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https://www.readbyqxmd.com/read/29388462/safety-and-tolerability-of-new-generation-anti-obesity-medications-a-narrative-review
#1
Dhiren K Patel, Fatima Cody Stanford
The prevalence of obesity and associated comorbidities is rising. Despite their weight-loss efficacy, new generation anti-obesity medications are only prescribed to a minority of adults with obesity, possibly, which in part may be due to safety concerns. This review presents detailed safety profiles for orlistat, phentermine/topiramate, lorcaserin, naltrexone/bupropion and liraglutide 3.0 mg, and discusses the associated risk-benefit profiles. Two anti-obesity medications presented safety issues that warranted further discussion; phentermine/topiramate (fetal toxicity) and liraglutide 3...
February 8, 2018: Postgraduate Medicine
https://www.readbyqxmd.com/read/29376439/pharmacotherapy-for-obesity-in-individuals-with-type-2-diabetes
#2
Tariq Chukir, Alpana P Shukla, Katherine H Saunders, Louis J Aronne
Type 2 diabetes (T2DM) is associated with significant morbidity and mortality. Obesity is one of the main risk factors for T2DM and its management requires a multidisciplinary approach, which may include pharmacotherapy. Areas covered: In this paper, data on efficacy, tolerability and safety of FDA-approved pharmacotherapies for obesity (orlistat, phentermine/topiramate extended-release, lorcaserin, bupropion sustained release/naltrexone sustained release and liraglutide) are reviewed, focusing on individuals with type 2 diabetes...
January 29, 2018: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/29363287/effect-of-lorcaserin-alone-and-in-combination-with-phentermine-on-food-cravings-after-12-week-treatment-a-randomized-substudy
#3
Candida J Rebello, Elena V Nikonova, Sharon Zhou, Louis J Aronne, Ken Fujioka, W Timothy Garvey, Steven R Smith, Ann A Coulter, Frank L Greenway
OBJECTIVE: This study evaluated the effect of lorcaserin 10 mg twice daily (LOR BID), or with phentermine 15 mg once daily (LOR BID + PHEN QD) and 15 mg twice daily (LOR BID + PHEN BID), in conjunction with energy restriction on food cravings. METHODS: Two hundred and thirty-five patients without diabetes but with obesity or overweight and ≥ 1 comorbidity received LOR BID, LOR BID + PHEN QD, or LOR BID + PHEN BID for 12 weeks in a randomized double-blind study...
February 2018: Obesity
https://www.readbyqxmd.com/read/29305933/effects-of-weight-loss-medications-on-cardiometabolic-risk-profiles-a-systematic-review-and-network-meta-analysis
#4
Rohan Khera, Ambarish Pandey, Apoorva K Chandar, Mohammad H Murad, Larry J Prokop, Ian J Neeland, Jarett Berry, Michael Camilleri, Siddharth Singh
BACKGROUND & AIMS: We performed a systematic review and network meta-analysis to evaluate the overall and comparative effects of weight-loss medications, approved by the Food and Drug Administration (FDA) for long-term use, on cardiometabolic risk profiles of obese adults. METHODS: We performed a systematic literature review through February 28, 2017 to identify randomized clinical trials of the effects of FDA-approved weight loss medications (orlistat, lorcaserin, naltrexone-bupropion, phentermine-topiramate, and liraglutide), administered to obese adults for 1 year or more, compared with placebo or another active agent...
January 3, 2018: Gastroenterology
https://www.readbyqxmd.com/read/29301630/obesity-pathophysiology-and-management
#5
REVIEW
Kishore M Gadde, Corby K Martin, Hans-Rudolf Berthoud, Steven B Heymsfield
Obesity continues to be among the top health concerns across the globe. Despite our failure to contain the high prevalence of obesity, we now have a better understanding of its pathophysiology, and how excess adiposity leads to type 2 diabetes, hypertension, and cardiovascular disease. Lifestyle modification is recommended as the cornerstone of obesity management, but many patients do not achieve long-lasting benefits due to difficulty with adherence as well as physiological and neurohormonal adaptation of the body in response to weight loss...
