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https://www.readbyqxmd.com/read/29677253/in-type-2-diabetes-weekly-semaglutide-reduced-hba1c-and-increased-weight-loss-more-than-weekly-exenatide-er
#1
Eleni Bekiari, Thomas Karagiannis, Apostolos Tsapas
No abstract text is available yet for this article.
April 17, 2018: Annals of Internal Medicine
https://www.readbyqxmd.com/read/29663628/exenatide-effects-on-gastric-emptying-and-oral-glucose-appearance-in-plasma-a-quantitative-assessment-using-an-integrative-systems-pharmacology-model
#2
Veronika Voronova, Kirill Zhudenkov, Robert C Penland, David W Boulton, Gabriel Helmlinger, Kirill Peskov
Glucagon-like peptide (GLP)-1 and synthetic GLP-1 receptor agonists (GLP-1RA) slow gastric emptying rate (GER), thereby decreasing the Glucose Rate of Appearance (GluRA) in plasma, which may contribute to postprandial plasma glucose (PPG) stabilization under GLP-1RA treatment. A quantitative systems pharmacology (QSP) approach was used to evaluate the effect of exenatide immediate release (IR), a short-acting GLP-1RA, on GER and GluRA. The proposed model is based on the data from multiple published sources including: (1) GLP-1 and exenatide plasma concentration-time profiles; (2) GER estimates under placebo, GLP-1 or exenatide IR dosing; (3) GluRA measurements upon food intake...
April 16, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29650603/top-studies-relevant-to-primary-care-practice
#3
REVIEW
Danielle Perry, Michael R Kolber, Christina Korownyk, Adrienne J Lindblad, Jamil Ramji, Joey Ton, G Michael Allan
OBJECTIVE: To summarize 10 high-quality studies from 2017 that have strong relevance to primary care practice. QUALITY OF EVIDENCE: Study selection involved routine literature surveillance by a group of primary care health professionals. This included screening abstracts of important journals and Evidence Alerts, as well as searching the American College of Physicians Journal Club. MAIN MESSAGE: Topics of the 2017 articles include whether treating subclinical hypothyroidism improves outcomes or symptoms; whether evolocumab reduces cardiovascular disease as well as low-density lipoprotein levels; whether lifestyle interventions reduce medication use in patients with diabetes; whether vitamin D prevents cardiovascular disease, cancer, or upper respiratory tract infections; whether canagliflozin reduces clinical events in patients with diabetes; how corticosteroid injections affect knee osteoarthritis; whether drained abscesses benefit from antibiotic treatment; whether patients with diabetes benefit from bariatric surgery; whether exenatide reduces clinical events in patients with diabetes; and whether tympanostomy tubes affect outcomes in recurrent acute otitis media or chronic otitis media...
April 2018: Canadian Family Physician Médecin de Famille Canadien
https://www.readbyqxmd.com/read/29619854/tf-ligand-receptor-mediated-exenatide-zn-2-complex-oral-delivery-system-for-penetration-enhancement-of-exenatide
#4
Liping Zhang, Yanan Shi, Yina Song, Dongyu Duan, Xuemei Zhang, Kaoxiang Sun, Youxin Li
Safe and effective oral delivery of peptide is a challenge. Here, we used exenatide and zinc ions (Zn2+ ) to form a complex to explore a meaningful oral-targeted drug-delivery system. Polyethylene glycol-poly(lactic acid-co-glycolic acid) (PEG-PLGA) was used to prepare nanoparticles (NPs) to escape the degradation caused by gastrointestinal enzymes. Transferrin (Tf) was used as a targeting group. PEG-PLGA-NPs and Tf-modified exenatide-Zn2+ -loaded NPs (Tf-PEG-PLGA-NPs) were uniformly sized spheres according to transmission electron microscopy...
April 5, 2018: Journal of Drug Targeting
https://www.readbyqxmd.com/read/29596853/exenatide-has-a-pronounced-effect-on-energy-intake-but-not-energy-expenditure-in-non-diabetic-subjects-with-obesity-a-randomized-double-blind-placebo-controlled-trial
#5
Alessio Basolo, Joshua Burkholder, Kristy Osgood, Alexis Graham, Sarah Bundrick, Joseph Frankl, Paolo Piaggi, Marie S Thearle, Jonathan Krakoff
AIMS: Exenatide is a glucagon-like peptide 1 (GLP-1) mimetic which induces weight loss predominantly, it is presumed, via decreased food intake. However, circulating GLP-1 is also a determinant of energy expenditure. We sought to quantify the effect of exenatide on energy expenditure (EE) and energy intake. MATERIALS AND METHODS: In this single-center, randomized double-blind placebo controlled trial, we randomized 80 healthy, non-diabetic volunteers with obesity (46 women, age: 34...
