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Vidya Narayanaswami, Linda P Dwoskin
Obesity is a global epidemic that contributes to a number of health complications including cardiovascular disease, type 2 diabetes, cancer and neuropsychiatric disorders. Pharmacotherapeutic strategies to treat obesity are urgently needed. Research over the past two decades has increased substantially our knowledge of central and peripheral mechanisms underlying homeostatic energy balance. Homeostatic mechanisms involve multiple components including neuronal circuits, some originating in hypothalamus and brain stem, as well as peripherally-derived satiety, hunger and adiposity signals that modulate neural activity and regulate eating behavior...
October 20, 2016: Pharmacology & Therapeutics
Anna Marcinkowska-Gapińska, Piotr Kowal
The aim of the study is to test the influence of in vivo magnetostimulation on the rheological properties of blood in neurological patients. Blood circulation in the body depends both on the mechanical properties of the circulatory system and on the physical and physicochemical properties of blood. The main factors influencing the rheological properties of blood are as follows: hematocrit, plasma viscosity, whole-blood viscosity, red cells aggregability, deformability, and the ability of red cells to orient in the flow...
2016: Electromagnetic Biology and Medicine
Matthew M Sherman, Sinziana Ungureanu, Jose A Rey
Naltrexone/bupropion ER (Contrave): newly approved treatment option for chronic weight management in obese adults.
March 2016: P & T: a Peer-reviewed Journal for Formulary Management
Caroline M Apovian
Contrave(®) is a combination of naltrexone hydrochloride extended release and bupropion hydrochloride extended release for the treatment of obesity, and is used with lifestyle modification. Its safety and efficacy were assessed in four randomized, double-blind, placebo-controlled, 56-week Phase III clinical trials in 4536 adult subjects: COR-1, COR-II, COR-BMOD and COR-DM. All four studies demonstrated statistically significant and clinically meaningful weight loss following up to 52 weeks of treatment with naltrexone/bupropion compared with placebo...
March 2016: Future Cardiology
Maksim L Maksimov, Andrey A Svistunov, Vadim V Tarasov, Vladimir N Chubarev, Marco Ávila-Rodriguez, George E Barreto, Olga V Dralova, Gjumrakch Aliev
Obesity and metabolic syndrome (MS) are risk factors for diabetes, cancer, some cardiovascular and musculoskeletal diseases. Pharmacotherapy should be used when the body mass index (BMI) exceeds 30 kg/m² or 27 kg/m² with comorbidity. Efficacy and safety of pharmacotherapy depend on the mechanism of action of drugs. In this context, drugs affecting the central and peripheral mediator systems such as cannabinoid receptor antagonists (Rimonabant), neuronal reuptake inhibitor of NE and 5 HT (Sibutramine), neuronal reuptake inhibitor of NE 5-HT DA (Tesofensine), agonist of 5 HT 2C receptors (Lorcaserin) have a high risk of side effects on the central nervous and cardiovascular systems when used for a long period...
2016: Current Pharmaceutical Design
W Scott Butsch
PURPOSE OF REVIEW: Lifestyle modification remains the mainstay of treatment for obesity despite the lack of substantial long-term efficacy. For many who do not respond to lifestyle therapy and are not candidates for weight loss surgery, pharmacotherapy is a viable treatment option. Advances in understanding mechanisms of appetite control, nutrient sensing, and energy expenditure have not only helped shape current drug development but have also changed the way in which antiobesity medications are prescribed...
October 2015: Current Opinion in Endocrinology, Diabetes, and Obesity
R L Kolotkin, S Chen, P Klassen, K Gilder, F L Greenway
Weight loss is associated with improved quality of life in some, but not all, weight loss trials. We evaluated changes at 56 weeks in quality of life, measured by the Impact of Weight on Quality of Life-Lite (IWQOL-Lite) questionnaire, in a pooled analysis of patient-level data from four randomized controlled Phase 3 studies of naltrexone/bupropion (NB32 or Contrave®). The total number of subjects was 3362 (NB32 = 2043; placebo = 1319; mean body mass index = 36.3 kg m(2); mean age = 46). Improvements in IWQOL-Lite Total Score were greater in subjects treated with NB32 (11...
October 2015: Clinical Obesity
Sarah L Greig, Gillian M Keating
Oral naltrexone extended-release/bupropion extended-release (naltrexone ER/bupropion ER; Contrave(®), Mysimba(™)) is available as an adjunct to a reduced-calorie diet and increased physical activity in adults with an initial body mass index (BMI) of ≥ 30 kg/m(2) (i.e. obese) or a BMI of ≥ 27 kg/m(2) (i.e. overweight) in the presence of at least one bodyweight-related comorbidity, such as type 2 diabetes mellitus, hypertension or dyslipidaemia. In 56-week phase III trials in these patient populations, oral naltrexone ER/bupropion ER 32/360 mg/day was significantly more effective than placebo with regard to percentage bodyweight reductions from baseline and the proportion of patients who achieved bodyweight reductions of ≥ 5 and ≥ 10%...
July 2015: Drugs
Jessica Early, Jean Suzin Whitten
No abstract text is available yet for this article.
April 15, 2015: American Family Physician
Andrea Pucci, Nicholas Finer
The management of obesity remains a major challenge. Dietary therapy often fails, whereas bariatric surgery, although successful, is demanding and applicable to a limited number of patients. Drug therapy has had many setbacks over the past 20 years because of serious adverse effects; however, several new drugs for the treatment of obesity are either licensed in some parts of the world, submitted for registration, or completing phase III trials. These include combinations (at low dose) of existing drugs, e.g...
