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Sulphonylurea

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https://www.readbyqxmd.com/read/29791172/-current-treatment-options-in-maturity-onset-diabetes-of-the-young
#1
Ludmila Brunerová, Jana Urbanová, Jan Brož
The discovery of MODY (Maturity-Onset Diabetes of the Young) and the elucidation of its heritability enabled more precise clinical characteristics of different MODY subtypes and led to understanding that glucokinase MODY (GCK-MODY) is not associated with vascular complications in long term follow-up, whereas MODY of transcription factors (e.g. HNF1A-MODY) is in case of bad metabolic control connected with the acceleration of particularly microvascular complications. There is a strong evidence of the needlessness of any specific antidiabetic treatment in prognosticaly favourable GCK-MODY (except for the pregnancy)...
2018: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/29772022/binding-of-sulphonylureas-to-plasma-proteins-a-katp-channel-perspective
#2
Peter Proks, Holger Kramer, Elizabeth Haythorne, Frances M Ashcroft
Sulphonylurea drugs stimulate insulin secretion from pancreatic β-cells primarily by inhibiting ATP sensitive potassium (KATP) channels in the β-cell membrane. The effective sulphonylurea concentration at its site of action is significantly attenuated by binding to serum albumin, which makes it difficult to compare in vitro and in vivo data. We therefore measured the ability of gliclazide and glibenclamide to inhibit KATP channels and stimulate insulin secretion in the presence of serum albumin. We used this data, together with estimates of free drug concentrations from binding studies, to predict the extent of sulphonylurea inhibition of KATP channels at therapeutic concentrations in vivo...
2018: PloS One
https://www.readbyqxmd.com/read/29739729/congenital-hyperinsulinism-and-evolution-to-sulfonylurea-responsive-diabetes-later-in-life-due-to-a-novel-homozygous-p-l171f-abcc8-mutation
#3
Emregül Işık, Huseyin Demirbilek, Jayne A L Houghton, Sian Ellard, Sarah E Flanagan, Khalid Hussain
BACKGROUND: Congenital hyperinsulinism (CHI) is the most common cause of persistent hypoglycemia in infants and children. Recessive inactivating mutations in the ABCC8 and KCNJ11 genes account for approximately 50 % of all CHI cases. Hyperinsulinaemic hypoglycaemia (HH) in infancy and diabetes in later life have been reported in subjects with HNF1A , HNF4A and ABCC8 mutations. CASE REPORT: Herein, we present a child who was diagnosed with CHI at birth, then developed diabetes mellitus at the age of 9 years due to a novel homozygous missense, p...
March 29, 2018: Journal of Clinical Research in Pediatric Endocrinology
https://www.readbyqxmd.com/read/29706097/fluoroenesulphonamides-n-sulphonylurea-isosteres-showing-nanomolar-selective-cancer-related-transmembrane-human-carbonic-anhydrase-inhibition
#4
Benoit Métayer, Andrea Angeli, Agnès Mingot, Kévin Jouvin, Gwilherm Evano, Claudiu T Supuran, Sébastien Thibaudeau
After hydrofluorination of ynesulphonamides in superacid or in the presence of hydrofluoric acid/base reagents, a series of α-fluoroenamides has been synthesised and tested for the inhibition of carbonic anhydrase (CA, EC 4.2.1.1) isoforms. This study reveals a new, highly selective family of cancer-related transmembrane human (h) CA IX/XII inhibitors. These original fluorinated ureido isosters do not inhibit the widespread cytosolic isoforms hCA I and II and selectively inhibit the transmembrane cancer-related hCA IX and XII, offering interesting new leads for future studies...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29679474/population-pharmacokinetics-of-gliclazide-in-normal-and-diabetic-rabbits
#5
Mastan Shaik, Shabana Shaik, Eswar Kumar Kilari
Gliclazide is a second-generation sulphonylurea drug widely used in the treatment of type 2 diabetes. However, there is no single report to describe the population pharmacokinetics of gliclazide in animal models. This study was aimed to evaluate the population pharmacokinetics (PK) of gliclazide in normal and alloxan-induced diabetic rabbits using nonlinear mixed effects modeling. A total of 90 New Zealand white rabbits were administered with 3 doses (4.13, 8.27 and 16.53 mg/kg b.wt) of gliclazide by an oral route...
April 21, 2018: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/29666033/antidiabetics-usage-in-type-2-diabetes-mellitus-are-prescribing-guidelines-adhered-to-a-single-centre-study
#6
Viviane Khalil, Christy Sajan, Tiffany Tsai, David Ma
AIM: The primary aim of this study was to examine the prescribing patterns of antidiabetic agents (AA) in this hospital according to current prescribing contraindications (PCI). The secondary aims are to assess factors affecting the prescribing of AA and to evaluate the pharmacist impact on their prescribing. METHOD: A retrospective cross sectional study was performed to review all prescribed AA over a 3 month period. Data extracted from medical records included: patients' demographics, management and pharmacists' interventions...
