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https://www.readbyqxmd.com/read/29141274/use-of-direct-oral-anticoagulants-in-the-first-year-after-market-entry-of-edoxaban-a-danish-nationwide-drug-utilization-study
#1
Anton Pottegård, Erik L Grove, Maja Hellfritzsch
OBJECTIVES: To describe the early uptake of edoxaban; the fourth direct oral anticoagulant (DOAC) to enter the market. METHODS: Using the Danish nationwide health registries, we identified new users of edoxaban (n = 609) from June 6 (day of marketing) through June 2017. For comparison, we also identified new users of dabigatran (n = 2211), rivaroxaban (n = 19 227), and apixaban (n = 14 736). Users were described regarding indication of use, previous anticoagulant experience, comorbidity, and co-medication...
November 15, 2017: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/29138963/synthesis-of-novel-tetrazole-containing-hybrid-ciprofloxacin-and-pipemidic-acid-analogues-and-preliminary-biological-evaluation-of-their-antibacterial-and-antiproliferative-activity
#2
Kommula Dileep, Sowjanya Polepalli, Nishant Jain, Sudheer Kumar Buddana, R S Prakasham, M S R Murty
A series of 1-substituted-1H-tetrazole-5-thiol building blocks were synthesized and introduced to the N-4 piperazinyl group at C-7 position of the quinolone core, and these novel compounds (5a-g and 8a-g) were screened for their antibacterial and antiproliferative activities. Bioactive assay studies manifested that most of new compounds exhibited significant antibacterial activity against the tested strains, including multi-drug-resistant MRSA in comparison with reference drugs ciprofloxacin, streptomycin B and pipemidic acid...
November 14, 2017: Molecular Diversity
https://www.readbyqxmd.com/read/29134510/drug-design-for-alk-positive-nsclc-an-integrated-pharmacophore-based-3d-qsar-and-virtual-screening-strategy
#3
Nivya James, V Shanthi, K Ramanathan
The increasing death rates related to anaplastic lymphoma kinase (ALK)-positive lung cancer culminated in a significant interest in the discovery of novel inhibitors for ALK. In the present research work, pharmacophore-based 3D QSAR modeling and virtual screening strategy have been carried out to address these issues. Initially, a five-point pharmacophore model was developed using the biological data of 50 compounds which includes an FDA-approved ALK inhibitor, crizotinib. Using the generated pharmacophore, a 3D QSAR model was developed and used as a query to screen the DrugBank database...
November 13, 2017: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/29133240/prediction-of-human-cns-pharmacokinetics-using-a-physiologically-based-pharmacokinetic-modeling-approach
#4
Yumi Yamamoto, Pyry A Välitalo, Yin Cheong Wong, Dymphy R Huntjens, Johannes H Proost, An Vermeulen, Walter Krauwinkel, Margot W Beukers, Hannu Kokki, Merja Kokki, Meindert Danhof, Johan G C van Hasselt, Elizabeth C M de Lange
Knowledge of drug concentration-time profiles at the central nervous system (CNS) target-site is critically important for rational development of CNS targeted drugs. Our aim was to translate a recently published comprehensive CNS physiologically-based pharmacokinetic (PBPK) model from rat to human, and to predict drug concentration-time profiles in multiple CNS compartments on available human data of four drugs (acetaminophen, oxycodone, morphine and phenytoin). Values of the system-specific parameters in the rat CNS PBPK model were replaced by corresponding human values...
November 10, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29133036/1-2-4-thiadiazolidin-3-5-diones-as-novel-hydrogen-sulfide-donors
#5
Beatrice Severino, Angela Corvino, Ferdinando Fiorino, Paolo Luciano, Francesco Frecentese, Elisa Magli, Irene Saccone, Paola Di Vaio, Valentina Citi, Vincenzo Calderone, Luigi Servillo, Rosario Casale, Giuseppe Cirino, Valentina Vellecco, Mariarosaria Bucci, Elisa Perissutti, Vincenzo Santagada, Giuseppe Caliendo
Hydrogen sulfide (H2S) is an endogenous modulator that plays significant physio-pathological roles in several biological systems. In this research field there is a large interest in developing selective CBS and CSE inhibitors and H2S releasing moieties, that could be either used as therapeutic agents or linked to known drugs. One of the major problem is the limited availability of chemicals that ensure a controlled release of H2S in vitro as well in vivo. Aiming to obtain novel H2S donors, whose release properties could be appropriately modulated, we have synthesized a series of 1,2,4-thiadiazolidine-3,5-diones (THIA 1-10) as innovative donors that could release H2S in controlled manner...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29132215/in-vivo-molecular-epr-based-spectroscopy-and-imaging-of-tumor-microenvironment-and-redox-using-functional-paramagnetic-probes
#6
Valery V Khramtsov
<i><b>Significance:</b></i> A key role of the tumor microenvironment (TME) in cancer progression, treatment resistance and as a target for therapeutic intervention is increasingly appreciated. Among physiological components of the TME are tissue hypoxia, acidosis, high reducing capacity, elevated concentrations of intracellular glutathione (GSH) and interstitial inorganic phosphate (Pi). Noninvasive <i>in vivo</i> assessment of these parameters provide unique insights into biological processes in TME, and may serve as a tool for pre-clinical screening of anticancer drugs and optimizing TME-targeted therapeutic strategies...
