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https://www.readbyqxmd.com/read/28641219/comparison-of-brand-versus-generic-antiepileptic-drug-adverse-event-reporting-rates-in-the-u-s-food-and-drug-administration-adverse-event-reporting-system-faers
#1
Md Motiur Rahman, Yasser Alatawi, Ning Cheng, Jingjing Qian, Annya V Plotkina, Peggy L Peissig, Richard L Berg, David Page, Richard A Hansen
OBJECTIVE: Despite the cost saving role of generic anti-epileptic drugs (AEDs), debate exists as to whether generic substitution of branded AEDs may lead to therapeutic failure and increased toxicity. This study compared adverse event (AE) reporting rates for brand vs. authorized generic (AG) vs. generic AEDs. Since AGs are pharmaceutically identical to brand but perceived as generics, the generic vs. AG comparison minimized potential bias against generics. METHODS: Events reported to the U...
June 13, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/28636894/effects-of-hpmc-substituent-pattern-on-water-up-take-polymer-and-drug-release-an-experimental-and-modelling-study
#2
Diego Caccavo, Gaetano Lamberti, Anna Angela Barba, Susanna Abrahmsén-Alami, Anna Viridén, Anette Larsson
The purpose of this study was to investigate the hydration behavior of two matrix formulations containing the cellulose derivative hydroxypropyl methylcellulose (HPMC). The two HPMC batches investigated had different substitution pattern along the backbone; the first one is referred to as heterogeneous and the second as homogenous. The release of both the drug molecule theophylline and the polymer was determined. Additionally, the water concentrations at different positions in the swollen gel layers were determined by Magnetic Resonance Imaging...
June 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28636889/complications-of-hematopoietic-stem-transplantation-fungal-infections
#3
REVIEW
Ali S Omrani, Reem S Almaghrabi
Patients undergoing allogeneic hematopoietic stem cell transplantation (HSCT) are at increased risk of invasive fungal infections, especially during the early neutropenic phase and severe graft-versus-host disease. Mold-active prophylaxis should be limited to the highest risk groups. Empiric antifungal therapy for HSCT with persistent febrile neutropenia is associated with unacceptable response rates, unnecessary antifungal therapy, increased risk of toxicity, and inflated costs. Empiric therapy should not be a substitute for detailed work up to identify the cause of fever in such patients...
June 13, 2017: Hematology/oncology and Stem Cell Therapy
https://www.readbyqxmd.com/read/28633998/changes-in-risk-behaviours-during-and-following-treatment-for-hepatitis-c-virus-infection-among-people-who-inject-drugs-the-activate-study
#4
Håvard Midgard, Behzad Hajarizadeh, Evan B Cunningham, Brian Conway, Markus Backmund, Philip Bruggmann, Julie Bruneau, Stefan Bourgeois, Adrian Dunlop, Graham R Foster, Margaret Hellard, Geert Robaeys, Maria C Thurnheer, Martin Weltman, Janaki Amin, Philippa S Marks, Sophie Quiene, Gregory J Dore, Olav Dalgard, Jason Grebely
BACKGROUND: The risk of hepatitis C virus (HCV) reinfection due to continued injecting risk behaviours might remain a barrier to HCV treatment among people who inject drugs. We aimed to evaluate changes in risk behaviours during and following HCV treatment among people with ongoing injecting drug use or receiving opioid substitution treatment (OST). METHODS: ACTIVATE was an international multicentre clinical trial conducted between 2012 and 2014. Participants with HCV genotypes 2/3 infection were treated with peg-interferon/ribavirin for 12 or 24 weeks and completed a self-administered behavioural questionnaire at each study visit...
June 17, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/28633989/efficacy-and-cytotoxicity-in-cell-culture-of-novel-%C3%AE-hydroxytropolone-inhibitors-of-hepatitis-b-virus-ribonuclease-h
#5
Elena Lomonosova, Jil Daw, Aswin K Garimallaprabhakaran, Nana B Agyemang, Yashkumar Ashani, Ryan P Murelli, John E Tavis
Chronic Hepatitis B virus (HBV) infection is a major worldwide public health problem. Current direct-acting anti-HBV drugs target the HBV DNA polymerase activity, but the equally essential viral ribonuclease H (RNaseH) activity is unexploited as a drug target. Previously, we reported that α-hydroxytropolone compounds can inhibit the HBV RNaseH and block viral replication. Subsequently, we found that our biochemical RNaseH assay underreports efficacy of the α-hydroxytropolones against HBV replication. Therefore, we conducted a structure-activity analysis of 59 troponoids against HBV replication in cell culture...
