keyword
https://read.qxmd.com/read/35612708/results-from-phase-i-studies-investigating-the-dose-linearity-of-finerenone-tablets-and-the-influence-of-food-or-ph-modifying-comedications-on-its-pharmacokinetics-in-healthy-male-volunteers
#21
JOURNAL ARTICLE
Roland Heinig, Johannes Nagelschmitz, Stephanie Loewen
BACKGROUND AND OBJECTIVES: Finerenone is a nonsteroidal mineralocorticoid receptor antagonist that reduces the risk of adverse kidney and cardiovascular outcomes in patients with chronic kidney disease associated with type 2 diabetes mellitus. Clinical phase I studies with finerenone were carried out to assess its pharmacokinetics and the influence of common covariables on its absorption after oral administration. METHODS: Three crossover studies in healthy male volunteers with single-dose administration of finerenone investigated the dose linearity of a film-coated tablet (1...
July 2022: European Journal of Drug Metabolism and Pharmacokinetics
https://read.qxmd.com/read/35560255/activation-of-aryl-hydrocarbon-receptor-stimulates-glut-mediated-glucose-transport-in-human-renal-proximal-tubular-cells
#22
JOURNAL ARTICLE
Kannaree Kaewsaro, Sunhapas Soodvilai
Aryl hydrocarbon receptor (AhR), a ligand-activated transcription factor, plays a major role in detoxification of xenobiotics. AhR deficiency has been shown to attenuate renal injury induced by diabetes. It is interesting whether the beneficial effect of AhR deficiency on renal injury in diabetes involve in alteration of intracellular glucose in renal tubular cells. The aim of this study was to investigate the effect and mechanism of AhR on glucose uptake into human renal proximal tubular cells. Exposure HK-2 cells, human renal proximal tubular cell line, with omeprazole, an AhR agonist, increased glucose transporter (GLUT)-mediated [3 H]-2-Deoxy-D glucose uptake into the cells in concentration-dependent manner...
May 2022: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://read.qxmd.com/read/34802943/omeprazole-inhibits-%C3%AE-glucosidase-activity-and-the-formation-of-nonenzymatic-glycation-products-activity-and-mechanism
#23
JOURNAL ARTICLE
Chen Yu, Zi-Yi Yu, Yi-Ting Wen, Wei-Ming Chai, Lin-Jun Wang, Mei-Zhen Lin
In this study, the inhibitory effect and mechanism of omeprazole on α-glucosidase and nonenzymatic glycation were investigated in vitro by using multi-spectroscopic methods and molecular docking. Enzyme kinetic results showed that omeprazole inhibited α-glucosidase in a reversible and noncompetitive manner (IC50 = 0.595 ± 0.003 mM). The results from fluorescence quenching and thermomechanical analyses signified that omeprazole reduced the fluorescence intensity of α-glucosidase by forming an omeprazole-α-glucosidase complex primarily driven by hydrogen bonds...
February 2022: Journal of Bioscience and Bioengineering
https://read.qxmd.com/read/34726935/prophylactic-use-of-proton-pump-inhibitors-post-cardiac-surgery
#24
JOURNAL ARTICLE
Matthew Azzopardi, Jean-Luc Paris, David Sladden
AIMS/BACKGROUND: Gastrointestinal bleeding significantly increases morbidity and mortality rates postoperatively in patients undergoing cardiac surgery. The prophylactic prescribing of proton pump inhibitors post-cardiac surgery is currently a class IIa recommendation of the European Association of Cardio-Thoracic Surgery. METHOD: A retrospective review of patients who underwent cardiac surgery between July and December 2019 in the authors' hospital was carried out, using discharge summaries...
October 2, 2021: British Journal of Hospital Medicine
https://read.qxmd.com/read/34470455/strange-coincidence-in-the-gut-pseudomelanosis-duodeni-diagnosed-by-capsule-endoscopy-and-active-bleeding-due-to-angiodysplasia
#25
JOURNAL ARTICLE
Albert Martín-Cardona, Montserrat Aceituno, Beatriz Arau, Ignacio Fernández-Urién
We present the case of an 82-year-old male with a medical history of hypertension, dyslipidemia, diabetes mellitus, chronic renal failure, ischemic heart disease and iron deficiency anemia. He was under therapy with hydralazine, furosemide, amlodipine, valsartan, nitroglycerin patches, bisoprolol, omeprazole, doxazosin, human insulin and oral iron. The patient presented at our institution with melena. Initial gastroscopy showed fresh blood and a gastric angiodysplasia that was treated with argon plasma coagulation (APC)...