March 26, 2018: Metabolism: Clinical and Experimental
https://www.readbyqxmd.com/read/29596830/liposome-encapsulated-clodronate-specifically-depletes-spinal-microglia-and-reduces-initial-neuropathic-pain
#6
Yi-Rui Wang, Xiao-Fang Mao, Hai-Yun Wu, Yong-Xiang Wang
Liposome-encapsulated clodronate (LEC) is a specific depletor of macrophages. Our study characterized the LEC depletory effects, given intrathecally, on spinal microglia and assessed its effects on initiation and maintenance of neuropathic pain. Measured by using the MTT assay, LEC treatment specifically inhibited cell viability of cultured primary microglia, but not astrocytes or neurons, from neonatal rats, with an IC50 of 43 μg/mL. In spinal nerve ligation-induced neuropathic rats, pretreatment (1 day but not 5 days earlier) with intrathecal LEC specifically depleted microglia (but not astrocytes or neurons) in both contralateral and ipsilateral dorsal horns by the same degree (63% vs...
March 28, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29574041/in-vivo-evaluation-of-an-oral-self-emulsifying-drug-delivery-system-sedds-for-exenatide
#7
Claudia Menzel, Thomas Holzeisen, Flavia Laffleur, Sergey Zaichik, Muthanna Abdulkarim, Mark Gumbleton, Andreas Bernkop-Schnürch
BACKGROUND: The aim of the study was to develop an oral self-emulsifying drug delivery system (SEDDS) for exenatide and to evaluate its in vivo efficacy. METHODS: Exenatide was lipidised via hydrophobic ion pairing with sodium docusate (DOC) and incorporated in SEDDS consisting of 35% Cremophor EL, 25% Labrafil 1944, 30% Capmul-PG 8 and 10% propylene glycol. Exenatide/DOC was characterized in terms of lipophilicity evaluating the octanol/water phase distribution (logP)...
March 21, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29573139/effects-of-exenatide-once-weekly-plus-dapagliflozin-exenatide-once-weekly-or-dapagliflozin-added-to-metformin-monotherapy-in-subgroups-of-patients-with-type-2-diabetes-in-the-duration-8-randomized-controlled-trial
#8
Juan P Frías, Elise Hardy, Azazuddin Ahmed, Peter Öhman, Serge Jabbour, Hui Wang, Cristian Guja
This analysis assessed whether responses with exenatide once weekly (QW) plus dapagliflozin (n=231), exenatide QW (n=230), or dapagliflozin (n=233) differed in key patient subpopulations of the DURATION-8 trial. Potential treatment-by-subgroup interactions for changes in glycated haemoglobin (HbA1c) and body weight after 28 weeks were evaluated among subgroups determined by baseline HbA1c, age, sex, body mass index, type 2 diabetes duration, race, ethnicity, and estimated glomerular filtration rate (eGFR). Exenatide QW plus dapagliflozin reduced HbA1c and body weight across all subgroups; least-squares mean (LSM) reductions ranged from -8...
March 23, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29551427/don-t-play-with-your-nodule-case-report-of-tachycardia-and-other-adverse-reactions-from-manipulation-of-an-exenatide-injection-site-nodule
#9
Caitlin Sandman, Benjamin Krainin, Jamie Roper
BACKGROUND: Type II diabetes mellitus (DM) is an increasingly prevalent cause of morbidity and mortality among U.S. adults, with increasing prevalence in emergency department (ED) visits. Multiple medications, such as exenatide, a glucagon-like peptide-1 agonist, have been developed in the past decade to combat this growing problem. This medication is well documented to cause gastrointestinal upset and skin nodules at the injection site. However, currently no documented cases exist regarding manipulation of injection nodules causing increased absorption or reports demonstrating an increase in adverse drug reactions...
March 15, 2018: Journal of Emergency Medicine
https://www.readbyqxmd.com/read/29541641/exenatide-with-metformin-ameliorated-visceral-adiposity-and-insulin-resistance
#10
Xuan Du, Wen Lu, Zijun Lu, Xinyu Shao, Chunhong Hu, Bimin Shi
Background: To study the effectiveness of exenatide with metformin and sequential treatment with exenatide and glargine added to metformin and their influence on insulin sensitivity and adipose distribution. Methods: 20 newly diagnosed obese type 2 diabetic patients were enrolled, and 2-month washout treatment of metformin, 6-month exenatide treatment, and 6-month glargine treatment were administrated sequentially accompanied with previous metformin. Glucolipid metabolic parameters were compared among groups...
