orlistat and Weight-Gain

Obesity management requires a multidisciplinary approach, as there are many factors that contribute to the development of obesity, as well as the preservation of excess weight once it has been gained. Diet, exercise, and behavior modification are key components of treatment. In addition to lifestyle changes, weight gain secondary to medications is an important modifiable risk factor. Even after appropriate lifestyle modification, and medication adjustments (where possible) to avoid agents that can contribute to weight gain, many patients are still unable to achieve clinically meaningful weight loss. Pharmacotherapy for obesity management can fill an important role for these patients. This article will review medications that can lead to weight gain and potential alternatives, currently approved anti-obesity medications and best practices to individualize the selection process, and the use of testosterone in men with hypogonadism and obesity.

Topics: Androgens; Anti-Obesity Agents; Antidepressive Agents; Antihypertensive Agents; Antipsychotic Agents; Appetite Depressants; Benzazepines; Bupropion; Drug Combinations; Fructose; Humans; Hypoglycemic Agents; Hypogonadism; Lactones; Liraglutide; Naltrexone; Obesity; Orlistat; Phentermine; Testosterone; Topiramate; Weight Gain

This article examines the transitions in pharmacological therapy for obesity. It reviews the current options approved by the Food and Drug Administration and several drugs approved for other indications that can be used to treat obesity as well. Because weight regulation is complex and redundant systems protect against perceived starvation, optimal treatment of obesity in individual patients will likely require different combinations of behavioral, nutritional, pharmacologic, endoscopic, and surgical therapies.

Topics: Anti-Obesity Agents; Appetite Depressants; Bariatric Surgery; Benzazepines; Bupropion; Cyclobutanes; Ephedrine; Fenfluramine; Humans; Lactones; Naltrexone; Obesity; Orlistat; Phentermine; Weight Gain; Weight Loss

Obesity is associated with considerable morbidity and decreased life expectancy. Weight gain is a commonly encountered problem associated with antipsychotic treatment. We reviewed the literature regarding the mechanisms of weight gain in response to these agents and eight substances implicated as potential obesity prevention or treatment: orlistat, sibutramine, fluoxetine, topiramate, amantadine, nizatidine and cimetidine, and metformin. Weight gain in response to antipsychotic treatment may be mediated through serotonergic, dopaminergic, adrenergic, cholinergic, histaminergic and glutaminergic receptors. Sex hormone dysregulation and altered insulin sensitivity have also been implicated. Two compounds, orlistat and sibutramine, have been shown to help prevent weight gain following a hypocaloric diet, but orlistat requires compliance with a fat-reduced diet, and sibutramine is unsuitable for patients taking serotonergic agents. The weight reducing effect of fluoxetine, even in conjunction with a hypocaloric diet, is only transient. Topiramate, amantadine and metformin may have adverse side-effects potentially outweighing the weight reducing potential. The effectiveness of cimetidine and nizatedine remains unclear. The hazards of these agents in a psychiatric population are discussed. It is concluded that the current evidence does not support the general use of pharmacological interventions for overweight patients treated with antipsychotic medication, although individually selected patients may benefit.

Topics: Amantadine; Antipsychotic Agents; Cimetidine; Cyclobutanes; Fluoxetine; Fructose; Humans; Lactones; Metformin; Nizatidine; Obesity; Orlistat; Topiramate; Weight Gain

In excess of 55% of adults in the United States are classified as either overweight (body mass index = 25-29.9 kg.m(-2)) or obese (body mass index > or = 30 kg.m(-2)). To address this significant public health problem, the American College of Sports Medicine recommends that the combination of reductions in energy intake and increases in energy expenditure, through structured exercise and other forms of physical activity, be a component of weight loss intervention programs. An energy deficit of 500-1000 kcal.d-1 achieved through reductions in total energy intake is recommended. Moreover, it appears that reducing dietary fat intake to <30% of total energy intake may facilitate weight loss by reducing total energy intake. Although there may be advantages to modifying protein and carbohydrate intake, the optimal doses of these macronutritents for weight loss have not been determined. Significant health benefits can be recognized with participation in a minimum of 150 min (2.5 h) of moderate intensity exercise per week, and overweight and obese adults should progressively increase to this initial exercise goal. However, there may be advantages to progressively increasing exercise to 200-300 min (3.3-5 h) of exercise per week, as recent scientific evidence indicates that this level of exercise facilitates the long-term maintenance of weight loss. The addition of resistance exercise to a weight loss intervention will increase strength and function but may not attenuate the loss of fat-free mass typically observed with reductions in total energy intake and loss of body weight. When medically indicated, pharmacotherapy may be used for weight loss, but pharmacotherapy appears to be most effective when used in combination with modifications of both eating and exercise behaviors. The American College of Sports Medicine recommends that the strategies outlined in this position paper be incorporated into interventions targeting weight loss and the prevention of weight regain for adults.

