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sitagliptin

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https://www.readbyqxmd.com/read/29144805/dpp4-inhibitor-sitagliptin-as-a-potential-treatment-option-in-metformin-intolerant-obese-women-with-polycystic-ovary-syndrome-a-pilot-randomized-study
#1
Simona Ferjan, Andrej Janez, Mojca Jensterle
OBJECTIVE: Metformin has an established role in the management of polycystic ovary syndrome (PCOS). Some patients cannot tolerate it due to associated gastrointestinal adverse events. The present study evaluated DPP4 inhibitor sitagliptin as a potential treatment option in metformin intolerant PCOS. DESIGN: We conducted a 12-week prospective randomized open-label study with 30 obese metformin intolerant women with PCOS (aged 35.0±7.2 years, BMI 36.9±5.5 kg/m(2))...
November 16, 2017: Endocrine Practice
https://www.readbyqxmd.com/read/29138226/insulin-secretory-effect-of-sitagliptin-assessment-with-a-hyperglycemic-clamp-combined-with-a-meal-challenge
#2
Sudha S Shankar, R Ravi Shankar, Lori A Mixson, Deborah L Miller, Helmut O Steinberg, Chan R Beals, David E Kelley
Sitagliptin,a dipeptidylpeptidase-IVinhibitor(DPP-4),sustains activity of the incretin hormones GLP-1andGIP and improves hyperglycemia inT2DM.It has however proven challenging to quantify the effect of sitagliptin on rates of insulin secretion(ISR) during a prandial challenge.The tight feedback governance ofISR by plasma glucose means that in the face of treatment-related lowering of postprandialglycemia,corresponding stimulation ofISR is lessened.We postulated that sustaining a stable level of moderate hyperglycemia prior to and during a mealchallenge(MC)would be a platform that enables greater clarity to assess the effect ofsitagliptin onISR and an approach that could be valuable to evaluate novel targets that increase insulin secretion directly and by augmenting incretins...
November 14, 2017: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29136947/the-effect-of-the-dipeptidyl-peptidase-4-inhibitor-sitagliptin-on-gentamicin-nephrotoxicity-in-mice
#3
Yousuf M Al Suleimani, Aly M Abdelrahman, Turan Karaca, Priyadarsini Manoj, Mohammed Ashique, Abderrahim Nemmar, Badreldin H Ali
This study aimed at investigating the possible ameliorative effects of sitagliptin in mice with gentamicin (GEN) nephrotoxicity. Sitagliptin was given to the animals at an oral dose of 10mgkg(-1) per day for 10days, and in some of these mice, GEN was injected intraperitoneally at a dose of 100mgkg(-1) per day during the last seven days of the treatment. Nephrotoxicity was evaluated histopathologically by light microscopy and biochemically by measuring several indices in plasma, urine and renal cortex homogenates...
November 9, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29134558/development-of-hyperkalemia-following-treatment-with-dapagliflozin-dapa-in-a-patient-with-type-2-diabetes-after-bilateral-adrenalectomy
#4
Daichi Miyaoka, Akihiro Tsuda, Noriyuki Hayashi, Norikazu Toi, Akiyo Yamasaki, Yuki Nagata, Shinya Nakatani, Masafumi Kurajoh, Shinsuke Yamada, Tomoaki Morioka, Yasuo Imanishi, Masanori Emoto, Masaaki Inaba
Dapagliflozin (DAPA), a sodium-glucose co-transporter 2 (SGLT2) inhibitor, is known to have a beneficial diuretic effect, in addition to a glucose-lowering effect. Although SGLT2 inhibitor has been reported, the increase of hyperkalemia in patients treated with renin-angiotensin-aldosterone system (RAAS) inhibitors, their mechanism of action is unclear. We report the first case of a type 2 diabetes (T2DM) patient with potential mineralocorticoid deficiency who developed hyperkalemia after administration of DAPA...
