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Sodium glucose transport inhibitors

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https://www.readbyqxmd.com/read/28105986/canagliflozin-dapagliflozin-and-empagliflozin-monotherapy-for-treating-type-2-diabetes-systematic-review-and-economic-evaluation
#1
Rhona Johnston, Olalekan Uthman, Ewen Cummins, Christine Clar, Pamela Royle, Jill Colquitt, Bee Kang Tan, Andrew Clegg, Saran Shantikumar, Rachel Court, J Paul O'Hare, David McGrane, Tim Holt, Norman Waugh
BACKGROUND: Most people with type 2 diabetes are overweight, so initial treatment is aimed at reducing weight and increasing physical activity. Even modest weight loss can improve control of blood glucose. If drug treatment is necessary, the drug of first choice is metformin. However, some people cannot tolerate metformin, which causes diarrhoea in about 10%, and it cannot be used in people with renal impairment. This review appraises three of the newest class of drugs for monotherapy when metformin cannot be used, the sodium-glucose co-transporter 2 (SGLT2) inhibitors...
January 2017: Health Technology Assessment: HTA
https://www.readbyqxmd.com/read/28101792/medical-management-of-diabesity-do-we-have-realistic-targets
#2
REVIEW
Joseph M Pappachan, Ananth K Viswanath
PURPOSE OF REVIEW: The global prevalence of "diabesity"-diabetes related to obesity-is increasing steadily over the past few decades because of the obesity epidemic. Although bariatric surgery is an effective treatment option for patients with diabesity, its limited availability, invasiveness, relatively high costs and the potential for surgical and postsurgical complications restrict its widespread use. Therefore, medical management is the only option for a majority of patients with diabesity...
January 2017: Current Diabetes Reports
https://www.readbyqxmd.com/read/28098449/targeting-type-2-diabetes-with-c-glucosyl-dihydrochalcones-as-selective-sodium-glucose-co-transporter-2-sglt2-inhibitors-synthesis-and-biological-evaluation
#3
Ana R Jesus, Diogo Vila-Viçosa, Miguel Machuqueiro, Ana P Marques, Timothy M Dore, Amélia P Rauter
Inhibiting glucose reabsorption by sodium glucose co-transporter proteins (SGLTs) in the kidneys is a relatively new strategy for treating type 2 diabetes. Selective inhibition of SGLT2 over SGLT1 is critical for minimizing adverse side effects associated with SGLT1 inhibition. A library of C-glucosyl dihydrochalcones and their dihydrochalcone and chalcone precursors was synthesized and tested as SGLT1/SGLT2 inhibitors using a cell-based fluorescence assay of glucose uptake. The most potent inhibitors of SGLT2 (IC50 = 9-23 nM) were considerably weaker inhibitors of SGLT1 (IC50 = 10-19 μM)...
January 18, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28086872/dapagliflozin-decreases-small-dense-low-density-lipoprotein-cholesterol-and-increases-high-density-lipoprotein-2-cholesterol-in-patients-with-type-2-diabetes-comparison-with-sitagliptin
#4
Toshiyuki Hayashi, Tomoyasu Fukui, Noriko Nakanishi, Saki Yamamoto, Masako Tomoyasu, Anna Osamura, Makoto Ohara, Takeshi Yamamoto, Yasuki Ito, Tsutomu Hirano
BACKGROUND: The sodium-glucose co-transporter-2 (SGLT-2) inhibitors have been reported to increase both low-density lipoprotein (LDL) and high-density lipoprotein (HDL)-cholesterol (C). This study aimed to determine how SGLT-2 inhibitors affect LDL and HDL-C subspecies. METHODS: This single center, open-label, randomized, prospective study included 80 patients with type 2 diabetes taking prescribed oral hypoglycemic agents. Patients were allocated to receive dapagliflozin (n = 40) or sitagliptin (n = 40) as add-on treatment...
January 13, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/28011230/sglt-2-inhibitors-their-pleiotropic-properties
#5
REVIEW
Natalia G Vallianou, Eleni Geladari, Christos E Kazazis
Type 2 diabetes mellitus has become a global pandemic. Nowadays, it is estimated that approximately 415 million people all over the world have diabetes. The sodium glucose co-transporters 2 inhibitors are a new class of glucose-lowering agents, which act through a novel mechanism by producing a decline in glucose re-absorption in the kidney, thereby increasing glycosuria and decreasing serum glucose levels. Data suggest that apart from lowering HbA1c, they produce a small but significant weight loss and a small decrease in blood pressure...