April 11, 2018: Diabetes & Metabolic Syndrome
https://www.readbyqxmd.com/read/29596951/a-randomized-controlled-trial-to-compare-the-effects-of-sulphonylurea-gliclazide-mr-modified-release-and-the-dpp-4-inhibitor-vildagliptin-on-glycemic-variability-and-control-measured-by-continuous-glucose-monitoring-cgm-in-brazilian-women-with-type-2-diabetes
#7
Andre Gustavo Daher Vianna, Claudio Silva Lacerda, Luciana Muniz Pechmann, Michelle Garcia Polesel, Emerson Cestari Marino, Jose Rocha Faria-Neto
AIMS: This study aims to evaluate whether there is a difference between the effects of vildagliptin and gliclazide MR (modified release) on glycemic variability (GV) in women with type 2 diabetes (T2DM) as evaluated by continuous glucose monitoring (CGM). METHODS: An open-label, randomized study was conducted in T2DM women on steady-dose metformin monotherapy which were treated with 50 mg vildagliptin twice daily or 60 to 120 mg of gliclazide MR once daily. CGM and GV indices calculation were performed at baseline and after 24 weeks...
March 26, 2018: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/29581078/alogliptin-in-patients-with-type-2-diabetes-on-metformin-and-sulfonylurea-therapies-in-the-examine-trial
#8
William B White, Simon R Heller, Christopher P Cannon, Heena Howitt, Kamlesh Khunti, Richard M Bergenstal
BACKGROUND: We evaluated the antihyperglycemic efficacy and safety of adding the dipeptidyl dipeptidase-4 inhibitor alogliptin to metformin and sulphonylurea in the treatment of type 2 diabetes in the EXAMINE Trial. METHODS: Patients with type 2 diabetes and recent acute coronary syndrome were randomized to alogliptin or placebo and standard of care. Participants were followed for up to 40 (median 18) months. In a subgroup taking metformin and sulphonylurea at baseline, we evaluated change from baseline in HbA1c, adverse events, cardiovascular outcomes, laboratory data, and other safety parameters...
March 23, 2018: American Journal of Medicine
https://www.readbyqxmd.com/read/29549214/does-a-prostate-cancer-diagnosis-affect-management-of-pre-existing-diabetes-results-from-pcbase-sweden-a-nationwide-cohort-study
#9
Danielle Crawley, Hans Garmo, Sarah Rudman, Pär Stattin, Björn Zethelius, Jo Armes, Lars Holmberg, Jan Adolfsson, Mieke Van Hemelrijck
OBJECTIVES: Both prostate cancer (PCa) and type 2 diabetes mellitus (T2DM) are increasingly prevalent conditions, which frequently coexist in men. Here, we set out to specifically examine the impact of a PCa diagnosis and its treatment on T2DM treatment. SETTING: This study uses observational data from Prostate Cancer database Sweden Traject. PARTICIPANTS: The study was undertaken in a cohort of 16 778 men with T2DM, of whom 962 were diagnosed with PCa during mean follow-up of 2...
March 16, 2018: BMJ Open
https://www.readbyqxmd.com/read/29537664/the-pattern-of-prescribing-of-glucose-modulating-agents-for-type-2-diabetes-in-general-practices-in-england-2016-17
#10
Adrian H Heald, Mark Livingston, Zuzanna Bien, Gabriela Y C Moreno, Ian Laing, Mike Stedman
BACKGROUND: In the financial year 2016/17 there were 52.0 million items prescribed for diabetes at a total net ingredient cost of £983.7 million - up from 28.9 million prescription items and £572.4 million in 2006/07. Anti-diabetes drugs (British National Formulary section 6.1.2) make up 45.1 per cent of the total £983.7 million net ingredient cost of drugs used in diabetes and account for 72.0 per cent of prescription items for all diabetes prescribing. METHODS: We examined the way that agents licensed to treat type 2 diabetes were used across GP practices in England in the year 2016/2017...