February 2022: Revista Española de Enfermedades Digestivas
https://read.qxmd.com/read/34063566/interaction-between-omeprazole-and-gliclazide-in-relation-to-cyp2c19-phenotype
#26
JOURNAL ARTICLE
Tanja Dujic, Sandra Cvijic, Amar Elezovic, Tamer Bego, Selma Imamovic Kadric, Maja Malenica, Alisa Elezovic, Ewan R Pearson, Aida Kulo
The antidiabetic drug gliclazide is partly metabolized by CYP2C19, the main enzyme involved in omeprazole metabolism. The aim of the study was to explore the interaction between omeprazole and gliclazide in relation to CYP2C19 phenotype using physiologically based pharmacokinetic (PBPK) modeling approach. Developed PBPK models were verified using in vivo pharmacokinetic profiles obtained from a clinical trial on omeprazole-gliclazide interaction in healthy volunteers, CYP2C19 normal/rapid/ultrarapid metabolizers (NM/RM/UM)...
May 3, 2021: Journal of Personalized Medicine
https://read.qxmd.com/read/33928172/ion-transport-modulators-differentially-modulate-inflammatory-responses-in-thp-1-derived-macrophages
#27
JOURNAL ARTICLE
Steven C Mitini-Nkhoma, Narmada Fernando, G K D Ishaka, Shiroma M Handunnetti, Sisira L Pathirana
Ion transport modulators are most commonly used to treat various noncommunicable diseases including diabetes and hypertension. They are also known to bind to receptors on various immune cells, but the immunomodulatory properties of most ion transport modulators have not been fully elucidated. We assessed the effects of thirteen FDA-approved ion transport modulators, namely, ambroxol HCl, amiloride HCl, diazoxide, digoxin, furosemide, hydrochlorothiazide, metformin, omeprazole, pantoprazole, phenytoin, verapamil, drug X, and drug Y on superoxide production, nitric oxide production, and cytokine expression by THP-1-derived macrophages that had been stimulated with ethanol-inactivated Mycobacterium bovis BCG...
2021: Journal of Immunology Research
https://read.qxmd.com/read/33597314/primary-hyperparathyroidism-and-zollinger-ellison-syndrome-during-pregnancy-a-case-report
#28
JOURNAL ARTICLE
Dalal Ali, Patrick Divilly, Ruth Prichard, Dermot O'Toole, Donal O'Shea, Rachel K Crowley
SUMMARY: Multiple endocrine neoplasia type 1 (MEN1) is a rare inherited endocrine disorder with a high rate of penetrance. The incidence of MEN1 is 1/30,000 in the general population; however, it is quite rare for a patient to present for medical attention with MEN1 for the first time in pregnancy. Primary hyperparathyroidism (PHPT) is one of the most common features of MEN1. The incidence of PHPT occurring in pregnancy is 1%. Despite advances in the medical, surgical and obstetric care over the years, management of this condition during pregnancy may be challenging...
February 17, 2021: Endocrinology, Diabetes & Metabolism Case Reports
https://read.qxmd.com/read/33345855/the-effect-of-metformin-on-indomethacin-induced-gastric-ulcer-involvement-of-nitric-oxide-rho-kinase-pathway
#29
JOURNAL ARTICLE
Eman Y AbdelAziz, Mariane G Tadros, Esther T Menze
Gastric ulcer is a very common disease that represent an economic burden. Non-steroidal anti-inflammatory drugs induce ulcer in old patients and in patients with comorbidities. Indomethacin is widely used to induce gastric ulcer in animal models. Diabetic patients are highly susceptible to develop gastric ulcer. Metformin, the first line medication for the treatment of type II diabetes melilites that have many off label uses in non-diabetic patients, has been recently reported to have anti-inflammatory activities...
February 5, 2021: European Journal of Pharmacology
https://read.qxmd.com/read/33115391/analysis-of-the-potential-association-of-drug-metabolizing-enzymes-cyp2c9-3-and-cyp2c19-3-gene-variations-with-type-2-diabetes-a-case-control-study
#30
JOURNAL ARTICLE
Imadeldin Elfaki, Rashid Mir, Faisel Mohammed Abu-Duhier, Chandan Kumar Jha, Adel Ibrahim Ahmad Al-Alawy, Abdullatif Taha Babakr, Salem Abd El-Hadi Habib
BACKGROUND: Cytochrome P450s (CYPs) are drug-metabolizing enzymes catalyzing the metabolism of about 75% of drug in clinical use. CYP2C9 represents 20% CYP proteins in liver cells and is a crucial member of CYPs superfamily. CYP2C19 metabolizes very important drugs such as antiulcer drug omeprazole, the antiplatelet drug clopidogrel and anticonvulsant mephenytoin. Single nucleotide polymorphisms (SNPs) of CYP genes have been associated with unexpected drug reactions and diseases in different populations...
