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Lorcaserin

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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
#1
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
#2
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
#3
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/m(2) or greater or BMI of 27 kg/m(2) 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
#4
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 FDA-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
#5
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
#6
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
#7
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/m(2) 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...
October 17, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/29042804/weight-loss-medications-in-canada-a-new-frontier-or-a-repeat-of-past-mistakes
#8
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
#9
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
#10
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
#11
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...
October 10, 2017: Obesity Reviews: An Official Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/29024552/current-pharmacotherapies-for-obesity-a-practical-perspective
#12
REVIEW
Angela Golden
BACKGROUND AND PURPOSE: To review the currently available pharmacotherapies for obesity management with a particular focus on the United States. METHODS: Narrative review based on literature searches and the latest prescribing information (up to July 2017). CONCLUSIONS: Obesity pharmacotherapies may assist those individuals who have obesity, or overweight with comorbidities, who have failed to maintain weight loss with lifestyle modifications alone (caloric restriction and increased physical activity)...
October 2017: Journal of the American Association of Nurse Practitioners
https://www.readbyqxmd.com/read/28974368/correlation-of-pharmacokinetics-and-brain-penetration-data-of-adult-zebrafish-with-higher-mammals-including-humans
#13
Pushkar Kulkarni, Raghavender Medishetti, Nagaraju Nune, Swapna Yellanki, Vijaykumar Sripuram, Pallavi Rao, Dharmarajan Sriram, Uday Saxena, Srinivas Oruganti, Perumal Yogeeswari
INTRODUCTION: Adult zebrafish pharmacology is evolving rapidly for creating efficacy and safety models for drug discovery. However, there is very limited research in understanding pharmacokinetics (PK) in adult zebrafish. Methods for understanding PK will help in conducting pharmacokinetic - pharmacodynamic (PK-PD) correlations and improving the quality and applicability of data obtained using zebrafish. METHODS: We conducted adult zebrafish PK and brain penetration studies on two known compounds (irinotecan and lorcaserin) with distinct PK and brain penetration properties using validated LCMS/MS method...
September 30, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28935287/past-present-and-future-of-pharmacotherapy-for-obesity
#14
David Benaiges, Juan Pedro-Botet, Juana A Flores-Le Roux, Elisenda Climent, Albert Goday
Conventional treatment for obesity with diet, exercise and bariatric surgery has limitations; thus, it is necessary to have pharmacological tools. In the past, different drugs were marketed that were withdrawn due to safety problems. There are currently 3 drugs approved by the European Medicines Agency (EMA) and the Food and Drug Administration (FDA) for obesity therapy (orlistat, combination of bupropion and delayed-release naltrexone and liraglutide) and two more only authorized by FDA (lorcaserin and the combination of phentermine and extended release topiramate)...
September 18, 2017: Clínica e Investigación en Arteriosclerosis
https://www.readbyqxmd.com/read/28891142/network-meta-analysis-of-lorcaserin-and-oral-hypoglycaemics-for-patients-with-type-2-diabetes-mellitus-and-obesity
#15
L M Neff, M S Broder, D Beenhouwer, E Chang, E Papoyan, Z W Wang
In addition to weight loss, randomized controlled trials have shown improvement in glycaemic control in patients taking lorcaserin. The aim of this study aim was to compare adding lorcaserin or other glucose lowering medications to metformin on weight and glycaemic control. A systematic review and network meta-analysis of randomized controlled trials were conducted. Included studies (published 1990-2014) were of lorcaserin or glucose lowering medications in type 2 diabetic patients compared to placebo or different active treatments...
