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https://www.readbyqxmd.com/read/29337033/gliclazide-a-katp-channel-blocker-inhibits-vascular-smooth-muscle-cell-proliferation-through-the-camkk%C3%AE-ampk-pathway
#1
Kyung Young Lee, Jae-Ryong Kim, Hyoung Chul Choi
Gliclazide, a sulfonylurea that is widely used to treat type II-diabetes, specifically blocks KATP channels and recombinant smooth muscle (SUR2B/Kir6.1) KATP channels with high potency. Furthermore, it exerts antioxidant properties and inhibits tumor cell proliferation. In this study, we investigated the inhibitory effect of gliclazide on vascular smooth muscle cell (VSMC) proliferation and tried to identify the underlying signaling pathway. We first investigated the effect of gliclazide-induced AMP-activated protein kinase (AMPK) activation on the proliferation of VSMCs...
January 11, 2018: Vascular Pharmacology
https://www.readbyqxmd.com/read/29327815/no-impact-of-pre-existing-cardiovascular-disease-on-prescribing-patterns-of-sulphonylureas-in-denmark-a-registry-based-nationwide-study
#2
Malin Nilsson, Jørgen Rungby, Nathan Lassota, Andreas Daugaard Jørgensen, Rikke Ibsen, Jakob Kjellberg
Uncertainty exists regarding cardiovascular (CV) safety of sulphonylureas (SUs) as reflected in package labels and treatment guidelines. This study evaluated clinical treatment practice for SUs by analysing prescription patterns for SUs relative to patient history of CV disease (CVD). Patients in Denmark initiating treatment with SU or other anti-hyperglycaemic drugs during 2006-2012 were retrospectively identified using national health registries. Pre-existing (previous 12 years) overall CVD, coronary heart disease (CHD) and myocardial infarction (MI) were subsequently identified...
January 12, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29319909/inhibitory-effects-of-sulfonylureas-and-non-steroidal-anti-inflammatory-drugs-on-in-vitro-metabolism-of-canagliflozin-in-human-liver-microsomes
#3
Sara Algeelani, Dalal Alkhelb, David J Greenblatt
Canagliflozin, used to treat type 2 diabetes mellitus (T2DM), is commonly co-administered with sulfonylureas. The objective of the present study was to evaluate the possible inhibitory effect of sulfonylureas and non-steroidal anti-inflammatory drugs (NSAIDs) on canagliflozin metabolism in vitro. Three sulfonylurea derivatives were evaluated as inhibitors: chlorpropamide, glimepiride, and gliclazide. Two other NSAIDs were used as positive control inhibitors: niflumic acid and diclofenac. The rate of formation of canagliflozin metabolites was determined by HPLC analysis of vitro incubations of canagliflozin as a substrate with and without inhibitors, using human liver microsomes (HLMs)...
January 10, 2018: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/29218453/energy-depletion-and-not-ros-formation-is-a-crucial-step-of-glucolipotoxicity-gltx-in-pancreatic-beta-cells
#4
Morgana Barroso Oquendo, Nikolas Layer, Rebecca Wagner, Peter Krippeit-Drews, Gisela Drews
We have shown previously that genetic or pharmacological deletion of KATP channels protect against beta cell dysfunction induced by reactive oxygen species (ROS). Since it is assumed that glucolipotoxicity (GLTx) causes ROS production, we aimed to evaluate whether suppression of KATP channel activity can also prevent beta cell damage evoked by GLTx. We used an in vitro model of GLTx and measured distinct parameters of stimulus-secretion coupling. GLTx gradually induced disturbances of Ca2+ oscillations over 3 days...
December 7, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/29171906/risk-of-a-first-ever-acute-myocardial-infarction-and-all-cause-mortality-with-sulphonylurea-treatment-a-population-based-cohort-study
#5
Judith van Dalem, Martijn C G J Brouwers, Coen D A Stehouwer, André Krings, Olaf H Klungel, Johanna H M Driessen, Frank de Vries, Andrea M Burden
We investigated the association between the current use of individual sulphonylureas and the risk of a first-ever acute myocardial infarction (AMI) and all-cause mortality, in a population-based cohort study, using primary care data from the Clinical Practice Research Datalink database (2004-2012). New users (N = 121 869), aged ≥18 years, with at least one prescription for a non-insulin antidiabetic agent were included. The first prescription defined start of follow-up. Time-dependent Cox proportional hazard models were used to estimate the risk of a first-ever AMI and all-cause mortality associated with the use of individual sulphonylureas, and other non-insulin glucose-lowering drugs...