2020: Current Drug Metabolism
https://read.qxmd.com/read/32970826/clopidogrel-dosing-current-successes-and-emerging-factors-for-further-consideration
#31
REVIEW
Manoranjenni Chetty, Paulien Ravenstijn, Pooja Manchandani
This review aimed to evaluate the clinical success of clopidogrel dosing based on CYP2C19 genotype and to identify the relevant additional factors that may be useful for consideration by the clinician when dosing individuals with clopidogrel. The results indicated that genotype-guided dosing in individuals with acute coronary syndrome undergoing percutaneous coronary intervention is frequently practiced, although the advantages remain controversial. Demographic factors, such as age, ethnicity, and some comorbidities, such as diabetes mellitus, can potentially contribute to further refinement of clopidogrel dosage but additional clinical studies to guide these practices are required...
May 2021: Clinical Pharmacology and Therapeutics
https://read.qxmd.com/read/32742601/evaluation-of-changes-in-cytochrome-p450-2c19-activity-in-type-2-diabetic-rats-before-and-after-treatment-by-using-isolated-perfused-liver-model
#32
JOURNAL ARTICLE
Navid Neyshaburinezhad, Mohammad Reza Rouini, Hanieh Entezari, Hoda Lavasani, Yalda Hosseinzadeh Ardakani
OBJECTIVES: Alteration in drug metabolism is very likely in diabetes mellitus. This study assessed changes in CYP2C19 enzymatic activity in the liver using omeprazole as a probe in the animal model of type II diabetes (T2DM) before and after treatment with metformin and cinnamon. MATERIALS AND METHODS: Twenty-eight male Wistar rats were randomly divided into seven groups. Fourteen days after induction of type 2 diabetic mellitus (T2DM), rats in the test group received metformin, cinnamon, and metformin plus cinnamon daily for 14 days...
May 2020: Iranian Journal of Basic Medical Sciences
https://read.qxmd.com/read/32647517/the-effect-of-proton-pump-inhibitors-on-glycaemic-control-in-diabetic-patients
#33
JOURNAL ARTICLE
Muhammad Ali Rajput, Fizzah Ali, Tabassum Zehra, Shahid Zafar, Gunesh Kumar
OBJECTIVE: This study aimed to evaluate the effect of proton pump inhibitors on glycaemic control amongst diabetic patients taking anti-diabetic medications. METHODS: This randomised interventional clinical study was conducted in Basic Medical Sciences Institute, Jinnah Postgraduate Medical Centre, Karachi. Eighty patients of either sex (aged 30-60 years) with type 2 diabetes mellitus and without any known comorbidities were equally divided into two groups (i.e...
June 2020: Journal of Taibah University Medical Sciences
https://read.qxmd.com/read/32337164/evaluating-the-effect-of-type-2-diabetes-mellitus-on-cyp450-enzymes-and-p-gp-activities-before-and-after-glycemic-control-a-protocol-for-a-case-control-pharmacokinetic-study
#34
JOURNAL ARTICLE
Navid Neyshaburinezhad, Mohammadreza Rouini, Nooshin Shirzad, Alireza Esteghamati, Manouchehr Nakhjavani, Soha Namazi, Yalda H Ardakani
Cytochrome P450s (CYP450) family is one of the most critical factors in the metabolism process. Hence, the present study aims to characterize the activity of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP3A4/5, and P-glycoprotein (P-gp) pump in patients with type 2 diabetes (T2DM). This characterization was performed before and after good glycemic control versus non-diabetic subjects following the administration of a substrate probe drug cocktail. This single-center clinical study proposes the characterization of T2DM impacts on major CYP450 drug-metabolizing enzyme and P-glycoprotein (P-gp) activities...
2020: MethodsX
https://read.qxmd.com/read/31923689/pharmaceutical-pollution-of-water-resources-in-nakivubo-wetlands-and-lake-victoria-kampala-uganda
#35
JOURNAL ARTICLE
Sahar Dalahmeh, Emma Björnberg, Anna-Klara Elenström, Charles B Niwagaba, Allan John Komakech
This study investigated the occurrence and removal in wastewater and water bodies in Nakivubo wetland area and Inner Murchison Bay, Lake Victoria, of common prescription and non-prescription pharmaceutically-active substances (PhACs) sold in Kampala city, Uganda. A questionnaire was sent to 20 pharmacies in Kampala, to identify the most commonly sold PhACs in the city. During two sampling campaigns, samples were collected from Bugolobi wastewater treatment plant (WWTP) influent and effluent and surface water samples from Nakivubo channel, Nakivubo wetland and Inner Murchison Bay...
