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Omeprazole

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https://www.readbyqxmd.com/read/29034770/association-with-polymorphic-marmoset-cytochrome-p450-2c19-of-in-vivo-hepatic-clearances-of-chirally-separated-r-omeprazole-and-s-warfarin-using-individual-marmoset-physiologically-based-pharmacokinetic-models
#1
Takashi Kusama, Akiko Toda, Makiko Shimizu, Shotaro Uehara, Takashi Inoue, Yasuhiro Uno, Masahiro Utoh, Erika Sasaki, Hiroshi Yamazaki
1. Simulated clearances of R-warfarin and efavirenz were recently reported for individual cynomolgus monkeys genotyped for cytochrome P450 2C19 and 2C9, respectively. To expand and verify this modeling procedure, simulations of R/S-omeprazole and R/S-warfarin clearances after oral administrations in individual marmosets were performed using individual simplified physiologically based pharmacokinetic (PBPK) modeling consisting of gut, liver, and central compartments. 2. Pharmacokinetics of R/S-omeprazole were chirally determined using the previously reported plasma microsamples in this study...
October 16, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29033601/urine-metabolic-ratio-of-omeprazole-in-relation-to-cyp2c19-polymorphisms-in-russian-peptic-ulcer-patients
#2
Natalia P Denisenko, Dmitriy A Sychev, Zhanna M Sizova, Valeriy V Smirnov, Kristina A Ryzhikova, Zhannet A Sozaeva, Elena A Grishina
BACKGROUND: CYP2C19 is known to be the main enzyme of biotransformation of proton pump inhibitors (PPIs), whereas the CYP2C19 gene is highly polymorphic. Genotyping and phenotyping together represent more reliable data about patient's CYP2C19 activity. PURPOSE: The aim of the study was to investigate the applicability of urine metabolic ratio of omeprazole for CYP2C19 phenotyping in Russian peptic ulcer patients with different CYP2C19 genotypes. PATIENTS AND METHODS: A total of 59 patients (19 men and 40 women) aged 18-91 years (mean age 53...
2017: Pharmacogenomics and Personalized Medicine
https://www.readbyqxmd.com/read/29024542/the-relative-bioavailability-food-effect-and-drug-interaction-with-omeprazole-of-momelotinib-tablet-formulation-in-healthy-subjects
#3
Yan Xin, Lixin Shao, Julie Maltzman, Dimitrios Stefanidis, Jeffrey Hemenway, Thomas Tarnowski, Wei Deng, Jeffrey A Silverman
Momelotinib is a potent and selective small-molecule inhibitor of JAK1/2 that is under investigation for the treatment of myeloproliferative neoplasms. In a phase 1/2 study in myelofibrosis patients, once-daily dosing of a 300-mg momelotinib capsule was selected for further development based on a favorable benefit:risk profile. A tablet formulation was recently developed for further clinical evaluation. In this study, the relative bioavailability of the tablet formulation versus the initial capsule formulation and the effect of food and omeprazole on the pharmacokinetics of a single-dose momelotinib tablet were evaluated in healthy subjects...
October 11, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/29024410/eight-weeks-of-omeprazole-20-mg-significantly-reduces-both-laryngopharyngeal-reflux-and-comorbid-chronic-rhinosinusitis-signs-and-symptoms-randomized-double-blind-placebo-controlled-trial
#4
Srđan Ante Anzić, Mirjana Turkalj, Ana Župan, Marina Labor, Davor Plavec, Tomislav Baudoin
OBJECTIVES: Gastroesophageal reflux recommended treatment (dose and duration) with proton pump inhibitor (PPI) compared to placebo significantly reduces the signs and symptoms of laryngopharyngeal reflux (LPR) and comorbid chronic rhinosinusitis (CRS). DESIGN: Double blind randomized placebo controlled trial. SETTING: Eight weeks of treatment with omeprazole 20 mg once daily (OD). PARTICIPANTS: 60 patients (28 women, aged 19-87 years) with diagnosed LPR and comorbid CRS...
October 11, 2017: Clinical Otolaryngology
https://www.readbyqxmd.com/read/28986475/pediatric-cytochrome-p450-activity-alterations-in-nonalcoholic-steatohepatitis
#5
Hui Li, Canet J Mark, John D Clarke, Dean Billheimer, Stavra A Xanthakos, Joel E Lavine, Robert P Erickson, Nathan J Cherrington
Variable drug responses(VDRs) are dependent upon individual variation in the activity of drug-metabolizing enzymes including cytochrome P450s(CYPs). As the most common chronic liver disease in children and adults, nonalcoholic steatohepatitis(NASH) has been identified as a source of significant inter-individual variation in hepatic drug metabolism. Compared to adults, children present age-related differences in pharmacokinetics and pharmacodynamics. The purpose of this study was to determine the impact of fatty liver disease severity on the activity of a variety of CYPs in children and adolescents...