March 14, 2018: International Journal of Clinical Practice
https://www.readbyqxmd.com/read/29520964/type-2-diabetes-mellitus-and-heart-failure-a-position-statement-from-the-heart-failure-association-of-the-european-society-of-cardiology
#11
REVIEW
Petar M Seferović, Mark C Petrie, Gerasimos S Filippatos, Stefan D Anker, Giuseppe Rosano, Johann Bauersachs, Walter J Paulus, Michel Komajda, Francesco Cosentino, Rudolf A de Boer, Dimitrios Farmakis, Wolfram Doehner, Ekaterini Lambrinou, Yuri Lopatin, Massimo F Piepoli, Michael J Theodorakis, Henrik Wiggers, John Lekakis, Alexandre Mebazaa, Mamas A Mamas, Carsten Tschöpe, Arno W Hoes, Jelena P Seferović, Jennifer Logue, Theresa McDonagh, Jillian P Riley, Ivan Milinković, Marija Polovina, Dirk J van Veldhuisen, Mitja Lainscak, Aldo P Maggioni, Frank Ruschitzka, John J V McMurray
The coexistence of type 2 diabetes mellitus (T2DM) and heart failure (HF), either with reduced (HFrEF) or preserved ejection fraction (HFpEF), is frequent (30-40% of patients) and associated with a higher risk of HF hospitalization, all-cause and cardiovascular (CV) mortality. The most important causes of HF in T2DM are coronary artery disease, arterial hypertension and a direct detrimental effect of T2DM on the myocardium. T2DM is often unrecognized in HF patients, and vice versa, which emphasizes the importance of an active search for both disorders in the clinical practice...
May 2018: European Journal of Heart Failure
https://www.readbyqxmd.com/read/29516618/sodium-glucose-co-transporter-2-inhibitors-the-latest-residents-on-the-block-impact-on-glycaemic-control-at-a-general-practice-level-in-england
#12
Adrian H Heald, Anthony A Fryer, Simon G Anderson, Mark Livingston, Mark Lunt, Mark Davies, Gabriela Y C Moreno, Roger Gadsby, Robert J Young, Mike Stedman
AIMS: To determine, using published general practice-level data, how differences in Type 2 diabetes mellitus (T2DM) prescribing patterns relate to glycaemic target achievement levels. METHODS: Multiple linear regression modelling was used to link practice characteristics and defined daily dose (DDD) of different classes of medication in 2015/2016 and changes between that year and the year 2014/2015 in medication to proportion of patients achieving target glycaemic control (glycated haemoglobin A1c [HbA1c] ≤58 mmol/mol [7...
March 8, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29512235/glycaemic-control-and-treatment-of-type-2-diabetes-in-adults-aged-75-years-or-older
#13
Antonio Rodriguez-Poncelas, Joan Barrot-de la-Puente, Gabriel Coll de Tuero, Carles López-Arpí, Bogdan Vlacho, Flora Lopéz-Simarro, Xavier Mundet Tudurí, Josep Franch-Nadal
AIM: The aim of this study was to assess glycaemic control and prescribing practices of antihyperglycaemic treatment in patients with diabetes mellitus type 2 aged 75 years or older. METHODS: We analysed data from health electronic records from 4,581 persons attended at primary healthcare centres of the Institut Català de la Salut (ICS), in the Girona Sud area of Catalonia, Spain, during 2013 and 2016. Variables such as age, gender, body mass index (BMI), diabetes duration, age at diabetes diagnosis, glycated haemoglobin (HbA1c), creatinine, glomerular filtrate rate and the albumin/creatinine ratio in urine were collected...
March 2018: International Journal of Clinical Practice
https://www.readbyqxmd.com/read/29501322/do-sulphonylureas-still-have-a-place-in-clinical-practice
#14
REVIEW
Kamlesh Khunti, Sudesna Chatterjee, Hertzel C Gerstein, Sophia Zoungas, Melanie J Davies
Sulphonylureas have been commercially available since the 1950s, but their use continues to be associated with controversy. Although adverse cardiovascular outcomes in some observational studies have raised concerns about sulphonylureas, findings from relatively recent, robust, and high-quality systematic reviews have indicated no increased risk of all-cause mortality associated with sulphonylureas compared with other active treatments. Results from large, multicentre, randomised controlled trials such as the UK Prospective Diabetes Study and ADVANCE have confirmed the microvascular benefits of sulphonylureas, a reduction in the incidence or worsening of nephropathy and retinopathy, and no increase in all-cause mortality, although whether these benefits were due to sulphonylurea therapy and not an overall glucose-lowering effect could not be confirmed...
February 28, 2018: Lancet Diabetes & Endocrinology
https://www.readbyqxmd.com/read/29480037/pharmacological-management-of-diabetes-in-severe-mental-illness-a-comprehensive-clinical-review-of-efficacy-safety-and-tolerability
#15
REVIEW
John Lally, Aonghus O' Loughlin, Brendon Stubbs, Allys Guerandel, Donal O'Shea, Fiona Gaughran
The increased prevalence of Type 2 diabetes mellitus (T2DM) in severe mental illness (SMI) contributes to increased cardiovascular morbidity and reduced life expectancy for people with SMI. Areas covered: In the present clinical review, we summarize the efficacy, safety and tolerability of selected diabetic pharmacotherapy options in SMI and discuss the quality and strength of evidence. Expert commentary: General principles for treating T2DM in SMI involve identifying treatments which promote weight loss and which have low or no risk of hypoglycemia...