November 13, 2017: CEN Case Reports
https://www.readbyqxmd.com/read/29132354/correction-to-dapagliflozin-decreases-small-dense-low-density-lipoprotein-cholesterol-and-increases-high-density-lipoprotein-2-cholesterol-in-patients-with-type-2-diabetes-comparison-with-sitagliptin
#5
Toshiyuki Hayashi, Tomoyasu Fukui, Noriko Nakanishi, Saki Yamamoto, Masako Tomoyasu, Anna Osamura, Makoto Ohara, Takeshi Yamamoto, Yasuki Ito, Tsutomu Hirano
Following publication of the original article [1], the authors identified a number of errors. In Result (P.3), Table 1 (P.4), Table 5 (P.9) and Supplementary Table 1, the correct unit for adiponectin was μg/mL. In Table 1 (P.4), the correct value for the post treatment body weight in dapagliflozin was 76.2±14.8. In Table 6 (P.10), the correct value for the pre treatment sd LDL/LDL-C in decreased LDL-C group was 0.38±0.10.
November 13, 2017: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/29122893/prospective-postmarketing-surveillance-of-acute-myocardial-infarction-in-new-users-of-saxagliptin-a-population-based-study
#6
Sengwee Toh, Marsha E Reichman, David J Graham, Christian Hampp, Rongmei Zhang, Melissa G Butler, Aarthi Iyer, Malcolm Rucker, Madelyn Pimentel, Jack Hamilton, Samuel Lendle, Bruce H Fireman
OBJECTIVE: The cardiovascular safety of saxagliptin, a dipeptidyl-peptidase 4 inhibitor, compared with other antihyperglycemic treatments is not well understood. We prospectively examined the association between saxagliptin use and acute myocardial infarction (AMI). RESEARCH DESIGN AND METHODS: We identified patients aged ≥18 years, starting from the approval date of saxagliptin in 2009 and continuing through August 2014, using data from 18 Mini-Sentinel data partners...
November 9, 2017: Diabetes Care
https://www.readbyqxmd.com/read/29114002/sdf-1%C3%AE-stromal-cell-derived-factor-1%C3%AE-induces-cardiac-fibroblasts-renal-microvascular-smooth-muscle-cells-and-glomerular-mesangial-cells-to-proliferate-cause-hypertrophy-and-produce-collagen
#7
Edwin K Jackson, Yumeng Zhang, Delbert D Gillespie, Xiao Zhu, Dongmei Cheng, Travis C Jackson
BACKGROUND: Activated cardiac fibroblasts (CFs), preglomerular vascular smooth muscle cells (PGVSMCs), and glomerular mesangial cells (GMCs) proliferate, cause hypertrophy, and produce collagen; in this way, activated CFs contribute to cardiac fibrosis, and activated PGVSMCs and GMCs promote renal fibrosis. In heart and kidney diseases, SDF-1α (stromal cell-derived factor 1α; endogenous CXCR4 [C-X-C motif chemokine receptor 4] receptor agonist) levels are often elevated; therefore, it is important to know whether and how the SDF-1α/CXCR4 axis activates CFs, PGVSMCs, or GMCs...
November 7, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/29113790/the-persistent-inhibitory-properties-of-saxagliptin-on-renal-dipeptidyl-peptidase-4-studies-with-hk-2-cells-in%C3%A2-vitro-and-normal-rats-in%C3%A2-vivo
#8
Masako Uchii, Mariko Sakai, Yuhei Hotta, Satoshi Saeki, Naoya Kimoto, Akinori Hamaguchi, Tetsuya Kitayama, Shunji Kunori
Saxagliptin, a potent and selective DPP-4 inhibitor, exhibits a slow dissociation from DPP-4. We investigated the sustained effects of saxagliptin on renal DPP-4 activity in a washout study using renal tubular (HK-2) cells, and in a pharmacodynamic study using normal rats. In HK-2 cells, the inhibitory potency of saxagliptin on DPP-4 activity persisted after washout, while that of sitagliptin was clearly reduced. In normal rats, a single treatment of saxagliptin or sitagliptin inhibited the plasma DPP-4 activity to similar levels...
