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Oral agentes antidiabetes

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https://www.readbyqxmd.com/read/29089569/novel-benzylidene-thiazolidinedione-derivatives-as-partial-ppar%C3%AE-agonists-and-their-antidiabetic-effects-on-type-2-diabetes
#1
Sabina Yasmin, Fabio Capone, Antonio Laghezza, Fabrizio Dal Piaz, Fulvio Loiodice, Viswanathan Vijayan, Velmurugan Devadasan, Susanta K Mondal, Özlem Atlı, Merve Baysal, Ashok K Pattnaik, Venkatesan Jayaprakash, Antonio Lavecchia
Peroxisome proliferator-activated receptor γ (PPARγ) has received significant attention as a key regulator of glucose and lipid homeostasis. In this study, we synthesized and tested a library of novel 5-benzylidene-thiazolidin-2,4-dione (BTZD) derivatives bearing a substituent on nitrogen of TZD nucleus (compounds 1a-1k, 2i-10i, 3a, 6a, and 8a-10a). Three compounds (1a, 1i, and 3a) exhibited selectivity towards PPARγ and were found to be weak to moderate partial agonists. Surface Plasmon Resonance (SPR) results demonstrated binding affinity of 1a, 1i and 3a towards PPARγ...
October 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29068991/the-prescribing-trend-of-oral-antidiabetic-agents-for-type-2-diabetes-in-taiwan-an-8-year-population-based-study
#2
Wei-Min Chu, Hsin-En Ho, Kuang-Hua Huang, Yu-Tse Tsan, Yi-Sheng Liou, Yueh-Hsin Wang, Meng-Chih Lee, Yu-Ching Li
The purpose of this study was to evaluate the prescription trend and pattern of oral antidiabetic (OAD) medications, which are extensively used worldwide for treating type 2 diabetes, in 2 age groups.In this population-based study, data obtained from the National Health Insurance Research Database, Taiwan, were analyzed to investigate the prescription trend of all types of OAD medications during 2005 to 2012. We used descriptive statistics to demonstrate the trend of prescription patterns stratified by age (aged 65 years and above or younger than 65)...
October 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29066867/clinical-and-pharmacological-hallmarks-of-rifapentine-s-use-in-diabetes-patients-with-active-and-latent-tuberculosis-do-we-know-enough
#3
REVIEW
Chunlan Zheng, Xiufen Hu, Li Zhao, Minhui Hu, Feng Gao
Rifapentine is a rifamycin derivate approved by the US Food and Drug Administration in 1998 for the treatment of active, drug-susceptible tuberculosis (TB). In 2014, rifapentine was approved for the treatment of latent TB infection in patients at high risk of progression to active disease and is currently under evaluation by the European Medicines Agency. Expanding indications of rifapentine largely affect diabetes patients, since about one-third of them harbor latent TB. Clinical consequences of rifapentine use in this population and potentially harmful interactions with hypoglycemic agents are widely underexplored and generally considered similar to the ones of rifampicin...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29058840/-use-of-oral-glucose-lowering-agents-in-patients-with-renal-impairment
#4
A J Scheen, N Paquot
Patients with type 2 diabetes (T2D) and chronic kidney disease (CKD) are increasingly numerous, especially in the elderly population. Surprisingly, this situation is often under-recognized or even neglected in clinical practice. Yet, most oral antidiabetic (OAD) agents have limitations in case of renal impairment, either because they require a dose reduction, or are contra-indicated mainly for safety reasons. This clinical case gives the opportunity to discuss the modalities of prescription and cautions to be taken when using most commonly prescribed OAD, metformin, insulin secretagogues (sulfonylureas, repaglinide), DPP-4 inhibitors (gliptins) and SGLT2 inhibitors, in a patient with T2D and CKD...
October 2017: Revue Médicale de Liège
https://www.readbyqxmd.com/read/29055800/anti-diabetic-potential-of-peptides-future-prospects-as-therapeutic-agents
#5
REVIEW
Marya, Haroon Khan, Seyed Mohammad Nabvi, Solomon Habtemariam
Diabetes mellitus is a metabolic disorder in which the glucose level in blood exceeds beyond the normal level and its effective control is recognized as a global challenge for clinician. Persistent hyperglycemia leads to diabetes late complication and obviously account for a large number of morbidity and mortality worldwide. Numerous therapeutic options are available for the treatment of diabetes including insulin for type I and oral tablets for type II, but its effective management is still a dream. Several options are under investigation in various research laboratories for efficacious and safer agents...
