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https://www.readbyqxmd.com/read/28214841/drug-dosing-and-estimated-renal-function-any-step-forward-from-effersoe
#1
Mads Hornum, Bo Feldt-Rasmussen
Drug dosing in accordance with the renal function is a long-standing challenge to clinicians. For many years it has been evident that in many clinical situations there is no easy way to correctly dose any drug that is mainly cleared by the kidneys. Despite the development of many formulas for estimating the glomerular filtration rate, they all have serious shortcomings. Much effort has been put in to develop estimation formulas to evaluate the renal function as an alternative to direct methods with the aim of safely dosing drugs that are mainly cleared by the kidneys...
February 18, 2017: Nephron
https://www.readbyqxmd.com/read/28214791/a-need-to-stand-united-reply-to-the-wame-secretary
#2
John H Noble
I believe Dr Winker and I agree more than differ about the need for authors of medical journal reports of randomised controlled trial (RCT) findings to acknowledge when they make post hoc adjustments to the original content that they submit to obtain FDA marketing approval for a new drug or medical device.
February 13, 2017: Indian Journal of Medical Ethics
https://www.readbyqxmd.com/read/28214754/new-pt-nnso-core-anticancer-agents-structural-optimization-and-investigation-of-their-anticancer-activity
#3
Shu Xian Chong, Yinxue Jin, Steve Chik Fun Au-Yeung, Kenneth Kin Wah To
A series of new platinum Pt(II) compounds possessing a bidentate leaving ligand modified from oxaliplatin has been synthesized, with one of the oxygen ligating atom substituted for a sulphur atom (resulting in a Pt-NNSO coordination core structure). The general structures are R,R-diaminocyclohexane (DACH)-Pt-(methylthio)acetic acid (K4) and DACH-Pt-(thiophenylacetic acid) (K4 derivatives). Substitution of an electron donating or withdrawing group at the ortho or para position on the phenyl ring of K4 derivatives was found to affect the complexes' stability, reactivity with the biological molecules (5'-guanosine monophosphate (5'-GMP) and L-methionine (L-Met)) and anticancer activity...
February 12, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28214739/characterizing-users-of-new-psychoactive-substances-using-psychometric-scales-for-risk-related-behavior
#4
Annabel Vreeker, Babette G van der Burg, Margriet van Laar, Tibor M Brunt
INTRODUCTION: Studies investigating risk-related behavior in relation to new psychoactive substance (NPS) use are sparse. The current study investigated characteristics of NPS users by comparing risk-related behavior of NPS users to that of illicit drugs (ID) users and licit substances users and non-users (NLC) users. METHODS: In this cross-sectional study we included 528 individuals across an age range of 18-72years. Using a web-based questionnaire we collected self-report data on substance use, sensation seeking, impulsivity, peer substance use and risk perception of substance use...
February 10, 2017: Addictive Behaviors
https://www.readbyqxmd.com/read/28214687/gastroprotective-effect-and-mechanism-of-action-of-croton-rhamnifolioides-essential-oil-in-mice
#5
Cinara Soares Vidal, Anita Oliveira Brito Pereira Bezerra Martins, Andressa de Alencar Silva, Maria Rayane Correia de Oliveira, Jaime Ribeiro-Filho, Thaís Rodrigues de Albuquerque, Henrique Douglas Melo Coutinho, Jackson Roberto Guedes da Silva Almeida, Lucindo Jose Quintans, Irwin Rose Alencar de Menezes
BACKGROUND: Croton rhamnifolioides Pax is a plant species that have been used in the folk medicine to treat ulcers, inflammations and hypertension. However, despite the relevant data obtained from ethnopharmacological studies, the pharmacological properties endorsing the efficacy of this plant to treat ulcer remain to be elucidated. HYPOTHESIS/PURPOSE: The present study aimed to characterize the chemical profile and evaluate the gastroprotective activity of the essential oil obtained from C...
