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sitagliptin

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https://www.readbyqxmd.com/read/27922176/dipeptidyl-peptidase-4-inhibitor-sitagliptin-reduces-inflammation-fibrosis-and-preserves-diastolic-function-in-a-rat-model-of-heart-failure-with-preserved-ejection-fraction
#1
Grazia Esposito, Donato Cappetta, Rosa Russo, Alessia Rivellino, Loreta Pia Ciuffreda, Fiorentina Roviezzo, Elena Piegari, L Liberato Berrino, Francesco Rossi, Antonella De Angelis, Konrad Urbanek
BACKGROUND AND PURPOSE: Heart failure with preserved ejection fraction (HFpEF) is a systemic syndrome driven by co-morbidities and its pathophysiology is poorly understood. Several studies suggesting that dipeptidyl peptidase 4 (DPP4) might be involved in the pathophysiology of heart failure prompted experimental and clinical investigations of DPP4 inhibitors on cardiovascular system. The aim of our study was to determine whether DPP4 inhibitor sitagliptin (SITA) affects the progression of HFpEF independently from the effects on glycaemia...
December 6, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27918671/dpp-4-inhibitor-treatment-in-chinese-type-2-diabetes-patients-a-meta-analysis
#2
Xiaoling Cai, Xueying Gao, Wenjia Yang, Yifei Chen, Lingli Zhou, Simin Zhang, Xueyao Han, Linong Ji
BACKGROUND: The aim of this meta-analysis was to assess the comprehensive clinical efficacy of dipeptidyl peptidase-IV (DPP-4) inhibitors in Chinese type 2 diabetes patients and to evaluate whether there is a different response to treatment with different kinds of DPP-4 inhibitors in those patients. METHODS: Databases were systematically searched, and qualifying clinical studies of Chinese type 2 diabetes patients were included. RESULTS: A total of 30 studies were included...
December 5, 2016: Diabetes Technology & Therapeutics
https://www.readbyqxmd.com/read/27916420/potential-involvement-of-jnk1-repression-in-the-hepatic-effect-of-sitagliptin-and-metformin-in-rats-subjected-to-high-fat-diet-and-chronic-mild-distress
#3
Yosra M Magdy, Omnyah A El-Kharashi, Enas S Nabih, Safaa M Shaker, Lobna F Abd-Elaziz, Sawsan Aboul-Fotouh
BACKGROUND: Depression and non-alcoholic steatohepatitis (NASH) are highly co-morbid, and hepatic JNK pathway may be involved in their relation. AIM: To evaluate the impact of depression on NASH through the involvement of JNK1 and to assess the effect of sitagliptin and metformin on hepatic JNK1 expression in both NASH and NASH associated with depression. METHODS: Eight groups of male Wistar rats were used: naïve rats, non-stressed NASH, non-stressed NASH sitagliptin treated, non-stressed NASH metformin treated, stressed, stressed NASH untreated, stressed NASH sitagliptin treated and stressed NASH metformin treated...
December 1, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27905912/effect-of-sitagliptin-on-blood-glucose-control-in-patients-with-type-2-diabetes-mellitus-who-are-treatment-naive-or-poorly-responsive-to-existing-antidiabetic-drugs-the-jamp-study
#4
Hiroshi Sakura, Naotake Hashimoto, Kazuo Sasamoto, Hiroshi Ohashi, Sumiko Hasumi, Noriko Ujihara, Tadasu Kasahara, Osamu Tomonaga, Hideo Nunome, Masashi Honda, Yasuhiko Iwamoto
BACKGROUND: To investigate the ameliorating effect of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on blood glucose control in patients with type 2 diabetes mellitus who were previously untreated with or who have a poor responsive to existing antidiabetic drugs. METHODS: Sitagliptin (50 mg/day) was added on to the pre-existing therapy for type 2 diabetes and changes in the glycated hemoglobin (HbA1c) level after 3 months of treatment were compared with the baseline and performed exploratory analysis...
December 1, 2016: BMC Endocrine Disorders
https://www.readbyqxmd.com/read/27904111/restoration-of-the-hypothalamic-pituitary-adrenal-response-to-hypoglycemia-in-type-2-diabetes-by-avoiding-chronic-hypoglycemia
#5
Shin-Ichi Tsuda, Kazunori Konishi, Toshiki Otoda, Takako Nagai, Ai Takeda-Watanabe, Megumi Kanasaki, Munehiro Kitada, Atsushi Nakagawa, Makoto Nishizawa, Keizo Kanasaki, Daisuke Koya
An impaired ability to sense and respond to drug-induced hypoglycemia is a common and serious complication in diabetic patients. The hypothalamic-pituitary-adrenal (HPA) axis activity plays a critical role in the counterregulatory response to hypoglycemia. We herein report a case that experienced restoration of a blunted HPA axis by avoiding hypoglycemia with the use of the DPP-4 inhibitor sitagliptin.