February 2015: Canadian Journal of Cardiology
Kunj Gohil
Naltrexone/bupropion (Contrave) for weight management; pembrolizumab (Keytruda) for melanoma; dolutegravir/abacavir/lamivudine (Triumeq) for HIV-1; and immune globulin infusion 10% (human) with recombinant human hyaluronidase (Hyqvia) for primary immunodeficiency.
November 2014: P & T: a Peer-reviewed Journal for Formulary Management
(no author information available yet)
No abstract text is available yet for this article.
November 10, 2014: Medical Letter on Drugs and Therapeutics
Assumpta Caixàs, Lara Albert, Ismael Capel, Mercedes Rigla
Obesity is an emerging disease worldwide. Changes in living habits, especially with increased consumption of high-calorie foods and decreased levels of physical activity, lead to an energy imbalance that brings weight gain. Overweight and obesity are major risk factors for several chronic diseases (including cardiovascular diseases, diabetes, and cancer), reduce quality of life, and are associated with higher mortality. For all these reasons, it is of the utmost importance that the trend be reversed and obese people enabled to lose weight...
2014: Drug Design, Development and Therapy
Honorata Nawrocka-Bogusz, Anna Marcinkowska-Gapińska
In this study we attempted to assess the effect of light of 855 nm wavelength (IR-light) on the rheological parameters of blood in vitro. As an anticoagulant, heparin was used. The source of IR-light was an applicator connected to the special generator--Viofor JPS®. The blood samples were irradiated for 30 min. During the irradiation the energy density was growing at twelve-second intervals starting from 1.06 J/cm2 to 8.46 J/cm2, then the energy density dropped to the initial value; the process was repeated cyclically...
2014: Biorheology
Anna Marcinkowska-Gapinska, Honorata Nawrocka-Bogusz
The influence of magnetic field on whole blood rheological properties remains a weakly known phenomenon. An in vitro analysis of the magnetic field influence on the rheological properties of healthy persons blood is presented in this work. The study was performed on blood samples taken from 25 healthy nonsmoking persons and included comparative analysis of the results of both the standard rotary method (flow curve measurement) and the oscillatory method known also as the mechanical dynamic analysis, performed before and after exposition of blood samples to magnetic field...
2013: BioMed Research International
W H Reinhart, F Cagienard, T Schulzki, R M Venzin
We investigated the influence of the passage of a hemodialysis filter on red blood cells (RBCs), platelets, and hemorheological parameters. After one hour of hemodialysis, blood was drawn from 15 patients immediately ahead and behind the dialysis filter. RBCs were fixed for morphological analysis. Blood viscosity was measured with a Couette viscometer (LS-30, Contraves), RBC aggregation with a Myrenne aggregometer, platelet aggregation in flowing whole blood and in platelet rich plasma. The passage of the hemodialysis filter increased the hematocrit from 34...
2014: Clinical Hemorheology and Microcirculation
Caroline M Apovian, Louis Aronne, Domenica Rubino, Christopher Still, Holly Wyatt, Colleen Burns, Dennis Kim, Eduardo Dunayevich
OBJECTIVE: To examine the effects of naltrexone/bupropion (NB) combination therapy on weight and weight-related risk factors in overweight and obese participants. DESIGN AND METHODS: CONTRAVE Obesity Research-II (COR-II) was a double-blind, placebo-controlled study of 1,496 obese (BMI 30-45 kg/m(2) ) or overweight (27-45 kg/m(2) with dyslipidemia and/or hypertension) participants randomized 2:1 to combined naltrexone sustained-release (SR) (32 mg/day) plus bupropion SR (360 mg/day) (NB32) or placebo for up to 56 weeks...
May 2013: Obesity
F Cagienard, T Schulzki, P Furlong, W H Reinhart
Severe side effects of cocaine consumption are vasoocclusive events such as myocardial infarction and stroke. We have hypothesized that cocaine could affect red blood cells (RBCs) and alter the rheological behaviour of blood. Heparinized blood from healthy volunteers was incubated with a final hematocrit of 45% with increasing cocaine concentrations: 0, 10, 100, 1000, and 10'000 μmol/L plasma. Time dependence of the shape change was tested in phosphate buffered saline containing cocaine. RBCs were fixed in 1% glutaraldehyde for morphological analysis...
2013: Clinical Hemorheology and Microcirculation
Susan L Mercer
Contrave is an investigational fixed-dose combination drug of naltrexone and bupropion currently in Phase III clinical trials for the treatment of obesity. Orexigen Therapeutics, Inc. has demonstrated efficacy of their product and is currently addressing FDA safety concerns and deciding future actions.
September 21, 2011: ACS Chemical Neuroscience
David J Heal, Jane Gosden, Sharon L Smith
Obesity is a global problem that is predominantly caused by the increasing adoption of a low-cost, Westernised diet that is rich in fat and sugar and a more sedentary lifestyle. The costs of this epidemic are substantial increases in Type 2 diabetes, cardiovascular disease and some types of cancer that are certain to place a huge burden on individuals, healthcare providers and society. In this review, we provide an overview of the chequered history of pharmacotherapy for the treatment of obesity and an analysis of the regulatory and commercial challenges for developing new centrally-acting drugs in this metabolic indication...
July 2012: Neuropharmacology
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