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https://www.readbyqxmd.com/read/29469947/evaluation-of-the-metabolic-capability-of-primary-human-hepatocytes-in-three-dimensional-cultures-on-microstructural-plates
#1
Satoshi Koyama, Hiroshi Arakawa, Manabu Itoh, Norio Masuda, Kentaro Yano, Hajime Kojima, Takuo Ogihara
The NanoCulture Plate (NCP) is a novel microstructural plate designed as a base for the three-dimensional culture of cells/tissues. Here, we examined whether or not the metabolic capability of human primary hepatocytes is well maintained during culture on NCPs. The hepatocytes formed aggregates after seeding and their ATP content was well maintained during culture for 21 days. Expression of CYP1A2, 2B6, 2C9, 2C19, 2D6, 2E1 and 3A4 mRNAs was detected throughout the 21-day culture period. Addition of CYP substrate drugs (midazolam, diclofenac, lamotrigine and acetaminophen) resulted in the formation of multiple metabolites with a corresponding decrease in the amounts of the unchanged compounds...
February 22, 2018: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/29468684/re-evaluation-of-the-regulation-of-omeprazole-in-racehorses-an-evidence-based-approach
#2
M Viljanto, L Hillyer, P Hincks, C Pearce, S W Paine
Medication control and doping control have been established in horse racing to ensure the integrity of the sport and the welfare of the horses. This ensures that horses do not compete under the influence of any drugs, including omeprazole, a therapeutic medication used to treat equine gastric ulcer syndrome. In this study, pharmacokinetic data were produced in equine plasma and urine following an oral administration of 4 mg/kg of generic buffered formulation of omeprazole to six Thoroughbred horses in five daily doses to determine an appropriate screening limit and detection time in equine plasma and to assess whether the current detection time of 72 hr in equine urine would be applicable when an alternative omeprazole product is administered...
February 22, 2018: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29467124/gastric-and-duodenal-ischaemia-after-transarterial-chemoembolisation-for-hepatocellular-carcinoma-an-unexpected-but-significant-complication
#3
Sai Pavan Chintalapati, Arpan Patel, Hari Conjeevaram
Transarterial chemoembolisation (TACE) is commonly used for unresectable intermediate-stage hepatocellular carcinoma (HCC). TACE is usually well-tolerated. We report a case of a patient who presented with a gastrointestinal bleed from TACE. A 64-year-old man presented with chronic hepatitis C cirrhosis and multifocal bilobar HCC. He had previously undergone multiple TACE sessions, radiofrequency ablation and stereotactic body radiation therapy. In the evening of his TACE procedure, he developed abdominal pain and haematemesis...
February 21, 2018: BMJ Case Reports
https://www.readbyqxmd.com/read/29465250/continuous-esomeprazole-infusion-versus-bolus-administration-and-second-look-endoscopy-for-the-prevention-of-rebleeding-in-children-with-a-peptic-ulcer
#4
Oana Belei, Laura Olariu, Maria Puiu, Cristian Jinca, Cristina Dehelean, Tamara Marcovici, Otilia Marginean
INTRODUCTION: the majority of studies of acute gastrointestinal bleeding in children are retrospective, focusing on therapeutic endoscopy. Previous studies performed in adult patients have demonstrated that both scheduled second look endoscopy and high dose continuous omeprazole infusion are effective in the prevention of peptic ulcer rebleeding. The aim of this study was to compare the efficacy of these two strategies using esomeprazole for the prevention of rebleeding following primary endoscopic hemostasis in children with peptic ulcers...
February 21, 2018: Revista Española de Enfermedades Digestivas
https://www.readbyqxmd.com/read/29449127/evaluating-the-effect-of-six-proton-pump-inhibitors-on-the-antiplatelet-effects-of-clopidogrel
#5
Eugene R Przespolewski, Erica S Westphal, Michelle Rainka, Nicholas M Smith, Vernice Bates, Fran M Gengo
BACKGROUND AND GOAL: Cytochrome P450 (CYP) enzymes are responsible for the conversion of clopidogrel into its active metabolite and the metabolism of proton pump inhibitors (PPIs), which may also inhibit CYP enzymes. A current Food and Drug Administration advisory suggests avoiding esomeprazole and omeprazole while taking clopidogrel because of concerns that PPIs may compromise clopidogrel's antiplatelet effects. The objective of the present study was to examine the robustness of this interaction using a well-controlled study design in a population of participants free of confounders...