November 13, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/29130688/from-classification-to-regression-multitasking-qsar-modeling-using-a-novel-modular-neural-network-simultaneous-prediction-of-anticonvulsant-activity-and-neurotoxicity-of-succinimides
#7
Davor Antanasijević, Jelena Antanasijević, Nemanja Trišović, Gordana Ušćumlić, Viktor Pocajt
Succinimides, which contain a pharmacophore responsible for anticonvulsant activity, are frequently used antiepileptic drugs and the synthesis of their new derivatives with improved efficacy and tolerability presents an important task. Nowadays, multitarget/tasking methodologies focused on quantitative-structure activity relationships (mt-QSAR/mtk-QSAR) have an important role in the rational design of drugs since they enable simultaneous prediction of several standard measures of biological activities at diverse experimental conditions and against different biological targets...
November 13, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29129386/atrial-fibrillation-in-patients-on-haemodialysis-in-andalusia-prevalence-clinical-profile-and-therapeutic-management
#8
Carmen Sánchez Perales, Teresa Vázquez Sánchez, Daniel Salas Bravo, Sonia Ortega Anguiano, Eduardo Vázquez Ruiz de Castroviejo
Atrial fibrillation (AF) represents an important social and healthcare problem. There is wide variability in the prevalence of this arrhythmia in studies analysing patients on haemodialysis (HD). OBJECTIVE: To investigate the prevalence, clinical profile and therapeutic management of patients with AF on HD in Andalusia. METHODS: We asked the public healthcare system of Andalusia to provide us with the number of patients who were being treated with HD. We asked attending nephrologists from all hospital and outpatient centres in 5 of the 8 Andalusian provinces to perform an electrocardiogram and to fill out a questionnaire on patients selected by simple random sampling...
November 9, 2017: Nefrología: Publicación Oficial de la Sociedad Española Nefrologia
https://www.readbyqxmd.com/read/29127277/dual-protein-kinase-and-nucleoside-kinase-modulators-for-rationally-designed-polypharmacology
#9
Kahina Hammam, Magali Saez-Ayala, Etienne Rebuffet, Laurent Gros, Sophie Lopez, Berengere Hajem, Martine Humbert, Emilie Baudelet, Stephane Audebert, Stephane Betzi, Adrien Lugari, Sebastien Combes, Sebastien Letard, Nathalie Casteran, Colin Mansfield, Alain Moussy, Paulo De Sepulveda, Xavier Morelli, Patrice Dubreuil
Masitinib, a highly selective protein kinase inhibitor, can sensitise gemcitabine-refractory cancer cell lines when used in combination with gemcitabine. Here we report a reverse proteomic approach that identifies the target responsible for this sensitisation: the deoxycytidine kinase (dCK). Masitinib, as well as other protein kinase inhibitors, such as imatinib, interact with dCK and provoke an unforeseen conformational-dependent activation of this nucleoside kinase, modulating phosphorylation of nucleoside analogue drugs...
November 10, 2017: Nature Communications
https://www.readbyqxmd.com/read/29127011/rational-design-of-small-molecules-that-modulate-the-transcriptional-function-of-the-response-regulator-phop
#10
Xiaoyu Qing, Ami De Weerdt, Marc De Maeyer, Hans Steenackers, Arnout Voet
The response regulator PhoP, which is part of the PhoP/PhoQ two-component system, regulates the expression of multiple genes involved in controlling virulence in Salmonella enterica serovar Typhimurium and other species of Gram-negative bacteria. Modulating the phosphorylation-mediated dimerization in the receiver domain may interfere with the transcriptional function of PhoP. In this study, we analyzed the therapeutic potential of the PhoP receiver domain by exploring it as a potential target for drug design...
