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Oral agentes antidiabetes

Neha Charaya, Deepti Pandita, Ajmer Singh Grewal, Viney Lather
Glucokinase (GK) is the main enzyme which controls the blood glucose levels in a safe and narrow physiological range in humans. GK activators are the novel type of therapeutic agents which act on GK enzyme and show their anti-diabetic potential. The present work was planned to synthesize and evaluate the antidiabetic potential of a new series of thiazole-2-yl benzamide derivatives as potential GK activators. A series of thiazole-2-yl benzamide derivatives were synthesized from benzoic acid and evaluated by in vitro enzymatic assay for GK activation...
February 27, 2018: Computational Biology and Chemistry
Bahendeka Silver, Kaushik Ramaiya, Swai Babu Andrew, Otieno Fredrick, Sarita Bajaj, Sanjay Kalra, Bavuma M Charlotte, Karigire Claudine, Anthony Makhoba
A diagnosis of diabetes or hyperglycemia should be confirmed prior to ordering, dispensing, or administering insulin (A). Insulin is the primary treatment in all patients with type 1 diabetes mellitus (T1DM) (A). Typically, patients with T1DM will require initiation with multiple daily injections at the time of diagnosis. This is usually short-acting insulin or rapid-acting insulin analogue given 0 to 15 min before meals together with one or more daily separate injections of intermediate or long-acting insulin...
March 5, 2018: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
Wesley Nuffer, Ashley Guesnier, Jennifer M Trujillo
There have been several new treatment approaches established for the management of hyperglycemia in type 2 diabetes (T2D), with treatment guidelines listing both glucagon-like peptide 1 receptor agonists (GLP-1 RAs) and basal insulin therapies as considerations for patients who have failed to control their blood glucose with oral antidiabetic agents. New studies have highlighted the importance of initiating combination therapy earlier in the T2D disease process to avoid clinical inertia and prevent the long-term complications arising from uncontrolled diabetes...
March 2018: Therapeutic Advances in Endocrinology and Metabolism
Richa Chaturvedi, Chetna Desai, Prakruti Patel, Asha Shah, Ram K Dikshit
Aims: This study aims to measure the quality of life (QOL), treatment satisfaction, and tolerability of antidiabetic drugs in patients suffering from type 2 diabetes mellitus (DM). Methods: The prospective, observational study was conducted in consenting patients of type 2 DM attending the outpatient department of a tertiary care hospital in Western India. The QOL instrument for Indian diabetes (QOLID) patients questionnaire and the Diabetes Treatment Satisfaction Questionnaire were administered to all patients at baseline, 3 months, and 6 months of treatment...
January 2018: Perspectives in Clinical Research
Panteleimon Pantelidis, Andreas Kalliakmanis, Christos Mitas, Michail Sideris, Charalampos Grassos, Andreas Pittaras, Athanasios Manolis
BACKGROUND: Sodium-glucose cotransporter 2 (SGLT-2) inhibitors are a new class of oral antidiabetic drugs. So far, there are three agents approved for use in Europe and in the USA, two in Japan and another four agents under testing. OBJECTIVE: The purpose of this study is to describe the mechanism of action and the favorable and adverse effects of SGLT-2 inhibitors. METHOD: A thorough review of literature indexed in PubMed, Scopus and Cochrane databases was conducted...
February 6, 2018: Cardiovascular & Hematological Disorders Drug Targets
Maria J Peláez-Jaramillo, Allison A Cárdenas-Mojica, Paula V Gaete, Carlos O Mendivil
Post-liver transplantation diabetes mellitus (PLTDM) develops in up to 30% of liver transplant recipients and is associated with increased risk of mortality and multiple morbid outcomes. PLTDM is a multicausal disorder, but the main risk factor is the use of immunosuppressive agents of the calcineurin inhibitor (CNI) family (tacrolimus and cyclosporine). Additional factors, such as pre-transplant overweight, nonalcoholic steatohepatitis and hepatitis C virus infection, may further increase risk of developing PLTDM...
February 6, 2018: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
Michelle Mocarski, Jason Yeaw, Victoria Divino, Mitch DeKoven, German Guerrero, Jakob Langer, Brian Larsen Thorsted
BACKGROUND: Clinical inertia in type 2 diabetes mellitus (T2DM) refers to the failure of clinicians to intensify therapy when indicated. Many T2DM patients remain suboptimally controlled after initiating basal insulin. OBJECTIVE: To examine the prevalence of patients treated with basal insulin but in poor glycemic control (hemoglobin A1c [A1c] ≥ 7%) after initiation and subsequent treatment intensification patterns and glycemic outcomes in a real-world setting...
November 16, 2017: Journal of Managed Care & Specialty Pharmacy
Gaurav Gupta, Terezinha de Jesus Andreoli Pinto, Dinesh K Chellappan, Anurag Mishra, Himaja Malipeddi, Kamal Dua
Diabetes mellitus (DM) is frequently increased in many countries and become a serious health problem worldwide. Diabetes is associated with dysfunction of different organs such as heart, eyes, blood vessels, nerves, and kidneys. There is a strong connection between diabetes and cancer. Metformin is one of the most commonly prescribed oral antidiabetic medicines and it is suggested as the firstline therapy due to its comparatively safe, inexpensive, effective and welltolerated. Some of the in vitro and in vivo investigations proved that metformin may have a direct anticancer action by preventing the proliferation of malignant cells and formations of the colony, inducing arrest of cell cycle and apoptosis and suppressing tumour growth...