October 18, 2017: Life Sciences
https://www.readbyqxmd.com/read/29042751/spotlight-on-ertugliflozin-and-its-potential-in-the-treatment-of-type-2-diabetes-evidence-to-date
#6
REVIEW
Francesca Cinti, Simona Moffa, Flavia Impronta, Chiara Ma Cefalo, Vinsin A Sun, Gian Pio Sorice, Teresa Mezza, Andrea Giaccari
Sodium-glucose cotransporter 2 (SGLT2) inhibitors are the latest therapeutic strategy in the treatment of type 2 diabetes mellitus (T2DM). Using an insulin-independent mechanism (glycosuria), they reduce glucose toxicity and improve insulin sensitivity and β-cell function. The promising results obtained in clinical trials show that SGLT2 significantly improves glycemic control and provides greater cardiovascular protection, combined with a reduction in body weight and blood pressure (BP). This review focuses on ertugliflozin, a new, highly selective, and reversible SGLT2 inhibitor...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29034194/evidence-based-study-of-antidiabetic-potential-of-c-maxima-seeds%C3%A2-%C3%A2-in%C3%A2-vivo
#7
Devesh Kumar Kushawaha, Manjulika Yadav, Sanjukta Chatterji, Amrita Kumari Srivastava, Geeta Watal
OBJECTIVE: In vitro antidiabetic efficacy of Cucurbita maxima seed extract (CMSE) has already been studied in our previous findings. Thus, in order to validate these findings in biological system, in vivo antidiabetic activity of aqueous extract was investigated in normal as well as diabetic experimental models. METHODS: Variable doses of extract were administered orally to normal and STZ induced mild diabetic rats during fasting blood glucose (FBG) and glucose tolerance test (GTT) studies...
October 2017: Journal of Traditional and Complementary Medicine
https://www.readbyqxmd.com/read/29016121/synthesis-binding-mode-and-antihyperglycemic-activity-of-potent-and-selective-5-imidazol-2-yl-4-phenylpyrimidin-2-yl-2-2-pyridylamino-ethyl-amine-inhibitors-of-glycogen-synthase-kinase-3
#8
Allan S Wagman, Rustum S Boyce, Sean P Brown, Eric Fang, Dane Goff, Johanna M Jansen, Vincent P Le, Barry H Levine, Simon C Ng, Zhi-Jie Ni, John M Nuss, Keith B Pfister, Savithri Ramurthy, Paul A Renhowe, David B Ring, Wei Shu, Sharadha Subramanian, Xiaohui A Zhou, Cynthia M Shafer, Stephen D Harrison, Kirk W Johnson, Dirksen E Bussiere
In an effort to identify new antidiabetic agents, we have discovered a novel family of (5-imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine analogues which are inhibitors of human glycogen synthase kinase 3 (GSK3). We developed efficient synthetic routes to explore a wide variety of substitution patterns and convergently access a diverse array of analogues. Compound 1 (CHIR-911, CT-99021, or CHIR-73911) emerged from an exploration of heterocycles at the C-5 position, phenyl groups at C-4, and a variety of differently substituted linker and aminopyridine moieties attached at the C-2 position...
October 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28977090/use-of-sglt-2-inhibitors-in-the-treatment-of-type-2-diabetes-mellitus
#9
REVIEW
Leyna Leite Santos, Fernando José Camello de Lima, Célio Fernando de Sousa-Rodrigues, Fabiano Timbó Barbosa
INTRODUCTION: Diabetes mellitus is one of the most common chronic diseases in the world, with high morbidity and mortality rates, resulting in a greatly negative socioeconomic impact. Although there are several classes of oral antidiabetic agents, most of the patients are outside the therapeutic goal range. OBJECTIVE: To review the use of SGLT-2 inhibitors in the treatment of type 2 diabetes mellitus, focusing on their favorable and unfavorable effects, as well as on cardiovascular profile...
July 2017: Revista da Associação Médica Brasileira
https://www.readbyqxmd.com/read/28965348/adulteration-of-proprietary-chinese-medicines-and-health-products-with-undeclared-drugs-experience-of-a-tertiary-toxicology-laboratory-in-hong-kong
#10
Chor Kwan Ching, Sammy Pak Lam Chen, Hencher Han Chih Lee, Ying Hoo Lam, Sau Wah Ng, Mo Lung Chen, Magdalene Huen Yin Tang, Suzanne Suk San Chan, Candy Wai Yan Ng, Jana Wing Lan Cheung, Tina Yee Ching Chan, Nike Kwai Cheung Lau, Yeow Kuan Chong, Tony Wing Lai Mak
AIMS: Proprietary Chinese medicines (pCMs) and health products, generally believed to be natural and safe, are gaining popularity worldwide. However, the safety of pCMs and health products has been severely compromised by the practice of adulteration. The current study aimed to examine the problem of adulteration of pCMs and health products in Hong Kong. METHODS: The present study was conducted in a tertiary referral clinical toxicology laboratory in Hong Kong. All cases involving the use of pCMs or health products, which were subsequently confirmed to contain undeclared adulterants, from 2005 to 2015 were reviewed retrospectively...
