Pharmacotherapy for Weight Reduction: Bupropion/Naltrexone Drugs for Obesity

2021 ◽  
Vol 15 (9) ◽  
pp. 2293-2295
Author(s):  
Sabeen Arjumand ◽  
Maira Bhatti ◽  
Zubaida Qayyum ◽  
Zarish Ghafoor ◽  
Fouzia Perveen
Keyword(s):  
Weight Loss ◽  
Food Intake ◽  
Combination Therapy ◽  
Weight Reduction ◽  
Eating Behaviors ◽  
Complex Interaction ◽  
Food Craving ◽  
Melanocortin System ◽  
Major Mechanism

Background: There is no valid and accurate documentation on the combination therapy of bupropion along with naltrexone. The experimentations on these actions of combination drugs have resulted in rare success. Methods: A complex interaction occurs in the central and peripheral nervous system for reducing weight loss. It is difficult to find out the major mechanism of action of these drugs on weight reduction. Naltrexone and bupropion is the experimental combination for reducing the weight. For obesity, the combination of naltrexone/bupropion therapy’s mechanism working is still unknown. Results: The attempts for weight loss rarely have a long-term effect. It is an outcome of more likely some complex interaction between various peripheral and Central Nervous systems, and an overwhelming lack of real obesity treatment may be explained. Based on the evidence that obesity involves a change in the hypothalamic melanocortin system in addition to a brain reward system, which causes food craving and mood swings, this investigational combination therapy of NB was developed. Naltrexone and bupropion work in an interesting way. Conclusion: It affects the parts of the brain that influences food craving, food intake, eating behaviors, and loss of body weight. We will have a review on the working of naltrexone, and bupropion separately, and Vivo, current in vitro, and clinical evidence will be provided, describing how NB affects food intake and food craving. Keywords: CNS, obesity, medicine, weight lose, NB, therapy.

Differences in Mechanisms Between Weight Reduction Sensitive and Insensitive Blood Pressure Reduction in Obese Subjects

Hypertension ◽  
2000 ◽  
Vol 36 (suppl_1) ◽  
pp. 725-725
Author(s):  
Kazuko Masuo ◽  
Hiroshi Mikami ◽  
Toshio Ogihara ◽  
Michael L Tuck
Keyword(s):  
Weight Loss ◽  
Family History ◽  
Weight Reduction ◽  
Blood Pressure Reduction ◽  
Study Groups ◽  
Plasma Norepinephrine ◽  
Ang Ii ◽  
Major Mechanism ◽  
History Of ◽  
History Of Obesity

P180 This study was conducted to clarify the differences in mechanisms between weight reduction (WR) sensitive and insensitive BP reduction, and to evaluate the contribution of family history of obesity (FH) to WR-induced BP reduction. In 61 obese hypertensive men (HT, 28.1±0.9 kg/m2, 35±3 years, 171±6/106±5 mmHg) and 52 obese normotensive men (NT, 27.9±0.6 kg/m2, 34±4 years, 131±5/83±4 mmHg), BMI, BP, fasting plasma norepinephrine (NE), angiotensin II (Ang II), PRA, leptin, insulin were measured every 2 week for 24 weeks with weight loss program (low caloric diet 1000kcal, 7gNaCl + excercise≥1 hr/day). WR and WR sensitive BP reduction were defined as >10% reduction in BMI or mean BP at week 12. 64% of HT and 63% of NT succeeded in WR, and 59% of HT with WR (sensitive vs insensitive P<.05) and 70% of NT with WR (P<.01) were sensitive in BP reduction. When FH+ was defined as at least one parent was obese (BMI>27.0 kg/m2), prevalence of FH+ was higher in 86% of HT and 95% of NT who failed in WR, and higher in 94% of HT and 80% of NT with WR insensitive BP reduction. Only the subjects who succeeded in WR were analyzed in this study. At entry, BP, NE, Ang II, PRA and insulin were higher in HT than in NT, although BMI and leptin were similar. However, the parameters at entry were similar between WR sensitive and insensitive BP reduction in each NT and HT. The decrements (Δ) in BP, NE, Ang II, leptin,insulin were significantly greater in subjects with WR sensitive BP reduction than subjects with WR insensitive BP reduction regardless of BP status during the study, although ΔBMI was similar. Significant decreases in the parameters were noted in earlier period in subjects with WR sensitive BP reduction than in subjects with insensitive BP reduction, and in NT than in HT. In the 4 study groups regardless of BP status or WR induced BP reduction, the decrease in NE preceded BP decline, and the decreases in Ang II, insulin, leptin & PRA followed BP decline with WR. These results suggest that a family history of obesity appears to contribute closely to resistance in weight loss and also to WR insensitive BP reduction. Suppression on sympathetic overactivity is a major mechanism in WR induced BP reduction.

