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Harumi Takahashi, Shihomi Hidaka, Chihiro Seki, Norihide Yokoi, Susumu Seino
The dynamics of insulin secretion stimulated by repaglinide, a glinide, and the combinatorial effects of repaglinide and incretin were investigated. At 4.4mM glucose, repaglinide induced insulin secretion with a gradually increasing first phase, showing different dynamics from that induced by glimepiride, a sulfonylurea. In the presence of glucagon-like peptide-1 (GLP-1), insulin secretion by repaglinide was augmented significantly but to lesser extent and showed different dynamics from that by glimepiride...
March 16, 2018: European Journal of Pharmacology
Johan Jendle, Xin Fang, Yang Cao, Leif Bojö, Bo K Nilsson, Fredric Hedberg, Irene Santos-Pardo, Thomas Nyström
In this post hoc study, we aimed to investigate liraglutide treatment on repetitive 24-hour blood pressure (BP) in patients with type II diabetes. Sixty-two individuals with type II diabetes (45 males) were randomized to 1.8 mg liraglutide once daily or 4 mg glimepiride together with 1 g metformin twice daily. Ambulatory 24-hour systolic and diastolic blood pressure (sBP/dBP) was repetitively measured at baseline, 2 weeks, and 18 weeks. Outcomes were evaluated as treatment change from baseline, 2 weeks, and 18 weeks...
February 16, 2018: Journal of the American Society of Hypertension: JASH
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
Sanjay Kalra, Silver Bahendeka, Rakesh Sahay, Sujoy Ghosh, Fariduddin Md, Abbas Orabi, Kaushik Ramaiya, Sameer Al Shammari, Dina Shrestha, Khalid Shaikh, Sachitha Abhayaratna, Pradeep K Shrestha, Aravinthan Mahalingam, Mazen Askheta, Aly Ahmed A Rahim, Fatimah Eliana, Hari K Shrestha, Sandeep Chaudhary, Nancy Ngugi, Jean Claude Mbanya, Than Than Aye, Tint Swe Latt, Zhanay A Akanov, Abbas Raza Syed, Nikhil Tandon, A G Unnikrishnan, S V Madhu, Ali Jawa, Subhankar Chowdhury, Sarita Bajaj, Ashok Kumar Das
For decades, sulfonylureas (SUs) have been important drugs in the antidiabetic therapeutic armamentarium. They have been used as monotherapy as well as combination therapy. Focus on newer drugs and concerns about the risk of severe hypoglycemia and weight gain with some SUs have led to discussion on their safety and utility. It has to be borne in mind that the adverse events associated with SUs should not be ascribed to the whole class, as many modern SUs, such as glimepiride and gliclazide modified release, are associated with better safety profiles...
January 2018: Indian Journal of Endocrinology and Metabolism
Muhammad Rouf Akram, Mahmood Ahmad, Asad Abrar, Rai Muhammad Sarfraz, Asif Mahmood
Background: The present work was conducted to prepare and evaluate transdermal patches with optimization of suitable polymeric blend of poly(meth) acrylates (Eudragit® ) (Ammonio Methacrylate Copolymer Ph Eur) for sustained transdermal delivery of glimepiride. Method: Polymeric matrix transdermal films were prepared by using Ammonio Methacrylate Copolymer Ph Eur RL 100 and Ammonio Methacrylate Copolymer Ph Eur RS 100 as the film former, and dibutyl phthalate (30% w/w) as the plasticizer...
2018: Drug Design, Development and Therapy
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
Yu Chen, Lin Chen, Hong Zhang, Shibo Huang, Yuqing Xiong, Chunhua Xia
Sulfonylureas (SUs) such as glibenclamide, gliclazide, glimepiride, glipizide and gliquidone are one of the first oral medicines available for the treatment of type 2 diabetes, and are widely used for the treatment of hyperglycaemia. The hepatic transporters, organic anion transporting polypeptide 1B1 (OATP1B1) and organic anion transporting polypeptide 1B3 (OATP1B3), play an important role in the disposition of a variety of drugs by mediating their uptake from blood into hepatocytes. Drug-drug interactions mediated by OATP1B1/1B3 may result in the hepatic transporting change for drug substrates...
March 2, 2018: Basic & Clinical Pharmacology & Toxicology
Thomas Nyström, Irene Santos-Pardo, Fredric Hedberg, Johan Wardell, Nils Witt, Yang Cao, Leif Bojö, Bo Nilsson, Johan Jendle
[This corrects the article on p. 325 in vol. 8, PMID: 29184539.].
