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https://www.readbyqxmd.com/read/28229517/affinity-capillary-electrophoresis-and-fluorescence-spectroscopy-for-studying-enantioselective-interactions-between-omeprazole-enantiomer-and-human-serum-albumin
#1
Yujing Xu, Tingting Hong, Xueping Chen, Yibing Ji
Baseline separation of omeprazole (OME) enantiomers was achieved by affinity capillary electrophoresis (ACE), using human serum albumin (HSA) as the chiral selector. The influence of several experimental variables such as HSA concentration, the type and content of organic modifiers, applied voltage and running buffer concentration on the separation was evaluated. The binding of esomeprazole (S-omeprazole, S-OME) and its R-enantiomer (R-omeprazole, R-OME) to HSA under simulated physiological conditions was studied by ACE and fluorescence spectroscopy which was considered as a reference method...
February 23, 2017: Electrophoresis
https://www.readbyqxmd.com/read/28229374/effect-of-short-term-fasting-on-systemic-cytochrome-p450-mediated-drug-metabolism-in-healthy-subjects-a-randomized-controlled-crossover-study-using-a-cocktail-approach
#2
Laureen A Lammers, Roos Achterbergh, Ron H N van Schaik, Johannes A Romijn, Ron A A Mathôt
BACKGROUND AND OBJECTIVE: Short-term fasting can alter drug exposure but it is unknown whether this is an effect of altered oral bioavailability and/or systemic clearance. Therefore, the aim of our study was to assess the effect of short-term fasting on oral bioavailability and systemic clearance of different drugs. METHODS: In a randomized, controlled, crossover trial, 12 healthy subjects received a single administration of a cytochrome P450 (CYP) probe cocktail, consisting of caffeine (CYP1A2), metoprolol (CYP2D6), midazolam (CYP3A4), omeprazole (CYP2C19) and warfarin (CYP2C9), on four occasions: an oral (1) and intravenous (2) administration after an overnight fast (control) and an oral (3) and intravenous (4) administration after 36 h of fasting...
February 22, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28215634/isolation-and-expansion-of-human-pluripotent-stem-cell-derived-hepatic-progenitor-cells-by-growth-factor-defined-serum-free-culture-conditions
#3
Takayuki Fukuda, Kazuo Takayama, Mitsuhi Hirata, Yu-Jung Liu, Kana Yanagihara, Mika Suga, Hiroyuki Mizuguchi, Miho K Furue
Limited growth potential, narrow ranges of sources, and difference in variability and functions from batch to batch of primary hepatocytes cause a problem for predicting drug-induced hepatotoxicity during drug development. Human pluripotent stem cell (hPSC)-derived hepatocyte-like cells in vitro are expected as a tool for predicting drug-induced hepatotoxicity. Several studies have already reported efficient methods for differentiating hPSCs into hepatocyte-like cells, however its differentiation process is time-consuming, labor-intensive, cost-intensive, and unstable...
February 16, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28215170/derivatives-of-6-nitrobenzimidazole-inhibit-fructose-mediated-protein-glycation-and-intracellular-reactive-oxygen-species-production
#4
Humera Jahan, Muhammad Iqbal Choudhary, Zarbad Shah, Khalid M Khan, Atta-Ur-Rahman
BACKGROUND: Benzimidazoles are important pharmacophores in drug discovery. Several of them are currently used drugs, such as flubendazole, omeprazole, and astemizole for the treatment of anthelmintic, antiulcerative, and antihistaminic diseases, respectively. OBJECTIVES: The aim of the current study was to study the antiglycation activity of nitrobenzimidazole derivatives against fructose-mediated human serum albumin (HSA) glycation. The study was also aimed to investigate effects of newly identified antiglycation inhibitors on AGEs-induced intracellular reactive oxygen species production, and associated impaired proliferation of the hepatocytes...
February 16, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28209602/a-novel-murine-model-of-esophageal-non-erosive-reflux-disease-nerd-from-inflammation-to-impairment-in-mucosal-integrity
#5
Renan O Silva, Francisco Fábio B Oliveira, Rudy D Bingana, Mailton O Arruda, Philip Woodland, Chung Lee, Miguel A Nobre E Souza, Pedro Marcos G Soares, Armenio A Santos, Daniel Sifrim, Marcellus H L P Souza
Non-erosive reflux disease (NERD) is a highly prevalent phenotype of the gastroesophageal reflux disease (GERD). In this study, we developed a novel murine model of NERD in mice with microscopic inflammation and impairment in the epithelial esophageal barrier. Female Swiss mice were subjected to the following surgical procedure: the transitional region between the forestomach and the glandular portion of the stomach was ligated, and a nontoxic ring was placed around the duodenum near the pylorus. The control group underwent sham surgery...