January 2, 2018: Journal of the American College of Cardiology
https://www.readbyqxmd.com/read/29288545/a-randomized-trial-of-lorcaserin-and-lifestyle-counseling-for-maintaining-weight-loss-achieved-with-a-low-calorie-diet
#6
Jena Shaw Tronieri, Thomas A Wadden, Robert I Berkowitz, Ariana M Chao, Rebecca L Pearl, Naji Alamuddin, Sharon M Leonard, Ray Carvajal, Zayna M Bakizada, Emilie Pinkasavage, Kathryn A Gruber, Olivia A Walsh, Nasreen Alfaris
OBJECTIVE: Improving the maintenance of lost weight remains a critical challenge, which can be addressed by long-term behavioral and/or pharmacological interventions. METHODS: This study investigated the efficacy of combined behavioral and pharmacological treatment in facilitating weight loss maintenance (WLM) in 137 adults (86.1% female; 68.6% black; BMI = 37.0 ± 5.6 kg/m2 ) who had lost ≥ 5% of initial weight during a 14-week low-calorie diet (LCD) program (mean = 9...
December 29, 2017: Obesity
https://www.readbyqxmd.com/read/29287757/efficacy-of-adjuvant-weight-loss-medication-after-bariatric-surgery
#7
Zubaidah Nor Hanipah, Elie C Nasr, Emre Bucak, Philip R Schauer, Ali Aminian, Stacy A Brethauer, Derrick Cetin
BACKGROUND: Some patients do not achieve optimal weight loss or regain weight after bariatric surgery. In this study, we aimed to determine the effectiveness of adjuvant weight loss medications after surgery for this group of patients. SETTING: An academic medical center. METHODS: Weight changes of patients who received weight loss medications after bariatric surgery from 2012 to 2015 at a single center were studied. RESULTS: Weight loss medications prescribed for 209 patients were phentermine (n = 156, 74...
January 2018: Surgery for Obesity and related Diseases: Official Journal of the American Society for Bariatric Surgery
https://www.readbyqxmd.com/read/29251366/liquid-chromatographic-separation-and-thermodynamic-investigation-of-lorcaserin-hydrochloride-enantiomers-on-immobilized-amylose-based-chiral-stationary-phase
#8
Dattatraya V Wani, Vipul P Rane, Santosh N Mokale
A novel liquid chromatographic method was developed for enantiomeric separation of lorcaserin hydrochloride on Chiralpak IA column containing chiral stationary phase immobilized with amylose tris (3.5-dimethylphenylcarbamate) as chiral selector. Baseline separation with resolution greater than 4 was achieved using mobile phase containing mixture of n-hexane/ethanol/methanol/diethylamine (95:2.5:2.5:0.1, v/v/v/v) at a flow rate of 1.2 mL/min. The limit of detection and limit of quantification of the S-enantiomer were found to be 0...
December 18, 2017: Chirality
https://www.readbyqxmd.com/read/29246856/the-behavioral-pharmacology-and-therapeutic-potential-of-lorcaserin-for-substance-use-disorders
#9
REVIEW
Gregory T Collins, Lisa R Gerak, Charles P France
Substance abuse is serious public health problem for which there are few effective pharmacotherapies. Traditional strategies for drug development have focused on antagonists to block the abuse-related effects of a drug at its site of action, and agonists to replace/mimic the effects of the abused substance. However, recent efforts have targeted receptors, such as serotonin (5-HT)2 receptors, that can indirectly modulate dopamine neurotransmission with the goal of developing a pharmacotherapy that might be effective at reducing the abuse-related effects of drugs more generally...
December 12, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29217539/inhibition-of-cocaine-and-3-4-methylenedioxypyrovalerone-mdpv-self-administration-by-lorcaserin-is-mediated-by-5-ht2c-receptors-in-rats
#10
Brenda M Gannon, Agnieszka Sulima, Kenner C Rice, Gregory T Collins
Lorcaserin is a serotonin (5-HT)2C receptor-preferring agonist approved by the US Food and Drug Administration to treat obesity. Lorcaserin has been shown to decrease cocaine self-administration in rats and monkeys. Although this effect is partially inhibited by a 5-HT2C receptor antagonist (SB 242084), lorcaserin also has effects at 5-HT2A and 5-HT1A receptors and the relative contribution of these receptors to its anti-cocaine effects has not been investigated. The goals of this study were to determine: (1) the potency and effectiveness of lorcaserin to decrease self-administration of cocaine and 3,4-methylenedioxypyrovalerone (MDPV), a common "bath salts" constituent; and (2) the receptor(s) mediating the effects of lorcaserin on cocaine and MDPV self-administration...