March 25, 2020: Science of the Total Environment
https://read.qxmd.com/read/31817776/proton-pump-inhibitors-and-hypomagnesaemia-in-kidney-transplant-recipients
#36
JOURNAL ARTICLE
Rianne M Douwes, António W Gomes-Neto, Joëlle C Schutten, Else van den Berg, Martin H de Borst, Stefan P Berger, Daan J Touw, Eelko Hak, Hans Blokzijl, Gerjan Navis, Stephan J L Bakker
Proton-pump inhibitors (PPIs) are commonly used after kidney transplantation and there is rarely an incentive to discontinue treatment. In the general population, PPI use has been associated with hypomagnesaemia. We aimed to investigate whether PPI use is associated with plasma magnesium, 24-h urinary magnesium excretion and hypomagnesaemia, in kidney transplant recipients (KTR). Plasma magnesium and 24-h urinary magnesium excretion were measured in 686 stable outpatient KTR with a functioning allograft for ≥1 year from the TransplantLines Food and Nutrition Biobank and Cohort-Study (NCT02811835)...
December 6, 2019: Journal of Clinical Medicine
https://read.qxmd.com/read/31618561/esophageal-candidiasis-in-patients-from-a-specialty-hospital
#37
JOURNAL ARTICLE
Luis Javier Méndez-Tovar, José Froylán Rodríguez-Sánchez, Patricia Manzano-Gayosso, Francisca Hernández-Hernández, Juan Manuel Blancas-Valencia, Israel Silva-González
Background: Esophageal candidiasis (EC) is the most common cause of infectious esophagitis. So far, its main risk factor has been HIV infection; in recent years, EC has been favoured by the increasing of diabetes mellitus, wide-spread use of acid-lowering agents, broad-spectrum antibiotics, and inhaled steroids. In Mexico EC has been poorly studied. Objectives: To determine the clinical and epidemiological characteristics of EC, and to identify its etiological agents as well as its antifungal susceptibility...
July 31, 2019: Revista Médica del Instituto Mexicano del Seguro Social
https://read.qxmd.com/read/31099895/modulation-of-cyp450-activities-in-patients-with-type-2-diabetes
#38
JOURNAL ARTICLE
Sophie Gravel, Jean-Louis Chiasson, Jacques Turgeon, Alexia Grangeon, Veronique Michaud
We conducted a comprehensive in vivo study evaluating the influence of type 2 diabetes (T2D) on major CYP450 activities. These activities were assessed in 38 T2D and 35 non-T2D subjects after a single oral administration of a cocktail of probe drugs: 100mg caffeine (CYP1A2), 100mg bupropion (CYP2B6), 250mg tolbutamide (CYP2C9), 20mg omeprazole (CYP2C19), 30mg dextromethorphan (CYP2D6), 2mg midazolam (CYP3As), and 250mg chlorzoxazone (alone) (CYP2E1). Mean metabolic activity for CYP2C19, CYP2B6 and CYP3A were decreased in T2D subjects by about 46%, 45% and 38% (p<0...
May 17, 2019: Clinical Pharmacology and Therapeutics
https://read.qxmd.com/read/30987326/-h-pylori-eradication-treatment-alters-gut-microbiota-and-glp-1-secretion-in-humans
#39
JOURNAL ARTICLE
Isabel Cornejo-Pareja, Gracia M Martín-Núñez, M Mar Roca-Rodríguez, Fernando Cardona, Leticia Coin-Aragüez, Lidia Sánchez-Alcoholado, Carolina Gutiérrez-Repiso, Araceli Muñoz-Garach, José C Fernández-García, Isabel Moreno-Indias, Francisco J Tinahones
Changes in the intestinal microbial community and some metabolic disturbances, including obesity and type2 diabetes, are related. Glucagon-like peptide-1 (GLP-1) regulates glucose homeostasis. Microbiota have been linked to incretin secretion. Antibiotic use causes changes in microbial diversity and composition. Our aim was to evaluate the relationship between microbiota changes and GLP-1 secretion. A prospective case-control study with a Helicobacter pylori -positive patient model involving subjects under eradication therapy (omeprazole, clarithromycin, and amoxicillin)...
April 4, 2019: Journal of Clinical Medicine
https://read.qxmd.com/read/30500110/pharmacokinetic-interaction-study-between-saxagliptin-and-omeprazole-famotidine-or-magnesium-and-aluminum-hydroxides-plus-simethicone-in-healthy-subjects-an-open-label-randomized-crossover-study
#40
RANDOMIZED CONTROLLED TRIAL
Song Ren, David W Boulton
Saxagliptin is an orally administered, highly potent, and selective dipeptidyl peptidase-4 inhibitor for the management of type 2 diabetes mellitus. This study was conducted to determine the effect of magnesium and aluminum hydroxides plus simethicone, famotidine, and omeprazole on the pharmacokinetics of saxagliptin and its active metabolite, 5-hydroxy saxagliptin. This was an open-label, randomized, 5-treatment, 5-period, 3-way crossover study in 15 healthy subjects. Mean Cmax of saxagliptin was 26% lower, but AUC was almost unchanged when saxagliptin was coadministered with Maalox Max...
May 2019: Clinical Pharmacology in Drug Development
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