June 17, 2017: Antiviral Research
https://www.readbyqxmd.com/read/28632475/generic-substitution-of-antiretrovirals-patients-and-health-care-providers-opinions
#6
Jennifer A Kieran, Eimear O'Reilly, Siobhan O'Dea, Colm Bergin, Aisling O'Leary
There is interest in introducing generic antiretroviral drugs (ARVs) into high-income countries in order to maximise efficiency in health care budgets. Studies examining patients' and providers' knowledge and attitudes to generic substitution in HIV are few. This was a cross-sectional, observational study with a convenience sample of adult HIV-infected patients and health care providers (HCPs). Data on demographics, knowledge of generic medicine and facilitators of generic substitution were collected. Descriptive and univariate analysis was performed using SPSS V...
January 1, 2017: International Journal of STD & AIDS
https://www.readbyqxmd.com/read/28631252/synthesis-and-characterization-of-novel-carboxymethyl-assam-bora-rice-starch-for-the-controlled-release-of-cationic-anticancer-drug-based-on-electrostatic-interactions
#7
Sharmistha Mohapatra, Anees Ahmad Siddiqui, Mohammed Anwar, Neha Bhardwaj, Sohail Akhter, Farhan Jalees Ahmad
Carboxymethyl Assam Bora rice starch (CM-ABRS) was chemically synthesized in non-aqueous medium with the optimum degree of substitution (DS) of 1.23, and physicochemically characterized by FT-IR, DSC, XRD, and SEM analysis. Comparative evaluation of CM-ABRS with native starch (ABRS) for powder flow characteristics, swelling index, apparent solubility, rheological properties, textural properties, and mucoadhesive studies were carried out. The aim of the current work was to investigate the potential of CM-ABRS as a novel carrier for the water-soluble chemotherapeutic, doxorubicin hydrochloride (DOX)...
June 19, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28629184/determination-of-structural-requirements-of-n-substituted-tetrahydro-%C3%AE-carboline-imidazolium-salt-derivatives-using-in-silico-approaches-for-designing-mek-1-inhibitors
#8
Jingwei Liang, Mingyang Wang, Xinyang Li, Xin He, Chong Cao, Fanhao Meng
Novel N-substituted tetrahydro-β-carboline imidazolium salt derivatives proved to have potent antitumor activity in past research. The Topomer CoMFA and CoMSIA function in Sybyl-X 2.0 software was applied for the identification of important features of N-substituted tetrahydro-β-carboline-imidazolium salt derivative moieties. In the case of Topomer CoMFA, all the compounds were split into two fragments which were used to generate a 3D invariant representation, the statistical results of the Topomer CoMFA model: q² value of 0...
June 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28629160/structural-characterization-of-a-rhamnogalacturonan-i-domain-from-ginseng-and-its-inhibitory-effect-on-galectin-3
#9
Huimin Shi, Li Yu, Yun Shi, Jiaojiao Lu, He Teng, Yifa Zhou, Lin Sun
A rhamnogalacturonan I domain, named RG-I-3A, was prepared from ginseng pectin by pectinase digestion and chromatography separation. Monosaccharide composition analysis revealed that it was mainly composed of galacturonic acid, rhamnose, galactose, and arabinose in a molar ratio of 32.5:11.2:31.9:16.5, with a molecular weight of 50 kDa. Partial acid hydrolysis, monoclonal antibody detection, and NMR spectra analysis suggested RG-I-3A was composed of →4)-α-GalpA-(1→2)-α-Rhap-(1→disaccharide repeating units as backbone, with β-1,4-galactan, α-1,5-arabinan, AG-I, and AG-II side chains substituted via the O-4 of Rhap...
June 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28629126/differentiated-thyroid-cancer-treatment-state-of-the-art
#10
REVIEW
Benedikt Schmidbauer, Karin Menhart, Dirk Hellwig, Jirka Grosse
Differentiated thyroid cancer (DTC) is a rare malignant disease, although its incidence has increased over the last few decades. It derives from follicular thyroid cells. Generally speaking, the prognosis is excellent. If treatment according to the current guidelines is given, cases of recurrence or persistence are rare. DTC requires special expertise by the treating physician. In recent years, new therapeutic options for these patients have become available. For this article we performed a systematic literature review with special focus on the guidelines of the American Thyroid Association, the European Association of Nuclear Medicine, and the German Society of Nuclear Medicine...