February 12, 2018: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
https://www.readbyqxmd.com/read/29440451/establishing-transcriptional-signatures-to-differentiate-pxr-car-and-ahr-mediated-regulation-of-drug-metabolism-and-transport-genes-in-cryopreserved-human-hepatocytes
#6
Jamie E Moscovitz, Amit S Kalgutkar, Kelly Nulick, Nathaniel Johnson, Zhiwu Lin, Theunis C Goosen, Yan Weng
The potential for drug-drug interactions (DDIs) arising from transcriptional regulation of drug disposition genes via activation of nuclear receptors (NRs) such as pregnane X receptor (PXR), constitutive androstane receptor (CAR), and/or aryl hydrocarbon receptor (AhR) remains largely unexplored, as highlighted in a recent guidance document from the European Medicines Agency. The goal of this research was to establish PXR/CAR/AhR-specific drug metabolizing enzyme (DME) and transporter gene expression signatures in sandwich-cultured cryopreserved human hepatocytes using selective activators of PXR (rifampin), CAR (CITCO) and AhR (omeprazole)...
February 12, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29439084/evaluating-the-impact-of-type-2-diabetes-mellitus-on-cyp450-metabolic-activities-protocol-for-a-case-control-pharmacokinetic-study
#7
Sophie Gravel, Jean-Louis Chiasson, Suzanne Dallaire, Jacques Turgeon, Veronique Michaud
INTRODUCTION: Diabetes affects more than 9% of the adult population worldwide. Patients with type 2 diabetes mellitus (T2DM) show variable responses to some drugs which may be due, in part, to variability in the functional activity of drug-metabolising enzymes including cytochromes P450 (CYP450s). CYP450 is a superfamily of enzymes responsible for xenobiotic metabolism. Knowledge must be gained on the impact of T2DM and related inflammatory processes on drug metabolism and its consequences on drug response...
February 8, 2018: BMJ Open
https://www.readbyqxmd.com/read/29434682/drug-induced-rowell-syndrome-a-rare-and-difficult-to-manage-disease-a-case-report
#8
Daciana Elena Brănișteanu, Simona Laura Ianoşi, Andreea Dimitriu, Gabriela Stoleriu, Alexandru Oanţǎ, Daniel Constantin Brănișteanu
Rowell syndrome is defined as the association between lupus erythematosus, erythema multiforme-like lesions and characteristic immunological changes including positive tests for rheumatoid factor, speckled antinuclear antibody, positive anti-Ro or anti-La antibodies. The present report presents the case of a 45-year-old female patient who was previously diagnosed in January 2010 with terbinafine-induced subacute cutaneous lupus erythematosus and was admitted for a skin eruption consisting of erythematous-papular erythema multiforme-like lesions, primarily on the trunk and limbs...
January 2018: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29430683/supramolecular-separation-mechanism-of-pentafluorophenyl-column-using-ibuprofen-and-omeprazole-as-markers-lc-ms-and-simulation-study
#9
Afzal Hussain, Mohamed F Alajmi, Imran Ali
Pentafluorophenyl (PFP) Column is emerging as a new advancement in separation science to analyze a wide range of analytes and, thus, its separation mechanism at supramolecular level is significant. We developed a mechanism for the separation of ibuprofen and omeprazole using different combinations (ranged from 50:50 to 60:40) of water-acetonitrile containing 0.1% formic acid as the mobile phase. The column used was Waters Acquity UPLC HSS PFP (75 x 2.1 mm, 1.8 μm). The reverse order of elution was observed in different combinations of the mobile phases...
February 12, 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29425645/repeated-administration-of-sailuotong-a-fixed-combination-of-panax-ginseng-ginkgo-biloba-and-crocus-sativus-extracts-for-vascular-dementia-alters-cyp450-activities-in-rats
#10
Ying Zhang, Lan Miao, Li Lin, Chang-Ying Ren, Jian-Xun Liu, Yi-Min Cui
BACKGROUND: Sailuotong (SLT) is a standard Chinese preparation made from extracts of Panax ginseng (ginseng), Ginkgo biloba (ginkgo), and Crocus sativus (saffron). Preliminary clinical trials and animal experiments have demonstrated that SLT could improve cognition of vascular dementia (VD). PURPOSE: To avoid incident drug-drug interaction which is easily encountered in patients of VD, the potential influence of SLT on main drug-metabolic cytochromes P450 enzymes (CYP450) was investigated...