November 24, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29171468/-glycemic-variability-and-oxidative-stress-in-patients-with-type-2-diabetes-mellitus-during-combined-glucose-lowering-therapy
#6
S G Butaeva, A S Ametov, A V Bugrov, V V Dolgov
AIM: To evaluate the impact of intensified glucose-lowering therapy on carbohydrate metabolic indicator, such as glycated hemoglobin, fasting blood glucose level (BGL) (FBGL), postprandial BGL (PBGL), and glycemic variability (GV) in patients with type 2 diabetes mellitus (T2DM) during metformin monotherapy before and 3 months after therapy intensification. SUBJECTS AND METHODS: The investigation enrolled 51 patients with T2DM treated with metformin 1000 mg twice daily, who failed to achieve satisfactory glycemic control...
2017: Terapevticheskiĭ Arkhiv
https://www.readbyqxmd.com/read/29103851/interaction-of-p-synephrine-on-the-pharmacodynamics-and-pharmacokinetics-of-gliclazide-in-animal-models
#7
Leela Krishna Vatsavai, Eswar Kumar Kilari
BACKGROUND: Type 2 diabetes is frequently seen in patients suffering from obesity. p-Synephrine and gliclazide are widely used medicines for the treatment of obesity and diabetes, respectively. Based on the relationship between obesity and diabetes, the present study was undertaken to determine the potential for herb-drug interactions between p-synephrine and gliclazide. METHODS: Influence of p-synephrine on the activity of gliclazide was determined by conducting single and multiple dose interaction studies in animal models...
November 3, 2017: Journal of Ayurveda and Integrative Medicine
https://www.readbyqxmd.com/read/29099241/in-vitro-and-in-vivo-delivery-of-gliclazide-loaded-mpeg-pcl-micelles-and-its-kinetic-release-and-solubility-study
#8
Hossein Danafar, Hoda Jaberizadeh, Sina Andalib
In this study, drug delivery system of gliclazide, a poorly soluble drug, was developed and evaluated in vitro and in vivo. We synthesized five series of mPEG-PCL di block copolymers. The structure of the copolymers was characterized by (1)H-NMR, Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and gel permeation chromatography (GPC) techniques. In this study, gliclazide was encapsulated within micelles through a single-step nano-precipitation method, leading to formation of gliclazide/mPEG-PCL micelles...
November 3, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29067264/outpatient-management-of-steroid-induced-hyperglycaemia-and-steroid-induced-diabetes-in-people-with-lymphoproliferative-disorders-treated-with-intermittent-high-dose-steroids
#9
Jennifer Vidler, Charlotte Rogers, Deborah Yallop, Stephen Devereux, Ellinor Wellving, Orla Stewart, Alison Cox, Katharine F Hunt, Shireen Kassam
High dose steroids (HDS) are used in the treatment of haematological malignancies. The reported risk of steroid-induced diabetes (SID) is high. However, screening is not consistently performed. We implemented a protocol for detection and management of SID and steroid-induced hyperglycamia (SIH) in haematology outpatients receiving HDS. Eighty-three people were diagnosed with a lymphoproliferative disorder, of whom 6 had known Type 2 diabetes. Fifty-three people without known diabetes were screened by HbA1c and random venous plasma glucose...
September 2017: Journal of Clinical & Translational Endocrinology
https://www.readbyqxmd.com/read/29039071/potential-applications-of-gliclazide-in-treating-type-1-diabetes-mellitus-formulation-with-bile-acids-and-probiotics
#10
Momir Mikov, Maja Đanić, Nebojša Pavlović, Bojan Stanimirov, Svetlana Goločorbin-Kon, Karmen Stankov, Hani Al-Salami
A major advancement in therapy of type 1 diabetes mellitus (T1DM) is the discovery of new treatment which avoids and even replaces the absolute requirement for injected insulin. The need for multiple drug therapy of comorbidities associated with T1DM increases demand for developing novel therapeutic alternatives with new mechanisms of actions. Compared to other sulphonylurea drugs used in the treatment of type 2 diabetes mellitus, gliclazide exhibits a pleiotropic action outside pancreatic β cells, the so-called extrapancreatic effects, such as antiinflammatory and cellular protective effects, which might be beneficial in the treatment of T1DM...
October 16, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28967594/rationale-and-design-of-the-darwin-t2d-dapagliflozin-real-world-evidence-in-type-2-diabetes-a-multicenter-retrospective-nationwide-italian-study-and-crowdsourcing-opportunity
#11
G P Fadini, G Zatti, A Consoli, E Bonora, G Sesti, A Avogaro
BACKGROUND: Randomized controlled trials (RCTs) in the field of diabetes have limitations inherent to the fact that design, setting, and patient characteristics may be poorly transferrable to clinical practice. Thus, evidence from studies using routinely accumulated clinical data are increasingly valued. AIMS: We herein describe rationale and design of the DARWIN-T2D (DApagliflozin Real World evIdeNce in Type 2 Diabetes), a multicenter retrospective nationwide study conducted at 50 specialist outpatient clinics in Italy and promoted by the Italian Diabetes Society...
