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https://www.readbyqxmd.com/read/28818558/current-and-emerging-pharmacotherapies-for-obesity-in-australia
#1
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 In addition, previous treatments such as phentermine-fenfluramine, rimonabant and sibutramine were withdrawn due to safety issues, resulting in lingering safety concerns.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
#2
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
#3
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)...
August 14, 2017: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/28636828/pharmacokinetic-drug-evaluation-of-extended-release-lorcaserin-for-the-treatment-of-obesity
#4
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
https://www.readbyqxmd.com/read/28600158/lorcaserin-plus-lifestyle-modification-for-weight-loss-maintenance-rationale-and-design-for-a-randomized-controlled-trial
#5
Jena Shaw Tronieri, Nasreen Alfaris, Ariana M Chao, Rebecca L Pearl, Naji Alamuddin, Zayna M Bakizada, Robert I Berkowitz, Thomas A Wadden
BACKGROUND/AIMS: Few studies have examined the efficacy of recently approved medications for chronic weight management in facilitating the maintenance of lost weight. This paper provides an overview of the design and rationale for a trial investigating whether lorcaserin, when combined with behavioral weight loss maintenance sessions (WLM), will facilitate the maintenance of losses of ≥5% of initial weight. METHODS: In this two-phase trial, participants with obesity will enroll in a 14-week run-in diet program consisting of weekly group lifestyle modification sessions and a 1000-1200kcal/d meal replacement diet...
August 2017: Contemporary Clinical Trials
https://www.readbyqxmd.com/read/28599864/the-anorectic-agent-lorcaserin-disturbs-estrous-cyclicity-and-produces-endometrial-hyperplasia-without-affecting-ovarian-population-in-female-rats
#6
Raghda T Abdel-Latif, Sawsan A Zaitone, Yousra Abdel-Mottaleb, Nabila N El-Maraghy
AIMS: The present study aims to investigate the effect of the new anorectic agent, lorcaserin, on estrous cyclicity, reproductive hormones and folliculogenesis in female mature rats. MATERIALS AND METHODS: Rats were divided into four groups; Group i: control group. Group ii-iv: rats treated with lorcaserin (5, 10 or 30mg/kg/day, p.o.), respectively. The treatment continued for 28days. KEY FINDINGS: Lorcaserin (5 or 10mg/kg) caused estrous cycle disturbance in 40% of treated rats while the high dose (30mg/kg) produced disturbances in 100% of the treated rats...
August 15, 2017: Life Sciences
https://www.readbyqxmd.com/read/28595525/obesity-induced-hypertension-new-insights
#7
Christina Antza, Stella Stabouli, Michalis Natsis, Ioannis Doundoulakis, Vasilios Kotsis
BACKGROUND: New insights on the relationship between weight loss and hypertension and the role of the newly approved anti-obesity drugs on hypertension will be discussed Methods: Weight loss is a major factor to reduce blood pressure when a patient with excess weight is advised from the health care provider to change his lifestyle. A healthy lifestyle with reduction in body weight, reduction in caloric intake, increased fruit and vegetables consumption and reduced salt intake concomitant with an increase in physical exercise can reduce body weight and hypertension in overweight and obese patients, but not all obese are able to reduce their blood pressure and lose weight without treatment and special dietary care...
June 7, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28462579/pharmacological-management-of-obesity
#8
Amanda Velazquez, Caroline M Apovian
Current management of obesity includes three main arms: behavioral modification, pharmacologic therapy, and bariatric surgery. Decades prior, the only pharmacological agents available to treat obesity were approved only for short-term use (≤ 12 weeks) by the Food and Drug Administration (FDA). However, in the last several years, the FDA has approved several medications for longer term treatment of obesity. This highlights the important progression that we, as a society, better appreciate now the chronicity and complexity of obesity as a disease...
April 28, 2017: Minerva Endocrinologica
https://www.readbyqxmd.com/read/28440045/coadministration-of-lorcaserin-and-phentermine-for-weight-management-a-12-week-randomized-pilot-safety-study
#9
Steven R Smith, W Timothy Garvey, Frank L Greenway, Sharon Zhou, Randi Fain, Robert Pilson, Ken Fujioka, Louis J Aronne
OBJECTIVE: To assess the short-term tolerability of lorcaserin alone or with two dose regimens of phentermine. METHODS: This was a 12-week, randomized, double-blind, pilot safety study of N = 238 nondiabetic patients with obesity or overweight with ≥1 comorbidity randomized to lorcaserin 10 mg twice daily (BID; LOR BID) alone or with phentermine 15 mg once daily (QD; LOR BID+PHEN QD) or 15 mg twice daily (LOR BID+PHEN BID). Patients reporting ≥ 1 of 9 potentially serotonergic adverse events (AEs), mean weight loss (WL), and ≥5% WL are reported...