2018: Journal of Diabetes Research
https://www.readbyqxmd.com/read/29537664/the-pattern-of-prescribing-of-glucose-modulating-agents-for-type-2-diabetes-in-general-practices-in-england-2016-17
#11
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
https://www.readbyqxmd.com/read/29525885/utilization-patterns-of-glucagon-like-peptide-1-receptor-agonists-in-patients-with-type-2-diabetes-mellitus-in-italy-a-retrospective-cohort-study
#12
Marco Orsini Federici, Janette McQuillan, Giovanni Biricolti, Serena Losi, Jeremie Lebrec, Catrina Richards, Cristiana Miglio, Kirsi Norrbacka
INTRODUCTION: Real-world evidence on glucagon-like peptide-1 receptor agonist (GLP-1 RAs) usage is emerging in different European countries but is lacking in Italy. This retrospective cohort study aimed to describe the real-world drug utilization patterns in patients initiating GLP-1 RAs for treating T2DM in Italy. METHODS: Adults aged ≥ 20 years and with ≥ 1 oral antidiabetic drug (alone or in combination with insulin) other than GLP-1 RAs in the 6 months prior to initiating exenatide twice daily (exBID), exenatide once weekly (exQW), dulaglutide once weekly (DULA), liraglutide once daily (LIRA) or lixisenatide once daily (LIXI) between March and July 2016 were retrospectively identified in the Italian IMS LifeLink™ longitudinal prescriptions database (retail pharmacy data)...
March 10, 2018: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/29488276/allelic-variant-in-the-glucagon-like-peptide-1-receptor-gene-associated-with-greater-effect-of-liraglutide-and-exenatide-on-gastric-emptying-a-pilot-pharmacogenetics-study
#13
V Chedid, P Vijayvargiya, P Carlson, K Van Malderen, A Acosta, A Zinsmeister, M Camilleri
BACKGROUND: Weight loss in response to the long-acting GLP-1 receptor (GLP1R) analog, liraglutide, is correlated with delay in gastric-emptying (GE). The aim of this pilot study was to assess whether specific genetic variants in GLP1R or TCF7L2 are associated with delayed GE and weight loss in obese patients treated with liraglutide or the short-acting GLP-1 agonist, exenatide. METHODS: We evaluated in obese individuals the associations of genetic variations of GLP1R (rs6923761) and TCF7L2 (rs7903146) on GE T1/2 and weight from two trials that evaluated separately exenatide, 5 μg BID for 30 days, or liraglutide, 3 mg daily for 5 weeks...
February 28, 2018: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/29480848/exenatide-once-weekly-for-smoking-cessation-study-protocol-for-a-randomized-clinical-trial
#14
Luba Yammine, Thomas R Kosten, Paul M Cinciripini, Charles E Green, Janet C Meininger, Jennifer A Minnix, Thomas F Newton
BACKGROUND: Cigarette smoking is the greatest preventable cause of morbidity and premature mortality in the United States. Approved pharmacological treatments for smoking cessation are marginally effective, underscoring the need for improved pharmacotherapies. A novel approach might use glucagon-like peptide-1 (GLP-1) agonists, which reduce alcohol and drug use in preclinical studies. GLP-1 is produced in the intestinal L-cells and in the hindbrain. The peptide maintains glucose homeostasis and reduces food intake...
January 2018: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29474443/amyloid-formation-reduces-protein-kinase-b-phosphorylation-in-primary-islet-%C3%AE-cells-which-is-improved-by-blocking-il-1%C3%AE-signaling
#15
Yun Zhang, Garth L Warnock, Ziliang Ao, Yoo Jin Park, Nooshin Safikhan, Aziz Ghahary, Lucy Marzban
Amyloid formation in the pancreatic islets due to aggregation of human islet amyloid polypeptide (hIAPP) contributes to reduced β-cell mass and function in type 2 diabetes (T2D) and islet transplantation. Protein kinase B (PKB) signaling plays a key role in the regulation of β-cell survival, function and proliferation. In this study, we used human and hIAPP-expressing transgenic mouse islets in culture as two ex vivo models of human islet amyloid formation to: 1. Investigate the effects of amyloid formation on PKB phosphorylation in primary islet β-cells; 2...