October 23, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29101811/ameliorative-potential-of-sitagliptin-and-or-resveratrol-on-experimentally-induced-clear-cell-renal-cell-carcinoma
#9
Ahmed M Kabel, Aliaa Atef, Remon S Estfanous
The aim of this study was to assess the effect of sitagliptin with or without resveratrol on carcinogen-induced clear cell renal cell carcinoma. Sixty male Wistar rats were divided into 6 equal groups as follows: control; clear cell renal cell carcinoma group; clear cell renal cell carcinoma+sitagliptin group; clear cell renal cell carcinoma+resveratrol group; clear cell renal cell carcinoma+carboxymethyl cellulose group and clear cell renal cell carcinoma+sitagliptin+resveratrol group. Blood urea, serum creatinine, creatinine clearance, urinary N-acetyl beta-d-glucosaminidase (NAG), gamma glutamyl transpeptidase (GGT) and urinary albumin excretion rate (UAER) were determined...
November 1, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29100378/sitagliptin-attenuates-high-glucose-induced-alterations-in-migration-proliferation-calcification-and-apoptosis-of-vascular-smooth-muscle-cells-through-erk1-2-signal-pathway
#10
Lili Shi, Ye Ji, Dandan Liu, Ying Liu, Ying Xu, Yang Cao, Xiaoyan Jiang, Changqing Xu
Background/Aims: This study investigated the effects of sitagliptin on migration, proliferation, calcification and apoptosis of vascular smooth muscle cells (VSMCs) under high glucose (HG) conditions. Methods: VSMCs were isolated from the thoracic aorta of Sprague Dawley rats. The cultured VSMCs were subjected to control medium, mannitol medium, HG medium (25 mM), pretreatment with 200 nM sitagliptin in control or HG medium, or the ERK1/2 inhibitor PD98059 in HG medium...
September 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/29099829/tratamiento-con-fosfato-de-sitagliptina-en-pacientes-con-hipoglucemia-reactiva-secundaria-a-disinsulinismo-estudio-controlado-aleatorizado-y-doble-ciego
#11
Daniel Cuevas-Ramos, Paloma Almeda-Valdés, Clara E Meza-Arana, Griselda Brito-Córdova, Doris Georgina Ruiz-Gómez, Christian Razo, Francisco J Gómez-Pérez
Objective: We evaluated the effect of sitagliptin in correction of symptomatic reactive hypoglycemia. Methods: Randomized, double blind, placebo-controlled clinical trial. Thirteen patients treated with sitagliptin and 15 with placebo, with mean age of 34.3 ± 10.6 years and body mass index of 24.6 ± 5.1 kg/m(2), mostly women (n = 24, 85.7%), were evaluated. Results: Basal glycemia was similar in placebo versus sitagliptin (92.3 ± 18.9 vs...
2017: Gaceta Médica de México
https://www.readbyqxmd.com/read/29098166/renoprotective-effects-of-the-dipeptidyl-peptidase-4-inhibitor-sitagliptin-a-review-in-type-2-diabetes
#12
REVIEW
Cristina Mega, Edite Teixeira-de-Lemos, Rosa Fernandes, Flávio Reis
Diabetic nephropathy (DN) is now the single commonest cause of end-stage renal disease (ESRD) worldwide and one of the main causes of death in diabetic patients. It is also acknowledged as an independent risk factor for cardiovascular disease (CVD). Since sitagliptin was approved, many studies have been carried out revealing its ability to not only improve metabolic control but also ameliorate dysfunction in various diabetes-targeted organs, especially the kidney, due to putative underlying cytoprotective properties, namely, its antiapoptotic, antioxidant, anti-inflammatory, and antifibrotic properties...