May 2017: Obesity
https://www.readbyqxmd.com/read/28421338/tailoring-pharmacotherapy-to-specific-eating-behaviours-in-obesity-can-recommendations-for-personalised-therapy-be-made-from-the-current-data
#10
Carl A Roberts, Paul Christiansen, Jason C G Halford
Pharmacotherapy provides an adjunct to behaviour modification in the management of obesity. There are a number of new drug therapies purportedly targeting appetite; liraglutide, and bupropion/naltrexone, which are European Medicines Agency and US Food and Drug Administration (FDA) approved, and lorcaserin and phentermine/topiramate, which have FDA approval only. Each of the six drugs, used singly or in combination, has distinct pharmacological, and presumably distinct behavioural, mechanisms of action, thus the potential to provide defined therapeutic options to personalise the management of obesity...
August 2017: Acta Diabetologica
https://www.readbyqxmd.com/read/28392927/liraglutide-for-weight-management-a-critical-review-of-the-evidence
#11
A Mehta, S P Marso, I J Neeland
OBJECTIVE: To review the efficacy, safety, and clinical applicability of liraglutide for weight management from phase III clinical trials. METHODS: A search of the English language literature was performed using PubMed search terms: "liraglutide", "glucagon-like peptide-1 receptor agonist", and "randomized clinical trial". Articles and bibliographies relevant to the subject were reviewed and additional references known to the authors were included. RESULTS: Five randomized, placebo-controlled trials of liraglutide for weight management were identified...
March 2017: Obesity Science & Practice
https://www.readbyqxmd.com/read/28378293/pharmacotherapy-of-obesity-clinical-trials-to-clinical-practice
#12
REVIEW
Kishore M Gadde, Y Pritham Raj
PURPOSE OF REVIEW: This review provides an overview of the current state of drug therapy for obesity, with a focus on four new drug therapies-lorcaserin, phentermine/topiramate, naltrexone/bupropion, and liraglutide 3.0 mg-which have been approved by the US Food and Drug Administration (FDA) for long-term management of obesity since 2012. Topics discussed in this paper include rationale for pharmacotherapy, history of antiobesity drugs, and efficacy and safety data from randomized controlled trials with implications for clinical practice...
May 2017: Current Diabetes Reports
https://www.readbyqxmd.com/read/28371396/use-of-lorcaserin-for-glycemic-control-in-patients-with-type-2-diabetes-mellitus
#13
Leon I Igel, Louis J Aronne
No abstract text is available yet for this article.
May 2017: Obesity
https://www.readbyqxmd.com/read/28365033/pharmacokinetics-and-tolerability-of-lorcaserin-in-special-populations-elderly-patients-and-patients-with-renal-or-hepatic-impairment
#14
Ronald J Christopher, Michael E Morgan, Yong Tang, Christen Anderson, Matilde Sanchez, William Shanahan
PURPOSE: To determine whether dosage adjustment is likely to be necessary for effective and well-tolerated use of a pharmaceutical agent, guidance documents from the US Food and Drug Administration recommend pharmacokinetics studies in patients with impaired renal or impaired hepatic function and in the elderly population. Three studies were conducted to evaluate the pharmacokinetic properties and tolerability of lorcaserin in these populations. METHODS: Lorcaserin was evaluated in single-dose pharmacokinetics studies of 3 overweight/obese populations: (1) elderly (aged >65 years) patients; (2) patients with impaired renal function; and (3) those with impaired hepatic function...
March 29, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28345809/effect-of-lorcaserin-on-glycemic-parameters-in-patients-with-type-2-diabetes-mellitus
#15
Faidon Magkos, Elena Nikonova, Randi Fain, Sharon Zhou, Tony Ma, William Shanahan
OBJECTIVE: Lorcaserin, a 5-HT2C receptor agonist approved for chronic weight management, is also associated with improvements in glycemic parameters in patients with/without type 2 diabetes mellitus (T2DM), but the extent to which these effects are mediated by weight loss is unknown. This post hoc analysis further examines glycemic data from the Phase III BLOOM-DM study stratified by weight changes. METHODS: Patients with T2DM were randomized to lorcaserin 10 mg twice daily or placebo...