December 9, 2016: Diabetes & Metabolic Syndrome
https://www.readbyqxmd.com/read/27989651/the-impact-of-sglt2-inhibitors-compared-with-insulin-on-diabetic-bone-disease-in-a-mouse-model-of-type-1-diabetes
#6
Kathryn M Thrailkill, Jeffry S Nyman, R Clay Bunn, Sasidhar Uppuganti, Katherine L Thompson, Charles K Lumpkin, Evangelia Kalaitzoglou, John L Fowlkes
Skeletal co-morbidities in type 1 diabetes include an increased risk for fracture and delayed fracture healing, which are intertwined with disease duration and the presence of other diabetic complications. As such, chronic hyperglycemia is undoubtedly a major contributor to these outcomes, despite standard insulin-replacement therapy. Therefore, using the streptozotocin (STZ)-induced model of hypoinsulinemic hyperglycemia in DBA/2J male mice, we compared the effects of two glucose lowering therapies on the fracture resistance of bone and markers of bone turnover...
October 28, 2016: Bone
https://www.readbyqxmd.com/read/27981497/factors-affecting-canagliflozin-induced-transient-urine-volume-increase-in-patients-with-type-2-diabetes-mellitus
#7
Hiroyuki Tanaka, Kazuhiko Takano, Hiroaki Iijima, Hajime Kubo, Nobuko Maruyama, Toshio Hashimoto, Kenji Arakawa, Masanori Togo, Nobuya Inagaki, Kohei Kaku
INTRODUCTION: Sodium glucose co-transporter 2 (SGLT2) inhibitors exhibit diuretic activity, which is a possible mechanism underlying the cardiovascular benefit of these inhibitors. However, the osmotic diuresis-induced increase in urine volume, and the risk of dehydration have been of concern with SGLT2 inhibitor treatment. This study aimed to investigate the mechanism underlying SGLT2 inhibitor canagliflozin-induced diuresis in Japanese type 2 diabetes mellitus (T2DM) patients. METHODS: Thirteen T2DM patients received a daily oral dose of 100 mg canagliflozin before breakfast for 6 days...
December 15, 2016: Advances in Therapy
https://www.readbyqxmd.com/read/27972174/the-cost-of-glycaemic-target-achievement-with-sodium-glucose-co-transporter-2-sglt2-inhibitors-in-patients-with-type-2-diabetes-mellitus-t2dm-inadequately-controlled-on-metformin-and-sulphonylurea-met-su-in-the-uk
#8
M Evans, M Schroeder, A Schubert, C Neslusan
No abstract text is available yet for this article.
November 2016: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
https://www.readbyqxmd.com/read/27972149/an-assessment-of-the-relative-efficacy-of-sodium-glucose-co-transporter-2-inhibitors-as-add-on-to-metformin-in-patients-with-type-2-diabetes-mellitus
#9
C Whittington, A Schubert, C Neslusan
No abstract text is available yet for this article.
November 2016: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
https://www.readbyqxmd.com/read/27965450/functional-characterization-of-pneumocystis-carinii-inositol-transporter-1
#10
Melanie T Cushion, Margaret S Collins, Thomas Sesterhenn, Aleksey Porollo, Anish Kizhakkekkara Vadukoot, Edward J Merino
: Fungi in the genus Pneumocystis live in the lungs of mammals, where they can cause a fatal pneumonia (PCP [Pneumocystis pneumonia]) in hosts with compromised immune systems. The absence of a continuous in vitro culture system for any species of Pneumocystis has led to limited understanding of these fungi, especially for the discovery of new therapies. We recently reported that Pneumocystis carinii, Pneumocystis murina, and most significantly, Pneumocystis jirovecii lack both enzymes necessary for myo-inositol biosynthesis but contain genes with homologies to fungal myo-inositol transporters...