October 1, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28956461/multicomponent-crystals-of-gliclazide-and-tromethamine-preparation-physico-chemical-and-pharmaceutical-characterization
#11
Giovanna Bruni, Vittorio Berbenni, Lauretta Maggi, Piercarlo Mustarelli, Valeria Friuli, Chiara Ferrara, Francesca Pardi, Federica Castagna, Alessandro Girella, Chiara Milanese, Amedeo Marini
OBJECTIVE: To improve the pharmaceutical behaviour of the oral antidiabetic agent gliclazide through the synthesis of multicomponent crystals with tromethamine. METHODS: Multicomponent crystals were prepared by solvent evaporation method, kneading and combining mechanical and thermal activation. DSC, FT-IR spectroscopy, X-ray diffraction, SEM-EDS and SSNMR were used to investigate their formation. Measurements of solubility and dissolution rate were carried out for the pharmaceutical characterization...
September 28, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28954218/effects-of-insulin-analogs-as-an-add-on-to-metformin-on-cutaneous-microcirculation-in-type-2-diabetic-patients
#12
Marinos Fysekidis, Emmanuel Cosson, Karim Takbou, Angela Sutton, Nathalie Charnaux, Isabella Banu, Eric Vicaut, Paul Valensi
BACKGROUND: A single insulin injection was shown to improve microcirculatory blood flow. Our aim was to examine the effects of 4weeks of insulin therapy by three randomly assigned insulin analog regimens (Detemir, Aspart, and their combination) on cutaneous blood flow (CBF) and microcirculatory endothelial function as an add-on to metformin in type 2 diabetic patients poorly controlled on oral antidiabetic treatment. METHODS: Fourty-two type 2 diabetic patients with no history of cardiovascular disease in secondary failure to oral antidiabetic agents had CBF measurements before and after acetylcholine (Ach) iontophoretic administration...
September 24, 2017: Microvascular Research
https://www.readbyqxmd.com/read/28928054/effect-of-the-antidiabetic-agent-pioglitazone-on-bone-metabolism-in-rats
#13
Junkichi Kanda, Nobuo Izumo, Yoshiko Kobayashi, Kenji Onodera, Taketoshi Shimakura, Noriaki Yamamoto, Hideaki E Takahashi, Hiroyuki Wakabayashi
Thiazolidinediones (TZDs) are synthetic peroxisome proliferator-activated receptor gamma (PPARγ) agonists used as therapy for type 2 diabetes. However, clinical studies reported that the therapeutic modulation of PPARγ activity using TZDs may induce negative effects on bone metabolism. This study aimed to evaluate the effect of the TZD pioglitazone on bone metabolism in rats. Male Wistar rats were treated orally with pioglitazone 5 or 20 mg/kg daily for 24 weeks. Bone strength was evaluated using a 3-point bending method, and bone histomorphometry was analyzed...
August 26, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28923179/drugs-and-hyperglycemia-a-practical-guide
#14
REVIEW
Vandana Jain, Ronak Kumar Patel, Zaureen Kapadia, Sneha Galiveeti, Maryann Banerji, Lisel Hope
Drug-induced diabetes is one of the factors contributing to the increasing incidence of diabetes worldwide. This review considers the frequency, pathogenesis and treatment of drug-induced diabetes. Drugs that induce diabetes include hormonal therapy, especially glucocorticoids and androgen blockers, cardiovascular drugs, especially statins, beta-blockers and diuretics, antipsychotics, especially clozapine, olanzapine and quetiapine, antiretrovirals (protease inhibitors and non-reverse transcriptase inhibitors - NRTIs) and other drugs (mechanistic target of rapamycin inhibitors -mTORs, post organ transplantation drugs, tyrosine kinase inhibitors and interferon-alpha)...
October 2017: Maturitas
https://www.readbyqxmd.com/read/28892956/short-term-efficacy-and-safety-of-insulin-glargine-in-type-2-diabetes-inadequately-controlled-with-single-or-two-oral-agents-a-prospective-open-label-study
#15
Ajay Aggarwal, Roopak Wadhwa
INTRODUCTION: Basal insulin is among the second line treatment options for Type 2 Diabetes Mellitus (T2DM). Efficacy and safety of basal insulin in patients of T2DM, uncontrolled with Oral Antidiabetic Agents (OAAs) remains understudied in the Indian setting. AIM: To assess the efficacy and safety of insulin glargine in patients with T2DM who have uncontrolled glycaemic levels despite single or two OAAs therapy. MATERIALS AND METHODS: In this prospective, open label study, T2DM patients above 40 years of age, having inadequate glycaemic control [Glycosylated Haemoglobin (HbA1c) above 8% and/or fasting glucose level of 140 mg/dl and above] with single or two OAAs over three consecutive months were included...
