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https://www.readbyqxmd.com/read/28349868/ultimate-biodegradability-and-ecotoxicity-of-orally-administered-antidiabetic-drugs
#1
Marta Markiewicz, Christian Jungnickel, Stefan Stolte, Anna Białk-Bielińska, Jolanta Kumirska, Wojciech Mrozik
Hypoglycaemic pharmaceuticals are recently more and more frequently detected in the environment. In our previous study, we have shown that even though many of them undergo significant primary degradation some are transformed to stable products or undergo such transformation that a large part of the structure is still preserved. One of the main routes of elimination from wastewaters or surface waters is biodegradation and a lack thereof leads to accumulation in the environment. Within this work we tested the ultimate biodegradability of six oral antidiabetics: metformin and its main metabolite guanylurea, acarbose, glibenclamide, gliclazide, glimepiride and repaglinide...
March 16, 2017: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/28332301/a-randomized-trial-comparing-gliclazide-liraglutide-and-metformin-effects-on-diabetes-with-nonalcoholic-fatty-liver-disease
#2
Wenhuan Feng, Caixia Gao, Yan Bi, Min Wu, Ping Li, Shanmei Shen, Wei Chen, Tingting Yin, Dalong Zhu
OBJECTIVE: To compare the effects of gliclazide, liraglutide, and metformin in type 2 diabetes mellitus (T2DM) patients with non-alcoholic fatty liver disease (NAFLD). METHODS: Eighty-seven subjects were randomized to receive liraglutide, metformin, or gliclazide for 24 weeks. Primary outcomes included hemoglobin A1c (HbA1c) levels, intrahepatic fat (IHF) content, and liver function. RESULTS: HbA1c levels and IHF content reduced after treatment in the three groups...
March 23, 2017: Journal of Diabetes
https://www.readbyqxmd.com/read/28323955/rapid-onset-of-diabetic-ketoacidosis-following-sglt2-inhibition-in-a-patient-with-unrecognized-acromegaly
#3
Marino Quarella, Daniel Walser, Michael Brändle, Jean-Yves Fournier, Stefan Bilz
Context: Diabetic ketoacidosis has been described as a rare complication of acromegaly and may be observed in 1% of affected patients. The well described direct lipolytic effect of growth hormone results in increased availability of free fatty acids (FFA) for hepatic ketogenesis and is an important pathogenic event. More recently, ketoacidosis has been identified as an important complication of sodium-glucose-transport-protein 2 inhibitors (SGLT2i). Increased pancreatic glucagon secretion, impaired renal ketone body clearance and an increase in FFA concentrations secondary to decreased insulin concentrations are likely precipitating factors...
February 21, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28271251/efficacy-and-safety-of-metformin-and-sitagliptin-based-triple-antihyperglycemic-therapy-strategy-a-multicenter-randomized-controlled-non-inferiority-clinical-trial
#4
Wen Xu, Yiming Mu, Jiajun Zhao, Dalong Zhu, Qiuhe Ji, Zhiguang Zhou, Bin Yao, Anhua Mao, Samuel S Engel, Bin Zhao, Yan Bi, Longyi Zeng, Xingwu Ran, Juming Lu, Linong Ji, Wenying Yang, Weiping Jia, Jianping Weng
Despite the current guideline's recommendation of a timely stepwise intensification therapy, the "clinical inertia", termed as the delayed treatment intensification, commonly exists in the real world, which may be partly due to the relatively little substantial evidence and no clear consensus regarding the efficacy and safety of triple oral agents in patients inadequately controlled with dual therapy. In this clinical trial performed in 237 centers in China, 5,535 type 2 diabetic patients inadequately controlled by previous therapies were treated with a stable metformin/sitagliptin dual therapy for 20 weeks...