February 16, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28214686/enhanced-anticancer-effect-of-combretastatin-a-4-phosphate-when-combined-with-vincristine-in-the-treatment-of-hepatocellular-carcinoma
#6
Esam M Aboubakr, Ashraf Taye, Omar M Aly, A M Gamal-Eldeen, Mohamed A El-Moselhy
Tubulin targeting agents have received considerable interest as a potential tumor-selective vascular disrupting agents, which represent another avenue for cancer growing therapeutic opportunities. Hence, the present study was conducted to investigate the anti-tumor activity of Combretastatin A-4 phosphate (CA4-P) and vincristine against hepatocellular carcinoma in rats, by individual administration and in combination. In vitro study was conducted using human hepatocellular carcinoma cell lines, showed that CA4-P and vincristine have a potent cell cytotoxic and tubulin inhibitory effect...
February 16, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28214543/theoretical-structural-characterization-of-lymphoguanylin-a-potential-candidate-for-the-development-of-drugs-to-treat-gastrointestinal-disorders
#7
Állan S Pires, William F Porto, Pryscilla O Castro, Octavio L Franco, Sérgio A Alencar
Guanylin peptides (GPs) are small cysteine-rich peptide hormones involved in salt absorption, regulation of fluids and electrolyte homeostasis. This family presents four members: guanylin (GN), uroguanylin (UGN), lymphoguanylin (LGN) and renoguanylin (RGN). GPs have been used as templates for the development of drugs for the treatment of gastrointestinal disorders. Currently, LGN is the only GP with just one disulfide bridge, making it a remarkable member of this family and a potential drug template; however, there is no structural information about this peptide...
February 15, 2017: Journal of Theoretical Biology
https://www.readbyqxmd.com/read/28214533/the-effect-and-mechanism-of-inhibiting-glucose-6-phosphate-dehydrogenase-activity-on-the-proliferation-of-plasmodium-falciparum
#8
Zhiqiang Zhang, Xiaodan Chen, Chengrui Jiang, Zishui Fang, Yi Feng, Weiying Jiang
We screened >40,000 patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency and found that the G6PD Kaiping allele was under the most positive selection for fighting against malaria in the Chinese population. However, the mechanism is unknown. The current study was designed to investigate the anti-malarial effect and mechanism of G6PD deficiency. Dehydroepiandrosterone (DHEA) was utilised for inhibiting the G6PD activity of erythrocytes. Giemsa staining of blood smears and quantitative real-time PCR were used for the detection and quantification of Plasmodium falciparum infection...
February 15, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28214526/recent-advances-in-human-genetics-and-epigenetics-of-adiposity-pathway-to-precision-medicine
#9
Tove Fall, Michael Mendelson, Elizabeth K Speliotes
Obesity is a heritable trait that contributes to substantial global morbidity and mortality. Here, we summarize findings from the last decade of genetic and epigenetic research focused on unravelling the underpinnings of adiposity. More than 140 genetic regions are now known to influence adiposity traits. The genetics of general adiposity, as measured by body mass index, and that of abdominal obesity, as measured by waist to hip ratio, have distinct biological backgrounds. Expression of genes associated with general adiposity are enriched in the nervous system...
February 15, 2017: Gastroenterology
https://www.readbyqxmd.com/read/28214518/potentiating-slc-transporter-activity-emerging-drug-discovery-opportunities
#10
REVIEW
Marie-Laure Rives, Jonathan A Javitch, Alan D Wickenden
Maintaining the integrity of cellular membranes is critical to protecting metabolic activities and genetic information from the environment. Regulation of transport across membranes of essential chemicals, including water, nutrients, hormones and many drugs, is therefore key to cellular homeostasis and physiological processes. The two main transporter superfamilies are ATP-binding cassette (ABC) transporters that primarily function as efflux transporters, and the solute carrier (SLC) transporters. SLC transporters encompass 52 gene families with almost 400 different human transporter genes...