2016: Internal Medicine
https://www.readbyqxmd.com/read/27895112/hepatic-dipeptidyl-peptidase-4-controls-pharmacokinetics-of-vildagliptin-in-vivo
#6
Mitsutoshi Asakura, Tatsuki Fukami, Miki Nakajima, Hideaki Fujii, Koichiro Atsuda, Tomoo Itoh, Ryoichi Fujiwara
The major metabolic pathway of vildagliptin, which is an inhibitor of dipeptidyl peptidase-4 (DPP-4), in humans is hydrolysis at the cyano group to produce a carboxylic acid metabolite M20.7. Our in vitro study previously demonstrated that DPP-4 itself greatly contributed to the hydrolysis of vildagliptin in mouse, rat, and human livers. To investigate whether hepatic DPP-4 contributes to the hydrolysis of vildagliptin in vivo, in the present study, we conducted in vivo pharmacokinetics studies of vildagliptin in mice co-administered with vildagliptin and sitagliptin, which is another DPP-4 inhibitor, and also in streptozotocin (STZ)-induced diabetic mice...
November 28, 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/27889414/changes-in-glucose-induced-plasma-active-glucagon-like-peptide-1-levels-by-co-administration-of-sodium-glucose-cotransporter-inhibitors-with-dipeptidyl-peptidase-4-inhibitors-in-rodents
#7
Takahiro Oguma, Chiaki Kuriyama, Keiko Nakayama, Yasuaki Matsushita, Kumiko Hikida, Minoru Tsuda-Tsukimoto, Akira Saito, Kenji Arakawa, Kiichiro Ueta, Masabumi Minami, Masaharu Shiotani
We investigated whether structurally different sodium-glucose cotransporter (SGLT) 2 inhibitors, when co-administered with dipeptidyl peptidase-4 (DPP4) inhibitors, could enhance glucagon-like peptide-1 (GLP-1) secretion during oral glucose tolerance tests (OGTTs) in rodents. Three different SGLT inhibitors-1-(β-d-Glucopyranosyl)-4-chloro-3-[5-(6-fluoro-2-pyridyl)-2-thienylmethyl]benzene (GTB), TA-1887, and canagliflozin-were examined to assess the effect of chemical structure. Oral treatment with GTB plus a DPP4 inhibitor enhanced glucose-induced plasma active GLP-1 (aGLP-1) elevation and suppressed glucose excursions in both normal and diabetic rodents...
October 28, 2016: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/27885251/postprandial-and-orthostatic-hypotension-treated-by-sitagliptin-in-a-patient-with-dementia-with-lewy-bodies
#8
Yoshihiro Saito, Joji Ishikawa, Kazumasa Harada
BACKGROUND Postprandial hypotension, induced by an absorption of glucose from intestine, could be treated by acarbose; however, it was unclear whether dipeptidyl peptidase-4 inhibitor reduced postprandial hypotension. CASE REPORT A 78-year-old woman who had experienced episodes of dizziness and hypotension after eating was admitted to our hospital. During 24-hour ambulatory blood pressure monitoring, there were repeated episodes of marked postprandial hypotension; i.e., a significant systolic blood pressure reduction within two hours after eating (from -58 to -64 mm Hg after meals)...
November 25, 2016: American Journal of Case Reports
https://www.readbyqxmd.com/read/27882107/effects-of-sitagliptin-as-initial-therapy-in-newly-diagnosed-elderly-type-2-diabetics-a-randomized-controlled-study
#9
Xiaoyan Xiao, Xiaopei Cui, Jianbo Zhang, Zhenxia Han, Yu Xiao, Nan Chen, Baoying Li, Mei Cheng, Haiqing Gao, Kuanxiao Tang
The objective of this study was to investigate the characteristics of blood glycemic excursion, incretins and pancreatic hormone secretion in elderly people with newly diagnosed type 2 diabetes mellitus (T2DM) and to study the effects of sitagliptin on glycemic excursion in these subjects. A total of 129 newly diagnosed T2DM patients were enrolled in the study from March 2012 to August 2013. Clinical data, serum incretin, pancreatic hormone and continuous glucose monitoring data were collected. Among these subjects, elderly patients (NEDM) randomly received metformin combined with sitagliptin phosphate or glimepiride for 24 weeks...