December 7, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29171917/increasing-motor-neuron-excitability-to-treat-weakness-in-sepsis
#11
Paul Nardelli, Randall Powers, Tim C Cope, Mark M Rich
OBJECTIVE: Weakness induced by critical illness (intensive care unit acquired weakness) is a major cause of disability in patients and is currently untreatable. We recently identified a defect in repetitive firing of lower motor neurons as a novel contributor to intensive care unit acquired weakness. In order to develop therapy for intensive care unit acquired weakness, it was necessary to determine the mechanism underlying the defect in repetitive firing. METHODS: Both computer simulation and in vivo dynamic voltage clamp of spinal motor neurons in septic rats were employed to explore potential mechanisms underlying defective repetitive firing...
November 24, 2017: Annals of Neurology
https://www.readbyqxmd.com/read/29156182/obesity-pharmacotherapy
#12
REVIEW
Katherine H Saunders, Devika Umashanker, Leon I Igel, Rekha B Kumar, Louis J Aronne
Although diet, physical activity, and behavioral modifications are the cornerstones of weight management, weight loss achieved by lifestyle modifications alone is often limited and difficult to maintain. Pharmacotherapy for obesity can be considered if patients have a body mass index (BMI) of 30 kg/m2 or greater or BMI of 27 kg/m2 or greater with weight-related comorbidities. The 6 most commonly used antiobesity medications are phentermine, orlistat, phentermine/topiramate extended release, lorcaserin, naltrexone sustained release (SR)/bupropion SR, and liraglutide 3...
January 2018: Medical Clinics of North America
https://www.readbyqxmd.com/read/29151591/us-health-policy-and-prescription-drug-coverage-of-fda-approved-medications-for-the-treatment-of-obesity
#13
G Gomez, F C Stanford
OBJECTIVE: Obesity is now the most prevalent chronic disease in the United States, which amounts to an estimated $147 billion in health care spending annually. The Affordable Care Act (ACA) enacted in 2010 included provisions for private and public health insurance plans that expanded coverage for lifestyle/behavior modification and bariatric surgery for the treatment of obesity. Pharmacotherapy, however, has not been included despite their evidence-based efficacy. We set out to investigate the coverage of Food and Drug Administration-approved medications for obesity within Medicare, Medicaid and ACA-established marketplace health insurance plans...
November 20, 2017: International Journal of Obesity: Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/29116785/a-positive-allosteric-modulator-of-the-serotonin-5-ht2c-receptor-for-obesity
#14
Javier García-Cárceles, Juan M Decara, Henar Vázquez-Villa, Ramón Rodríguez, Eva Codesido, Jacobo Cruces, José Brea, María I Loza, Francisco Alén, Joaquin Botta, Peter J McCormick, Juan A Ballesteros, Bellinda Benhamú, Fernando Rodríguez de Fonseca, María L López-Rodríguez
The 5-HT2CR agonist lorcaserin, clinically approved for the treatment of obesity, causes important side effects mainly related to subtype selectivity. In the search for 5-HT2CR allosteric modulators as safer antiobesity drugs, a chemical library from Vivia Biotech was screened using ExviTech platform. Structural modifications of identified hit VA240 in synthesized analogues 6-41 afforded compound 11 (N-[(1-benzyl-1H-indol-3-yl)methyl]pyridin-3-amine, VA012), which exhibited dose-dependent enhancement of serotonin efficacy, no significant off-target activities, and low binding competition with serotonin or other orthosteric ligands...
November 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29072522/role-of-impulsivity-and-reward-in-the-anti-obesity-actions-of-5-ht2c-receptor-agonists
#15
Guy A Higgins, Fiona D Zeeb, Paul J Fletcher
The selective 5-HT2C receptor agonist lorcaserin entered clinical obesity trials with the prevalent view that satiety was a primary mechanism of action. Subsequent Phase II and III trials demonstrated efficacy in terms of weight loss, although the overall effect size (~3% placebo-corrected change) is considered modest. Lorcaserin has been approved by the FDA for the treatment of obesity with lifestyle modification, but since its introduction in 2013 its sales are in decline, probably due to its overall modest effect...
