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Lorcaserin

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https://www.readbyqxmd.com/read/29676530/short-and-long-term-changes-in-health-related-quality-of-life-with-weight-loss-results-from-a-randomized-controlled-trial
#1
Rebecca L Pearl, Thomas A Wadden, Jena Shaw Tronieri, Robert I Berkowitz, Ariana M Chao, Naji Alamuddin, Sharon M Leonard, Raymond Carvajal, Zayna M Bakizada, Emilie Pinkasavage, Kathryn A Gruber, Olivia A Walsh, Nasreen Alfaris
OBJECTIVE: The objective of this study was to determine the effects of weight loss and weight loss maintenance (WLM) on weight-specific health-related quality of life in a 66-week trial. METHODS: Adults with obesity (N = 137, 86.1% female, 68.6% black, mean age = 46.1 years) who had lost ≥ 5% of initial weight in a 14-week intensive lifestyle intervention/low-calorie diet (LCD) program were randomly assigned to lorcaserin or placebo for an additional 52-week WLM program...
April 20, 2018: Obesity
https://www.readbyqxmd.com/read/29624732/effect-of-a-5-ht2c-receptor-agonist-on-urethral-closure-mechanisms-in-female-rats
#2
Mifuka Ouchi, Takeya Kitta, Yukiko Kanno, Madoka Higuchi, Mio Togo, Kimihiko Moriya, Nobuo Shinohara
AIMS: The serotonin (5-HT2c) receptor is known to be involved in the mechanism of urethral closure in a model of stress incontinence. Lorcaserin (Belviq®) has received Food and Drug Administration approval for the treatment of obesity. However, it is unclear whether this selective 5-HT2c receptor agonist enhances urethral closure in stress urinary incontinence (SUI) models. Therefore, we investigated whether lorcaserin could enhance urethral closure in female rats with vaginal distention (VD)...
April 6, 2018: Neurourology and Urodynamics
https://www.readbyqxmd.com/read/29498158/preclinical-evidence-for-combining-the-5-ht-2c-receptor-agonist-lorcaserin-and-varenicline-as-a-treatment-for-nicotine-dependence
#3
Paul J Fletcher, Zhaoxia Li, Leo B Silenieks, Cam MacMillan, Ines DeLannoy, Guy A Higgins
Varenicline, a nicotinic acetylcholine receptor partial agonist, is used to treat nicotine dependence. Lorcaserin, a 5-HT2C receptor agonist has been approved in some countries to treat obesity. Based on preclinical and preliminary clinical evidence, lorcaserin may have potential to treat nicotine dependence. These experiments examined in rats the effects of combining varenicline (0.5 or 1 mg/kg) and lorcaserin (0.3, 0.6 and 1 mg/kg) on nicotine self-administration, reinstatement of nicotine seeking, responding for food and impulsive action...
March 2, 2018: Addiction Biology
https://www.readbyqxmd.com/read/29496415/synthesis-of-enantiopure-antiobesity-drug-lorcaserin
#4
Ivana Gazic Smilovic, Jerome Cluzeau, Frank Richter, Sven Nerdinger, Erwin Schreiner, Gerhard Laus, Herwig Schottenberger
Acylation of enantiomerically pure (R)-2-(3-chlorophenyl)propan-1-amine using chloroacetyl chloride, followed by borane reduction and aluminum chloride catalyzed cyclization yielded enantiopure lorcaserin.
February 21, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29388462/safety-and-tolerability-of-new-generation-anti-obesity-medications-a-narrative-review
#5
REVIEW
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...
March 2018: Postgraduate Medicine
https://www.readbyqxmd.com/read/29376439/pharmacotherapy-for-obesity-in-individuals-with-type-2-diabetes
#6
REVIEW
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...
February 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
#7
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
#8
Rohan Khera, Ambarish Pandey, Apoorva K Chandar, Mohammad H Murad, Larry J Prokop, Ian J Neeland, Jarett D 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 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 Food and Drug Administration-approved weight-loss medications (ie, orlistat, lorcaserin, naltrexone-bupropion, phentermine-topiramate, and liraglutide) administered to obese adults for 1 year or more, compared with placebo or another active agent...
April 2018: Gastroenterology
https://www.readbyqxmd.com/read/29301630/obesity-pathophysiology-and-management
#9
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
#10
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...
February 2018: Obesity
https://www.readbyqxmd.com/read/29287757/efficacy-of-adjuvant-weight-loss-medication-after-bariatric-surgery
#11
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
#12
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...
March 2018: Chirality
https://www.readbyqxmd.com/read/29246856/the-behavioral-pharmacology-and-therapeutic-potential-of-lorcaserin-for-substance-use-disorders
#13
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
#14
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 decreases cocaine self-administration in rats and monkeys. Although this effect is partially inhibited by a 5-HT2C receptor antagonist (SB242084), 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...
March 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29171917/increasing-motor-neuron-excitability-to-treat-weakness-in-sepsis
#15
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. 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...
December 2017: Annals of Neurology
https://www.readbyqxmd.com/read/29156182/obesity-pharmacotherapy
#16
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
#17
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...
March 2018: 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
#18
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
#19
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
#20
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
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