October 6, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28964908/interchageable-use-of-proton-pump-inhibitors-based-on-relative-potency
#6
David Y Graham, Aylin Tansel
Although proton pump inhibitors (PPIs) are widely used, their relative potency and ideal dosing regimens remain unclear. We analyzed data from randomized clinical trials that performed pH testing in patients receiving solid-dose PPI formulations (omeprazole, esomeprazole, lansoprazole, pantoprazole, rabeprazole) for a minimum of 5 days. We used omeprazole equivalency and the surrogate biomarker, pH4time (percentage time pH>4 over 24-hour period), to compare PPI effectiveness for different PPIs given once, twice or three times daily...
September 28, 2017: Clinical Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28961574/the-role-of-gastroesophageal-reflux-in-provoking-high-blood-pressure-episodes-in-patients-with-hypertension
#7
Zhi-Tong Li, Feng Ji, Xin-Wei Han, Li Wang, Yong-Qiang Yue, Zhong-Gao Wang
GOALS: We assessed the relationship between gastroesophageal reflux disease (GERD) and hypertension and whether antiacid therapy could be used to control blood pressure (BP) on hypertension in patients with GERD. BACKGROUND: Gastroesophageal reflux disease (GERD) may provoke cardiovascular disease. Many factors are involved in the development of essential hypertension, but whether GERD has a role needs further study. STUDY: Patients with essential hypertension (n=86) were studied by 24-hour continuous BP monitoring and esophageal impedance and pH monitoring...
September 28, 2017: Journal of Clinical Gastroenterology
https://www.readbyqxmd.com/read/28954042/antisecretory-treatment-for-pediatric-gastroesophageal-reflux-disease-a-systematic-review
#8
Ângelo Zambam de Mattos, Gabriela Meirelles Marchese, Bárbara Brum Fonseca, Carlos Kupski, Marta Brenner Machado
BACKGROUND: Proton pump inhibitors and histamine H2 receptor antagonists are two of the most commonly prescribed drug classes for pediatric gastroesophageal reflux disease, but their efficacy is controversial. Many patients are treated with these drugs for atypical manifestations attributed to gastroesophageal reflux, even that causal relation is not proven. OBJECTIVE: To evaluate the use of proton pump inhibitors and histamine H2 receptor antagonists in pediatric gastroesophageal reflux disease through a systematic review...
September 21, 2017: Arquivos de Gastroenterologia
https://www.readbyqxmd.com/read/28953640/comparative-effectiveness-and-acceptability-of-the-fda-licensed-proton-pump-inhibitors-for-erosive-esophagitis-a-prisma-compliant-network-meta-analysis
#9
Mei-Juan Li, Qing Li, Min Sun, Li-Qin Liu
BACKGROUND: This study compared the effectiveness and acceptability of all Food and Drug Administration (FDA)-recommended dose proton pump inhibitors (PPIs) in erosive esophagitis (EE): Dexlansoprazole 60 mg, Esomeprazole 40 mg, Esomeprazole 20 mg, Pantoprazole 40 mg, Lansoprazole 30 mg, Rabeprazole 20 mg, Omeprazole 20 mg. METHODS: A systematic literature search was performed using PubMed, Embase, and Cochrane Library. Totally, 25 randomized controlled trials (RCTs) met study selection criteria and were incorporated in this network meta-analysis (NMA) study...
September 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28942222/the-effect-of-astragaloside-iv-on-ethanol-induced-gastric-mucosal-injury-in-rats-involvement-of-inflammation
#10
Shumin Qin, Keer Huang, Zhigang Fang, Jinjin Yin, Ruwei Dai
The present study aimed to investigate the potential protective effects of Astragaloside IV (AS-IV) against ethanol-induced gastric mucosal injury in rats. The animals were divided into 7 groups and pretreated with vehicle, various doses of AS-IV (1,2 and 4mg/kg, i.p.) or omeprazole (40mg/kg), 75min later, the gastric mucosal injury was induced by oral administration of ethanol. One hour after ethanol ingestion, the rats were euthanized and gastric tissues were collected to biochemical analyze. Myeloperoxidase (MPO), tumor necrosis factor α (TNF-α), interleukin 1β (IL-1β), interleukin 10 (IL-10), nuclear factor kappa B (NF-κB) p65 protein, TNF receptor-associated factor 2 (TRAF2) and nuclear NF-κB (nNF-κB) proteins were estimated by enzyme-linked immunosorbent assay or western blot analysis...
