng Zhao, Ghulam Ilyas, Francesca Cingolani, Jae Ho Choi, François Ravenelle, Kathryn E Tanaka, Mark J Czaja
Toxin-induced liver diseases lack effective therapies despite increased understanding of the role factors such as an overactive innate immune response play in the pathogenesis of this form of hepatic injury. Pentamidine is an effective antimicrobial agent against several human pathogens, but studies have also suggested that this drug inhibits inflammation. This potential anti-inflammatory mechanism of action, together with the development of a new oral form of pentamidine isethionate VLX103, led to investigations of the effectiveness of this drug in the prevention and treatment of hepatotoxic liver injury...
May 3, 2017: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/28443518/limitations-of-current-therapeutic-options-possible-drug-targets-and-scope-of-natural-products-in-control-of-leishmaniasis
#12
Neeraj Tiwari, Mallikarjuna Rao Gedda, Vinod K Tiwari, Surya P Singh, Rakesh K Singh
Soon after the identification of Leishmania parasites,the pentavalent antimony compounds have been the mainstay to treat leishmanial infections, worldwide. These compounds were also considered true antileishmanial but the growing incidences of resistance have forced clinicians to use other options. However, due to unavailability of antileishmanial compounds, few drugs like pentamidine (antimicrobial), amphotericin B (antifungal) or miltefosine (antitumor) agents, which are associated with serious side effects, are currently being used...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28437733/the-establishment-of-in%C3%A2-vitro-culture-and-drug-screening-systems-for-a-newly-isolated-strain-of-trypanosoma-equiperdum
#13
Keisuke Suganuma, Shino Yamasaki, Nthatisi Innocentia Molefe, Peter Simon Musinguzi, Batdorj Davaasuren, Ehab Mossaad, Sandagdorj Narantsatsral, Banzragch Battur, Badgar Battsetseg, Noboru Inoue
Dourine is caused by Trypanosoma equiperdum via coitus with an infected horse. Although dourine is distributed in Equidae worldwide and is listed as an internationally important animal disease by the World Organization for Animal Health (OIE), no effective treatment strategies have been established. In addition, there are no reports on drug discovery, because no drug screening system exists for this parasite. A new T. equiperdum strain was recently isolated from the genital organ of a stallion that showed typical symptoms of dourine...
August 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28406408/leishmaniose-cutan%C3%A3-e-et-pentamidine
#14
P Bourée
No abstract text is available yet for this article.
February 1, 2017: Médecine et Santé Tropicales
https://www.readbyqxmd.com/read/28362799/organic-cation-transporter-1-oct1-is-involved-in-pentamidine-transport-at-the-human-and-mouse-blood-brain-barrier-bbb
#15
Gayathri N Sekhar, Ana R Georgian, Lisa Sanderson, Gema Vizcay-Barrena, Rachel C Brown, Paula Muresan, Roland A Fleck, Sarah A Thomas
Pentamidine is an effective trypanocidal drug used against stage 1 Human African Trypanosomiasis (HAT). At the blood-brain barrier (BBB), it accumulates inside the endothelial cells but has limited entry into the brain. This study examined transporters involved in pentamidine transport at the human and mouse BBB using hCMEC/D3 and bEnd.3 cell lines, respectively. Results revealed that both cell lines expressed the organic cation transporters (OCT1, OCT2 and OCT3), however, P-gp was only expressed in hCMEC/D3 cells...
2017: PloS One
https://www.readbyqxmd.com/read/28358927/aquaglyceroporin-null-trypanosomes-display-glycerol-transport-defects-and-respiratory-inhibitor-sensitivity
#16
Laura Jeacock, Nicola Baker, Natalie Wiedemar, Pascal Mäser, David Horn
Aquaglyceroporins (AQPs) transport water and glycerol and play important roles in drug-uptake in pathogenic trypanosomatids. For example, AQP2 in the human-infectious African trypanosome, Trypanosoma brucei gambiense, is responsible for melarsoprol and pentamidine-uptake, and melarsoprol treatment-failure has been found to be due to AQP2-defects in these parasites. To further probe the roles of these transporters, we assembled a T. b. brucei strain lacking all three AQP-genes. Triple-null aqp1-2-3 T. b. brucei displayed only a very moderate growth defect in vitro, established infections in mice and recovered effectively from hypotonic-shock...