October 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/29044720/observational-comparative-effectiveness-of-pharmaceutical-treatments-for-obesity-within-the-veterans-health-administration
#16
Ted R Grabarczyk
STUDY OBJECTIVE: To compare the effectiveness of weight-management medications used to assist with weight loss in real-world clinical practice in the Veterans Health Administration (VHA). DESIGN: Retrospective, multicenter, observational cohort study. DATA SOURCE: National VA Corporate Data Warehouse. PATIENTS: A total of 66,035 VA patients aged 18 years or older with a body mass index of 25 kg/m2 or greater who had an initial fill for a study medication (orlistat [6153 patients], phentermine [304 patients], lorcaserin [298 patients], or phentermine-topiramate extended release [233 patients]) or participation in the VA's MOVE! weight-management program with at least three total visits in a clinic coded as a MOVE clinic in the subsequent 24 weeks (59,047 patients) between January 1, 2012, and July 1, 2016...
January 2018: Pharmacotherapy
https://www.readbyqxmd.com/read/29042804/weight-loss-medications-in-canada-a-new-frontier-or-a-repeat-of-past-mistakes
#17
Sean Wharton, Jasmine Lee, Rebecca Ag Christensen
Current methods for the treatment of excess weight can involve healthy behavior changes, pharmacotherapy, and surgical interventions. Many individuals are able to lose some degree of weight through behavioral changes; however, they are often unable to maintain their weight loss long-term. This is in part due to physiological processes that cannot be addressed through behavioral changes alone. Bariatric surgery, which is the most successful treatment for excess weight to date, does result in physiological changes that can help with weight loss and weight maintenance...
2017: Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy
https://www.readbyqxmd.com/read/29040827/effects-of-lorcaserin-belviq-%C3%A2-on-nicotine-and-food-maintained-responding-in-non-human-primates
#18
David S Jacobs, Claire E Barkin, Michelle R Kohut, Jack Bergman, Stephen J Kohut
BACKGROUND: Accumulating evidence suggests that the FDA-approved serotonin 5-HT2C receptor agonist, lorcaserin (Belviq(®)), may be a promising candidate for the management of substance use disorders, including nicotine addiction. The present study was conducted to determine the efficacy and selectivity of acute or continuous lorcaserin treatment for decreasing the reinforcing effects of nicotine in a primate species. METHODS: Adult rhesus monkeys (n=4) with a history of nicotine self-administration (>2years) responded for injections of nicotine (0...
October 10, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29031711/lorcaserin-improves-glycemic-control-via-a-melanocortin-neurocircuit
#19
Luke K Burke, Emmanuel Ogunnowo-Bada, Teodora Georgescu, Claudia Cristiano, Pablo B Martinez de Morentin, Lourdes Valencia Torres, Giuseppe D'Agostino, Christine Riches, Nicholas Heeley, Yue Ruan, Marcelo Rubinstein, Malcolm J Low, Martin G Myers, Justin J Rochford, Mark L Evans, Lora K Heisler
OBJECTIVE: The increasing prevalence of type 2 diabetes (T2D) and associated morbidity and mortality emphasizes the need for a more complete understanding of the mechanisms mediating glucose homeostasis to accelerate the identification of new medications. Recent reports indicate that the obesity medication lorcaserin, a 5-hydroxytryptamine (5-HT, serotonin) 2C receptor (5-HT2CR) agonist, improves glycemic control in association with weight loss in obese patients with T2D. Here we evaluate whether lorcaserin has an effect on glycemia without body weight loss and how this effect is achieved...
October 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/29024559/comparative-efficacy-of-five-long-term-weight-loss-drugs-quantitative-information-for-medication-guidelines
#20
REVIEW
Z Dong, L Xu, H Liu, Y Lv, Q Zheng, L Li
Quantitative information is scarce in current obesity medication guidelines, and they do not clearly reflect the differences in the efficacy characteristics among various drugs. This study quantitatively assessed the efficacy characteristics of five FDA-approved long-term weight loss drugs. Potentially eligible studies were obtained from public databases. Using the differences in the weight change from baseline between the drug group and the corresponding placebo group as the major indicator of efficacy, a time-effect model was established, and crucial pharmacodynamic parameters, such as the maximal efficacy, drug onset time and rate of body weight regain after the maximal efficacy point, were used to reflect the differences in efficacy among the five drugs...
December 2017: Obesity Reviews: An Official Journal of the International Association for the Study of Obesity
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