August 8, 2017: Nutrition, Metabolism, and Cardiovascular Diseases: NMCD
https://www.readbyqxmd.com/read/28956461/multicomponent-crystals-of-gliclazide-and-tromethamine-preparation-physico-chemical-and-pharmaceutical-characterization
#12
Giovanna Bruni, Vittorio Berbenni, Lauretta Maggi, Piercarlo Mustarelli, Valeria Friuli, Chiara Ferrara, Francesca Pardi, Federica Castagna, Alessandro Girella, Chiara Milanese, Amedeo Marini
OBJECTIVE: To improve the pharmaceutical behaviour of the oral antidiabetic agent gliclazide through the synthesis of multicomponent crystals with tromethamine. METHODS: Multicomponent crystals were prepared by solvent evaporation method, kneading and combining mechanical and thermal activation. DSC, FT-IR spectroscopy, X-ray diffraction, SEM-EDS and SSNMR were used to investigate their formation. Measurements of solubility and dissolution rate were carried out for the pharmaceutical characterization...
September 28, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28951332/involvement-of-glucose-regulated-protein-78-and-spliced-x-box-binding-protein-1-in-the-protective-effect-of-gliclazide-in-diabetic-nephropathy
#13
Ying-Wen Zhang, Xiuping Wang, Xiaodan Ren, Manling Zhang
AIMS: To testing whether endoplasmic reticulum (ER) stress contributes to the development of diabetic nephropathy. Investigated the effect of gliclazide, an oral antihyperglycemic agent, in a rat model of diabetic nephropathy and the underlying mechanism related to the ER stress response. METHODS: Sixty SD rats were divided into six groups. Diabetic nephropathy was induced in 30 rats with a streptozotocin (STZ) injection and high fat diet, which were then treated with saline, gliclazide or 4-PBA...
May 4, 2017: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/28943269/ramadan-fasting-in-diabetes-exercise-in-problem-solving
#14
Banshi Saboo
AIM: Appropriate management of a diabetic patient with co-morbidities, who is willing to fast during Ramadan. Case presentation A 45 year old male patient with T2DM for 5 years, current A1c of 8.3% and other co-morbidities is currently treated with metformin 500mg BID and glimepiride 2mg. During the pre-Ramadan assessment, glimepiride 2mg was changed to extended release gliclazide 60mg. It resulted in an improvement in his glycemic and microalbuminuria status without any hypoglycemic episodes...
July 29, 2017: Diabetes & Metabolic Syndrome
https://www.readbyqxmd.com/read/28917544/effects-on-the-incidence-of-cardiovascular-events-of-the-addition-of-pioglitazone-versus-sulfonylureas-in-patients-with-type-2-diabetes-inadequately-controlled-with-metformin-tosca-it-a-randomised-multicentre-trial
#15
Olga Vaccaro, Maria Masulli, Antonio Nicolucci, Enzo Bonora, Stefano Del Prato, Aldo P Maggioni, Angela A Rivellese, Sebastiano Squatrito, Carlo B Giorda, Giorgio Sesti, Paolo Mocarelli, Giuseppe Lucisano, Michele Sacco, Stefano Signorini, Fabrizio Cappellini, Gabriele Perriello, Anna Carla Babini, Annunziata Lapolla, Giovanna Gregori, Carla Giordano, Laura Corsi, Raffaella Buzzetti, Gennaro Clemente, Graziano Di Cianni, Rossella Iannarelli, Renzo Cordera, Olga La Macchia, Chiara Zamboni, Cristiana Scaranna, Massimo Boemi, Ciro Iovine, Davide Lauro, Sergio Leotta, Elisabetta Dall'Aglio, Emanuela Cannarsa, Laura Tonutti, Giuseppe Pugliese, Antonio C Bossi, Roberto Anichini, Francesco Dotta, Antonino Di Benedetto, Giuseppe Citro, Daniela Antenucci, Lucia Ricci, Francesco Giorgino, Costanza Santini, Agostino Gnasso, Salvatore De Cosmo, Donatella Zavaroni, Monica Vedovato, Agostino Consoli, Maria Calabrese, Paolo di Bartolo, Paolo Fornengo, Gabriele Riccardi
BACKGROUND: The best treatment option for patients with type 2 diabetes in whom treatment with metformin alone fails to achieve adequate glycaemic control is debated. We aimed to compare the long-term effects of pioglitazone versus sulfonylureas, given in addition to metformin, on cardiovascular events in patients with type 2 diabetes. METHODS: TOSCA.IT was a multicentre, randomised, pragmatic clinical trial, in which patients aged 50-75 years with type 2 diabetes inadequately controlled with metformin monotherapy (2-3 g per day) were recruited from 57 diabetes clinics in Italy...