2018: Frontiers in Endocrinology
Kanta Fujimoto, Yui Shibayama, Eriko Yamaguchi, Sachiko Honjo, Akihiro Hamasaki, Yoshiyuki Hamamoto
BACKGROUND: Glucose excursions and hypoglycemia are associated with cardiovascular complications. However, no studies have evaluated glucose excursions and the frequency of hypoglycemia in patients treated with mitiglinide/voglibose versus glimepiride as add-on to dipeptidyl peptidase-4 inhibitor therapy. METHODS: This cross-over trial included 20 patients with type 2 diabetes. After initiating vildagliptin 100 mg, patients were randomly assigned to receive mitiglinide/voglibose 10 mg/0...
March 1, 2018: Journal of Diabetes
John F Marcinak, Melvin S Munsaka, Paul B Watkins, Takashi Ohira, Neila Smith
INTRODUCTION: Fasiglifam (TAK-875) is a G protein-coupled receptor 40 agonist that was being investigated for treatment of type 2 diabetes mellitus (T2DM). A development program was terminated late in phase III clinical trials due to liver safety concerns. METHODS: The liver safety of fasiglifam was assessed from data based on six phase II and nine phase III double-blind studies and two open-label studies with emphasis on pooled data from 15 double-blind studies from both global and Japanese development programs...
February 28, 2018: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
Zhimin Huang, Juan Liu, Kaka Ng, Xuesi Wan, Lijuan Xu, Xiaoying He, Zhihong Liao, Yanbing Li
AIMS: Glimepiride is a sulfonylurea known to have unique insulin mimetic and sensitizing effect. We aimed to study the efficacy of glimepiride in a patient with type A insulin resistance syndrome. METHODS: A 15-year-old female with type A insulin resistance syndrome was treated with glimpiride for 6 months. Self-monitoring of blood glucose was recorded, OGTTs on glucose and insulin were measured during the treatment. Hyperinsulinemic euglycemic clamp was used to evaluate whole body insulin sensitivity before and after the treatment...
February 22, 2018: Journal of Diabetes Investigation
W Timothy Garvey, Luc Van Gaal, Lawrence A Leiter, Ujjwala Vijapurkar, James List, Robert Cuddihy, Jimmy Ren, Michael J Davies
OBJECTIVE: Type 2 diabetes and obesity are pro-inflammatory states associated with increased risk of cardiovascular disease. Canagliflozin, an SGLT2 inhibitor, demonstrated superiority in lowering HbA1c versus glimepiride with less hypoglycemia and greater weight reduction via loss of fat mass in a 52-week trial of type 2 diabetes patients. This post hoc, exploratory analysis assessed the effects of canagliflozin versus glimepiride on select adipokines, inflammatory biomarkers, and chemokines...
February 13, 2018: Metabolism: Clinical and Experimental
Ashwitha Shruti Dass, Sarala Narayana, P N Venkatarathnamma
Diabetes mellitus (DM) and its complications have been implicated in hyperglycemia-induced oxidative stress. Antioxidants can improve glycemic control, lipid profile, and cognitive functions. We assessed the effect of Vitamin E and omega 3 fatty acids (OFA) on the above parameters. One hundred patients with type 2 DM receiving metformin 500 mg and glimepiride 1 mg were randomized to receive add-on therapy of Vitamin E 400 mg or OFA once daily for 12 weeks and the third group served as control. Fasting blood sugar (FBS), postprandial blood sugar (PPBS), glycated hemoglobin (HbA1c), body mass index (BMI), waist-hip ratio (WHR), lipid profile, and mini-mental state examination were done at baseline and 12 weeks...
January 2018: Journal of Advanced Pharmaceutical Technology & Research
Charles E Leonard, Colleen M Brensinger, Christina L Aquilante, Warren B Bilker, Denise M Boudreau, Rajat Deo, James H Flory, Joshua J Gagne, Margaret J Mangaali, Sean Hennessy
OBJECTIVE: To examine the association between individual antidiabetic sulfonylureas and outpatient-originating sudden cardiac arrest and ventricular arrhythmia (SCA/VA). RESEARCH DESIGN AND METHODS: We conducted a retrospective cohort study using 1999-2010 U.S. Medicaid claims from five large states. Exposures were determined by incident use of glyburide, glimepiride, or glipizide. Glipizide served as the reference exposure, as its effects are believed to be highly pancreas specific...