March 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28327439/an-in-silico-functional-annotation-and-screening-of-potential-drug-targets-derived-from-leishmania-spp-hypothetical-proteins-identified-by-immunoproteomics
#17
Miguel A Chávez-Fumagalli, Mônica S Schneider, Daniela P Lage, Ricardo A Machado-de-Ávila, Eduardo A F Coelho
Leishmaniasis is a parasitic disease caused by the protozoan of the Leishmania genus. While no human vaccine is available, drugs such as pentavalent antimonials, pentamidine and amphotericin B are used for treat the patients. However, the high toxicity of these pharmaceutics, the emergence of parasite resistance and/or their high cost have showed to the urgent need of identify new targets to be employed in the improvement of the treatment against leishmaniasis. In a recent immunoproteomics approach performed in the Leishmania infantum species, 104 antigenic proteins were recognized by antibodies in sera of visceral leishmaniasis (VL) dogs...
May 2017: Experimental Parasitology
https://www.readbyqxmd.com/read/28280256/late-onset-cerebral-toxoplasmosis-after-allogeneic-hematopoietic-stem-cell-transplantation
#18
Ahmed M Khalaf, Mahmoud A Hashim, Mohammed Alsharabati, Kenneth Fallon, Joel K Cure, Peter Pappas, Shin Mineishi, Ayman Saad
BACKGROUND Toxoplasmosis is an uncommon but potentially fatal complication following allogeneic hematopoietic stem cell transplantation (HCT). Post-transplant toxoplasmosis is often a reactivation of prior infection and typically occurs within the first 6 months of transplant. Herein, we report that cerebral toxoplasmosis may occur 22 months after allogeneic hematopoietic stem cell transplantation. CASE REPORT We describe a case of cerebral toxoplasmosis that occurred 22 months after an allogeneic HCT while the patient was on aerosolized pentamidine for Pneumocystis jiroveci pneumonia (PCP) prophylaxis...
March 10, 2017: American Journal of Case Reports
https://www.readbyqxmd.com/read/28263303/pentamidine-sensitizes-gram-negative-pathogens-to-antibiotics-and-overcomes-acquired-colistin-resistance
#19
Jonathan M Stokes, Craig R MacNair, Bushra Ilyas, Shawn French, Jean-Philippe Côté, Catrien Bouwman, Maya A Farha, Arthur O Sieron, Chris Whitfield, Brian K Coombes, Eric D Brown
The increasing use of polymyxins(1) in addition to the dissemination of plasmid-borne colistin resistance threatens to cause a serious breach in our last line of defence against multidrug-resistant Gram-negative pathogens, and heralds the emergence of truly pan-resistant infections. Colistin resistance often arises through covalent modification of lipid A with cationic residues such as phosphoethanolamine-as is mediated by Mcr-1 (ref. 2)-which reduce the affinity of polymyxins for lipopolysaccharide(3). Thus, new strategies are needed to address the rapidly diminishing number of treatment options for Gram-negative infections(4)...
March 6, 2017: Nature Microbiology
https://www.readbyqxmd.com/read/28174101/evaluation-on-the-leishmanicidal-activity-of-2-n-n-dialkylamino-1-4-naphthoquinone-derivatives
#20
Morgana V de Araújo, Cibelle Cabral David, José Clementino Neto, Luiz A P L de Oliveira, Karoline Cristina Jatobá da Silva, Jefferson Miguel Dos Santos, João Kayke S da Silva, Victoria B C de A Brandão, Tania M S Silva, Celso A Camara, Magna S Alexandre-Moreira
Parasites of the Leishmania genus are the causative agents of leishmaniasis in humans, a disease that affects more than 12 million people worldwide. In this study was evaluated in vitro leishmanicidal activity of 2-N,N'-dialkylamino-1,4-naphthoquinone derivatives, covering a series of fourteen 2-N-morpholino-, 2-N-thiomorpholino, 2-N-piperidino, 2-N-(N(4)-methyl)-piperazino naphthoquinones (1a-n) derived from nor-lapachol and lawsone, belong to some other di-alkyaminoderivatives. At the cytotoxicity assay on peritoneal macrophages, the compounds possessing larger alkyl groups and N-methyl-piperazino moiety (1d, 1h, 1i and 1k), showed toxic effects similar to the standard drug used pentamidine...
May 2017: Experimental Parasitology
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