November 2017: Lancet Diabetes & Endocrinology
https://www.readbyqxmd.com/read/28914437/salutary-potential-of-ethanolic-extract-of-avocado-fruit-on-anomalous-carbohydrate-metabolic-key-enzymes-in-hepatic-and-renal-tissues-of-hyperglycaemic-albino-rats
#16
U S Mahadeva Rao
OBJECTIVE: To assess the beneficial potential of ethanolic extract of avocado fruit on abnormal carbohydrate metabolic key enzymes in hepatic and renal tissues in streptozotocin (STZ) induced hyperglycemic albino rats. METHODS: Twenty-four male albino rats were randomly divided into four groups with six in each group by simple random sampling method. Group 1 as control rats; Group 2 as STZ induced diabetic rats; Group 3 as diabetic rats treated with avocado fruit extract (AFE), 300 mg/kg as aqueous suspension orally for 30 days; Group 4 as diabetic rats treated with gliclazide (5 mg/kg) in aqueous solution orally for 30 days...
September 15, 2017: Chinese Journal of Integrative Medicine
https://www.readbyqxmd.com/read/28912863/a-novel-mutation-in-the-hepatocyte-nuclear-factor-1%C3%AE-gene-in-maturity-onset-diabetes-of-the-young-5-with-multiple-renal-cysts-and-pancreas-hypogenesis-a-case-report
#17
You Lv, Zhuo Li, Kan He, Ying Gao, Xianchao Xiao, Yujia Liu, Guixia Wang
A 17-year-old Chinese male was hospitalized exhibiting hyperglycemia and increased serum urea nitrogen and creatinine levels in addition to weight loss. The patient was treated with gliclazide. The patient was 150 cm tall, weighed 35 kg and had no family history of diabetes or kidney disease. Physical examination revealed cephalus quadratus, rachitic rosary and a visible toe-out gait. Laboratory examinations revealed that the patient's fasting plasma glucose and glycosylated hemoglobin levels were markedly increased, fasting plasma C-peptide level was slightly increased and no peak 2 h postprandial was observed...
October 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28901251/case-report-severe-hematological-muscle-and-liver-toxicity-caused-by-drugs-and-artichoke-infusion-interaction-in-an-elderly-polymedicated-patient
#18
M G Campos, J Machado, M L Costa, S Lino, F Correia, F Maltez
Case report, in a patient with a history of diabetes and hypertension, treated with metformin, gliclazide, enalapril + hydrochlorothiazide, amlodipine, aspirin and diazepam, recently medicated for a gouty crisis with colchicine and clonixin without improvement. Believing it could help in the treatment of gouty crisis symptoms he took about 1.5 L of artichoke infusion (Cynara cardunculus). He felt better and did agriculture work but developed a distal muscle pain, severe anemia, standard biochemical liver cholestasis, increase of alkaline phosphatase and marked increase of inflammatory parameters (hyperleucocytosis) and enters in the emergency department at the hospital...
September 12, 2017: Current Drug Safety
https://www.readbyqxmd.com/read/28888191/the-effect-of-glycation-on-bovine-serum-albumin-conformation-and-ligand-binding-properties-with-regard-to-gliclazide
#19
Ewa Żurawska-Płaksej, Anna Rorbach-Dolata, Katarzyna Wiglusz, Agnieszka Piwowar
Albumin, the major serum protein, plays a variety of functions, including binding and transporting endogenous and exogenous ligands. Its molecular structure is sensitive to different environmental modifiers, among which glucose is one of the most significant. In vivo albumin glycation occurs under physiological conditions, but it is increased in diabetes. Since bovine serum albumin (BSA) may serve as a model protein in in vitro experiments, we aimed to investigate the impact of glucose-mediated BSA glycation on the binding capacity towards gliclazide, as well as the ability of this drug to prevent glycation of the BSA molecule...
September 6, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28864502/pharmacologic-differences-of-sulfonylureas-and-the-risk-of-adverse-cardiovascular-and-hypoglycemic-events
#20
Antonios Douros, Hui Yin, Oriana Hoi Yun Yu, Kristian B Filion, Laurent Azoulay, Samy Suissa
OBJECTIVE: Sulfonylureas have been associated with an increased risk of cardiovascular adverse events and hypoglycemia, but it is unclear if these risks vary with different agents. We assessed whether the risks of acute myocardial infarction, ischemic stroke, cardiovascular death, all-cause mortality, and severe hypoglycemia differ between sulfonylureas grouped according to pancreas specificity and duration of action. RESEARCH DESIGN AND METHODS: Using the U.K. Clinical Practice Research Datalink, linked with the Hospital Episodes Statistics and the Office for National Statistics databases, we conducted a cohort study among patients with type 2 diabetes initiating monotherapy with sulfonylureas between 1998 and 2013...
November 2017: Diabetes Care
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