January 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29415150/kaempferol-protects-ethanol-induced-gastric-ulcers-in-mice-via-pro-inflammatory-cytokines-and-no
#11
Qinchen Li, Xinxin Hu, Yanhan Xuan, Jianghua Ying, Yujia Fei, Jielu Rong, Yong Zhang, Jian Zhang, Chunyan Liu, Zheng Liu
Gastric ulcers (GUs) are common pathologies that affect many people around the world. Excessive alcohol consumption is one of the main causes of GUs; however, there are still lack of effective drugs for the prevention or therapy of GUs. In this study, we evaluated the protective effects and possible mechanisms of kaempferol (KAE) against acute ethanol-induced lesions to the gastric mucosa in mice. Fasted mice were orally given vehicle (0.9% saline), omeprazole (20 mg/kg), or KAE (40, 80, or 160 mg/kg) for 1 h in different experimental sets prior to the establishment of the GU model by challenge with absolute ethanol (10 ml/kg)...
February 3, 2018: Acta Biochimica et Biophysica Sinica
https://www.readbyqxmd.com/read/29414895/a-case-of-spontaneous-pneumomediastinum-with-subcutaneous-emphysema-in-children
#12
Said Benlamkaddem, Mohamed Adnane Berdai, Smael Labib, Mustapha Harandou
Spontaneous pneumomediastinum is defined as free air or gas contained within the mediastinum, which almost invariably originates from the alveolar space or the conducting airways. It is rare in pediatric patients; however, occasional cases are reported to result from forced Valsalva's maneuver due to cough, emesis, a first attack of wheeze, or asthma exacerbations. We report the case of a 7-year-old previously healthy girl, with a history of persistent dry cough one day before, who was brought to our unit with face, neck and chest swelling...
February 7, 2018: Children
https://www.readbyqxmd.com/read/29411268/a-phase-1-pharmacokinetic-study-of-cysteamine-bitartrate-delayed-release-capsules-following-oral-administration-with-orange-juice-water-or-omeprazole-in-cystinosis
#13
Danielle Armas, Robert J Holt, Nils F Confer, Gregg C Checani, Mohammad Obaidi, Yuli Xie, Meg Brannagan
INTRODUCTION: Cystinosis is a rare, metabolic, autosomal recessive, genetic lysosomal storage disorder characterized by an accumulation of cystine in various organs and tissues. Cysteamine bitartrate (CB) is a cystine-depleting aminothiol agent approved in the United States and Europe in immediate-release and delayed-release (DR) formulations for the treatment of nephropathic cystinosis in children and adults. It is recommended that CBDR be administered with fruit juice (except grapefruit juice) for maximum absorption...
February 6, 2018: Advances in Therapy
https://www.readbyqxmd.com/read/29403569/-alexa-refill-my-omeprazole
#14
EDITORIAL
David B Nash
No abstract text is available yet for this article.
December 2017: American Health & Drug Benefits
https://www.readbyqxmd.com/read/29398173/design-of-a-randomized-placebo-controlled-trial-to-assess-dabigatran-and-omeprazole-in-patients-with-myocardial-injury-after-noncardiac-surgery-manage
#15
Emmanuelle Duceppe, Salim Yusuf, Vikas Tandon, Reitze Rodseth, Bruce M Biccard, Denis Xavier, Wojciech Szczeklik, Christian S Meyhoff, Maria Grazia Franzosi, Jessica Vincent, Sadeesh K Srinathan, Joel Parlow, Patrick Magloire, John Neary, Mangala Rao, Navneet K Chaudhry, Bongani Mayosi, Miriam de Nadal, Ekaterine Popova, Juan Carlos Villar, Fernando Botto, Otavio Berwanger, Gordon Guyatt, John W Eikelboom, Daniel I Sessler, Clive Kearon, Shirley Pettit, Stuart J Connolly, Mukul Sharma, Shrikant I Bangdiwala, P J Devereaux
BACKGROUND: Worldwide approximately 200 million adults undergo major surgery annually, of whom 8 million are estimated to suffer a myocardial injury after noncardiac surgery (MINS). There is currently no trial data informing the management of MINS. Antithrombotic agents such as direct oral anticoagulants might prevent major vascular complications in patients with MINS. METHODS: The Management of Myocardial Injury After Noncardiac Surgery (MANAGE) trial is a large international blinded randomized controlled trial of dabigatran vs placebo in patients who suffered MINS...