January 25, 2018: Panminerva Medica
Guillermo E Umpierrez, Saumeth Cardona, David Chachkhiani, Maya Fayfman, Sahebi Saiyed, Heqiong Wang, Priyathama Vellanki, J Sonya Haw, Darin E Olson, Francisco J Pasquel, Theodore M Johnson
OBJECTIVES: Safe and easily implemented treatment regimens are needed for the management of patients with type 2 diabetes mellitus (T2DM) in long-term care (LTC) and skilled nursing facilities. DESIGN: This 6-month open-label randomized controlled trial compared the efficacy and safety of a DPP4 inhibitor (linagliptin) and basal insulin (glargine) in LTC residents with T2DM. SETTINGS: Three LTC institutions affiliated with a community safety-net hospital, US Department of Veterans Affairs and Emory Healthcare System in Atlanta, Georgia...
December 27, 2017: Journal of the American Medical Directors Association
Kosuke Kaji, Norihisa Nishimura, Kenichiro Seki, Shinya Sato, Soichiro Saikawa, Keisuke Nakanishi, Masanori Furukawa, Hideto Kawaratani, Mitsuteru Kitade, Kei Moriya, Tadashi Namisaki, Hitoshi Yoshiji
Sodium-glucose cotransporter 2 inhibitors (SGLT2-Is) comprise a new class of antidiabetic agents that inhibit glucose reabsorption in the renal proximal tubules. Although a recent report demonstrated the potential ability of SGLT2-Is to attenuate cancer growth of SGLT2-expressing cancer cells, little is known about the effects of SGLT2-Is on hepatocellular carcinoma (HCC). Here, we investigate the anti-cancer properties of a SGLT2-I, canagliflozin, against human liver cancer cells. SGTL2 mRNA and protein expression were detected in Huh7 and HepG2 cells, although not in HLE as well as primary human hepatocytes and hepatic stellate cells...
April 15, 2018: International Journal of Cancer. Journal International du Cancer
Mohamed Hassanein, Akram Salim Echtay, Rachid Malek, Mahomed Omar, Shehla Sajid Shaikh, Magnus Ekelund, Kadriye Kaplan, Nor Azmi Kamaruddin
AIMS: To compare the efficacy and safety of insulin degludec/insulin aspart (IDegAsp) and biphasic insulin aspart 30 (BIAsp 30) before, during and after Ramadan in patients with type 2 diabetes mellitus (T2DM) who fasted during Ramadan. METHODS: In this multinational, randomised, treat-to-target trial, patients with T2DM who intended to fast and were on basal, pre- or self-mixed insulin ± oral antidiabetic drugs for ≥90 days were randomised (1:1) to IDegAsp twice daily (BID) or BIAsp 30 BID...
January 2018: Diabetes Research and Clinical Practice
Mariana Millan Fachi, Letícia Paula Leonart, Flávia Lada Degaut Pontes, Raquel de Oliveira Vilhena, Letícia Bonancio Cerqueira, Roberto Pontarolo
Type 2 diabetes mellitus, a disease which prevalence has been progressively increasing worldwide, is characterized by chronic hyperglycemia resulting from the combination of inappropriate insulin secretion and/or resistance to insulin action. If left uncontrolled, diabetes is associated with complications such as dysfunction and failure of various organs, and even premature death. Along with lifestyle-modification strategies, several classes of oral antidiabetic agents can be employed for glycemic control. Thus, therapeutic drug monitoring of these drugs is essential to maintain appropriate treatment...
December 2017: Bioanalysis
Tanja Pekez-Pavlisko, Maja Racic, Srebrenka Kusmuk
Background: During the transition processes, the Western Balkan countries were affected by conflicts and transition-related changes. Life expectancy in these countries is lower, while the mortality from non-communicable diseases (NCDs) is higher in comparison with western and northern parts of Europe. The primary aim of this study was to analyze the treatment possibilities for the most common NCDs in the Western Balkan countries. The secondary aim was to understand and compare the policies regarding prescribing-related competencies of family physicians...
2017: Frontiers in Public Health
Masaki Nakagaito, Shuji Joho, Ryuichi Ushijima, Makiko Nakamura, Tadakazu Hirai, Koichiro Kinugawa
Patients with stage D heart failure (HF) frequently become dependent on high doses of diuretics and inotropic agents. Recently, a sodium-glucose cotransporter 2 inhibitor (SGLT2i), an oral antidiabetic agent, has been demonstrated to have favorable effects in preventing HF. However, it remains unknown whether SGLT2i is reliable for patients with decompensated HF. We experienced a case of a patient with stage D HF for whom attempting intravenous dobutamine withdrawal was difficult even after the administration of all conventional pharmacological treatment...
December 12, 2017: International Heart Journal
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
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)
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
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
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
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
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