December 13, 2016: MBio
https://www.readbyqxmd.com/read/27898586/an-update-on-sodium-glucose-co-transporter-2-inhibitors-for-the-treatment-of-diabetes-mellitus
#11
Daniel S Hsia, Owen Grove, William T Cefalu
PURPOSE OF REVIEW: Sodium-glucose co-transporter-2 (SGLT2) inhibitors are the newest class of oral antihyperglycemic agents that have been approved for the treatment of diabetes mellitus. Over the past year, there have been significant developments in both the safety and efficacy of this class of medications that are presented in this review. RECENT FINDINGS: Apart from data on the glucose-lowering effect of SGLT2 inhibitors, other metabolic benefits have been demonstrated for this class of medications...
February 2017: Current Opinion in Endocrinology, Diabetes, and Obesity
https://www.readbyqxmd.com/read/27896705/does-gender-influence-the-cardiovascular-benefits-observed-with-sodium-glucose-co-transporter-2-sglt-2-inhibitors-a-meta-regression-analysis
#12
Ahmed N Mahmoud, Islam Y Elgendy, Marwan Saad, Akram Y Elgendy, Amr F Barakat, Amgad Mentias, Ahmed Abuzaid, Anthony A Bavry
INTRODUCTION: Although a large recent trial had shown improved cardiovascular outcomes of diabetic patients on sodium glucose co-transporter-2 (SGLT-2) inhibitors, the influence of gender differences on such outcomes is not known. Thus, we aimed to assess the impact of gender on such outcomes in the patients with type 2 diabetes mellitus receiving SGLT-2 inhibitors. METHODS: A search of electronic databases was conducted for all randomized trials comparing SGLT-2 inhibitors with placebo in patients with diabetes mellitus...
November 28, 2016: Cardiology and Therapy
https://www.readbyqxmd.com/read/27895093/stroke-paradox-with-sglt-2-inhibitors-a-play-of-chance-or-a-viscosity-mediated-reality
#13
REVIEW
Konstantinos P Imprialos, Chrysoula Boutari, Konstantinos Stavropoulos, Michael Doumas, Asterios I Karagiannis
Diabetes mellitus is a major risk factor for cardiovascular morbidity and mortality. Current therapeutic strategies have not provided constant beneficial cardiovascular-related results. Sodium-glucose co-transporters 2 (SGLT-2) inhibitors have emerged as a novel antidiabetic class of drugs that exert favourable results in a variety of other cardiovascular risk factors too, such as increased blood pressure and body weight. The Empagliflozin, Cardiovascular Outcomes, and Mortality in Type 2 Diabetes (EMPA-REG OUTCOME) study was the first trial that evaluated cardiovascular outcomes in patients with diabetes with the use of empagliflozin, a member of this new class of drugs...
November 28, 2016: Journal of Neurology, Neurosurgery, and Psychiatry
https://www.readbyqxmd.com/read/27894216/bone-effects-of-canagliflozin-a-sodium-glucose-co-transporter-2-inhibitor-in-patients-with-type-2-diabetes-mellitus
#14
Thomas C Blevins, Azeez Farooki
Canagliflozin, a sodium glucose co-transporter 2 (SGLT2) inhibitor approved for the treatment of type 2 diabetes mellitus (T2DM), lowers blood glucose by inhibiting renal glucose reabsorption and increasing urinary glucose excretion. It has been reported that SGLT2 inhibitors may have potential adverse effects on bone, including increased fracture risk and decreased bone mineral density (BMD). Across clinical studies, canagliflozin was not associated with meaningful changes in serum or urine calcium, vitamin D, or parathyroid hormone...
November 28, 2016: Postgraduate Medicine
https://www.readbyqxmd.com/read/27883364/determination-of-s-methyl-l-methionine-smm-from-brassicaceae-family-vegetables-and-characterization-of-the-intestinal-transport-of-smm-by-caco-2-cells
#15
Ji-Hoon Song, Hae-Rim Lee, Soon-Mi Shim
The objectives of the current study were to determine S-methyl-L-methionine (SMM) from various Brassicaceae family vegetables by using validated analytical method and to characterize the intestinal transport mechanism of SMM by the Caco-2 cells. The SMM is well known to provide therapeutic activity in peptic ulcers. The amount of SMM from various Brassicaceae family vegetables ranged from 89.08 ± 1.68 μg/g to 535.98 ± 4.85 μg/g of dry weight by using validated ultra-performance liquid chromatography-electrospray ionization-mass spectrometry method...
