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Esomeprazole

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https://www.readbyqxmd.com/read/27875488/esomeprazole-fda-approval-in-children-with-gerd-exposure-matching-and-exposure-response
#1
Justin C Earp, Nitin Mehrotra, Kristina E Peters, Robert P Fiorentino, Donna Griebel, Sue Chih Lee, Andrew Mulberg, Kerstin Röhss, Marie Sandström, Amy Taylor, Christoffer W Tornøe, Erica L Wynn, Jan-Stefan Van der Walt, Christine Garnett
OBJECTIVES: FDA approval of proton-pump inhibitors for infantile GERD has been limited by intra-patient variability in the clinical assessment of GERD. For children 1-17 years old, extrapolating efficacy from adults for IV esomeprazole was accepted. The oral formulation was previously approved in children. Exposure-response and exposure matching analyses were sought to identify approvable pediatric doses. METHODS: Intragastric pH biomarker comparisons between children and adults were conducted...
November 19, 2016: Journal of Pediatric Gastroenterology and Nutrition
https://www.readbyqxmd.com/read/27862093/bioanalytical-method-for-the-estimation-of-co-administered-esomeprazole-leflunomide-and-ibuprofen-in-human-plasma-and-in-pharmaceutical-dosage-forms-using-micellar-liquid-chromatography
#2
Wael Talaat
The present study represents a connection between basic science and clinical applied science through providing a bioanalytical method for the analysis of certain co-administered drugs used for the treatment of rheumatoid arthritis. The studied drugs are esomeprazole, leflunomide and ibuprofen. The proposed bioanalytical method is a simple reversed phase high performance liquid chromatographic method using micellar mobile phase. The method is conducted using a Shim-pack VP-ODS (150 mm × 4.6 mm ID) stainless steel column at ambient temperature with ultraviolet detection at 285 nm...
October 13, 2016: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/27802417/blood-pressure-lowering-effect-of-orally-ingested-nitrite-is-abolished-by-a-proton-pump-inhibitor
#3
Marcelo F Montenegro, Michaela L Sundqvist, Filip J Larsen, Zhengbing Zhuge, Mattias Carlström, Eddie Weitzberg, Jon O Lundberg
Inorganic nitrate and nitrite from dietary and endogenous sources are metabolized to NO and other bioactive nitrogen oxides that affect blood pressure. The mechanisms for nitrite bioactivation are unclear, but recent studies in rodents suggest that gastric acidity may influence the systemic effects of this anion. In a randomized, double-blind, placebo-controlled crossover study, we tested the effects of a proton pump inhibitor on the acute cardiovascular effects of nitrite. Fifteen healthy nonsmoking, normotensive subjects, aged 19 to 39 years, were pretreated with placebo or esomeprazole (3×40 mg) before ingesting sodium nitrite (0...
October 31, 2016: Hypertension
https://www.readbyqxmd.com/read/27801778/antiviral-screening-of-multiple-compounds-against-ebola-virus
#4
Stuart D Dowall, Kevin Bewley, Robert J Watson, Seshadri S Vasan, Chandradhish Ghosh, Mohini M Konai, Gro Gausdal, James B Lorens, Jason Long, Wendy Barclay, Isabel Garcia-Dorival, Julian Hiscox, Andrew Bosworth, Irene Taylor, Linda Easterbrook, James Pitman, Sian Summers, Jenny Chan-Pensley, Simon Funnell, Julia Vipond, Sue Charlton, Jayanta Haldar, Roger Hewson, Miles W Carroll
In light of the recent outbreak of Ebola virus (EBOV) disease in West Africa, there have been renewed efforts to search for effective antiviral countermeasures. A range of compounds currently available with broad antimicrobial activity have been tested for activity against EBOV. Using live EBOV, eighteen candidate compounds were screened for antiviral activity in vitro. The compounds were selected on a rational basis because their mechanisms of action suggested that they had the potential to disrupt EBOV entry, replication or exit from cells or because they had displayed some antiviral activity against EBOV in previous tests...
October 27, 2016: Viruses
https://www.readbyqxmd.com/read/27796466/randomised-trial-of-the-effect-of-a-gastrin-cck2-receptor-antagonist-on-esomeprazole-induced-hypergastrinaemia-evidence-against-rebound-hyperacidity
#5
Malcolm Boyce, Frans van den Berg, Toni Mitchell, Kate Darwin, Steve Warrington
PURPOSE: Hypergastrinaemia induced by proton pump inhibitor (PPI) therapy may cause ECL-cell and parietal-cell hyperplasia and rebound hyperacidity and dyspepsia after PPI withdrawal. The aim of the study was to assess the effect of different dosage-regimens of netazepide, a gastrin/CCK2 receptor antagonist, on PPI-induced hypergastrinaemia and elevated chromogranin A (CgA). METHODS: Six groups of eight healthy subjects participated in a randomised, double-blind study of esomeprazole 40 mg daily for 28 days, in combination with netazepide 1, 5 or 25 mg or placebo, daily, during the last 14 days of esomeprazole or during 14 days after treatment withdrawal...