November 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28932294/aspirin-induced-gastric-lesions-alters-egfr-and-pecam-1-immunoreactivity-in-wistar-rats-modulatory-action-of-flavonoid-fraction-of-musa-paradisiaca
#11
Margaret Olutayo Alese, Stephen Olarinde Adewole, Kemi Feyisayo Akinwunmi, Abidemi Emmanuel Omonisi, Oluwole Ojo Alese
AIM: In this study, Epithelial Growth Factor Receptor and Platelet Endothelial Cell Adhesion Molecule-1 were localised to investigate the healing effects of a flavonoid-rich fraction of M. paradisiaca fruit in the gastric corpus of Wistar rats following aspirin-induced gastric lesion. MATERIALS AND METHODS: Mature, unripe fruits of M. paradisiaca were peeled; air dried, pulverised, extracted with 70% methanol, concentrated and partitioned. Ninety male Wistar rats were randomly assigned into 6 groups of 15 rats each...
August 15, 2017: Open Access Macedonian Journal of Medical Sciences
https://www.readbyqxmd.com/read/28932128/a-suspected-case-of-autoinduction-of-voriconazole-metabolism-in-a-patient-with-cerebral-aspergillosis
#12
Martin J Ferguson, Maria L Randles, Declan G de Freitas
OBJECTIVE: This study aims to report a case of accelerated metabolism of voriconazole in a patient with cerebral aspergillosis. CASE SUMMARY: A 36-year-old woman developed cerebral aspergillosis after immunosuppressive treatment for suspected atypical hemolytic uremic syndrome/thrombotic thrombocytopenic purpura. She was treated with voriconazole using therapeutic drug monitoring to guide dosing. After an initial high level, her dose was reduced, but over the following weeks, she required several dose increases in order to achieve a voriconazole level within the target range...
2017: Drug, Healthcare and Patient Safety
https://www.readbyqxmd.com/read/28932080/comparison-between-tocotrienol-and-omeprazole-on-gastric-growth-factors-in-stress-exposed-rats
#13
Mohd Fahami Nur Azlina, Hj Mohd Saad Qodriyah, Kien Hui Chua, Yusof Kamisah
AIM: To investigate and compare the effects of tocotrienol and omeprazole on gastric growth factors in rats exposed to water-immersion restraint stress (WIRS). METHODS: Twenty-eight male Wistar rats were randomly assigned to four groups of seven rats. The two control groups were administered vitamin-free palm oil (vehicle) and the two treatment groups were given omeprazole (20 mg/kg) or tocotrienol (60 mg/kg) by oral gavage. After 28 d of treatment, rats from one control group and both treated groups were subjected to WIRS one time for 3...
August 28, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28929443/short-term-fasting-alters-pharmacokinetics-of-cytochrome-p450-probe-drugs-does-protein-binding-play-a-role
#14
Laureen A Lammers, Roos Achterbergh, Johannes A Romijn, Ron A A Mathôt
BACKGROUND AND OBJECTIVES: Short-term fasting differentially alters cytochrome P450 (CYP) mediated drug metabolism. This has been established by using CYP-enzyme selective probe drugs. However, the observed effects of fasting on the pharmacokinetics of these probe drugs may also include the effects of altered plasma protein binding of these drugs. Therefore, we studied the effect of short-term fasting on protein binding of five commonly used probe drugs [caffeine (CYP1A2), metoprolol (CYP2D6), midazolam (CYP3A4), omeprazole (CYP2C19) and S-warfarin (CYP2C9)]...
September 19, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28891561/online-monitoring-of-hepatic-rat-metabolism-by-coupling-a-liver-biochip-and-a-mass-spectrometer
#15
Franck Merlier, Rachid Jellali, Eric Leclerc
A microfluidic liver biochip was coupled with a mass spectrometer to detect in real time the drug metabolism of hepatocytes. The hepatocytes were cultivated in the biochip for 35 h. The biochip was placed in a small-scale incubator in which the temperature and CO2 concentration were controlled. The biochip was connected serially to a mass spectrometer, a peristaltic pump and a culture medium reservoir. The injection in the mass spectrometer was performed every 10 min for 11 h. The metabolism of midazolam, phenacetin, omeprazole, dextromethorphan, repaglinide, rosuvastatin, tolbutamide and caffeine was investigated...