June 17, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28629083/effects-on-insulin-adsorption-due-to-zinc-and-strontium-substitution-in-hydroxyapatite
#11
Luisa A Scudeller, Elena Mavropoulos, Marcelo N Tanaka, Andrea M Costa, Carolina A C Braga, Elvis O López, Alexandre Mello, Alexandre M Rossi
Insulin-loaded calcium phosphate nanoparticles have been proposed as a potential drug delivery system for the oral treatment of diabetes and to stimulate bone cell proliferation and bone mineralization. The kinetics of insulin incorporation onto hydroxyapatite (HA) and Sr (SrHA)- and Zn (ZnHA)-substituted hydroxyapatite nanoparticles was investigated using X-ray photoelectron spectroscopy (XPS), Fourier transform infrared (FTIR) spectroscopy, zeta potential measurements and circular dichroism (CD) spectroscopy...
October 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28628926/synthesis-characterisation-molecular-docking-anti-microbial-and-anti-diabetic-screening-of-substituted-4-indolylphenyl-6-arylpyrimidine-2-imine-derivatives
#12
Veerasamy Ramya, Santhirakasu Vembu, Ganesan Ariharasivakumar, Manathusamy Gopalakrishnan
The purpose of the research is to synthesise a novel series of (E)-2-(4-(1H-indol-3-yl)-6-p-substituted phenylpyrimidin-2-yl)dimethylguanidine derivatives since 3-(1H-indol-3-yl)-1-p-substituted phenylprop-2-en-1-one and evaluate their molecular docking studies, antimicrobial, and anti-diabetic activities. Among all the synthesized compounds (11a-g), compound 11a exhibits excellent CDOCKER energy (-11.36 kcal/mol). The entire compounds (11a-g) confirm very good antimicrobial activity towards the tested microorganisms...
June 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28628897/diverted-medications-and-new-psychoactive-substances-a-chemical-network-analysis-of-discarded-injecting-paraphernalia-in-hungary
#13
Valéria Anna Gyarmathy, Anna Péterfi, Tamás Figeczki, József Kiss, Katalin Medgyesi-Frank, János Posta, József Csorba
BACKGROUND: Until about 2010, people who inject drugs (PWIDs) injected almost exclusively heroin and amphetamines in Hungary. After 2010, self-reported studies have indicated a dominance of new psychoactive substances on the drug market for injectable drugs. METHODS: Between March 2015 and February 2016, we collected used and discarded injecting paraphernalia. We utilized chemical analysis to assess and UCINet to visualize the connections between the most prevalent main substances and their respective co-occurring additional components at 7 locations in Hungary...
June 16, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/28628859/structural-and-functional-effects-of-nucleotide-variation-on-the-human-tb-drug-metabolizing-enzyme-arylamine-n-acetyltransferase-1
#14
Ruben Cloete, Wisdom A Akurugu, Cedric J Werely, Paul D van Helden, Alan Christoffels
The human arylamine N-acetyltransferase 1 (NAT1) enzyme plays a vital role in determining the duration of action of amine-containing drugs such as para-aminobenzoic acid (PABA) by influencing the balance between detoxification and metabolic activation of these drugs. Recently, four novel single nucleotide polymorphisms (SNPs) were identified within a South African mixed ancestry population. Modeling the effects of these SNPs within the structural protein was done to assess possible structure and function changes in the enzyme...
June 10, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28628737/analysis-of-structure-activity-relationships-based-on-the-hcv-sliib-ires-rna-targeting-gghyrfk-cu-complex
#15
Martin J Ross, Insiya Fidai, James Allan Cowan
New therapeutics for the targeting of the hepatitis C virus have been released in recent years. Although these therapies are less prone to resistance, they are still administered in cocktails as a combination of drugs targeting various aspects of the viral life cycle. Herein, we aim to contribute to an arsenal of new HCV therapeutics by targeting HCV internal ribosomal entry sequence (IRES) RNA via development of catalytic metallodrugs that function to degrade rather than inhibit the target molecule. Based on a previously characterized HCV IRES stem-loop IIb RNA-targeting metallopeptide Cu-GGHYrFK (1-Cu), an all L-analogue (3-Cu) and a series of additional complexes with single alanine substitutions in the targeting domain were prepared and screened to determine the influence each amino acid side-chain on RNA localization and recognition, and catalytic reactivity toward the RNA...