November 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/27881129/impact-of-dipeptidyl-peptidase-4-inhibitors-on-serum-adiponectin-a-meta-analysis
#10
Xin Liu, Peng Men, Yuhui Wang, Suodi Zhai, George Liu
BACKGROUND: Adiponectin, an adipose-specific protein, is negatively correlated with pro-atherogenic low-density lipoprotein cholesterol (LDL-C) and other cardiovascular risk factors such as insulin resistance. Therefore, low levels of adiponectin are associated with a higher risk for diabetes and cardiovascular disease. Dipeptidyl peptidase-4 inhibitors (DPP4i) have been used for the treatment of type 2 diabetes mellitus (T2DM) as reversible inhibitors through interacting with DPP4 substrate and increase serum incretins such as glucagon-like peptide-1 (GLP-1)...
November 23, 2016: Lipids in Health and Disease
https://www.readbyqxmd.com/read/27870481/glycemic-effect-and-safety-of-a-systemic-partial-glucokinase-activator-pf-04937319-in-patients-with-type-2-diabetes-mellitus-inadequately-controlled-on-metformin-a-randomized-crossover-active-controlled-study
#11
William S Denney, Douglas S Denham, Michael R Riggs, Neeta B Amin
Glucokinase enhances glucose conversion to glucose-6-phosphate, causing glucose-stimulated insulin secretion from pancreatic β cells and increased hepatic glucose uptake. PF-04937319 is a partial glucokinase activator designed to maintain efficacy with reduced hypoglycemia risk. In this randomized, double-blind, double-dummy, 3-period crossover phase 1b study, patients aged 18-70 years with type 2 diabetes mellitus and on metformin received once-daily PF-04937319 (300 mg), split-dose PF-04937319 (150+100 mg; breakfast+lunch), or sitagliptin (100 mg once daily)...
November 2016: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/27851501/1866-angioedema-from-combination-sitagliptin-and-lisinopril-in-a-diabetic-patient
#12
Melissa Thompson Bastin, Allie Curlin, Alexander Flannery
No abstract text is available yet for this article.
December 2016: Critical Care Medicine
https://www.readbyqxmd.com/read/27844335/cardiovascular-safety-of-incretin-based-therapies-in-type-2-diabetes-systematic-review-of-integrated-analyses-and-randomized-controlled-trials
#13
REVIEW
Edoardo Mannucci, Matteo Monami
INTRODUCTION: Regulatory requirements mandate that new drugs for treatment of patients with type 2 diabetes mellitus (T2DM), such as dipeptidyl peptidase-4 (DPP-4) inhibitors and glucagon-like peptide-1 (GLP-1) receptor agonists, are evaluated to show that they do not increase cardiovascular (CV) risk. METHODS: A systematic review was undertaken to evaluate the association between DPP-4 inhibitor and GLP-1 receptor agonist use and major adverse cardiac events (MACE)...
November 14, 2016: Advances in Therapy
https://www.readbyqxmd.com/read/27835045/cardiovascular-outcomes-of-new-medications-for-type-2-diabetes
#14
Jennifer M Trujillo, Sara A Wettergreen, Wesley A Nuffer, Samuel L Ellis, Michael T McDermott
Cardiovascular (CV) disease remains the leading cause of death in people with diabetes, highlighting the importance of using treatment options that do not increase CV risk or possibly decrease CV outcomes. Since 2008, the Food and Drug Administration has required demonstration of CV safety for all new medications developed for the glycemic management of diabetes. Seven trials have been published that have established CV safety for three DPP-4 inhibitors (alogliptin, saxagliptin, and sitagliptin), three GLP-1 receptor agonists (liraglutide, lixisenatide, and semaglutide), and one sodium-glucose cotransporter-2 inhibitor (empagliflozin)...
November 11, 2016: Diabetes Technology & Therapeutics
https://www.readbyqxmd.com/read/27832184/comparative-binding-analysis-of-dipeptidyl-peptidase-iv-dpp-4-with-antidiabetic-drugs-an-ab-initio-fragment-molecular-orbital-study
#15
Sundaram Arulmozhiraja, Naoya Matsuo, Erika Ishitsubo, Seiji Okazaki, Hitoshi Shimano, Hiroaki Tokiwa
Dipeptidyl peptidase IV (DPP-4) enzyme is responsible for the degradation of incretins that stimulates insulin secretion and hence inhibition of DPP-4 becomes an established approach for the treatment of type 2 diabetics. We studied the interaction between DPP-4 and its inhibitor drugs (sitagliptin 1, linagliptin 2, alogliptin 3, and teneligliptin 4) quantitatively by using fragment molecular orbital calculations at the RI-MP2/cc-pVDZ level to analyze the inhibitory activities of the drugs. Apart from having common interactions with key residues, inhibitors encompassing the DPP-4 active site extensively interact widely with the hydrophobic pocket by their hydrophobic inhibitor moieties...