February 7, 2017: Science China. Life Sciences
https://www.readbyqxmd.com/read/28105986/canagliflozin-dapagliflozin-and-empagliflozin-monotherapy-for-treating-type-2-diabetes-systematic-review-and-economic-evaluation
#5
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/28017142/gliclazide-induced-insulin-autoimmune-syndrome-a-rare-case-report-and-review-on-literature
#6
Xiu Feng, Lu Yuan, Hu Yun, Yunqing Zhu, Fan Yang, Lanlan Jiang, Rengna Yan, Yong Luo, Enhui Zhao, Chenxiao Liu, Ying Wang, Qi Li, Xin Cao, Qian Li, Jianhua Ma
Insulin Autoimmune Syndrome (IAS) is a rare condition characterized by the combination of recurrent severely spontaneous hypoglycemia without evidence of exogenous insulin administration, high concentration of total serum insulin, and the presence of a high titer of insulin autoantibody (IAA)[ ]. But now we describe a case with IAS caused by gliclazide and hardly occuring hypoglycemia. A 70-year-old man with type 2 diabetes presented to our department with poor glycemic control without evidence of hypoglycemia, but the levels of serum insulin and IAA were very high...
December 23, 2016: Endocrine, Metabolic & Immune Disorders Drug Targets
https://www.readbyqxmd.com/read/28000562/synchronized-fast-spe-and-uflc-methods-for-the-analyses-of-eight-antidiabetic-drugs-in-human-plasma
#7
Imran Ali, Kamlesh Dutta, A K Jain
The number of the diabetic patients is increasing rapidly globally. The treatment of these patients is a complex phenomenon due to the use of the different drugs. The present article reports a synchronized fast SPE-UFLC separation of eight antidiabetic drugs in human plasma. The separated drugs include metformin HCl, vildagliptin, gliclazide, linagliptin, sitagliptin, pioglitazone, glimepiride and repaglinide. The column used was Sunshell C18 (150 x 4.6 mm, 2.6 µm) with mobile phase of acetate buffer (0.05% TEA in 0...
December 20, 2016: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/27930700/simultaneous-quantification-of-antidiabetic-agents-in-human-plasma-by-a-uplc-qtof-ms-method
#8
Mariana Millan Fachi, Letícia Bonancio Cerqueira, Letícia Paula Leonart, Thais Martins Guimarães de Francisco, Roberto Pontarolo
An ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry method for the simultaneous quantification of chlorpropamide, glibenclamide, gliclazide, glimepiride, metformin, nateglinide, pioglitazone, rosiglitazone, and vildagliptin in human plasma was developed and validated, using isoniazid and sulfaquinoxaline as internal standards. Following plasma protein precipitation using acetonitrile with 1% formic acid, chromatographic separation was performed on a cyano column using gradient elution with water and acetonitrile, both containing 0...
2016: PloS One
https://www.readbyqxmd.com/read/27904436/effects-of-metformin-on-blood-and-urine-pro-inflammatory-mediators-in-patients-with-type-2-diabetes
#9
Wei Chen, Xiaojie Liu, Shandong Ye
BACKGROUND: Metformin has been used for the treatment of type 2 diabetes by suppressing hepatic gluconeogenesis. It has been shown that the subclinical inflammatory responses play important roles in the pathogenesis of type 2 diabetes. In the present study, we determined the effects of metformin on the levels of pro-inflammatory cytokines (i.e., IL-6, TNF-α, and MCP-1) and anti-inflammatory mediator IL-10 in blood and urine of patients with type 2 diabetes. There were 210 patients with type 2 diabetes, which were randomized into metformin (n = 112) and non-metformin (gliclazide, acarbose, and repaglinide, n = 98) groups...
2016: Journal of Inflammation
https://www.readbyqxmd.com/read/27829515/primary-degradation-of-antidiabetic-drugs
#10
Marta Markiewicz, Christian Jungnickel, Stefan Stolte, Anna Białk-Bielińska, Jolanta Kumirska, Wojciech Mrozik
Type 2 diabetes is a chronic disease affecting a large portion of the world population and is treated by orally administered drugs. Since these drugs are often taken in high doses and are excreted unchanged or partially metabolised many of them are nowadays detected in surface waters or wastewater treatment plants effluents. Unmetabolised antidiabetics or some of their transformation products retain their pharmacological activity, therefore their presence in the environment is highly undesired. One of the main routes of elimination from wastewaters or surface waters is biodegradation...