Level of satiety: in vitro energy metabolism in brain during hypophagic and hyperphagic body weight recovery

1989 ◽  
Vol 257 (6) ◽  
pp. R1322-R1327 ◽  
Author(s):  
T. R. Kasser ◽  
R. B. Harris ◽  
R. J. Martin
Keyword(s):  
Weight Loss ◽  
Body Weight ◽  
Fatty Acid ◽  
Food Intake ◽  
Fatty Acid Oxidation ◽  
Glucose Oxidation ◽  
Area Postrema ◽  
Tube Feeding ◽  
Acid Oxidation

Rates of in vitro glucose and fatty acid oxidation were examined in four brain sites during hypophagic and hyperphagic recovery of normal body weight. Rats were fed 40, 100, or 160% of normal intake, via gastric intubation, for 3 wk. Another group of rats was starved until body weight loss was equivalent to weight loss in 40%-fed rats. Groups of rats were killed at the conclusion of tube feeding or fasting and at specific periods during recovery of body weight. Brain sites examined were the ventrolateral hypothalamus (VLH), ventromedial hypothalamus (VMH), a caudal brain stem site encompassing the area postrema-nucleus of the solitary tract (AP-NTS), and cortex. During recovery, rats previously fed 160% of normal intake (anorectic) maintained low rates of VLH fatty acid oxidation and were hypophagic until most excess fat was depleted. Conversely, rats previously fed 40% of normal intake (hungry) maintained high rates of VLH fatty acid oxidation and were hyperphagic until most deficient fat was repleted. Rats previously starved maintained high rates of VLH fatty acid oxidation during hyperphagic recovery, although levels of VLH fatty acid oxidation and food intake were initially low on refeeding. Rates of glucose oxidation in the brain sites examined did not relate well to energy balance status and the needed adjustments in food intake. The results indicated that the level of glucose oxidation in the VLH and AP-NTS responded to the level of energy immediately coming into the system (food intake).(ABSTRACT TRUNCATED AT 250 WORDS)

scholarly journals Long-Acting and Selective Oxytocin Peptide Analogs Show Antidiabetic and Antiobesity Effects in Male Mice

2019 ◽  
Vol 3 (7) ◽  
pp. 1423-1444 ◽  
Author(s):  
Brandy Snider ◽  
Andrea Geiser ◽  
Xiao-peng Yu ◽  
Emily Cathleen Beebe ◽  
Jill Amanda Willency ◽  
...  
Keyword(s):  
Weight Loss ◽  
Food Intake ◽  
Glycemic Control ◽  
Physiological Stress ◽  
Glucagon Secretion ◽  
Body Weight Reduction ◽  
Peptide Analog ◽  
Vasopressin Receptors

AbstractOxytocin (OXT) has been shown to suppress appetite, induce weight loss, and improve glycemic control and lipid metabolism in several species, including humans, monkeys, and rodents. However, OXT’s short half-life in circulation and lack of receptor selectivity limit its application and efficacy. In this study, we report an OXT peptide analog (OXTGly) that is potent and selective for the OXT receptor (OXTR). OXT, but not OXTGly, activated vasopressin receptors in vitro and acutely increased blood pressure in vivo when administered IP. OXT suppressed food intake in mice, whereas OXTGly had a moderate effect on food intake when administered IP or intracerebroventricularly. Both OXT (IP) and OXTGly (IP) improved glycemic control in glucose tolerance tests. Additionally, both OXT (IP) and OXTGly (IP) stimulated insulin, glucagon-like peptide 1, and glucagon secretion in mice. We generated lipid-conjugated OXT (acylated-OXT) and OXTGly (acylated-OXTGly) and demonstrated that these molecules have significantly extended half-lives in vivo. Compared with OXT, 2-week treatment of diet-induced obese mice with acylated-OXT [subcutaneous(ly) (SC)] resulted in enhanced body weight reduction, an improved lipid profile, and gene expression changes consistent with increased lipolysis and decreased gluconeogenesis. Treatment with acylated-OXTGly (SC) also resulted in a statistically significant weight loss, albeit to a lesser degree compared with acylated-OXT treatment. In conclusion, we demonstrate that selective activation of the OXTR pathway results in both acute and chronic metabolic benefits, whereas potential activation of vasopressin receptors by nonselective OXT analogs causes physiological stress that contributes to additional weight loss.