April 2018: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/29429476/-diagnosis-and-treatment-of-maturity-onset-diabetes-of-the-young-type-3
#16
Kathrine Rose, Alexander Sidelmann Christensen, Heidi Storgaard, Sofie Hædersdal, Torben Hansen, Filip Krag Knop, Tina Vilsbøll
Maturity onset diabetes of the young type 3 (MODY3) is the most prevalent type of monogenetic diabetes. Treatment guidelines differ from both Type 1 diabetes and Type 2 diabetes. First-line treatment is a long-acting sulphonylurea, which lowers the plasma glucose level effectively, however with the risk of hypoglycaemia. When hypoglycaemia is a problem, short-acting sulphonylureas, glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors may be used as alternatives. Metformin, glitazones and sodium glucose transporter 2-inhibitors have only limited applicability in MODY3...
February 5, 2018: Ugeskrift for Laeger
https://www.readbyqxmd.com/read/29371776/mutations-in-hnf1a-gene-are-not-a-common-cause-of-familial-young-onset-diabetes-in-iran
#17
Meysam Moghbeli, Bahram Naghibzadeh, Martha Ghahraman, Sedigheh Fatemi, Morteza Taghavi, Rahim Vakili, Mohammad Reza Abbaszadegan
Mutations in hepatocyte nuclear factor-1 alpha (HNF1A) as a homeodomain transcription factor which regulates variety of genes, are the most common cause of maturity-onset diabetes of the young (MODY). Detection of HNF1A mutations not only classifies the subtype, but also predicts the likely clinical course and may alters the method of treatment from insulin to the oral sulphonylureas, which is shown to improve glycemic control. The coding and promoter regions of HNF1A gene were screened for mutations in 34 unrelated Iranian MODY patients...
January 2018: Indian Journal of Clinical Biochemistry: IJCB
https://www.readbyqxmd.com/read/29368615/glitazones-and-alpha-glucosidase-inhibitors-as-the-second-line-oral-anti-diabetic-agents-added-to-metformin-reduce-cardiovascular-risk-in-type-2-diabetes-patients-a-nationwide-cohort-observational-study
#18
Cheng-Wei Chan, Chu-Leng Yu, Jiunn-Cherng Lin, Yu-Cheng Hsieh, Che-Chen Lin, Chen-Ying Hung, Cheng-Hung Li, Ying-Chieh Liao, Chu-Pin Lo, Jin-Long Huang, Ching-Heng Lin, Tsu-Juey Wu
OBJECTIVE: Metformin is the standard first-line drug for patients with Type 2 diabetes (T2DM). However, the optimal second-line oral anti-diabetic agent (ADA) remains unclear. We investigated the cardiovascular risk of various ADAs used as add-on medication to metformin in T2DM patients from a nationwide cohort. METHODS: T2DM patients using different add-on oral ADAs after an initial metformin therapy of > 90 days were identified from the Taiwan National Health Insurance Database...
January 24, 2018: Cardiovascular Diabetology
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
#19
Malin Nilsson, Jørgen Rungby, Nathan Lassota, Andreas D 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 2006-12 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/29322610/safety-and-efficacy-of-once-weekly-semaglutide-vs-additional-oral-antidiabetic-drugs-in-japanese-people-with-inadequately-controlled-type-2-diabetes-a-randomized-trial
#20
Kohei Kaku, Yuichiro Yamada, Hirotaka Watada, Atsuko Abiko, Tomoyuki Nishida, Jeppe Zacho, Arihiro Kiyosue
AIM: To evaluate the safety and efficacy of once-weekly subcutaneous semaglutide as monotherapy or combined with an oral antidiabetic drug (OAD) vs an additional OAD added to background therapy in Japanese people with type 2 diabetes (T2D) inadequately controlled on diet/exercise or OAD monotherapy. METHODS: In this phase III, open-label trial, adults with T2D were randomized 2:2:1 to semaglutide 0.5 mg or 1.0 mg, or one additional OAD (a dipeptidyl peptidase-4 inhibitor, biguanide, sulphonylurea, glinide, α-glucosidase inhibitor or thiazolidinedione) with a different mode of action from that of background therapy...
January 11, 2018: Diabetes, Obesity & Metabolism
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