February 15, 2017: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/27666900/treatment-of-type-2-diabetes-with-a-breakable-extended-release-gliclazide-formulation-in-primary-care-the-xrise-study
#11
V Mohan, V Chopra, D Sanyal, S Jain, J Jayaprakashsai
OBJECTIVE: This study examines whether a new, scored and breakable once daily gliclazide tablet formulation, gliclazide XR 60 mg, that enables a simple 2-steps titration, can improve glycemic control rates in the community. METHODS: In a prospective multicenter study of 4 months duration, organised in the primary care setting of urban India, type 2 diabetes patients, uncontrolled with diet alone or metformin monotherapy, received 1 (60 mg), 1½ (90 mg), or 2 (120 mg) tablets of gliclazide XR 60 mg to achieve a target fasting plasma glucose of 126 mg/dl, or HbA1c of 7%...
December 2015: Journal of the Association of Physicians of India
https://www.readbyqxmd.com/read/27499787/inhibition-of-p-glycoprotein-expression-and-function-by-anti-diabetic-drugs-gliclazide-metformin-and-pioglitazone-in-vitro-and-in-situ
#12
Mehran Mesgari Abbasi, Hadi Valizadeh, Hamed Hamishehkar, Parvin Zakeri-Milani
P-glycoprotein (P-gp) is a trans-membrane drug efflux pump. Several drugs are P-gp substrates. Some drugs may affect the activity of P-gp by inhibiting its function, resulting in significant drug-drug interactions (DDIs). It is critical to understand which drugs are inhibitors of P-gp so that adverse DDIs can be minimized or avoided. This study investigated the effects of gliclazide, metformin, and pioglitazone on the function and expression of P-gp. Rhodamine 123 (Rh 123) efflux assays in Caco-2 cells and western blot testing were used to study in vitro the effect of the drugs on P-gp function and expression...
May 2016: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27459533/metformin-increases-cortisol-regeneration-by-11%C3%AE-hsd1-in-obese-men-with-and-without-type-2-diabetes-mellitus
#13
Anna J Anderson, Ruth Andrew, Natalie Z Homer, Gregory C Jones, Kenneth Smith, Dawn E Livingstone, Brian R Walker, Roland H Stimson
CONTEXT: The mechanism of action of metformin remains unclear. Given the regulation of the cortisol-regenerating enzyme 11βhydroxysteroid dehydrogenase 1 (11βHSD1) by insulin and the limited efficacy of selective 11βHSD1 inhibitors to lower blood glucose when co-prescribed with metformin, we hypothesized that metformin reduces 11βHSD1 activity. OBJECTIVE: To determine whether metformin regulates 11βHSD1 activity in vivo in obese men with and without type 2 diabetes mellitus...
October 2016: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/27426428/hypoglycaemia-when-adding-sulphonylurea-to-metformin-a-systematic-review-and-network-meta-analysis
#14
REVIEW
Stig Ejdrup Andersen, Mikkel Christensen
AIMS: The risk of hypoglycaemia may differ among sulphonylureas (SUs), but evidence from head-to-head comparisons is sparse. Performing a network meta-analysis to use indirect evidence from randomized controlled trials (RCTs), we compared the relative risk of hypoglycaemia with newer generation SUs when added to metformin. METHODS: A systematic review identified RCTs lasting 12-52 weeks and evaluating SUs added to inadequate metformin monotherapy (≥1000 mg/day) in type 2 diabetes...
November 2016: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27222601/search-for-compounds-with-hypoglycemic-activity-in-the-series-of-1-2-1h-tetrazol-5-yl-r-1-phenyl-3-r-2-phenyl-ethyl-ureas-and-r-1-tetrazolo-1-5-c-quinazolin-5-6h-ones
#15
Oleksii M Antypenko, Sergiy I Kovalenko, Galina O Zhernova
Methods of 1-[2-(1H-tetrazol-5-yl)-R(1)-phenyl]-3-R(2)-phenyl(ethyl)ureas and R(1)-tetrazolo[1,5-c]quinazolin-5(6H)-ones synthesis were designed. IR, LC-MS, (1)H NMR, and elemental analysis data evaluated the structure and purity of the obtained compounds. Different products, depending on the reaction conditions, were distinguished and discussed. The preliminary hypoglycemic activity of 36 synthesized compounds was revealed. Docking studies to 11β-hydroxysteroid dehydrogenase 1, γ-peroxisome proliferator-activated receptor, and dipeptidyl peptidase-4 were conducted...