The synthesis and release of gonadotropins in response to gonadotropin-releasing hormone of the rat anterior pituitary gland during weight reduction

1990 ◽  
Vol 122 (5) ◽  
pp. 628-632 ◽  
Author(s):  
Fumikazu Kotsuji ◽  
Takeshi Aso ◽  
Naoyuki Kamitani ◽  
Toshiro Tominaga
Keyword(s):  
Weight Loss ◽  
Pituitary Gland ◽  
Weight Reduction ◽  
Female Rats ◽  
Serum Lh ◽  
Female Wistar Rats ◽  
Progressive Weight Loss ◽  
Lh Release ◽  
Lh Secretion

Abstract. It is well recognized that weight reduction produces the suppression of serum LH but not FSH level in rodents. In order to clarify the mechanism by which the discrepancy between LH and FSH levels is brought about, the influence of weight loss on the pituitary function was explored using female rats. The changes of the pituitary response to GnRH and the basal secretion of gonadotropins with progressive weight loss were investigated by in vitro short-term incubation of the pituitary gland after prolonged weight loss in female Wistar rats. On the first day of diestrous and until day 14 of the diet, GnRH induced LH and FSH release from the pituitary and a decrease in pituitary content of them, but the total amount of gonadotropin in culture medium and pituitary tissue was not affected. On day 30 of the diet, the decrease in pituitary content disappeared. On day 60 LH release disappeared, whereas pituitary FSH and the total amount of gonadotropins were increased by GnRH. Non-stimulated FSH but not LH secretion per mg of pituitary was augmented during dieting. The data indicate that pituitary responsiveness to GnRH and non-stimulated FSH release were modified by weight loss: the LH-releasing action of GmRH was diminished, the gonadotropin-synthesizing action of GnRH was augmented, and non-stimulated FSH release was increased.

scholarly journals ORLISTAT IN COMBINATION THERAPY OF OBESITY AND TYPE 2 DIABETES

2017 ◽  
pp. 68-74 ◽  
Author(s):  
A. M. Mkrtumyan ◽  
E. V. Biryukova
Keyword(s):  
Type 2 Diabetes ◽  
Weight Loss ◽  
Clinical Trials ◽  
Food Intake ◽  
Combination Therapy ◽  
Systemic Effects ◽  
The Past ◽  
Prevention And Treatment ◽  
Treatment Of Obesity

Over the past years, the focus has been growing on the prevention and treatment of obesity. Obesity has long been considered not just as excess body fat but as a chronic relapsing disease, the result of energy disbalance, which develops with an increase in food intake and reduced energy expenditure and is closely associated with a number of serious complications. Orlistat (Xenical), a peripherally acting drug without systemic effects [11, 24, 27], has been widely used in pharmacological treatment of obesity. Xenical is the most well-studied medication for weight loss. More than 30,000 patients with obesity were involved in clinical trials, of which over 2,500 patients had type 2 diabetes. Till today, the drug remains a breakthrough in the treatment of overweight/obesity.

scholarly journals Toward a Medical Gastric Bypass: Chronic Feeding Studies With Liraglutide + PYY3-36 Combination Therapy in Diet-Induced Obese Rats

2021 ◽  
Vol 11 ◽  
Author(s):  
Ulrich Dischinger ◽  
Julia Hasinger ◽  
Malina Königsrainer ◽  
Carolin Corteville ◽  
Christoph Otto ◽  
...  
Keyword(s):  
Weight Loss ◽  
Gastric Bypass ◽  
Food Intake ◽  
Combination Therapy ◽  
Gut Hormones ◽  
Abnormal Behavior ◽  
Sham Operation ◽  
High Fat ◽  
Beneficial Effects ◽  
Male Wistar Rats