2018: PloS One
https://www.readbyqxmd.com/read/29473704/effect-of-exenatide-qw-or-placebo-both-added-to-titrated-insulin-glargine-in-uncontrolled-type-2-diabetes-the-duration-7-randomized-study
#16
Cristian Guja, Juan P Frías, Aniko Somogyi, Serge Jabbour, Hui Wang, Elise Hardy, Julio Rosenstock
AIMS: To compare the efficacy and safety of adding the glucagon-like peptide-1 receptor agonist exenatide once weekly (QW) 2 mg or placebo among patients with type 2 diabetes inadequately controlled despite titrated insulin glargine (IG) ± metformin. METHODS: This multicentre, double-blind study randomized (1:1) patients with persistent hyperglycaemia after 8-week IG titration (glycated haemoglobin [HbA1c] 7.0-10.5% [53-91 mmol/mol]) to exenatide QW or placebo...
February 23, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29463450/glucagon-like-peptide-1-receptor-agonists-and-cardiovascular-events-class-effects-versus-individual-patterns
#17
REVIEW
Soo Lim, Kyoung Min Kim, Michael A Nauck
Several new glucose-lowering medications have been approved, such as dipeptidyl peptidase-4 inhibitors, glucagon-like peptide-1 receptor agonists (GLP-1RAs), and sodium glucose cotransporter-2 inhibitors. Among GLP-1RAs, lixisenatide, a short-acting drug, did not show cardiovascular (CV) benefits in patients with Type 2 diabetes mellitus (T2D) and acute coronary syndrome. Extended-release exenatide was also not significantly better for CV outcomes. By contrast, once daily liraglutide and once weekly semaglutide, both long-acting GLP-1RAs, decreased the incidence of major adverse CV events and mortality...
February 17, 2018: Trends in Endocrinology and Metabolism: TEM
https://www.readbyqxmd.com/read/29439603/sgemaglutide-in-type-2-diabetes-is-it-the-best-glucagon-like-peptide-1-receptor-agonist-glp-1r-agonist
#18
REVIEW
Sheila A Doggrell
Glucagon-like peptide-1 (GLP-1) is produced by the gut, and in a glucose-dependent manner stimulates insulin secretion while inhibiting glucagon secretion, reduces appetite and energy intake, and delays gastric emptying. The GLP-1R agonist semaglutide has recently been registered to treat type 2 diabetes. Area covered: This review is of semaglutide in type 2 diabetes, and considers which properties of this GLP-1R agonist, may be responsible for its clinical outcome benefits . Expert opinion: The pharmacokinetics of semaglutide make it ideal for once-weekly dosing...
March 2018: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29424239/assessment-of-cardiovascular-risk-with-glucagon-like-peptide-1-receptor-agonists-in-patients-with-type-2-diabetes-using-an-alternative-measure-to-the-hazard-ratio
#19
Masayuki Kaneko, Mamoru Narukawa
BACKGROUND: Randomized clinical trials with the aim of evaluating the cardiovascular risks associated with glucagon-like peptide 1 (GLP-1) receptor agonists, lixisenatide, liraglutide, semaglutide, and exenatide, have been conducted. They showed different results among the agents, but the reason has not been explained. OBJECTIVE: To evaluate the cardiovascular risks associated with GLP-1 receptor agonists by using an alternative measure to the hazard ratio. METHODS: We used the difference in restricted mean survival time (RMST) as a measure of cardiovascular risks...
February 1, 2018: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/29414148/exenatide-modulates-metalloproteinase-expression-in-human-cardiac-smooth-muscle-cells-via-the-inhibition-of-akt-signaling-pathway
#20
Enrique Gallego-Colon, Agnieszka Klych-Ratuszny, Agnieszka Kosowska, Wojciech Garczorz, Mohammad Reza F Aghdam, Michal Wozniak, Tomasz Francuz
BACKGROUND: Incretin analogue drugs, a FDA-approved treatment in diabetes, has been tested for its therapeutic properties as modulators of atherosclerosis. We investigated the effects of incretin drugs on the modulation of gene expression and protein levels of matrix metalloproteinases (MMPs) as well as their inhibitors - tissue inhibitors of metalloproteinases (TIMPs) in coronary artery smooth muscle cells (hCASMC) in the context of atherosclerotic plaque formation and inflammation. METHODS: TNFα-stimulated hCASMC were treated with Glucagon-like Peptide 1 (GLP-1) (10 nM and 100 nM) and Exendin-4 (1 nM and 10 nM)...
October 4, 2017: Pharmacological Reports: PR
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