February 16, 2017: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/28207542/rifampicin-induced-disseminated-intravascular-coagulation-in-pulmonary-tuberculosis-treatment-a-case-report-and-literature-review
#6
Guo Chen, Jian-Qing He
RATIONALE: Disseminated intravascular coagulation (DIC) induced by daily rifampicin therapy is rare, especially the patient is absent of malignancy, severe infection, and prior exposure to rifampicin. PATIENT CONCERNS: We report a case of DIC induced by daily rifampicin treatment for pulmonary tuberculosis. A 22-year-old, previously healthy man received an anti-tuberculosis therapy consisting of isoniazid, rifampicin, ethambutol, and pyrazinamide on the daily dose recommended by the World Health Organization tuberculosis guidelines after a diagnosis of pulmonary tuberculosis...
February 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28207313/continuous-radiotelemetric-monitoring-of-intragastric-ph-in-a-dog-with-peptic-ulceration
#7
Michael B Lane, Jeanne C Larson, Jennifer E Stokes, M Katherine Tolbert
CASE DESCRIPTION A 6-year-old castrated male Boxer was evaluated for a 5-week history of frequent vomiting, melena, and signs of abdominal pain following accidental ingestion of 5 to ten 15-mg meloxicam tablets (approx ingested dose, 3.1 to 6.2 mg/kg [1.4 to 2.8 mg/lb]). CLINICAL FINDINGS Clinical signs persisted despite 3 weeks of treatment with sucralfate (41.8 mg/kg [19 mg/lb], PO, q 8 h) and omeprazole (0.8 mg/kg [0.36 mg/lb], PO, q 24 h). Results of a CBC and serum biochemical analysis were unremarkable...
March 1, 2017: Journal of the American Veterinary Medical Association
https://www.readbyqxmd.com/read/28201961/development-and-characterization-pulsatile-microspheres-of-nifedipine-for-hypertension
#8
Rahul Taneja, Ghanshyam Das Gupta
AIM AND BACKGROUND: To develop pulsatile microspheres of Nifedipine blend of polymers Carbopol 971P and Eudragit RS100 for antihypertensive to release the drug at a particular lag time. METHODS: Pulsatile nifedipine microspheres were prepared using blend of Carbopol 971P and Eudragit RS100 at different ratio in a mixture of solvents. Formulations were prepared and optimized on the basis of particle size, percentage yield and drug entrapment efficiency. Optimized formulations were further analyzed at different resolutions per minute (rpm) by optical microscopy, scanning electron microscopy (SEM), in-vitro dissolution studies and kinetics model...
February 12, 2017: Recent Patents on Drug Delivery & Formulation
https://www.readbyqxmd.com/read/28197557/doubly-charged-trimeric-cluster-ions-effective-in-mutual-chiral-recognition-of-tadalafil-and-three-proton-pump-inhibitors
#9
Lu Wang, Yunfeng Chai, Wenquan Zhu, Yuanjiang Pan, Cuirong Sun, Su Zeng
Mutual chiral recognition of four stereoisomers of tadalafil and three pairs of enantiomers of proton pump inhibitors (PPIs) including pantoprazole, lansoprazole, and omeprazole, as well as quantitative analysis of enantiomeric excess is achieved on the basis of the competitive fragmentation of doubly charged trimeric Ni(II) cluster ions. Compared with a singly charged trimeric cluster ion, a doubly charged trimeric cluster ion was proved efficient in the recognition of chiral drugs with one or multiple chiral centers, due to its rich fragmentation ions...
February 15, 2017: Analyst
https://www.readbyqxmd.com/read/28182955/application-of-nickel-zinc-ferrite-graphene-nanocomposite-as-a-modifier-for-fabrication-of-a-sensitive-electrochemical-sensor-for-determination-of-omeprazole-in-real-samples
#10
Abbas Afkhami, Atousa Bahiraei, Tayyebeh Madrakian
In the present study, a simple and highly sensitive sensor for the determination of omeprazole based on nickel-zinc ferrite/graphene modified glassy carbon electrode is reported. The morphology and electro analytical performance of the fabricated sensor were characterized with X-ray diffraction spectrometry, Fourier transform infrared spectrometry, scanning electron microscopy, electrochemical impedance spectroscopy, cyclic voltammetry, differential pulse voltammetry and operation of the sensor. Results were compared with those achieved at the graphene modified glassy carbon electrode and bare glassy carbon electrode...