BackgroundCombination therapies of anorectic gut hormones partially mimic the beneficial effects of bariatric surgery. Thus far, the effects of a combined chronic systemic administration of Glucagon-like peptide-1 (GLP-1) and peptide tyrosine tyrosine 3-36 (PYY3-36) have not been directly compared to Roux-en-Y gastric bypass (RYGB) in a standardized experimental setting.MethodsHigh-fat diet (HFD)-induced obese male Wistar rats were randomized into six treatment groups: (1) RYGB, (2) sham-operation (shams), (3) liraglutide, (4) PYY3-36, (5) PYY3-36+liraglutide (6), saline. Animals were kept on a free choice high- and low-fat diet. Food intake, preference, and body weight were measured daily for 4 weeks. Open field (OP) and elevated plus maze (EPM) tests were performed.ResultsRYGB reduced food intake and achieved sustained weight loss. Combined PYY3-36+liraglutide treatment led to similar and plateaued weight loss compared to RYGB. Combined PYY3-36+liraglutide treatment was superior to PYY3-36 (p ≤ 0.0001) and liraglutide (p ≤ 0.05 or p ≤ 0.01) mono-therapy. PYY3-36+liraglutide treatment and RYGB also reduced overall food intake and (less pronounced) high-fat preference compared to controls. The animals showed no signs of abnormal behavior in OF or EPM.ConclusionsLiraglutide and PYY3-36 combination therapy vastly mimics reduced food intake, food choice and weight reducing benefits of RYGB.

Effect of parenteral nutrition on protein turnover in endotoxaemic rats

1989 ◽  
Vol 76 (6) ◽  
pp. 659-666 ◽  
Author(s):  
S. A. Ash ◽  
G. E. Griffin
Keyword(s):  
Skeletal Muscle ◽  
Weight Loss ◽  
Protein Synthesis ◽  
Food Intake ◽  
Parenteral Nutrition ◽  
Total Parenteral Nutrition ◽  
Intravenous Infusion ◽  
Protein Turnover

1. Intravenous infusion of endotoxin into rats over 18 h caused a reduction in food intake to 20% of normal levels, weight loss, hypoalbuminaemia and a fall in rates of protein synthesis in vivo in heart and skeletal muscle. 2. Measurements of protein turnover in vitro in skeletal muscle of endotoxaemic animals, showed a 50% fall in protein synthesis rates and a 200% increase in rates of protein degradation. 3. Total parenteral nutrition was only partially able to reverse endotoxin-induced weight loss. Total parenteral nutrition did not reverse endotoxin-induced catabolism in cardiac or skeletal muscle, but was able to reverse the catabolism of protein in skeletal muscle produced by starvation. 4. Endotoxin treatment elevated rates of protein synthesis in vivo in liver. The combination of parenteral nutrition and endotoxaemia further increased the rate of protein synthesis in the liver. Parenteral nutrition did not influence endotoxin-induced hypoalbuminaemia.

scholarly journals The effectiveness of a monetary reimbursement model for weight reduction via a smartphone application: a preliminary retrospective study

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Jungeun Lee ◽  
Sujin Bae ◽  
Dohyung Park ◽  
Youngin Kim ◽  
Jisun Park
Keyword(s):  
Weight Loss ◽  
Retrospective Study ◽  
Food Intake ◽  
Weight Reduction ◽  
Financial Incentives ◽  
Retention Rate ◽  
Smartphone Application ◽  
Analysis Of Covariance ◽  
Related Information ◽  
Health Related

Abstract Weight loss for obese populations has been a challenging subject. There are numerous mobile applications to address weight loss, but the low retention rate is a barrier for the intervention. This is a retrospective study, aiming to investigate the effectiveness of financial incentives to achieve weight loss via a monetary reimbursement model on a smartphone application. Participants voluntarily purchased a 16-week mobile weight loss application program, and those who logged food intake three times a day received monetary reimbursement up to the full amount they initially paid. We analyzed health-related information and logged in-app activities from participants (N = 2,803) including age, sex, weight, food intake, and physical activity on their mobile healthcare application called Noom from January 2017 to April 2019. Analysis of covariance (ANCOVA) was used to compare differences between groups who succeeded and failed at food logging, controlling for baseline BMI. The ANCOVA found that participants who completed the food logging successfully for 16 weeks (N = 1,565) lost significantly more weight than those who failed food logging (N = 1,238, F = 56.0, p < 0.001). In addition, participants who were able to log their food intake successfully exercised more (F = 41.5, p < 0.001), read more in-app articles (F = 120.7, p < 0.001), and consumed more quantity of healthy foods (F = 12.8, p < 0.001). Monetary reimbursement is an effective tool for weight reduction by encouraging participants to monitor their health-related behaviors regularly.