February 15, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28214078/the-optimize-heart-failure-care-program-initial-lessons-from-global-implementation
#11
Martin R Cowie, Yuri M Lopatin, Clara Saldarriaga, Cândida Fonseca, David Sim, Jose Antonio Magaña, Denilson Albuquerque, Marcelo Trivi, Gustavo Moncada, Baldomero A González Castillo, Mario Osvaldo Speranza Sánchez, Edward Chung
Hospitalization for heart failure (HF) places a major burden on healthcare services worldwide, and is a strong predictor of increased mortality especially in the first three months after discharge. Though undesirable, hospitalization is an opportunity to optimize HF therapy and advise clinicians and patients about the importance of continued adherence to HF medication and regular monitoring. The Optimize Heart Failure Care Program (www.optimize-hf.com), which has been implemented in 45 countries, is designed to improve outcomes following HF hospitalization through inexpensive initiatives to improve prescription of appropriate drug therapies, patient education and engagement, and post-discharge planning...
February 12, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/28213871/thieno-2-3-b-pyridine-derivatives-a-new-class-of-antiviral-drugs-against-mayaro-virus
#12
Raquel Amorim, Marcelo Damião Ferreira de Meneses, Julio Cesar Borges, Luiz Carlos da Silva Pinheiro, Lucio Ayres Caldas, Claudio Cesar Cirne-Santos, Marcos Vinícius Palmeira de Mello, Alessandra Mendonça Teles de Souza, Helena Carla Castro, Izabel Christina Nunes de Palmer Paixão, Renata de Mendonça Campos, Ingrid E Bergmann, Viviana Malirat, Alice Maria Rolim Bernardino, Moacyr Alcoforado Rebello, Davis Fernandes Ferreira
Mayaro virus (MAYV) is an arthropod-borne virus and a member of the family Togaviridae, genus Alphavirus. Its infection leads to an acute illness accompanied by long-lasting arthralgia. To date, there are no antiviral drugs or vaccines against infection with MAYV and resources for the prevention or treatment of other alphaviruses are very limited. MAYV has served as a model to study the antiviral potential of several substances on alphavirus replication. In this work we evaluated the antiviral effect of seven new derivatives of thieno[2,3-b]pyridine against MAYV replication in a mammalian cell line...
February 17, 2017: Archives of Virology
https://www.readbyqxmd.com/read/28213660/evidence-of-an-unidentified-extracellular-heat-stable-factor-produced-by-lysobacter-enzymogenes-oh11-that-degrade-fusarium-graminearum-ph1-hyphae
#13
Benard Omondi Odhiambo, Gaoge Xu, Guoliang Qian, Fengquan Liu
Lysobacter enzymogenes OH11 produces heat-stable antifungal factor (HSAF) and lytic enzymes possessing antifungal activity. This study bio-prospected for other potential antifungal factors besides those above. The cells and extracellular metabolites of L. enzymogenes OH11 and the mutants ΔchiA, ΔchiB, ΔchiC, Δclp, Δpks, and ΔpilA were examined for antifungal activity against Fusarium graminearum PH1, the causal agent of Fusarium head blight (FHB). Results evidenced that OH11 produces an unidentified extracellular heat-stable degrading metabolite (HSDM) that exhibit degrading activity on F...
February 17, 2017: Current Microbiology
https://www.readbyqxmd.com/read/28213527/advancing-viral-rna-structure-prediction-measuring-the-thermodynamics-of-pyrimidine-rich-internal-loops
#14
Andy Phan, Katherine Mailey, Jessica Sakai, Xiaobo Gu, Susan J Schroeder
Accurate thermodynamic parameters improve RNA structure predictions and thus accelerate understanding of RNA function and the identification of RNA drug binding sites. Many viral RNA structures, such as internal ribosome entry sites, have internal loops and bulges that are potential drug target sites. Current models used to predict internal loops are biased towards small, symmetric purine loops, and thus poorly predict asymmetric, pyrimidine-rich loops with more than 6 nucleotides that occur frequently in viral RNA...
February 17, 2017: RNA
https://www.readbyqxmd.com/read/28213486/new-drugs-and-dosage-forms
#15
(no author information available yet)
No abstract text is available yet for this article.