February 2, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28179883/new-microrna-biomarkers-for-drug-induced-steatosis-and-their-potential-to-predict-the-contribution-of-drugs-to-non-alcoholic-fatty-liver-disease
#11
Mireia López-Riera, Isabel Conde, Laia Tolosa, Ángela Zaragoza, José V Castell, María J Gómez-Lechón, Ramiro Jover
Background and Aims: Drug-induced steatosis is a major reason for drug failure in clinical trials and post-marketing withdrawal; and therefore, predictive biomarkers are essential. These could be particularly relevant in non-alcoholic fatty liver disease (NAFLD), where most patients show features of the metabolic syndrome and are prescribed with combined chronic therapies, which can contribute to fatty liver. However, specific biomarkers to assess the contribution of drugs to NAFLD are lacking. We aimed to find microRNAs (miRNAs) responsive to steatotic drugs and to investigate if they could become circulating biomarkers for drug-induced steatosis...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28177671/the-effect-of-short-term-oral-treatment-with-omeprazole-or-pantoprazole-on-the-function-of-polymorphonuclear-neutrophils
#12
Maja Kostrzewska, Marzena Garley, Wioletta Ratajczak, Ewa Jablonska, Jacek Jamiołkowski, Andrzej Dabrowski
Recent studies report an increased risk of enteric infections in patients treated with proton pump inhibitors (PPIs). Polymorphonuclear neutrophils (PMNs) play a key role in host response to bacterial infection. We have evaluated the effect of omeprazole and pantoprazole treatment on the PMNs function. Fifteen patients were treated with omeprazole 20 mg daily and 15 patients with pantoprazole 40 mg daily for 7 days. Treatment with omeprazole or pantoprazole had no effect on spontaneous nitroblue tetrazolium (NBT) test results...
January 22, 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28159657/dose-optimisation-of-voriconazole-with-therapeutic-drug-monitoring-in-children-a-single-centre-experience-in-china
#13
Liang Liu, Xing Zhou, Tingting Wu, Hongliang Jiang, Sitao Yang, Yang Zhang
The pharmacokinetic profile of voriconazole is highly variable, rendering inconsistent and/or inadequate dosing, especially in children <2 years old. A retrospective analysis was performed in children receiving voriconazole with at least one plasma trough level (Ctrough) monitored. Statistical analyses were performed to examine the dose-exposure relationship as well as other factors potentially affecting voriconazole Ctrough in children of different ages. A total of 107 paediatric patients were included, of whom 75 were <2 years old...
January 31, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28159656/influence-of-different-proton-pump-inhibitors-on-the-pharmacokinetics-of-voriconazole
#14
Fang Qi, Liqin Zhu, Na Li, Tingyue Ge, Gaoqi Xu, Shasha Liao
This study aimed to determine the influence of proton pump inhibitors (PPIs) on the pharmacokinetics of voriconazole and to characterise potential drug-drug interactions (DDIs) between voriconazole and various PPIs (omeprazole, esomeprazole, lansoprazole and rabeprazole). Using adjusted physicochemical data and the pharmacokinetic (PK) parameters of voriconazole and PPIs, physiologically based pharmacokinetic (PBPK) models were built and were verified in healthy subjects using GastroPlus(TM) to predict the plasma concentration-time profiles of voriconazole and PPIs...
January 31, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28155129/drug-interaction-potential-of-osilodrostat-lci699-based-on-its-effect-on-the-pharmacokinetics-of-probe-drugs-of-cytochrome-p450-enzymes-in-healthy-adults
#15
Sara Armani, Lillian Ting, Nicholas Sauter, Christelle Darstein, Anadya Prakash Tripathi, Lai Wang, Bing Zhu, Helen Gu, Dung Yu Chun, Heidi J Einolf, Swarupa Kulkarni
BACKGROUND AND OBJECTIVES: Osilodrostat (LCI699) is an adrenal steroidogenesis inhibitor currently in late-phase clinical development as a potential treatment for Cushing's disease. This study evaluated the inhibitory effect of osilodrostat on the pharmacokinetics of probe substrates of the cytochrome P450 (CYP) enzymes CYP1A2, CYP2C19, CYP2D6, and CYP3A4. METHODS: Healthy adult volunteers received single-dose cocktail probe substrates [caffeine (100 mg), omeprazole (20 mg), dextromethorphan (30 mg), and midazolam (2 mg)] followed by a 6-day washout...