November 7, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29126724/dual-or-multi-targeting-inhibitors-the-next-generation-anticancer-agents
#11
REVIEW
Nulgumnalli Manjunathaiah Raghavendra, Divya Pingili, Sundeep Kadasi, Akhila Mettu, S V U M Prasad
Dual-targeting/Multi-targeting of oncoproteins by a single drug molecule represents an efficient, logical and alternative approach to drug combinations. An increasing interest in this approach is indicated by a steady upsurge in the number of articles on targeting dual/multi proteins published in the last 5 years. Combining different inhibitors that destiny specific single target is the standard treatment for cancer. A new generation of dual or multi-targeting drugs is emerging, where a single chemical entity can act on multiple molecular targets...
October 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29119928/rational-basis-for-nutraceuticals-in-the-treatment-of-glaucoma
#12
Morrone Luigi Antonio, Rombola Laura, Adornetto Annagrazia, Corasaniti Maria Tiziana, Russo Rossella
Glaucoma, the second leading cause of blindness worldwide, is a chronic optic neuropathy characterized by progressive retinal ganglion cell (RGC) axons degeneration and death. The pathogenesis of primary open-angle glaucoma (OAG), the most common type, is still largely unknown and it is often associated with increased intraocular pressure (IOP) although IOP-independent mechanisms play also a role. Neurodegenerative process, including oxidative stress, excitotoxicity and neuroinflammation, and an impaired ocular blood flow are examples of mechanisms supposed to contribute to the IOP independent deterioration in OAG...
November 9, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/29118096/the-sgc-beyond-structural-genomics-redefining-the-role-of-3d-structures-by-coupling-genomic-stratification-with-fragment-based-discovery
#13
REVIEW
Anthony R Bradley, Aude Echalier, Michael Fairhead, Claire Strain-Damerell, Paul Brennan, Alex N Bullock, Nicola A Burgess-Brown, Elisabeth P Carpenter, Opher Gileadi, Brian D Marsden, Wen Hwa Lee, Wyatt Yue, Chas Bountra, Frank von Delft
The ongoing explosion in genomics data has long since outpaced the capacity of conventional biochemical methodology to verify the large number of hypotheses that emerge from the analysis of such data. In contrast, it is still a gold-standard for early phenotypic validation towards small-molecule drug discovery to use probe molecules (or tool compounds), notwithstanding the difficulty and cost of generating them. Rational structure-based approaches to ligand discovery have long promised the efficiencies needed to close this divergence; in practice, however, this promise remains largely unfulfilled, for a host of well-rehearsed reasons and despite the huge technical advances spearheaded by the structural genomics initiatives of the noughties...
November 8, 2017: Essays in Biochemistry
https://www.readbyqxmd.com/read/29117236/effects-of-cd49d-targeted-antisense-oligonucleotide-on-%C3%AE-4-integrin-expression-and-function-of-acute-lymphoblastic-leukemia-cells-results-of-in-vitro-and-in-vivo-studies
#14
Yann Duchartre, Stefanie Bachl, Hye Na Kim, Eun Ji Gang, Solah Lee, Hsiao-Chuan Liu, Kirk Shung, Ruth Xu, Aaron Kruse, George Tachas, Halvard Bonig, Yong-Mi Kim
We recently demonstrated the effectiveness of blocking CD49d with anti-functional antibodies or small molecule inhibitors as a rational targeted approach to the treatment of acute leukemia in combination with chemotherapy. Antisense oligonucleotide promises to be no less specific than antibodies and inhibitors, but more interesting for pharmacokinetics and pharmacodynamics. We addressed this using the published CD49d antisense drug ATL1102. In vitro, we incubated/nucleofected the ALL cell line Kasumi-2 with ATL1102...
2017: PloS One
https://www.readbyqxmd.com/read/29117144/cell-penetrating-peptides-design-strategies-beyond-primary-structure-and-amphipathicity
#15
REVIEW
Daniela Kalafatovic, Ernest Giralt
Efficient intracellular drug delivery and target specificity are often hampered by the presence of biological barriers. Thus, compounds that efficiently cross cell membranes are the key to improving the therapeutic value and on-target specificity of non-permeable drugs. The discovery of cell-penetrating peptides (CPPs) and the early design approaches through mimicking the natural penetration domains used by viruses have led to greater efficiency of intracellular delivery. Following these nature-inspired examples, a number of rationally designed CPPs has been developed...
November 8, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29116218/improvement-in-clinical-outcome-and-infection-control-using-molecular-diagnostic-techniques-for-early-detection-of-mdr-tuberculous-spondylitis-a-multicenter-retrospective-study
#16
Wenjie Wu, Jingtong Lyu, Peng Cheng, Yuan Cheng, Zehua Zhang, Litao Li, Yonghong Zheng, Jianzhong Xu
There has been limited research on the therapeutic efficacy of molecular diagnosis of spinal tuberculosis. We attempted to determine whether the utilization of molecular diagnosis to detect multidrug-resistant spinal tuberculosis can improve clinical outcomes. A multicenter retrospective study was conducted from February 2009 to June 2015. Ninety-two consecutive culture-confirmed multidrug-resistant tuberculosis (MDR-TB) patients with spinal tuberculosis who were diagnosed clinically and by imaging were enrolled in the study...