February 2, 2018: Diabetes Care
A Hemdan, Omar Abdel-Aziz
Run time is a predominant factor in HPLC for quality control laboratories especially if there is large number of samples have to be analyzed. Working at high flow rates cannot be attained with silica based particle packed column due to elevated backpressure issues. The use of monolithic column as an alternative to traditional C-18 column was tested for fast separation of pharmaceuticals, where the results were very competitive. The performance comparison of both columns was tested for separation of anti-diabetic combination containing Metformin, Pioglitazone and Glimepiride using Gliclazide as an internal standard...
February 7, 2018: Journal of Chromatographic Science
Tatsuhiko Urakami
The principal treatment for children and adolescents with type 2 diabetes is dietary and exercise management. However, the blood glucose levels of some patients receiving this treatment fail to improve; thus, pharmacological treatment is eventually required. The pathophysiology of type 2 diabetes in pediatric patients appears to be similar to that in adults; thus, the range of antidiabetic drugs used in adults is likely to be effective in pediatric patients as well. However, in the majority of countries, including Japan, only metformin, glimepiride, and insulin have been approved for use in pediatric patients...
2018: Clinical Pediatric Endocrinology: Case Reports and Clinical Investigations: Official Journal of the Japanese Society for Pediatric Endocrinology
Rana Refaat Makar, Randa Latif, Ehab Ahmed Hosni, Omaima Naim El Gazayerly
Purpose: Triple solid dispersion adsorbates (TSDads) and spherical agglomerates (SA) present new techniques that extensively enhance dissolution of poorly soluble drugs. The aim of the present study is to hasten the onset of hypoglycemic effect of glimepiride through enhancing its rate of release from tablet formulation prepared from either technique. Methods: Drug release from TSDads or SA tablets with different added excipients was explored. Scanning electron microscopy (SEM) and effect of compression on dissolution were illustrated...
December 2017: Advanced Pharmaceutical Bulletin
Sarvi Yadav Rajesh, Sachin Kumar Singh, Narendra Kumar Pandey, Parth Sharma, Palak Bawa, Bimlesh Kumar, Monica Gulati, Subheet Jain, K Gowthamarajan, Saurabh Singh
Development of self-nanoemulsifying drug delivery systems (SNEDDS) of glimepiride is reported with the aim to achieve its oral delivery. Lauroglycol FCC, tween-80, and ethanol were used as oil, surfactant and co-surfactant, respectively as independent variables. The optimized composition of SNEDDS formulation (F1) was 10% v/v Lauroglycol FCC, 45% v/v Tween 80, 45%v/v ethanol, and 0.005% w/v glimepiride. Further, the optimized liquid SNEDDS were solidified through spray drying using various hydrophilic and hydrophobic carriers...
January 23, 2018: Drug Development and Industrial Pharmacy
Geert Jan Biessels, Jolien Janssen, Esther van den Berg, Bernard Zinman, Mark A Espeland, Michaela Mattheus, Odd Erik Johansen
BACKGROUND: Type 2 diabetes mellitus is associated with cognitive dysfunction and an increased risk of dementia. Linagliptin is a glucose-lowering agent of the dipeptidyl peptidase-IV (DPP-IV) inhibitor class that is of particular interest for the prevention of accelerated cognitive decline, because it may potentially benefit the brain through pleiotropic effects, beyond glucose lowering. This paper presents the design of a study that aims to establish if linagliptin is superior to the sulfonylurea glimepiride in the prevention of accelerated cognitive decline in patients with type 2 diabetes mellitus...
January 15, 2018: BMC Neurology
Sara Algeelani, Dalal Alkhelb, David J Greenblatt
Canagliflozin, used to treat type 2 diabetes mellitus (T2DM), is commonly co-administered with sulfonylureas. The objective of the present study was to evaluate the possible inhibitory effect of sulfonylureas and non-steroidal anti-inflammatory drugs (NSAIDs) on canagliflozin metabolism in vitro. Three sulfonylurea derivatives were evaluated as inhibitors: chlorpropamide, glimepiride and gliclazide. Two other NSAIDs were used as positive control inhibitors: niflumic acid and diclofenac. The rate of formation of canagliflozin metabolites was determined by HPLC analysis of in vitro incubations of canagliflozin as a substrate with and without inhibitors, using human liver microsomes (HLMs)...
January 10, 2018: Biopharmaceutics & Drug Disposition
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