April 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/27197687/metformin-associated-lactic-acidosis-in-a-patient-with-normal-renal-function
#16
Ahmed Omar, Ruth Ellen, Alexander Sorisky
We report a case of metformin-associated lactic acidosis (MALA) in the setting of normal renal function and review the relevant medical literature. A 77-year-old female diagnosed with type 2 diabetes mellitus previously treated with insulin and gliclazide MR was started on metformin. A few weeks later, she was found to have lactic acidosis. Renal function was normal, and no severe underlying illness was identified. Metformin was discontinued, and lactate levels normalized within 4 days, suggesting metformin was a reversible precipitant of the lactic acidosis...
August 2016: Canadian Journal of Diabetes
https://www.readbyqxmd.com/read/27042415/effects-of-gliclazide-add-on-metformin-on-serum-omentin-1-levels-in-patients-with-type-2-diabetes-mellitus
#17
Ali I Al-Gareeb, Haidar F Alrubai, Sammar M Suliaman
BACKGROUND: Omentin is a newly identified adipokine that has beneficial influence against cardiovascular disorders. Hence, considering the impact of anti-diabetic drug on omentin levels may provide an adjuvant strategy to protect diabetic patients against valuable clinical hazards. AIM OF THE STUDY: To investigate the influence of metformin alone or in combination with gliclazide on the level of serum omentin among patients with type 2 diabetes mellitus (T2DM). PATIENTS AND METHODS: A total of 70 newly diagnosed patients with T2DM were enrolled in this randomized, double-blind prospective study, and divided into two equal groups based on treatment regimen in which Group 1 treated with metformin (1000 mg) and Group 2 treated with metformin (1000 mg) plus gliclazide (80 mg)...
March 2016: Indian Journal of Endocrinology and Metabolism
https://www.readbyqxmd.com/read/27017701/-effectiveness-of-cytoflavin-for-the-correction-of-cognitive-impairments-in-patients-with-type-2-diabetes-mellitus
#18
RANDOMIZED CONTROLLED TRIAL
I V Gatskikh, O F Veselova, I N Brikman, T P Shalda, E L Varygina, M N Kuznetsov, A V Shul'min, M M Petrova
Authors studied the efficacy of cytoflavin in the correction of cognitive impairment in patients with type 2 diabetes mellitus and the drug influence on the level of brain-derived neurotrophic factor (BDNF) in blood serum. The results of treatment and examination of 60 patients with type 2 diabetes diagnosis have been analyzed. The majority (49-81.6%) of patients initially exhibited light (35-71.4%) and moderate (14-28.6%) cognitive impairments. All patients received standard treatment with oral antidiabetic drugs: metformin monotherapy (26 patients or 43...
2015: Eksperimental'naia i Klinicheskaia Farmakologiia
https://www.readbyqxmd.com/read/26997508/a-dizygotic-twin-pregnancy-in-a-mody-3-affected-woman
#19
O Bitterman, D Iafusco, F Torcia, N Tinto, A Napoli
BACKGROUND: MODY diabetes includes rare familiar forms due to genetic mutations resulting in β-cell dysfunction. MODY 3 is due to mutations in the gene transcription factor HNF-1α, with diabetes diagnosis in adolescence or early adult life. Few data are available about MODY 3 in pregnancy. CASE REPORT: A 36-year-old Italian woman came to our unit at the 5th week of pregnancy. She was diagnosed with diabetes at 18 years, with negative autoimmunity and a strong familiarity for diabetes...
October 2016: Acta Diabetologica
https://www.readbyqxmd.com/read/26983335/-risk-and-benefit-of-sulfonylureas-their-role-in-view-of-new-treatment-options-for-type-2-diabetes
#20
REVIEW
Ingo Rustenbeck
Currently, the therapy with oral antidiabetic drugs undergoes major changes. The use of sulfonylureas is in marked decline. The major argument in favor of newer oral antidiabetic drugs is the lower risk of hypoglycemia. At the present time however, it is unclear whether DDP4 inhibitors or SGLT2 inhibitors lead to better outcomes with respect to cardiovascular events and overall mortality. Most evidence on the therapeutic use of sulfonylureas has been gained with glibenclamide and to some degree sulfonylureas and glibenclamide have become synonymous...
February 2016: Medizinische Monatsschrift Für Pharmazeuten
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