February 2, 2018: Canadian Journal of Cardiology
https://www.readbyqxmd.com/read/29379346/novel-quinazoline-and-acetamide-derivatives-as-safe-anti-ulcerogenic-agent-and-anti-ulcerative-colitis-activity
#16
Fatmah A S Alasmary, Amani S Awaad, Ahmed M Alafeefy, Reham M El-Meligy, Saleh I Alqasoumi
Two novel quinazoline derivatives named as; 3-[(4-hydroxy-3-methoxy-benzylidene)-amino]-2-p-tolyl-3H-quinazolin-4-one (5) and 2-p-Tolyl-3-[3,4,5-trimethoxy-benzylidene-amino]-3H-quinazolin-4-one (6) in addition to one acetamide derivative named as 2-(2-Hydroxycarbonylphenylamino)-N-(4-aminosulphonylphenyl) 11 were synthesized, and evaluated for their anti-ulcerogenic & Anti-Ulcerative colitis activities. All of the three compounds showed curative activity against acetic acid induced ulcer model at a dose of 50 mg/kg, they produced 65%, 85% & 57...
January 2018: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/29377228/developmental-pharmacogenetics-of-cyp2c19-in-neonates-and-young-infants-omeprazole-as-a-probe-drug
#17
Wei Zhao, Stéphanie Leroux, Valérie Biran, Evelyne Jacqz-Aigrain
BACKGROUND: Although substantial progress has been made in understanding of ontogeny of drug metabolism, there is still a gap of knowledge in developmental pharmacogenetics in neonates. We hypothesized that both age and pharmacogenetics might explain the developmental pattern of CYP2C19. We conducted a population pharmacokinetic-pharmacogenetic study to quantify the developmental pharmacogenetics of CYP2C19 in neonates and young infants using omeprazole as a probe drug. METHODS: Pharmacokinetic samples were collected from 51 Caucasian neonates and young infants, who were receiving omeprazole treatment...
January 28, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29376492/is-the-use-of-proton-pump-inhibitors-a-risk-factor-for-alzheimer-s-disease-molecular-mechanisms-and-clinical-implications
#18
Kazuki Ide, Norihiro Matsuoka, Koji Kawakami
Proton-pump inhibitors (PPIs), such as omeprazole, lansoprazole, and rabeprazole, are used for the treatment of gastroesophageal reflux disease and peptic ulcer disease. The use of PPIs has increased, especially in older individuals, and a pharmacoepidemiological study indicated that the use of PPIs peaks in people aged 80 years or older. In this population, Alzheimer's disease (AD) is a common neurological disorder and type of dementia, occurring with a frequency of approximately 10%. Currently, over 45 million people are estimated to have dementia worldwide, and it is a major cause of death in the elderly...
January 28, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29357810/cytochrome-p450-1a2-messenger-rna-is-a-more-reliable-marker-than-cytochrome-p450-1a2-activity-phenacetin-o-deethylation-for-assessment-of-induction-potential-of-drug-metabolizing-enzymes-using-heparg-cells
#19
Akira Ogasawara, Nozomu Kato, Nao Torimoto, Fumika Aohara, Rikiya Ohashi, Yasuhiro Yamada, Hideki Taniguchi
BACKGROUND: The HepaRG cells have key drug metabolism functionalities comparable to those of primary human hepatocytes. Many studies have reported that this cell line can be used as a reliable in vitro model for human drug metabolism studies, including the assessment of cytochrome P450 (CYP) induction. OBJECTIVES: The objective of this study is to determine whether CYP mRNA level measurement is superior to the CYP enzyme activity measurement as a convenient high-throughput method for evaluating CYP induction potential using HepaRG cells...
January 18, 2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29348104/disposition-kinetics-of-omeprazole-in-healthy-female-volunteers-in-faisalabad
#20
Sadia Ashraf, Tanweer Khaliq, Ijaz Javed, Bilal Aslam, Nazia Qadir, Nadia Noor
Omeprazole (OMP) a proton pump inhibitor is widely used to suppress gastric acid secretions of parietal cells of stomach and metabolized predominantly by CYP2C19. The objective of the present study was to investigate the pharmacokinetics and dosage regimen of OMP, after its single oral administration in eight healthy adult female subjects. Blood samples were collected at different time intervals after oral administration and their pH was measured. Plasma concentration of OMP was determined by high performance liquid chromatography (HPLC) system equipped with UV-visible Detector...
January 2018: Pakistan Journal of Pharmaceutical Sciences
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