September 10, 2017: Clinical Obesity
https://www.readbyqxmd.com/read/28868576/choice-between-delayed-food-and-immediate-opioids-in-rats-treatment-effects-and-individual-differences
#16
Leigh V Panlilio, Maria E Secci, Charles W Schindler, Charles W Bradberry
RATIONALE: Addiction involves maladaptive choice behavior in which immediate drug effects are valued more than delayed nondrug rewards. OBJECTIVES AND METHODS: To model this behavior and extend our earlier work with the prescription opioid oxycodone, we allowed rats to choose between immediate intravenous delivery of the short-acting opioid remifentanil and delayed delivery of highly palatable food pellets. Treatment drugs were tested on a baseline where remifentanil was preferred over food...
November 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28818558/current-and-emerging-pharmacotherapies-for-obesity-in-australia
#17
REVIEW
Samantha Hocking, Anthony Dear, Michael A Cowley
BACKGROUND: Obesity is a major issue in Australia and globally. Many individuals struggle to maintain weight loss with lifestyle modification, and adjunctive pharmacotherapy may help. Historically, there have been limited pharmacotherapies for managing obesity. In addition, previous treatments such as phentermine-fenfluramine, rimonabant and sibutramine were withdrawn due to safety issues, resulting in lingering safety concerns. METHODS: This is a narrative review of published data examining four new pharmacotherapy options for weight management in Australia...
August 14, 2017: Obesity Research & Clinical Practice
https://www.readbyqxmd.com/read/28815987/health-related-quality-of-life-in-randomized-controlled-trials-of-lorcaserin-for-obesity-management-what-mediates-improvement
#18
R L Kolotkin, R D Crosby, Z Wang
Lorcaserin, plus diet and exercise, has demonstrated significant weight loss and improved cardiometabolic parameters vs. placebo in patients with overweight/obesity in three randomized, placebo-controlled trials. We examined whether lorcaserin is also associated with greater improvements in health-related quality of life (HRQOL) and whether these improvements are wholly attributable to weight loss. Pooled data from Behavioral Modification and Lorcaserin for Overweight and Obesity Management (BLOOM), Behavioral Modification and Lorcaserin Second Study for Obesity Management (BLOSSOM) and BLOOM-Diabetes Mellitus (BLOOM-DM) trials were analysed (n = 5624)...
August 17, 2017: Clinical Obesity
https://www.readbyqxmd.com/read/28805659/the-atypical-antipsychotic-olanzapine-causes-weight-gain-by-targeting-serotonin-receptor-2c
#19
Caleb C Lord, Steven C Wyler, Rong Wan, Carlos M Castorena, Newaz Ahmed, Dias Mathew, Syann Lee, Chen Liu, Joel K Elmquist
Atypical antipsychotics such as olanzapine often induce excessive weight gain and type 2 diabetes. However, the mechanisms underlying these drug-induced metabolic perturbations remain poorly understood. Here, we used an experimental model that reproduces olanzapine-induced hyperphagia and obesity in female C57BL/6 mice. We found that olanzapine treatment acutely increased food intake, impaired glucose tolerance, and altered physical activity and energy expenditure in mice. Furthermore, olanzapine-induced hyperphagia and weight gain were blunted in mice lacking the serotonin 2C receptor (HTR2C)...
September 1, 2017: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/28636828/pharmacokinetic-drug-evaluation-of-extended-release-lorcaserin-for-the-treatment-of-obesity
#20
REVIEW
Kathryn M Hurren, Marissa W Dunham
Lorcaserin is a serotonin 2C receptor antagonist that was FDA approved in 2012. Lorcaserin is recently available as an extended-release (ER) formulation for the treatment of obesity as an adjunct to lifestyle modification. Areas covered: The pharmacokinetics, pharmacodynamics, efficacy, and safety of lorcaserin ER will be reviewed. Expert opinion: Lorcaserin ER 20mg daily provides drug exposure bioequivalent to lorcaserin immediate release (IR) 10mg twice daily. Lorcaserin IR is associated with 3.3 and 3.0% placebo-subtracted weight loss in patients without and with diabetes, respectively...
August 2017: Expert Opinion on Drug Metabolism & Toxicology
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