January 2017: Journal of Food Science
https://www.readbyqxmd.com/read/27867961/cardio-renal-protection-with-empagliflozin
#16
Richard J MacIsaac, George Jerums, Elif I Ekinci
Cardiovascular (CV) and kidney disease are common and significant complications in people with type 2 diabetes (T2DM). CV disease is the leading cause of death, morbidly and hospitalisations for people with T2DM. Furthermore, diabetic kidney disease is a major risk factor for CV disease and is the main reason why patients need renal replacement therapy. In this perspective, we highlight the results of the recent landmark EMPA-REG OUTCOME trial which has shown that empagliflozin, a member of the sodium-glucose co-transporter 2 (SGLT-2) inhibitor class of glucose lowering medications, reduces death from CV causes, hospitalisation for heart failure and progression to end stage kidney disease in patients with T2DM and established CV disease...
October 2016: Annals of Translational Medicine
https://www.readbyqxmd.com/read/27863704/cardiovascular-effects-of-glucose-lowering-therapies-for-type-2-diabetes-new-drugs-in-perspective
#17
REVIEW
Peter L Thompson, Timothy M E Davis
PURPOSE: The purpose of this study was to review the results of clinical trials assessing the cardiovascular effects of drugs for type 2 diabetes and the cardiovascular effects of newer available drugs. METHODS: We performed a detailed search of PubMed-listed publications, reports from international meetings, and ongoing studies from clinical trials.gov. FINDINGS: Currently available drugs have neutral or, in some cases, negative effects on cardiovascular outcomes...
November 15, 2016: Clinical Therapeutics
https://www.readbyqxmd.com/read/27858115/-the-new-esc-guidelines-for-acute-and-chronic-heart-failure-2016
#18
C U Oeing, C Tschöpe, B Pieske
The new guidelines for the diagnosis and treatment of acute and chronic heart failure (HF) were presented in May 2016 during the congress of the Heart Failure Association (HFA) of the European Society of Cardiology (ESC) in Florence. An important amendment affects the classification of HF which now differentiates between HF with preserved ejection fraction (HFpEF) and left ventricular EF (LVEF) > 50%, HF with reduced ejection fraction (HFrEF, LVEF < 40%) and the new entity HF with mid-range ejection fraction (HFmrEF, LVEF 40-49%)...
December 2016: Herz
https://www.readbyqxmd.com/read/27854055/fixed-dose-combination-of-canagliflozin-and-metformin-for-the-treatment-of-type-2-diabetes-an-overview
#19
REVIEW
Jaime A Davidson, Lance Sloan
: Metformin is recommended as a first-line therapy for patients with type 2 diabetes mellitus (T2DM). However, many patients do not achieve glycemic goals with metformin monotherapy and require subsequent combination therapy with other antihyperglycemic agents (AHAs). For newly diagnosed patients with high blood glucose, initial combination therapy may be required to achieve glycemic control. The American Association for Clinical Endocrinologists algorithm for the treatment of T2DM recommends metformin plus a sodium glucose co-transporter 2 (SGLT2) inhibitor as the first oral combination in patients who present with HbA1c ≥7...
January 2017: Advances in Therapy
https://www.readbyqxmd.com/read/27853064/impact-of-the-8-week-administration-of-tofogliflozin-for-glycemic-control-and-body-composition-in-japanese-patients-with-type-2-diabetes-mellitus
#20
Sachie Hirose, Shinsuke Nakajima, Yasuyuki Iwahashi, Akane Seo, Tetsuya Takahashi, Yoshikazu Tamori
Objective The adverse effects of selective sodium-glucose co-transporter 2 (SGLT2) inhibitors generally appear within about two or three months after treatment initiation in Japan. Therefore, we investigated the impact of tofogliflozin, a class of SGLT2 inhibitors, on glycemic control and body composition during this period in Japanese patients with type 2 diabetes mellitus. Methods This single-arm open-label study enrolled 20 patients. Patients received tofogliflozin 20 mg once daily for 8 weeks. At week 8, changes from baseline in body weight, serum metabolic markers, and body composition were evaluated...
2016: Internal Medicine
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