October 29, 2016: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27782887/comparison-of-the-effects-of-esomeprazole-40-mg-rabeprazole-20-mg-lansoprazole-30-mg-and-pantoprazole-40-mg-on-intragastr%C3%A4-c-ph-in-extensive-metabolizer-patients-with-gastroesophageal-reflux-disease
#6
Altay Çelebi, Dinçer Aydın, Orhan Kocaman, Buğra Tolga Konduk, Ömer Şentürk, Sadetin Hülagü
BACKGROUND/AIMS: Studies on the therapeutic efficacy of proton pump inhibitors (PPIs) in patients with gastroesophageal reflux disease (GERD) have been recently published. In most of these studies, comparison of only two PPIs have been made. There are few studies on the comparison of four or more PPIs. We aimed to compare the acid inhibitory effects of esomeprazole 40 mg, rabeprazole 20 mg, lansoprazole 30 mg, and pantoprazole 40 mg on days 1 and 5 of treatment in patients with GERD, who were extensive metabolizers in regard to the CYP2C19 genotype...
September 2016: Turkish Journal of Gastroenterology: the Official Journal of Turkish Society of Gastroenterology
https://www.readbyqxmd.com/read/27771990/spectroscopic-and-molecular-modeling-approaches-to-investigate-the-binding-of-proton-pump-inhibitors-to-human-serum-albumin
#7
Suma K Pawar, Reeta Punith, Roopa S Naik, J Seetharamappa
The interaction between two proton pump inhibitors viz., omeprazole (OME) and esomeprazole (EPZ) with human serum albumin (HSA) was studied by fluorescence, absorption, circular dichroism (CD), fourier transform infrared spectroscopy (FT-IR), voltammetry and molecular modeling approaches. The Stern-Volmer quenching constants (Ksv) for OME-HSA and EPZ-HSA systems obtained at different temperatures revealed that both OME and EPZ quenched the intensity of HSA through dynamic mode of quenching mechanism. The binding constants of OME-HSA and EPZ-HSA increased with temperature, indicating the increased stability of these systems at higher temperatures...
October 24, 2016: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/27734291/clinical-pharmacokinetics-and-pharmacodynamics-of-cabozantinib
#8
Steven A Lacy, Dale R Miles, Linh T Nguyen
Cabozantinib inhibits receptor tyrosine kinases involved in tumor angiogenesis and metastasis. The capsule formulation (Cometriq(®)) is approved for the treatment of progressive metastatic medullary thyroid cancer at a 140-mg free base equivalent dose. The tablet formulation (Cabometyx™, 60-mg free base equivalent dose) is approved for the treatment of renal cell carcinoma following anti-angiogenic therapy. Cabozantinib displays a long terminal plasma half-life (~120 h) and accumulates ~fivefold by day 15 following daily dosing based on area under the plasma concentration-time curve (AUC)...
October 12, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/27733667/association-between-proton-pump-inhibitors-and-microscopic-colitis-implications-for-practice-and-future-research
#9
Ernest H Law, Melissa Badowski, Yu-Ting Hung, Kimberly Weems, Angelica Sanchez, Todd A Lee
OBJECTIVE: Microscopic colitis (MC) is a chronic inflammatory disease of the colon that is characterized by chronic, watery, nonbloody diarrhea. Concern regarding a potential association between proton-pump inhibitors (PPIs) and MC has recently emerged. We sought to systematically review and summarize the evidence for the potential association between PPIs and MC. DATA SOURCES: We systematically searched EMBASE, MEDLINE, Cochrane Database of Systematic Reviews, International Pharmaceutical Abstracts, and Google Scholar using the terms proton-pump inhibitors (omeprazole, lansoprazole, dexlansoprazole, rabeprazole, pantoprazole, or esomeprazole), microscopic colitis, collagenous colitis, and lymphocytic colitis STUDY SELECTION: Full-text, English-language reports of case reports/series, observational studies, experimental studies, and systematic reviews/meta-analyses published between January 2000 to August 2016 were included...
October 12, 2016: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/27698544/esomeprazole-or-rabeprazole-based-triple-therapy-eradicated-helicobacter-pylori-comparably-regardless-of-clarithromycin-susceptibility-and-cyp2c19-genotypes
#10
Tadayoshi Okimoto, Kazuhiro Mizukami, Ryo Ogawa, Kazuhisa Okamoto, Mitsutaka Shuto, Kensuke Fukuda, Masaaki Kodama, Kazunari Murakami
The aim of this study was to assess the efficacy of esomeprazole-based triple therapy compared with rabeprazole-based triple therapy according to CYP2C19 genotype and clarithromycin susceptibility status for first-line eradication therapy of Helicobacter pylori (H. pylori) in Japan. We enrolled 219 H. pylori-infected patients, and randomly allocated patients to the EAC group (esomeprazole 20 mg, clarithromycin 200 mg, amoxicillin 750 mg for one week, with all drugs given twice daily) or RAC group (rabeprazole 10 mg, clarithromycin 200 mg, amoxicillin 750 mg for one week, with all drugs given twice daily)...