March 1, 2017: American Journal of Health-system Pharmacy: AJHP
https://www.readbyqxmd.com/read/28213330/drug-discovery-strategies-in-the-field-of-tumor-energy-metabolism-limitations-by-metabolic-flexibility-and-metabolic-resistance-to-chemotherapy
#16
REVIEW
N D Amoedo, E Obre, R Rossignol
The search for new drugs capable of blocking the metabolic vulnerabilities of human tumors has now entered the clinical evaluation stage, but several projects already failed in phase I or phase II. In particular, very promising in vitro studies could not be translated in vivo at preclinical stage and beyond. This was the case for most glycolysis inhibitors that demonstrated systemic toxicity. A more recent example is the inhibition of glutamine catabolism in lung adenocarcinoma that failed in vivo despite a strong addiction of several cancer cell lines to glutamine in vitro...
February 14, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28213177/tiered-analytics-for-purity-assessment-of-macrocyclic-peptides-in-drug-discovery-analytical-consideration-and-method-development
#17
Jingfang Jenny Qian Cutrone, Xiaohua Stella Huang, Edward S Kozlowski, Ye Bao, Yingzi Wang, Christopher S Poronsky, Dieter M Drexler, Adrienne A Tymiak
Synthetic macrocyclic peptides with natural and unnatural amino acids have gained considerable attention from a number of pharmaceutical/biopharmaceutical companies in recent years as a promising approach to drug discovery, particularly for targets involving protein-protein or protein-peptide interactions. Analytical scientists charged with characterizing these leads face multiple challenges including dealing with a class of complex molecules with the potential for multiple isomers and variable charge states and no established standards for acceptable analytical characterization of materials used in drug discovery...
February 3, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28213099/polymeric-nanoparticles-loaded-with-dexamethasone-or-%C3%AE-tocopheryl-succinate-to-prevent-cisplatin-induced-ototoxicity
#18
Sergio Martín-Saldaña, Raquel Palao-Suay, María Rosa Aguilar, Rafael Ramírez-Camacho, Julio San Román
: The aim of this work is the development of highly protective agents to be administered locally within the middle ear to avoid cisplatin-induced ototoxicity, which affects to 100% of the clinical patients at ultra-high concentrations (16 mg/kg). The protective agents are based on polymeric nanoparticles loaded with dexamethasone or α-tocopheryl succinate as anti-inflammarory and anti-apoptotic molecules. Dexamethasone and α-tocopheryl succinate are poorly soluble in water and present severe side effects when systemic administered during long periods of time...
February 14, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28213015/lettuce-and-fruits-as-a-source-of-multidrug-resistant-acinetobacter-spp
#19
Ana Carvalheira, Joana Silva, Paula Teixeira
The role of ready-to-eat products as a reservoir of pathogenic species of Acinetobacter remains unclear. The objective of the present study was to evaluate the presence of Acinetobacter species in lettuces and fruits marketed in Portugal, and their susceptibility to antimicrobials. Acinetobacter spp. were isolated from 77.9% of the samples and these microorganisms were also found as endophytes (i.e. present within the plant tissue) in 12 of 20 samples of lettuces analysed. Among 253 isolates that were identified as belonging to this genus, 181 presented different PFGE profiles, representing different strains...
June 2017: Food Microbiology
https://www.readbyqxmd.com/read/28212985/nonsteroidal-anti-inflammatory-drugs-in-clinical-and-experimental-epilepsy
#20
REVIEW
Beatrice Mihaela Radu, Florin Bogdan Epureanu, Mihai Radu, Paolo Francesco Fabene, Giuseppe Bertini
Current antiepileptic drugs have limited efficacy and provide little or no benefits in 30% of the patients. Given that a role for brain inflammation in epilepsy has been repeatedly reported in recent years, the potential of anti-inflammatory drugs should be explored in depth, as they may provide new therapeutical approaches in preventing or reducing epileptogenesis. Here, we review preclinical (both in vivo and in vitro) and clinical epilepsy studies in which nonsteroidal antiinflammatory drugs (NSAIDs), i...
February 9, 2017: Epilepsy Research
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