November 8, 2017: Emerging Microbes & Infections
https://www.readbyqxmd.com/read/29114561/awareness-about-rational-use-of-medicines-among-fresh-bachelor-of-medicine-and-bachelor-of-surgery-graduates
#17
Vijaya Laxman Chaudhari, Smita N Mali, Amruta V Dawari, Tushar B Nishandar
CONTEXT: Fresh Bachelor of Medicine and Bachelor of Surgery graduates (FMGs) are responsible for the majority of prescription errors and irrational use of medicines. Little research has explored their knowledge on rational prescribing practices. AIMS: The present study aimed to evaluate the awareness of rational use of medicines (RUMs) among the FMGs. SETTINGS AND DESIGN: A multicentric, cross-sectional, and questionnaire-based study was conducted among 308 FMGs during the internship orientation program...
2017: Journal of Education and Health Promotion
https://www.readbyqxmd.com/read/29112410/pyrrolobenzodiazepine-dimer-antibody-drug-conjugates-synthesis-and-evaluation-of-non-cleavable-drug-linkers
#18
Stephen J Gregson, Luke A Masterson, Binqing Wei, Thomas H Pillow, Susan D Spencer, Gyoung-Dong Kang, Shang-Fan Yu, Helga Raab, Jeffrey Lau, Guangmin Li, Gail D Lewis Phillips, Janet Gunzner-Toste, Brian S Safina, Rachana Ohri, Martine Darwish, Katherine R Kozak, Josefa Dela Cruz-Chuh, Andrew Polson, John A Flygare, Philip W Howard
Three rationally designed pyrrolobenzodiazepine (PBD) drug-linkers have been synthesized via intermediate 19 for use in antibody-drug conjugates (ADCs). They lack a cleavable trigger in the linker and consist of a maleimide for cysteine antibody conjugation, a hydrophilic spacer, and either an alkyne (6), triazole (7) or piperazine (8) link to the PBD. In vitro IC50s were 11-48 ng/mL in HER2 3+ SK-BR-3 and KPL-4 (7 inactive) for the anti-HER2 ADCs (HER2 0 MCF7, all inactive) and 0.10-1.73 µg/mL (7 inactive) in CD22 3+ BJAB and WSU-DLCL2 for anti-CD22 ADCs (CD22 0 Jurkat, all inactive at low doses)...
November 7, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29111402/monitoring-both-procalcitonin-and-c-reactive-protein-in-the-early-period-after-tetralogy-of-fallot-correction-in-children-promotes-rational-antibiotic-use
#19
Radoslaw Jaworski, Ireneusz Haponiuk, Ninela Irga-Jaworska, Mariusz Steffens, Maciej Chojnicki, Konrad Paczkowski, Jacek Zielinski
PURPOSE: This retrospective cohort study aimed to identify the early postoperative kinetics of C-reactive protein (CRP) and procalcitonin (PCT) in children undergoing tetralogy of Fallot (ToF) correction. The ability of these inflammatory markers to guide rational antibiotic usage was also determined. MATERIALS AND METHODS: All consecutive children who underwent ToF correction in 2009-2016 in our referral pediatric cardiac surgery clinic in Gdansk, Poland and did not exhibit infection signs on early postoperative days (POD) were identified...
October 27, 2017: Advances in Medical Sciences
https://www.readbyqxmd.com/read/29111261/recommendations-of-the-spanish-society-of-rheumatology-on-treatment-and-use-of-systemic-biological-and-non-biological-therapies-in-psoriatic-arthritis
#20
Juan Carlos Torre Alonso, Petra Díaz Del Campo Fontecha, Raquel Almodóvar, Juan D Cañete, Carlos Montilla Morales, Mireia Moreno, Chamaida Plasencia-Rodríguez, Julio Ramírez García, Rubén Queiro
OBJECTIVE: The main purpose of this recommendation statement is to provide clinicians with the best available evidence and the best opinion agreed upon by the panelists for a rational use of synthetic disease modifying antirheumatic drugs (DMARDs) and biologicals in psoriatic arthritis (PsA) patients. The present document also focuses on important aspects in the management of PsA, such as early diagnosis, therapeutic objectives, comorbidities and optimization of treatment. METHODS: The recommendations were agreed by consensus by a panel of 8 expert rheumatologists, previously selected by the Spanish Society of Rheumatology (SER) through an open call...
October 27, 2017: Reumatología Clinica
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