September 2016: Journal of Clinical Biochemistry and Nutrition
https://www.readbyqxmd.com/read/27676074/selective-deuteration-of-pyridylmethyl-sulfinyl-benzimidazole-antisecretory-drugs-a-nmr-study-where-dmso-d6-acts-as-deuteration-agent
#11
Jordi Redondo, Carlos Jaime, Albert Marqués
The use of deuterated drug bioisosteres to obtain superior pharmacokinetic properties or to investigate biotransformations at the molecular level is a growing field of pharmaceutical research. This work presents a NMR study on the deuteration of three structurally related antisecretory proton-pump inhibitors, the sodium salts of esomeprazole, 1, pantoprazole, 2, and rabeprazole, 3. It has been found that the methylene adjacent to the sulfinyl group displays stereoselective deuteration when the sodium salts of these products are dissolved at room temperature in D2O or CD3OD, a process that also occurs very efficiently in DMSO-d6 (a solvent considered non-deuterating) if a catalytic amount of NaOH is added...
November 30, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27669706/proton-pump-inhibition-enhances-the-cytotoxicity-of-paclitaxel-in-cervical-cancer
#12
Taejong Song, Hye-Kyung Jeon, Ji Eun Hong, Jung-Joo Choi, Tae-Joong Kim, Chel Hun Choi, Duk-Soo Bae, Byoung-Gie Kim, Jeong-Won Lee
Purpose: This study was conducted to investigate whether a proton pump inhibitor (PPI) could enhance chemosensitivity via the inhibition of vacuolar-type H+ ATPase (V-ATPase) in cervical cancer. Materials and Methods: The expression of V-ATPase was evaluated in 351 formalin-fixed, paraffin-embedded human cervical cancer tissues using immunohistochemistry and compared with clinicopathologic risk factors for disease prognosis. The influence of cell proliferation and apoptosis following V-ATPase siRNA transfection or esomeprazole pretreatment was assessed in cervical cancer cell lines using MTT and ELSIA assay, respectively...
September 27, 2016: Cancer Research and Treatment: Official Journal of Korean Cancer Association
https://www.readbyqxmd.com/read/27648103/effects-of-transcutaneous-electrical-acustimulation-on-refractory-gastroesophageal-reflux-disease
#13
Li-Na Meng, Shanshan Chen, Jiande D Z Chen, Hai-Feng Jin, Bin Lu
Objective. To investigate effects and possible mechanisms of transcutaneous electrical acustimulation (TEA) performed by a wearable watch-size stimulator for refractory gastroesophageal reflux disease (RGERD). Methods. Twenty patients diagnosed as RGERD were enrolled in the study and randomly divided into four groups: esomeprazole group (Group A), esomeprazole combined with TEA group (Group B), esomeprazole combined with sham-TEA group (Group C), and esomeprazole combined with domperidone group (Group D). HRM and 24 h pH-impedance monitoring and GerdQ score were used to measure related indexes before and after treatment...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/27628008/proton-pump-inhibitors-in-cardiovascular-disease-drug-interactions-with-antiplatelet-drugs
#14
Morten Würtz, Erik L Grove
Aspirin and P2Y12 receptor antagonists are widely used across the spectrum of cardiovascular diseases. Upper gastrointestinal complications, including ulcer and bleeding, are relatively common during antiplatelet treatment and, therefore, concomitant proton pump inhibitor (PPI) treatment is often prescribed.PPIs provide gastroprotection by changing the intragastric milieu, essentially by raising intragastric pH. In recent years, it has been heavily discussed whether PPIs may reduce the cardiovascular protection by aspirin and, even more so, clopidogrel...
September 15, 2016: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/27610149/development-of-ph-sensitive-nanoparticles-for-intestinal-drug-delivery-using-chemically-modified-guar-gum-co-polymer
#15
Vegesna Naga Sravan Kumar Varma, Hosakote Gurumalappa Shivakumar, Veerna Balamuralidhara, Manne Navya, Umme Hani
The aim of the research work was to chemically modify guargum (GG) as a pH sensitive co-polymer and formulating intestinal targeting ESO nanoparticles (NPs) using the synthesized co-polymer. Poly acrylamide-grafted-guar gum (PAAm-g-GG) co-polymer was synthesized by free radical polymerization. Chemical modification of PAAm-g-GG by alkaline hydrolysis results in formation of a pH-sensitive co-polymer. The effect of GG and acryl amide (AAm) on grafting was studied. Esomeprazole magnesium (ESO) loaded pH sensitive NPs were prepared by nano-emulsification polymer crosslinking method and characterized...