2016: PloS One
https://www.readbyqxmd.com/read/27832040/a-randomized-controlled-study-of-sitagliptin-for-treating-diabetes-mellitus-complicated-by-nonalcoholic-fatty-liver-disease
#16
Xiao-Long Deng, Rui Ma, Hong-Xia Zhu, Jun Zhu
BACKGROUND: This study aimed to evaluate the efficacy and safety of sitagliptin for treating Chinese patients with type 2 diabetes mellitus (T2DM) with nonalcoholic fatty liver disease (NAFLD). METHODS: In total, 72 Chinese T2DM patients with NAFLD were divided randomly into two groups of 36 patients each group. All 72 patients were assigned to receive either sitagliptin or diet and exercise for 52 weeks between January 2013 and December 2015. The outcomes' measurements included serum levels of hemoglobin A1c, fasting plasma glucose, aspartate aminotransferase, and alanine aminotransferase...
November 9, 2016: European Journal of Gastroenterology & Hepatology
https://www.readbyqxmd.com/read/27830456/liraglutide-improves-cardiac-function-in-patients-with-type-2-diabetes-and-chronic-heart-failure
#17
F Arturi, E Succurro, S Miceli, C Cloro, M Ruffo, R Maio, M Perticone, G Sesti, F Perticone
PURPOSE: To compare the effect of liraglutide, sitagliptin and insulin glargine added to standard therapy on left ventricular function in post-ischemic type-2 diabetes mellitus patients. METHODS: We evaluated 32 type-2 diabetes mellitus Caucasians with history of post-ischemic chronic heart failure NYHA class II/III and/or left ventricular ejection fraction ≤45 %. Participants underwent laboratory determinations, electrocardiogram, echocardiogram, Minnesota Living with Heart Failure questionnaire and 6 min walking test at baseline and following 52 weeks treatment...
November 9, 2016: Endocrine
https://www.readbyqxmd.com/read/27809848/impact-of-glycemic-control-with-sitagliptin-on-the-2-year-progression-of-arterial-stiffness-a-sub-analysis-of-the-prologue-study
#18
Hirofumi Tomiyama, Takashi Miwa, Kenshi Kan, Munehide Matsuhisa, Haruo Kamiya, Mamoru Nanasato, Tomoki Kitano, Hiroaki Sano, Jun Ohno, Masato Iida, Masataka Sata, Hirotsugu Yamada, Koji Maemura, Atsushi Tanaka, Toyoaki Murohara, Koichi Node
BACKGROUND: No conclusive evidence has been obtained yet on the significance of the effects of dipeptidyl peptidase-4 (DPP-4 inhibitor) treatment on the arterial stiffness in clinical settings. In addition, the effects of good glycemic control on the arterial stiffness have also not been clarified yet. As a sub-analysis of the PROLOGUE study, we examined the effect of a DPP-4 inhibitor (sitagliptin) on the 2-year progression of the arterial stiffness and also to determine the effect of good glycemic control on the rate of progression of the arterial stiffness...
November 3, 2016: Cardiovascular Diabetology
https://www.readbyqxmd.com/read/27805342/management-of-sitagliptin-and-metformin-combination-toxic-overdose
#19
Sudhish Sehra, Shalini Jaggi, Devindra Sehra, Rajesh Aggarwal, Vikas Saraswat, Deven Juneja
Metformin and Sitagliptin are often used in combination in the management of non-insulin dependent diabetes mellitus. Though toxicity is rare, but occurs more frequently in cases of intentional or unintentional overdose of these drugs. Here, we present a case of an intentional overdose of a metformin- sitagliptin combination (70g metformin and 3500mg sitagliptin) in a suicide attempt by a young non-diabetic female who presented with severe lactic acidosis and was successfully treated with prompt hemodialysis and bicarbonate therapy...
November 2016: Journal of the Association of Physicians of India
https://www.readbyqxmd.com/read/27789327/chronic-administration-of-ethanol-leaf-extract-of-moringa-oleifera-lam-moringaceae-may-compromise-glycaemic-efficacy-of-sitagliptin-with-no-significant-effect-in-retinopathy-in-a-diabetic-rat-model
#20
Comfort Olurishe, Helen Kwanashie, Abdulkadiri Zezi, Nuhu Danjuma, Bisalla Mohammed
ETHNOPHARMACOLOGICAL RELEVANCE: Moringa oleifera Lam. (Moringaceae) has gained awareness for its antidiabetic effect, and is used as alternative therapy or concurrently with orthodox medicines such as sitagliptin in diabetes mellitus. This is without ascertaining the possibility of drug-herb interactions, which could either lead to enhanced antidiabetic efficacy, increased toxicity, or compromised glycaemic control with negative consequence in diabetic retinopathy. AIM OF THE STUDY: To investigate the effect, of sitagliptin (50mg/kg), Moringa oleifera (300mg/kg) leaf extract, and a combination of both on glycaemic control parameters, lenticular opacity and changes in retinal microvasculature in alloxan (150mg/kg i...
October 24, 2016: Journal of Ethnopharmacology
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