June 19, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28628684/megasessions-efficacy-of-fewer-longer-treatment-sessions-for-fat-reduction-in-noninvasive-body-contouring-using-a-radiofrequency-based-device
#16
Diane Duncan
<p>While the field of noninvasive body contouring is booming, many patients still note a lesser result than they might achieve with a single session of liposuction or dermolipectomy. The duration of a noninvasive fat reduction treatment series can be daunting. Patients have questioned the worth of these procedures when the expected benefit is modest and the time they devote to the project is significant. An eight-patient mini-study was performed to see if two or three "megasessions" could be substituted for eight weekly sessions of bipolar radiofrequency based fat reduction treatments...
May 1, 2017: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/28627264/utility-of-in-vitro-and-in-vivo-systems-for-studying-the-permeability-of-capsaicin-and-nonivamide-through-different-intestinal-regions
#17
Lian Duan, Huaidong Peng, Guangcan Li, Ruolun Wang, Yanfang Chen
1. The present study determined and compared the permeability of capsaicin and nonivamide along the length of the intestine in rats. Accordingly, to evaluate this synthetic analog as a clinical substitute for capsaicin. 2. Permeabilities of capsaicin and nonivamide were measured in experiments utilizing Ussing chambers and in vivo methods. Capsaicin concentrations were examined by Liquid chromatography tandem mass spectrometry (LC-MS/MS). 3. Both capsaicin (0.80 × 10(-6) cm/s) and nonivamide (0.22 × 10(-6) cm/s, P > 0...
June 19, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28626531/saccharin-aza-bioisosteres-synthesis-and-preclinical-property-comparisons
#18
Yantao Chen, Carl-Johan Aurell, Anna Pettersen, Richard J Lewis, Martin A Hayes, Matti Lepistö, Anna C Jonson, Hanna Leek, Linda Thunberg
Saccharin is a well-known scaffold in drug discovery. Herein, we report the synthesis and preclinical property comparisons of three bioisosteres of saccharin: aza-pseudosaccharins (cluster B), and two new types of aza-saccharins (clusters C and D). We demonstrate a convenient protocol to selectively synthesize products in cluster C or D when primary amines are used. Preclinical characterization of selected matched-pair products is reported. Through comparison of two diastereomers, we highlight how stereochemistry affects the preclinical properties...
June 8, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28626267/a-facile-semi-synthetic-approach-towards-halogen-substituted-aminobenzoic-acid-analogues-of-platensimycin
#19
Lin Qiu, Kai Tian, Jian Pan, Lin Jiang, Hu Yang, Xiangcheng Zhu, Ben Shen, Yanwen Duan, Yong Huang
Platensimycin (PTM), produced by several strains of Streptomyces platensis, is a promising drug lead for infectious diseases and diabetes. The recent pilot-scale production of PTM from S. platensis SB12026 has set the stage for the facile semi-synthesis of a focused library of PTM analogues. In this study, gram-quantity of platensic acid (PTMA) was prepared by the sulfuric acid-catalyzed ethanolysis of PTM, followed by a mild hydrolysis in aqueous lithium hydroxide. Three PTMA esters were also obtained in near quantitative yields in a single step, suggesting a facile route to make PTMA aliphatic esters...
February 9, 2017: Tetrahedron
https://www.readbyqxmd.com/read/28625684/brand-medications-and-medicare-part-d-how-eye-care-providers-prescribing-patterns-influence-costs
#20
Paula Anne Newman-Casey, Maria A Woodward, Leslie M Niziol, Paul P Lee, Lindsey B De Lott
PURPOSE: To quantify costs of eye care providers' Medicare Part D prescribing patterns for ophthalmic medications and to estimate the potential savings of generic or therapeutic drug substitutions and price negotiation. DESIGN: Retrospective cross-sectional study. PARTICIPANTS: Eye care providers prescribing medications through Medicare Part D in 2013. METHODS: Medicare Part D 2013 prescriber public use file and summary file were used to calculate medication costs by physician specialty and drug...
June 16, 2017: Ophthalmology
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