July 2017: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/28861952/use-of-sodium-glucose-cotransporter%C3%A2-2-inhibitors-in-older-patients-with-type%C3%A2-2-diabetes-mellitus
#16
Takahiro Kambara, Rei Shibata, Hiroyuki Osanai, Yoshihito Nakashima, Hiroshi Asano, Kazuyoshi Sakai, Toyoaki Murohara, Masayoshi Ajioka
AIM: Sodium-glucose cotransporter 2 (SGLT2) inhibitors are antidiabetic agents that act on the proximal renal tubules to lower blood glucose levels by inhibiting glucose reabsorption and promoting urinary glucose excretion. The present study assessed the long-term use of SGLT2 inhibitors in older patients with diabetes. METHODS: A total of 117 older patients with type 2 diabetes who were given SGLT2 inhibitors were enrolled from April 2014 to March 2016. RESULTS: The mean age of the patients was 73...
September 1, 2017: Geriatrics & Gerontology International
https://www.readbyqxmd.com/read/28844525/oral-antidiabetic-agents-and-cardiovascular-outcomes
#17
Manan Pareek, Deepak L Bhatt
Cardiovascular disease is the leading cause of morbidity and mortality among patients with type 2 diabetes; however, a direct protective effect of tight glycemic control remains unproven. In fact, until 2008, when concerns related to rosiglitazone prompted regulatory agencies to mandate assessment of cardiovascular safety of new antidiabetic agents, little was known about how these medications affected cardiovascular outcomes. Since then, there has been a considerable increase in the number of cardiovascular trials, which employ a noninferiority design and focus on high-risk populations to establish safety in the shortest time possible...
July 29, 2017: Current Problems in Cardiology
https://www.readbyqxmd.com/read/28840639/use-of-oral-antidiabetic-drugs-in-the-treatment-of-maturity-onset-diabetes-of-the-young-a-mini-review
#18
REVIEW
Ludmila Brunerova, Dario Rahelić, Antonio Ceriello, Jan Broz
MODY (maturity-onset diabetes of the young) is a genetically linked group of clinically heterogeneous subtypes of diabetes. Roughly 5% of people with diabetes mellitus diagnosed prior to age 45 have MODY diabetes. Most of them have been erroneously diagnosed as patients with either type 1 or type 2 diabetes and, as a result, have been improperly treated. Genetic identification of MODY diabetes and its subtypes allows proper treatment and enables clinicians to switch many patients to oral antidiabetic agents, mainly sulphonylureas...
August 24, 2017: Diabetes/metabolism Research and Reviews
https://www.readbyqxmd.com/read/28835229/does-dapagliflozin-regress-left-ventricular-hypertrophy-in-patients-with-type-2-diabetes-a-prospective-double-blind-randomised-placebo-controlled-study
#19
Alexander J M Brown, Chim Lang, Rory McCrimmon, Allan Struthers
BACKGROUND: Patients with diabetes have a two to fourfold increased risk for development of and death from cardiovascular disease [CVD]. The current oral hypoglycaemic agents result in limited reduction in this cardiovascular risk. Sodium glucose linked co-transporter type 2 [SGLT2] inhibitors are a relatively new class of antidiabetic agent that have been shown to have potential cardiovascular benefits. In support of this, the EMPA-REG trial showed a striking 38% and 35% reduction in cardiovascular mortality and heart failure [HF] hospitalisation respectively...
August 23, 2017: BMC Cardiovascular Disorders
https://www.readbyqxmd.com/read/28811775/metformin-attenuate-ptz-induced-apoptotic-neurodegeneration-in-human-cortical-neuronal-cells
#20
Fehmida Bibi, Ikram Ullah, Myeong Ok Kim, Muhammad Imran Naseer
OBJECTIVE: Seizures are one of the neurodegenerative disorders of human being. Metformin has antioxidant properties and commonly used as an oral antidiabetic drug. The current study was aimed to observe the neuroprotective effect of metformin against PTZ-induced apoptotic neurodegeneration in human cortical neuronal cell culture. METHODS: To observe that exposure of pentylenetetrazol (PTZ) at the dose of (30mM) for 30 minutes induced neuronal cell death by activation of caspase-3 in human cortical neuronal 2 (HCN-2) cell line...
May 2017: Pakistan Journal of Medical Sciences Quarterly
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