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https://www.readbyqxmd.com/read/29251018/cardiovascular-outcomes-with-canagliflozin-is-it-on-the-canvas
#1
Sheila Doggrell
Sodium-glucose cotransporter 2 (SGLT2) inhibitors (the 'gliflozins') promote the excretion of glucose from the kidney to lower HbA1c. Empagliflozin was the first gliflozin shown to improve cardiovascular and renal outcomes in subjects with type 2 diabetes and cardiovascular disease. Areas covered: In the Canagliflozin Cardiovascular Assessment Study (CANVAS) Program, there were improvements in the primary cardiovascular and exploratory renal outcomes with canagliflozin, compared to placebo. The safety outcome finding, which was of most interest, was that there was a higher risk of amputation of toes, feet, or legs with canagliflozin than in the placebo group...
December 18, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/29212337/-status-of-pharmacotherapy-in-current-care-of-obese
#2
Petr Sucharda
Weight loss drugs or anti-obesity drugs have a long history but are still far from being successful. Only in two last decades have the drugs been launched, which, when appropriately indicated, may be significantly beneficial to patients in need of weight loss as they are comparably effective to intensive programs to promote changes in eating habits and lifestyles. The combination naltrexone/bupropion is promising for food intake control including the reward mechanism, but the experience with its use has only been short-term...
2017: Casopís Lékar̆ů C̆eských
https://www.readbyqxmd.com/read/29211300/fluorine-directed-glycosylation-enables-the-stereocontrolled-synthesis-of-selective-sglt2-inhibitors-for-type-ii-diabetes
#3
Anna Sadurní, Gerald Kehr, Marie Ahlqvist, Helena Peilot Sjögren, Cecilia Kankkonen, Laurent Knerr, Ryan Gilmour
Inhibition of the sodium-glucose co-transporters (SGLT1 and SGLT2) is a validated strategy to address the increasing prevalence of type II diabetes mellitus. However, achieving selective inhibition of human SGLT1 or SGLT2 remains challenging. Orally available small molecule drugs based on the D-glucose core of the natural product Gliflozin have proven to be clinically effective in this regard, effectively impeding glucose reabsorption. Herein, we disclose the influence of molecular editing with fluorine at the C2 position of the pyranose ring of Phlorizin analogues Remogliflozin Etabonate and Dapagliflozin (Farxiga®) to concurrently direct β-selective glycosylation, as is required for biological efficacy, and enhance aspects of the physicochemical profile...
December 6, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29148749/glycosyl-cross-coupling-of-anomeric-nucleophiles-scope-mechanism-and-applications-in-the-synthesis-of-aryl-c-glycosides
#4
Feng Zhu, Jacob Rodriguez, Tianyi Yang, Ilia Kevlishvili, Eric Miller, Duk Yi, Sloane O'Neill, Michael Rourke, Peng Liu, Maciej A Walczak
Stereoselective manipulations at the C1 anomeric position of saccharides are one of the central goals of preparative carbohydrate chemistry. Historically, the majority of reactions forming a bond with anomeric carbon has focused on reactions of nucleophiles with saccharide donors equipped with a leaving group. Here, we describe a novel approach to stereoselective synthesis of C-aryl glycosides capitalizing on the highly stereospecific reaction of anomeric nucleophiles. First, methods for the preparation of anomeric stannanes have been developed and optimized to afford both anomers of common saccharides in high anomeric selectivities...
November 17, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29144574/sglt-2-inhibitors-and-ketoacidosis-a-disproportionality-analysis-in-the-world-health-organization-s-adverse-drug-reactions-database
#5
Abdel Nasser Ado Moumouni, Perrine Robin, Dominique Hillaire-Buys, Jean-Luc Faillie
SGLT-2 inhibitors, also called gliflozins, are a new class of drugs used in type 2 diabetes. Since their marketing, several cases of ketoacidosis, including life-threatening conditions, were reported with their use. The objective of this study was to investigate the disproportionality of pharmacovigilance reports of ketoacidosis between gliflozins and other drugs used for type 2 diabetes. We performed a case non-case study within the World Health Organization's pharmacovigilance database, VigiBase. We selected all reports of serious adverse drug reaction associated with a glucose-lowering drug in patients aged 40 years and older, from January 2013 to March 2016...
November 16, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/29127757/-gliflozins-slow-down-the-progression-of-diabetic-kidney-disease
#6
Vladimír Tesař, Jan Vachek
Until recently progression of diabetic kidney disease could have been slowed down only by the inhibition of the renin-angiotensin system. Inhibitors of SGLT2 (sodium-glucose transporter 2) in the proximal tubulus of the kidney induce natriuresis and by the activation of the tubuloglomerular feedback increase the tone of the afferent arteriole and decrease the glomerular pressure. Empagliflozin in the study EMPA-REG Outcome significantly decreased the risk of progression of diabetic kidney disease and further analyses also demonstrated its potent antiproteinuric effect...