2017: Journal of Diabetes Research
https://www.readbyqxmd.com/read/29072800/effect-of-sitagliptin-on-glucose-control-in-type-2-diabetes-mellitus-after-roux-en-y-gastric-bypass-surgery
#13
Ankit Shah, Kiarra Levesque, Esmeralda Pierini, Betsy Rojas, Michael Ahlers, Sarah Stano, Marlena Holter, Roxanne Dutia, Scott Belsley, James McGinty, Blandine Laferrère
This is a 4-week randomized trial to assess the efficacy and safety of sitagliptin, a dipeptidyl-peptidase-4 inhibitor, in persistent or recurring type 2 diabetes after gastric bypass surgery (RYGB). Subjects (n=32) completed a mixed meal test (MMT) and home glucose monitoring (SPMG) before and 4 weeks after randomization to either sitagliptin 100 mg daily (S) or placebo daily (P). Questionnaires were administered to assess gastrointestinal discomfort. Outcome variables were glucose, active GLP-1 and β-cell function during the MMT and glucose levels during SPMG...
October 26, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29070077/linagliptin-versus-sitagliptin-in-patients-with-type-2-diabetes-mellitus-a-network-meta-analysis-of-randomized-clinical-trials
#14
REVIEW
Khosro Keshavarz, Farhad Lotfi, Ehsan Sanati, Mahmood Salesi, Amir Hashemi-Meshkini, Mojtaba Jafari, Mohammad M Mojahedian, Behzad Najafi, Shekoufeh Nikfar
BACKGROUND: Diabetes is one of the most common chronic and costly diseases worldwide and type 2 diabetes is the most common type which accounts for about 90% of cases with diabetes. New medication-therapy regimens such as those containing linagliptin alone or in combination with other medications (within the category of DDP-4 inhibitors) must be evaluated in terms of efficacy and compared with other currently used drugs and then enter the medication list of the country. Hence, this study aimed to compare the clinical efficacy of the two drugs, i...
October 25, 2017: Daru: Journal of Faculty of Pharmacy, Tehran University of Medical Sciences
https://www.readbyqxmd.com/read/29064743/dipeptidyl-peptidase-4-inhibitor-sitagliptin-prevented-weight-regain-in-obese-women-with-polycystic-ovary-syndrome-previously-treated-with-liraglutide-a-pilot-randomized-study
#15
Simona Ferjan, Andrej Janez, Mojca Jensterle
BACKGROUND: Weight loss is often nonsustainable after liraglutide cessation. The present study is the first insight into the potential prevention of weight regain in obese subjects who have been withdrawn from liraglutide. We evaluated whether dipeptidyl peptidase-4 (DPP-4) inhibitor sitagliptin in adjunct to metformin prevents body weight regain more effectively than metformin alone in obese polycystic ovary syndrome (PCOS) previously treated with liraglutide. METHODS: A 12-week prospective randomized open-label study was conducted with 24 obese women with PCOS who had been pretreated with liraglutide 3...
October 24, 2017: Metabolic Syndrome and related Disorders
https://www.readbyqxmd.com/read/29057545/modelling-incremental-benefits-on-complications-rates-when-targeting-lower-hba1c-levels-in-people-with-type-2-diabetes-and-cardiovascular-disease
#16
S A Mostafa, R L Coleman, O F Agbaje, A M Gray, R R Holman, M A Bethel
AIM: Glucose-lowering interventions in Type 2 diabetes mellitus have demonstrated reductions in microvascular complications and modest reductions in macrovascular complications. However, the degree to which targeting different HbA1c reductions might reduce risk is unclear. METHODS: Participant-level data for Trial Evaluating Cardiovascular Outcomes with Sitagliptin (TECOS) participants with established cardiovascular disease were used in a Type 2 diabetes-specific simulation model to quantify the likely impact of different HbA1c decrements on complication rates...