September 25, 2017: Analyst
https://www.readbyqxmd.com/read/28889052/a-rapid-fourier-transform-infrared-spectroscopic-method-for-analysis-of-certain-proton-pump-inhibitors-in-binary-and-ternary-mixtures
#16
Pakinaz Y Khashaba, Hassan Refat H Ali, Mohamed M El-Wekil
A simple and non-destructive FTIR method was used to determine certain proton pump inhibitors (PPIs) in binary and ternary mixtures. Proton pump inhibitors (PPIs); omeprazole (OMZ), esomeprazole (EZM), lansoprazole (LAN), pantoprazole sodium (PAN sodium) and rabeprazole sodium (RAB sodium) in binary mixture with domperidone (DOM) and ternary mixture of OMZ, clarithromycin (CLM) and tinidazole (TNZ) were determined in the solid-state by FTIR spectroscopy for the first time. The method was validated according to ICH-guidelines where linearity was ranged from 20 to 850μg/g and 20-360μg/g for PPIs and DOM, respectively in binary mixtures and 10-400, 100-8000 and 150-14,000μg/g for OMZ, CLM and TNZ, respectively...
September 5, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28885223/prescription-audit-of-nsaids-and-gastroprotective-strategy-in-elderly-in-primary-care
#17
Khalid Ahmed Jassim Al Khaja, Sindhan Veeramuthu, Husain Ahmed Isa, Reginald Paul Sequeira
BACKGROUND: The use of non-steroidal anti-inflammatory drug (NSAIDs) is deemed a major risk factor for peptic ulcer disease in elderly population that requires concomitant therapy with gastroprotective agents (GPAs). OBJECTIVE: This study evaluated the rational prescribing of NSAIDs and GPAs, and extent of adherence to the guideline recommendations in primary care. METHODS: Nationwide audit of prescriptions issued to elderly patients (≥65 years) with hypertension or diabetic hypertension in primary care...
2017: International Journal of Risk & Safety in Medicine
https://www.readbyqxmd.com/read/28866861/effects-of-the-proton-pump-inhibitors-omeprazole-and-pantoprazole-on-the-cytochrome-p450-mediated-metabolism-of-venlafaxine
#18
Maxim Kuzin, Georgios Schoretsanitis, Ekkehard Haen, Benedikt Stegmann, Christoph Hiemke, Gerhard Gründer, Michael Paulzen
BACKGROUND AND OBJECTIVE: An increasing trend in prescribing proton pump inhibitors (PPIs) inevitably increases the risk of unwanted drug-drug interactions (DDIs). The aim of this study was to uncover pharmacokinetic interactions between two PPIs-omeprazole and pantoprazole-and venlafaxine. METHODS: A therapeutic drug monitoring database contained plasma concentrations of venlafaxine and its active metabolite O-desmethylvenlafaxine. We considered three groups: a group of patients who received venlafaxine without confounding medications (non-PPI group, n = 906); a group of patients who were comedicated with omeprazole (n = 40); and a group of patients comedicated with pantoprazole (n = 40)...
September 2, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28865153/evaluation-of-the-pharmacokinetic-drug-interaction-potential-of-tivantinib-arq-197-using-cocktail-probes-in-patients-with-advanced-solid-tumours
#19
Masaya Tachibana, Kyriakos P Papadopoulos, John H Strickler, Igor Puzanov, Roohi Gajee, Yibin Wang, Hamim Zahir
AIM: This phase 1, open-label, crossover study sought to evaluate drug-drug interactions between tivantinib and cytochrome P450 (CYP) substrates and tivantinib and P-glycoprotein. METHODS: The effect of tivantinib doses on the pharmacokinetics of the probe drugs for CYP1A2 (caffeine), CYP2C9 (warfarin), CYP2C19 (omeprazole), and CYP3A4 (midazolam), and for P-glycoprotein (digoxin) was investigated in 28 patients with advanced cancer using a cocktail probe approach...
September 2, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28859856/gastrin-induces-nuclear-export-and-proteasome-degradation-of-menin-in-enteric-glial-cells
#20
Sinju Sundaresan, Cameron A Meininger, Anthony J Kang, Amanda L Photenhauer, Michael M Hayes, Nirakar Sahoo, Jolanta Grembecka, Tomasz Cierpicki, Lin Ding, Thomas J Giordano, Tobias Else, David J Madrigal, Malcolm J Low, Fiona Campbell, Ann-Marie Baker, Haoxing Xu, Nicholas A Wright, Juanita L Merchant
BACKGROUND & AIMS: The multiple endocrine neoplasia, type 1 (MEN1) locus encodes the nuclear protein and tumor suppressor menin. MEN1 mutations frequently cause neuroendocrine tumors (NETs) such as gastrinomas, characterized by their predominant duodenal location and local metastasis at time of diagnosis. Diffuse gastrin cell hyperplasia precedes the appearance of MEN1 gastrinomas, which develop within submucosal Brunner's glands. We investigated how menin regulates expression of the gastrin gene and induces generation of submucosal gastrin-expressing cell hyperplasia...
August 28, 2017: Gastroenterology
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