May 2017: Obesity
https://www.readbyqxmd.com/read/28338324/studies-to-examine-potential-tolerability-differences-between-the-5-ht2c-receptor-selective-agonists-lorcaserin-and-cp-809101
#16
Guy A Higgins, Leonardo B Silenieks, Amy Patrick, Ines A M De Lannoy, Paul J Fletcher, Linda A Parker, Neil J MacLusky, Laura C Sullivan, Teresa A Chavera, Kelly A Berg
Lorcaserin (LOR) is a selective 5-HT2C receptor agonist that has been FDA approved as a treatment for obesity. The most frequently reported side-effects of LOR include nausea and headache, which can be dose limiting. We have previously reported that in the rat, while LOR produced unconditioned signs characteristic of nausea/malaise, the highly selective 5-HT2C agonist CP-809101 (CP) produced fewer equivalent signs. Because this may indicate a subclass of 5-HT2C agonists having better tolerability, the present studies were designed to further investigate this apparent difference...
March 24, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28294132/5-ht2c-agonists-modulate-schizophrenia-like-behaviors-in-mice
#17
Vladimir M Pogorelov, Ramona M Rodriguiz, Jianjun Cheng, Mei Huang, Claire M Schmerberg, Herbert Y Meltzer, Bryan L Roth, Alan P Kozikowski, William C Wetsel
All FDA-approved antipsychotic drugs (APDs) target primarily dopamine D2 or serotonin (5-HT2A) receptors, or both; however, these medications are not universally effective, they may produce undesirable side effects, and provide only partial amelioration of negative and cognitive symptoms. The heterogeneity of pharmacological responses in schizophrenic patients suggests that additional drug targets may be effective in improving aspects of this syndrome. Recent evidence suggests that 5-HT2C receptors may be a promising target for schizophrenia since their activation reduces mesolimbic nigrostriatal dopamine release (which conveys antipsychotic action), they are expressed almost exclusively in CNS, and have weight-loss-promoting capabilities...
April 12, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28265714/a-short-history-of-the-5-ht2c-receptor-from-the-choroid-plexus-to-depression-obesity-and-addiction-treatment
#18
REVIEW
Jose M Palacios, Angel Pazos, Daniel Hoyer
This paper is a personal account on the discovery and characterization of the 5-HT2C receptor (first known as the 5-HT1C receptor) over 30 years ago and how it translated into a number of unsuspected features for a G protein-coupled receptor (GPCR) and a diversity of clinical applications. The 5-HT2C receptor is one of the most intriguing members of the GPCR superfamily. Initially referred to as 5-HT1CR, the 5-HT2CR was discovered while studying the pharmacological features and the distribution of [(3)H]mesulergine-labelled sites, primarily in the brain using radioligand binding and slice autoradiography...
May 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28245771/current-drug-targets-in-obesity-pharmacotherapy-a-review
#19
Sangeeta P Bhat, Arun Sharma
Obesity, an impending global pandemic, is not being effectively controlled by current measures such as lifestyle modifications, bariatric surgery or available medications. Its toll on health and economy compels us to look for more effective measures. Fortunately, the advances in biology and molecular technology have been in our favour for delineating new pathways in the pathophysiology of obesity and have led to subsequent development of new drug targets. Development of anti-obesity drugs has often been riddled with problems in the past...
February 27, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28107783/lorcaserin-suppresses-oxycodone-self-administration-and-relapse-vulnerability-in-rats
#20
Harshini Neelakantan, Erica D Holliday, Robert G Fox, Sonja J Stutz, Sandra D Comer, Margaret Haney, Noelle C Anastasio, F Gerard Moeller, Kathryn A Cunningham
Opioid use disorder (OUD) is a major public health problem. High relapse rates and poor treatment retention continue to pose major challenges in OUD treatment. Of the abused opioids, oxycodone is well described to maintain self-administration and evoke the durable conditioned responses ("cue reactivity") that result from pairing of opioid-related stimuli (e.g., paraphernalia) with repeated abuse. Serotonin (5-HT) neurotransmission, particularly through the 5-HT2C receptor (5-HT2CR), regulates psychostimulant reward and cue reactivity, and in the present experiments, we investigated the hypothesis that the selective 5-HT2CR agonist lorcaserin, which is approved by the United States Food and Drug Administration (FDA) for the treatment of obesity, will suppress oxycodone self-administration and oxycodone-associated cue reactivity in rats...
May 17, 2017: ACS Chemical Neuroscience
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