October 23, 2017: Diabetic Medicine: a Journal of the British Diabetic Association
https://www.readbyqxmd.com/read/29042993/sitagliptin-ameliorates-high-glucose-induced-cell-proliferation-and-expression-of-the-extracellular-matrix-in-glomerular-mesangial-cells
#17
Guan-Ying Zhang, Dong-Dong Wang, Zheng Cao, Tong Wei, Chen-Xu Liu, Qun-Li Wei
Diabetic nephropathy (DN) is one of the most important causes that leads to end-stage renal disease and the efficacy of strategies currently available for the prevention of DN remains unsatisfactory. Sitagliptin (SIT), which is a dipeptidyl peptidase-4 inhibitor, exhibited a modest beneficial effect on glycated hemoglobin levels and is capable of ameliorating renal ischemia reperfusion injury. By determining the expression of transforming growth factor-β1 (TGF-β1), connective tissue growth factor (CTGF), collagen type IV (ColIV) and fibronectin (FN) levels in high glucose-cultured glomerular mesangial cells (MCs), the present study aimed to assess the anti-proliferative and anti-fibrotic effects of SIT on the therapeutic potential for the prevention of DN and its mechanism...
October 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29032011/sitagliptin-enhances-the-neuroprotective-effect-of-pregabalin-against-pentylenetetrazole-induced-acute-epileptogenesis-in-mice-implication-of-oxidative-inflammatory-apoptotic-and-autophagy-pathways
#18
Manar A Nader, Hayam Ateyya, Mohamed El-Shafey, Nagla A El-Sherbeeny
The current investigation aimed at studying the anti-epileptogenic effect of sitagliptin. The possible effect of the drug in combination with pregabalin in pentylenetetrazole (PTZ)- induced seizures was studied. In addition, the postulated mechanisms that could mediate such effect were explored namely, suppression of oxidative stress and neuro-inflammatory markers, autophagy and apoptosis. Seven days prior to PTZ (60 mg/kg, sc) injection, mice were treated with sitagliptin (5, 15, and 60 mg/kg, twice daily, orally) or pregabalin (30 mg/kg, once daily, orally) or their combination...
October 11, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/29026740/diabetes-and-ramadan-a-concise-and-practical-update
#19
REVIEW
Mohamed H Ahmed, Nazik Elmalaika Husain, Wadie M Elmadhoun, Sufian K Noor, Abbas A Khalil, Ahmed O Almobarak
Despite the fact that the month of Ramadan includes 29-30 days and the duration of fasting for each day can last for between 12 and 16 h, it was estimated that a large number of individuals with diabetes do fast during Ramadan. In light of recent advancement of new pharmacological agents, drugs such as vildagliptin, sitagliptin, and liraglutide were found to be safe to use during this month of fasting. These therapeutic agents can also be used in combination with metformin. The use of sulfonylureas, in most of the recent guidelines about diabetes and Ramadan, seems not to gain much support due to the risk of hypoglycemia...
January 2017: Journal of Family Medicine and Primary Care
https://www.readbyqxmd.com/read/29025406/impact-of-empagliflozin-on-subclinical-left-ventricular-dysfunctions-and-on-the-mechanisms-involved-in-myocardial-disease-progression-in-type-2-diabetes-rationale-and-design-of-the-empa-heart-trial
#20
Andrea Natali, Lorenzo Nesti, Iacopo Fabiani, Enrico Calogero, Vitantonio Di Bello
BACKGROUND: Asymptomatic left ventricular (LV) dysfunction is highly prevalent in type 2 diabetes patients. Unlike the other hypoglycemic drugs, SGLT2 inhibitors have shown potential benefits for reducing cardiovascular death and risk factors, aside from lowering plasma glucose levels. With this study we aim at determining whether the treatment with empagliflozin is associated with an improvement in LV functions in diabetic patients with asymptomatic LV dysfunction against Sitagliptin, which is presumably neutral on myocardial function...
October 12, 2017: Cardiovascular Diabetology
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