February 2, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/28145783/the-budget-impact-of-using-enteric-coated-aspirin-325mg-immediate-release-omeprazole-40mg-to-prevent-recurrent-cardiovascular-events
#16
Wenjie Zhang, Yi Han, John G Fort, David Schofield, James P Tursi
OBJECTIVE: Aspirin (acetylsalicylic acid; ASA) is commonly used for secondary prevention of cardiovascular (CV) events but may be associated with gastrointestinal (GI) adverse events, which can reduce adherence. Use of ASA co-therapy with proton pump inhibitors in patients at risk may be suboptimal. PA32540 (Yosprala(TM)) is a coordinated-delivery tablet combining EC-ASA 325 mg and immediate-release omeprazole 40 mg. The objective of this flexible budget impact model was to project the financial consequences of introducing PA32540 325 mg/40 mg to prevent recurrent CV events while reducing ASA-associated GI events in US adults...
February 1, 2017: Journal of Medical Economics
https://www.readbyqxmd.com/read/28128088/gestational-pityriasis-rosea-suggestions-for-approaching-affected-pregnant-women
#17
Alexandra Monastirli, Efstathia Pasmatzi, George Badavanis, Dionysios Tsambaos
Dear Editor, Pityriasis rosea is a common, acute, and self-limiting dermatosis, which is associated with the endogenous systemic reactivation of human herpesvirus (HHV)-6 and/or HHV-7 (1). It predominantly affects individuals of both sexes in their second or third decade of life and is clinically characterized by the occurrence of an initial erythematosquamous plaque followed by the appearance of disseminated similar but smaller lesions one or two weeks later. Several patients develop systemic symptoms such as nausea, anorexia, malaise, headache, fever, arthralgia, and lymphadenopathy that may precede or accompany the eruption; the latter follows the cleavage lines of the trunk creating the configuration of a Christmas tree and spontaneously resolves within 4 to 8 weeks...
December 2016: Acta Dermatovenerologica Croatica: ADC
https://www.readbyqxmd.com/read/28125857/new-bismuth-containing-quadruple-therapy-in-patients-infected-with-helicobacter-pylori-a-first-italian-experience-in-clinical-practice
#18
Antonio Tursi, Francesco Di Mario, Marilisa Franceschi, Rudi De Bastiani, Walter Elisei, Gianluca Baldassarre, Antonio Ferronato, Simone Grillo, Stefano Landi, Maria Zamparella, Manuela De Polo, Laura Boscariolo, Marcello Picchio
BACKGROUND: Rising antibiotic resistance requires the evaluation of new and effective therapies. AIMS: To test the efficacy and safety of the new bismuth-containing quadruple therapy in patients infected with Helicobacter pylori. MATERIAL AND METHODS: Consecutive H. pylori-positive dyspeptic patients were enrolled, either naïve or with previous failure treatment. Patients were treated with Pylera(®) (three-in-one capsules containing bismuth subcitrate potassium 140 mg, metronidazole 125 mg, and tetracycline 125 mg) three capsules q...
January 26, 2017: Helicobacter
https://www.readbyqxmd.com/read/28118652/yosprala-a-combination-of-aspirin-and-omeprazole
#19
REVIEW
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No abstract text is available yet for this article.
January 30, 2017: Medical Letter on Drugs and Therapeutics
https://www.readbyqxmd.com/read/28117490/the-effects-of-dose-and-diet-on-the-pharmacodynamics-of-esomeprazole-in-the-horse
#20
B W Sykes, C Underwood, P C Mills
BACKGROUND: Esomeprazole warrants further investigation as a treatment for Equine Gastric Ulcer Syndrome. OBJECTIVES: To investigate the duration of intra-day acid suppression achieved with two doses of esomeprazole under two dietary conditions. STUDY DESIGN: A 4-way cross-over design. METHODS: Six adult Thoroughbreds instrumented with percutaneous gastrotomy tubes were used. Intra-gastric pH was measured for continuous 23 hour periods (8...
January 24, 2017: Equine Veterinary Journal
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