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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
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
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
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
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
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
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
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
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
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
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
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
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
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
Qiang Niu, Zhongsu Wang, Yong Zhang, Jiangrong Wang, Pei Zhang, Cong Wang, Xiangcui Yin, Yinglong Hou
BACKGROUND: Published data indicated that combination use of clopidogrel and proton pump inhibitors (PPIs) may increase the incidence of major adverse cardiovascular events (MACEs). This has been a highly controversial topic for years. DESIGN: The present study was performed to evaluate whether combination therapy of clopidogrel and PPIs is associated with increased risk of MACEs than with clopidogrel alone in patients with coronary artery disease. METHODS: A systematic search of MEDLINE, EMBASE, and the Cochrane Library was conducted for studies recording the occurrence of MACEs in patients with exposure to concomitant use of clopidogrel and PPIs up to February 2015...
August 10, 2016: Journal of Cardiovascular Pharmacology and Therapeutics
Daisuke Maruoka, Makoto Arai, Shingo Kasamatsu, Hideaki Ishigami, Takashi Taida, Kenichiro Okimoto, Keiko Saito, Tomoaki Matsumura, Tomoo Nakagawa, Tatsuro Katsuno, Osamu Yokosuka
BACKGROUND AND AIM: Proton pump inhibitors (PPI) are effective at healing artificial ulcers after endoscopic submucosal dissection (ESD) for gastric neoplasms; however, the efficacy of vonoprazan is not completely understood. The aim of the present study was to determine the healing effect of vonoprazan on artificial ulcers post-gastric ESD relative to PPI. METHODS: Thirty-five patients who underwent gastric ESD between April and November 2015 were treated with vonoprazan 20 mg/day for 4 weeks and subsequently underwent endoscopy for evaluation of ulcer size (V group)...
August 4, 2016: Digestive Endoscopy: Official Journal of the Japan Gastroenterological Endoscopy Society
Kenji Ikemura, Yugo Hamada, Chinatsu Kaya, Tomoyuki Enokiya, Yuichi Muraki, Hiroki Nakahara, Hajime Fujimoto, Tetsu Kobayashi, Takuya Iwamoto, Masahiro Okuda
Pemetrexed, a multitargeted antifolate, is eliminated by tubular secretion via human organic anion transporter 3 (hOAT3). Although proton pump inhibitors (PPIs) are frequently used in cancer patients, the drug interaction between PPIs and pemetrexed remains to be clarified. In this study, we examined the drug interaction between pemetrexed and PPIs in hOAT3-expressing cultured cells, and retrospectively analyzed the impact of PPIs on the development of hematologic toxicity in 108 patients who received pemetrexed and carboplatin treatment of nonsquamous non-small cell lung cancer for the first time between January 2011 and June 2015...
October 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Yiqiao Xin, Jan Manson, Lindsay Govan, Robin Harbour, Jenny Bennison, Eleanor Watson, Olivia Wu
BACKGROUND: Approximately half of the world's population is infected with Helicobacter pylori (H.pylori), a bacterium shown to be linked with a series of gastrointestinal diseases. A growing number of systematic reviews (SRs) have been published comparing the effectiveness of different treatments for H.pylori infection but have not reached a consistent conclusion. The objective of this study is to provide an overview of SRs of pharmacological therapies for the eradication of H.pylori...
2016: BMC Gastroenterology
Neil J Parrott, Li J Yu, Ryusuke Takano, Mikiko Nakamura, Peter N Morcos
Alectinib, a lipophilic, basic, anaplastic lymphoma kinase (ALK) inhibitor with very low aqueous solubility, has received Food and Drug Administration-accelerated approval for the treatment of patients with ALK+ non-small-cell lung cancer. This paper describes the application of physiologically based absorption modeling during clinical development to predict and understand the impact of food and gastric pH changes on alectinib absorption. The GastroPlus(™) software was used to develop an absorption model integrating in vitro and in silico data on drug substance properties...
July 22, 2016: AAPS Journal
Petros Zezos, Ziv Harel, Fred Saibil
A large variety of medications can cause pill-induced esophagitis. Herein we present a case of cloxacillin-induced esophagitis. A 66-year-old male presented with an acute onset of epigastric and retrosternal pain on the 5th day of a course of oral cloxacillin prescribed for erysipelas. Initial clinical and imaging assessment was negative and he was sent home. A few days later, he returned with persistent severe retrosternal pain; endoscopy at the same day revealed a normal upper esophagus, several small stellate erosions in the midesophagus, and a normal squamocolumnar junction with a small hiatus hernia...
2016: Canadian Journal of Gastroenterology & Hepatology
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