2016: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/27605258/a-randomized-double-blind-active-controlled-multi-center-study-of-ilaprazole-in-the-treatment-of-reflux-esophagitis
#16
Yan Xue, Xianghong Qin, Liya Zhou, Sanren Lin, Ling Wang, Haitang Hu, Jielai Xia
BACKGROUND AND OBJECTIVE: Proton pump inhibitors (PPIs) are the main drugs for the treatment of reflux esophagitis. Previous studies have indicated ilaprazole to be safer and more effective in treating duodenal ulcers as compared with omeprazole. Being a novel PPI, ilaprazole may be used in the treatment of reflux esophagitis. The purpose of this study was to evaluate the safety and efficacy of ilaprazole tablets in the treatment of reflux esophagitis. METHODS: This study used a randomized, double-blind, multi-center, active-comparison design...
September 7, 2016: Clinical Drug Investigation
https://www.readbyqxmd.com/read/27590563/efficacy-of-triple-therapy-with-esomeprazole-amoxicillin-and-sitafloxacin-as-a-third-line-helicobacter-pylori-eradication-regimen
#17
Yoshihiro Hirata, Takako Serizawa, Satoki Shichijo, Nobumi Suzuki, Kosuke Sakitani, Yoku Hayakawa, Atsuo Yamada, Kazuhiko Koike
OBJECTIVE: To examine the efficacy of third-line Helicobacter pylori eradication therapy with esomeprazole, amoxicillin, and sitafloxacin for patients with clarithromycin- and metronidazole-based first- and second-line therapy failure. METHODS: Thirty patients with first- and second-line H. pylori eradication failure were treated prospectively with esomeprazole 20mg twice daily, amoxicillin 750mg twice daily, and sitafloxacin 100mg twice daily for 7 days. After 8-12 weeks, the outcome of eradication therapy was assessed by (13)C-urea breath test or stool antigen test...
August 30, 2016: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/27574989/esomeprazole-immediate-release-tablets-gastric-mucosa-ex-vivo-permeation-absorption-and-antisecretory-activity-in-conscious-rats
#18
Camillo Benetti, Lisa Flammini, Valentina Vivo, Paolo Colombo, Gaia Colombo, Lisa Elviri, Carmelo Scarpignato, Francesca Buttini, Ruggero Bettini, Elisabetta Barocelli, Alessandra Rossi
The aim of this work was to study the esomeprazole activity on the control of gastric secretion after administration of a novel immediate release tablet. The ex vivo permeation of esomeprazole across porcine gastric mucosa from immediate release tablets, containing sodium carbonate or magnesium oxide as alkalinizing agents, was firstly assessed. Pharmacokinetics and pharmacodynamics studies in conscious rats following the administration of immediate release tablets with sodium carbonate, in comparison with delayed-release tablets having the same formula, were also conducted...
October 10, 2016: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/27545320/effect-of-food-and-esomeprazole-on-the-pharmacokinetics-of-alectinib-a-highly-selective-alk-inhibitor-in-healthy-subjects
#19
Peter N Morcos, Elena Guerini, Neil Parrott, Georgina Dall, Steven Blotner, Katrijn Bogman, Carolina Sturm, Bogdana Balas, Meret Martin-Facklam, Alex Phipps
Alectinib, an anaplastic lymphoma kinase (ALK) inhibitor, is approved for treatment of patients with ALK+ non-small-cell lung cancer who have progressed on, or are intolerant to, crizotinib. This study assessed the effect of a high-fat meal and the proton pump inhibitor, esomeprazole, on the pharmacokinetics (PK) of alectinib. This was an open-label, 2-group study in healthy subjects. In Group 1 (n = 18), subjects were randomly assigned to a 2-treatment (A: fasted conditions, B: following a high-fat meal), 2-sequence (AB or BA) crossover assessment, separated by a 10-day washout...
August 22, 2016: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/27539734/proton-pump-inhibitors-risk-for-myopathy
#20
Evan W Colmenares, Ashley L Pappas
OBJECTIVE: The purpose of this article is to describe the relationship between proton pump inhibitors (PPIs) and symptoms of myopathy based on case reports. DATA SOURCES: A literature search was conducted in PubMed (1946 to June 2016) using MeSH terms proton pump inhibitors, omeprazole, esomeprazole, lansoprazole, dexlansoprazole, rabeprazole, pantoprazole, and muscular diseases Additionally, a search was conducted in ToxNet and EMBASE using similar search criteria...
August 18, 2016: Annals of Pharmacotherapy
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