scholarly journals The dual amylin and calcitonin receptor agonist KBP-089 and the GLP-1 receptor agonist liraglutide act complimentarily on body weight reduction and metabolic profile

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Anna Thorsø Larsen ◽  
Sofie Gydesen ◽  
Nina Sonne ◽  
Morten Asser Karsdal ◽  
Kim Henriksen
Keyword(s):  
Weight Loss ◽  
Body Weight ◽  
Gastric Emptying ◽  
Food Intake ◽  
Glucose Metabolism ◽  
Glucose Tolerance ◽  
Weight Reduction ◽  
Receptor Agonist ◽  
Calcitonin Receptor ◽  
Body Weight Reduction

Abstract Background Weight loss therapy is becoming more and more important, and two classes of molecules, namely amylin receptor and GLP-1 receptor agonists, have shown promise in this regard. Interestingly, these molecules have several overlapping pharmacological effects, such as suppression of gastric emptying, reduction of glucagon secretion and weight loss in common; however, they also have distinct effects on prandial insulin secretion. Hence, a combination of these two mechanisms is of significant interest. Methods In this study, we investigated the add-on potential of the dual amylin and calcitonin receptor agonist (DACRA) KBP-089 in combination with the GLP-1 receptor agonist liraglutide as obesity treatment in high-fat diet (HFD) fed rats. Results Increasing doses of KBP-089 and liraglutide alone and in combination were studied with respect to their effects on body weight, food intake and glucose metabolism during a 9-week intervention study conducted in HFD rats. Further, the gastric emptying rate during an oral glucose tolerance was assessed. Treatment with KBP-089 and liraglutide dose-dependently lowered body weight 15% (at 2.5 μg/kg/day) and 7% (at 400 μg/kg/day) in HFD rats, respectively, while the combination resulted in a 21% body weight reduction, which was mirrored by reduction in fat depot sizes. Gastric emptying and glucose metabolism were improved, primarily by KBP-089, although liraglutide led to a reduction in fasting plasma glucagon. Conclusion DACRAs complement GLP-1 on food intake, body weight, and glucose tolerance indicating the potential for an add-on therapy.

scholarly journals The Dual Amylin and Calcitonin Receptor Agonist KBP-089 and the GLP-1 receptor agonist liraglutide act complimentarily on body weight reduction and metabolic profile 

2020 ◽  
Author(s):  
Anna Thorsø Larsen ◽  
Sofie Gydesen ◽  
Nina Sonne ◽  
Morten Asser Karsdal ◽  
Kim Henriksen
Keyword(s):  
Weight Loss ◽  
Body Weight ◽  
Gastric Emptying ◽  
Food Intake ◽  
Glucose Metabolism ◽  
Glucose Tolerance ◽  
Weight Reduction ◽  
Receptor Agonist ◽  
Calcitonin Receptor ◽  
Body Weight Reduction

Abstract Background: Weight loss therapy is becoming more and more important, and two classes of molecules, namely amylin receptor and GLP-1 receptor agonists, have shown promise in this regard. Interestingly, these molecules have several overlapping pharmacological effects, such as suppression of gastric emptying, reduction of glucagon secretion and weight loss in common; however, they also have distinct effects on prandial insulin secretion. Hence, a combination of these two mechanisms is of significant interest. Methods: In this study, we investigated the add-on potential of the dual amylin and calcitonin receptor agonist (DACRA) KBP-089 in combination with the GLP-1 receptor agonist liraglutide as obesity treatment in high-fat diet (HFD) fed rats. Results: Increasing doses of KBP-089 and liraglutide alone and in combination were studied with respect to their effects on body weight, food intake and glucose metabolism during a 9-week intervention study conducted in HFD rats. Further, the gastric emptying rate during an oral glucose tolerance was assessed. Treatment with KBP-089 and liraglutide dose-dependently lowered body weight 15% (at 2.5 µg/kg/day) and 7% (at 400 µg/kg/day) in HFD rats, respectively, while the combination resulted in a 21% body weight reduction, which was mirrored by reduction in fat depot sizes. Gastric emptying and glucose metabolism were improved, primarily by KBP-089, although liraglutide led to a reduction in fasting plasma glucagon. Conclusion: DACRAs complement GLP-1 on food intake, body weight, and glucose tolerance indicating the potential for an add-on therapy.

Sign in / Sign up

Export Citation Format

Share Document