2017: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/29127756/-diabetes-mellitus-and-cognitive-disorders-from-the-diabetologists-perspective
#7
Alena Šmahelová
Diabetes mellitus is associated with cognitive impairment which may convert to vascular or neurodegenerative dementia. Impairment of cognitive functions affects patients with type 1 and especially type 2 diabetes, with a number of vascular, metabolic and psychosocial factors involved in its development. As hyperglycemia and hypoglycemia also play an important role, important is the correct strategy of diabetes therapy which utilizes a combination of metformin with modern safe antidiabetics (incretin drugs, gliflozins, insulin analogues)...
2017: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/29127747/-treatment-strategy-of-type-2%C3%A2-diabetes-used-in-czech-republic-after-metformin-therapy-failure
#8
Štěpán Svačina, Petra Ovesná, Matyáš Kuhn, Martina Nováčková
INTRODUCTION: Type 2 diabetes is an enormous medical problem caused by increasing prevalence of the disease and increasing prevalence of severe chronic complications of diabetes. New ADA/EASD guidelines and also Czech diabetes society guidelines enable effective individual approach to the patient. Goal of the therapy is optimal compensation of diabetes and prevention of acute and chronic complications of diabetes and decrease of mortality. Diabetes therapy is started by education in diet a regime combined with metformin...
2017: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/28845946/-nephrolithiasis-coexisting-with-type-2-diabetes-current-concept-of-the-features-of-stone-formation-and-the-effects-of-hypoglycemic-therapy-on-lithogenesis
#9
REVIEW
S K Yarovoi, S A Golovanov, M R Khaziakhmetova, O V Dzhalilov
The article analyzes Russian and international literature examining specific features of the pathogenesis of renal stones in the setting of carbohydrate metabolism disorders. The authors outline the renal effects of the main pharmacological groups of oral hypoglycemic drugs regarding metaphylaxis of nephrolithiasis. An increased risk of nephrolithiasis in type 2 diabetes mellitus is realized through hyperuricemia with concurrent urine acidification. Current literature is lacking studies on the effects of oral hypoglycemic drugs on urine properties...
July 2017: Urologii︠a︡
https://www.readbyqxmd.com/read/28837279/-cardiorenal-protection-with-sglt2-inhibitors-gliflozins-from-empa-reg-outcome-to-canvas
#10
André J Scheen, Philippe Ernest, Bernard Jandrain
The cardiovascular (CV) and renal protection reported with empagliflozin in EMPA-REG OUTCOME is now confirmed with canagliflozin in CANVAS in patients with type 2 diabetes and high cardiovascular risk: similar and significant reductions in major CV events (-14 vs. -14%), in hospitalisations for heart failure (-35 vs. -33%) and in renal events (-39 vs. -40%). The greater reduction in CV mortality (-38 vs. - 13%) and all-cause mortality (-32 vs. -13%) in EMPA-REG OUTCOME than in CANVAS may be explained by the greater proportion of patients with CV disease (secondary prevention : 99 vs...
August 23, 2017: Revue Médicale Suisse
https://www.readbyqxmd.com/read/28837278/-therapeutic-options-for-a-type-2-diabetic-patient-not-well-controlled-with-metformin-plus-basal-insulin
#11
André J Scheen, Nicolas Paquot
In a patient with type 2 diabetes not well controlled with a basal insulin - metformin combination, several therapeutic options may be considered: intensifying insulin therapy with different schemes (appropriate titration using a more favourable basal insulin analogue, adding one, two or three rapid-acting insulin analogues, shift to two or three premix insulin injections), adding a dipeptidyl peptidase-4 inhibitor (gliptin) or an inhibitor of sodium-glucose cotransporters type 2 (gliflozin), or combining a glucagon-like peptide-1 receptor agonist with basal insulin...
August 23, 2017: Revue Médicale Suisse
https://www.readbyqxmd.com/read/28837277/-dpp-4-or-sglt2-inhibitor-added-to-metformin-alone-in-type-2-diabetes
#12
Nicolas Paquot, André J Scheen
After failure of a monotherapy with metformin, dipeptidyl peptidase-4 inhibitors (gliptins) and sodium-glucose cotransporters type 2 (gliflozins) offer an alternative to the add-on of a sulphonylurea, especially in diabetic patients at risk of hypoglycaemia. The choice between a gliptin and a gliflozin may be guided by the individual patient characteristics : rather a gliptin in a patient without obesity or severe hyperglycaemia, in an elderly patient, with a frailty profile or with renal impairment; rather a gliflozin in an obese patient, with hypertension, hyperuricaemia, antecedents of cardiovascular disease (especially heart failure), without advanced renal insufficiency and with a low risk of urinary/genital infections or events linked to dehydration such as hypotension...
August 23, 2017: Revue Médicale Suisse
https://www.readbyqxmd.com/read/28790046/gliflozins-and-reducing-cardiovascular-events-and-other-stories
#13
(no author information available yet)
No abstract text is available yet for this article.
August 8, 2017: BMJ: British Medical Journal
https://www.readbyqxmd.com/read/28760223/clinical-profile-of-patients-with-type-2-diabetes-mellitus-treated-with-sodium-glucose-cotransporter-2-inhibitors-and-experience-in-real-world-clinical-practice-in-spain
#14
Gabriel Cuatrecasas, Fernando Goñi-Goicoechea
The main aim of the treatment of type 2 diabetes is overall control of cardiovascular risk factors. Almost 50% of patients with type 2 diabetes do not achieve glycaemic targets, and a much higher percentage do not achieve weight and blood pressure targets, despite the therapeutic arsenal that has appeared in the last decade for the treatment of this disease. In addition, antidiabetic secretatogues and insulin are associated with weight gain and an increased risk of hyperglycaemic episodes. Clinical practice guidelines recommend sodium-glucose cotransporter-2 inhibitors (SGLT2i) as an alternative in the same therapeutic step as the other options after initiation of metformin therapy...
November 2016: Medicina Clínica
https://www.readbyqxmd.com/read/28671793/-gliptin-gliflozin-combination-for-treating-type-2-diabetes
#15
André J Scheen, Nicolas Paquot
Type 2 diabetes (T2D) is a complex disease with multiple defects, which generally require a combination of several pharmacological approaches to control hyperglycaemia. Combining a dipeptidyl peptidase-4 inhibitor (DPP-4i) and a sodium-glucose cotransporter type 2 inhibitor (SGT2i) appears to be an attractive approach because the two drugs exert different and potentially complementary glucose-lowering effects. Dual therapy (initial combination or stepwise approach) is more potent than either monotherapy in patients treated with diet and exercise or already treated with metformin...
August 24, 2016: Revue Médicale Suisse
https://www.readbyqxmd.com/read/28592411/gliflozins-and-reducing-cardiovascular-events-and-other-stories
#16
(no author information available yet)
No abstract text is available yet for this article.
June 7, 2017: BMJ: British Medical Journal
https://www.readbyqxmd.com/read/28520449/-novelties-in-the-treatment-of-heart-failure
#17
REVIEW
Filip Souček, Jan Novak
Heart failure (HF) is a complex clinical syndrome which is manifested by characteristic symptoms and objective signs of cardiac insufficiency. The incidence of HF, particularly its chronic form, is estimated 0.4-2 % in the central and western Europe, with an increase in higher age groups, affecting 10-20 % of the population aged over 80. With respect to its growing incidence and prevalence, novel modalities of pharmacological and non-pharmacological treatment are being developed in order to improve quality of life and survival of the affected patients...
December 0: Vnitr̆ní Lékar̆ství
https://www.readbyqxmd.com/read/28387494/-optimizing-basal-insulin-therapy-in-type-2-diabetes
#18
A J Scheen, N Paquot
Because of the natural history of type 2 diabetes and the increasing life expectancy, more and more patients are treated with insulin after failure of oral therapy. International guidelines give the preference to basal insulin, most often while maintaining metformin. If this treatment does not allow to reach the glycaemic objectives, optimizing therapy is mandatory. This clinical case offers the opportunity of discussing both advantages and disadvantages of three therapeutic options : the shift from basal insulin to a basal-plus or a basal-bolus insulin regimen, the addition of another oral glucose-lowering agent, either a dipeptidyl peptidase-4 inhibitor (gliptin) or an inhibitor of cotransporters sodium-glucose type 2 cotransporters (gliflozin), or the combination of basal insulin and a glucagon-like peptide-1 receptor agonist...
March 2017: Revue Médicale de Liège
https://www.readbyqxmd.com/read/28387100/-about-the-choice-between-a-dpp-4-inhibitor-and-a-sglt-2-inhibitor-tor-treating-type-2-diabetes
#19
REVIEW
A J Scheen, N Paquot
Two new classes of oral antidiabetic agents play an increasing role in the management of type 2 diabetes, dipeptidyl peptidase-4 (DPP-4) inhibitors (gliptins) and sodiumglucose cotransporters type 2 (SGLT2) inhibitors (gliflozins). After failure of a monotherapy with metformin (first pharmacological choice in type 2 diabetes), both may offer an alternative to the add-on of a sulphonylurea, especially in patients at risk of hypoglycaemia. However, the choice between a DPP-4 inhibitor and a SGLT2 inhibitor is not easy and should be oriented based upon the individual patient characteristics...
December 2016: Revue Médicale de Liège
https://www.readbyqxmd.com/read/28138853/sodium-glucose-co-transporter-2-sglt2-inhibitors-comparing-trial-and-real-world-use-study-protocol
#20
Andrew McGovern, Michael Feher, Neil Munro, Simon de Lusignan
BACKGROUND: Sodium-glucose co-transporter-2 (SGLT2) inhibitors (gliflozins) are the newest class of medication available to treat type 2 diabetes (T2DM). Recent findings from the first complete cardiovascular safety trial in SGLT2 inhibitors, the Empagliflozin, Cardiovascular Outcomes, and Mortality in type 2 diabetes (EMPA-REG OUTCOMES) trial, demonstrated reduced cardiovascular outcomes in people with high cardiovascular risk. How to apply these findings to clinical practice remains unclear, with questions remaining on who will reap this cardiovascular benefit...
April 2017: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
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