Topics: Adult; Body Mass Index; Cyclobutanes; Diet Therapy; Dietary Fats; Energy Intake; Exercise Therapy; Health Behavior; Humans; Lactones; Life Style; Obesity; Orlistat; Physical Endurance; Secondary Prevention; Weight Gain; Weight Lifting; Weight Loss

Obesity increases the risk of several serious health problems, including heart disease, type II diabetes mellitus, hypertension, and osteoarthritis. Patients taking certain psychotropic medications may gain a significant amount of weight (as much as a 5% increase in body weight within 1 to 2 months), placing them at risk for obesity. Body weight monitoring and prudent drug selection are the best approaches to preventing weight gain in patients taking psychotropic drugs. When weight gain (> 5% of initial body weight) is unavoidable, intervention counseling should begin. Nonpharmacologic measures for managing weight gain include a balanced deficit diet of 1000 calories and higher, depending on the patient's weight; 30 to 60 minutes of physical activity daily; and behavioral training to restrain excess caloric intake. Each of these measures requires a considerable commitment on the part of the patient and works best with support from the physician and weight-loss support groups. Drug therapy for weight loss is available (at present, sibutramine is the only approved appetite suppressant in the United States); however, for most patients already being treated with a psychotropic agent, the risks (such as drug interactions, adverse events, compliance problems) of adding an antiobesity agent probably outweigh the benefits. Surgical intervention for obesity should be reserved for morbidly obese patients whose disease is intractable to medical therapy.

Topics: Anti-Obesity Agents; Appetite Depressants; Behavior Therapy; Cyclobutanes; Diet, Reducing; Energy Intake; Exercise; Humans; Lactones; Obesity; Obesity, Morbid; Orlistat; Psychotropic Drugs; Self-Help Groups; Weight Gain

Prevention and treatment of obesity are major clinical problems encountered in the management of Type 2 diabetes mellitus (DM); indeed, up to 90% of such patients are regarded as being overweight. Except for a brief period following diagnosis, when presumably enthusiasm to adopt lifestyle change is at its greatest, weight gain is generally progressive unless severe hyperglycaemia or complications intervene. Even a relatively modest weight loss of 10% can have major benefits in terms not only of reducing the risk of developing DM in the first place, but also in improving metabolic control after the disorder has become established. Behavioural therapy (BT) in combination with hypocaloric diet achieves weight loss in the short-term, but is poorly sustained in the long-term. Exercise has metabolic benefits beyond its rather minimal effects on short-term weight loss in that it may also aid long-term weight control. The difficulties encountered in maintaining lifestyle change do, however, suggest the need for ongoing intervention--perhaps including a regular period on a stricter dietary regimen (800-1000 kcalday-1), possibly a very low calorie diet (VLCD)(< 800 kcalday-1) or even the use of orlistat, a pancreatic lipase inhibitor which reduces the absorption of dietary fat. Realistically, the aim should be for long-term weight stability.

Topics: Anti-Obesity Agents; Behavior Therapy; Diabetes Mellitus, Type 2; Diet, Diabetic; Diet, Reducing; Exercise; Humans; Lactones; Life Style; Obesity; Orlistat; Weight Gain; Weight Loss

Topics: Anti-Obesity Agents; Cyclobutanes; Diet, Fat-Restricted; Family Practice; Humans; Intestinal Absorption; Lactones; Obesity; Orlistat; Weight Gain

Identifying pretreatment dietary habits that are associated with weight-loss intervention outcomes could help guide individuals' selection of weight-loss approach among competing options. A pretreatment factor that may influence weight-loss outcomes is macronutrient intake.. Overweight and obese Durham Veterans Affairs outpatients were randomised to a weight-loss intervention with a low-carbohydrate diet (n = 71) or orlistat medication therapy plus a low-fat diet (n = 73). Percentage fat, carbohydrate and protein intake prior to treatment were measured using 4-day food records. Linear mixed-effects models were used to determine whether pretreatment percentage macronutrient intake influenced weight trajectories and weight loss in each weight-loss condition.. Participant's mean age was 53 years, baseline body mass index was 39.3 kg m(-2) and 72% were male. A higher pretreatment percentage carbohydrate intake was associated with less rapid initial weight loss (P = 0.02) and less rapid weight regain (P = 0.03) in the low-carbohydrate diet condition but was not associated with weight trajectories in the orlistat plus low-fat diet condition. In both conditions, a higher pretreatment percentage fat intake was associated with more rapid weight regain (P < 0.01). Pretreatment percentage protein intake was not associated with weight trajectories. None of the pretreatment macronutrients were associated with weight loss on study completion in either condition.. Selection of a weight-loss approach on the basis of pretreatment macronutrient intake is unlikely to improve weight outcomes at the end of a 1-year treatment. However, pretreatment macronutrient intake may have implications for tailoring of interventions to slow weight regain after weight loss.

Topics: Adult; Anti-Obesity Agents; Diet, Carbohydrate-Restricted; Diet, Fat-Restricted; Diet, Reducing; Dietary Carbohydrates; Dietary Fats; Dietary Proteins; Energy Intake; Feeding Behavior; Female; Humans; Lactones; Male; Middle Aged; Obesity; Orlistat; Weight Gain; Weight Loss

To investigate the efficacy of orlistat on the maintenance of weight loss over 3 years following a major weight loss induced by very-low-energy diet (VLED) in obese patients with metabolic risk factors such as dyslipidemia, impaired fasting glucose, and diet-treated type 2 diabetes.. Initially, weight loss was induced by an 8-week VLED (600-800 kcal/day) in 383 patients with a mean BMI of 37.5 kg/m(2) (range 30.0-45.2). Those who lost > or = 5% of their body weight (309 of 383 patients) were then randomized to receive lifestyle counseling for 3 years together with either orlistat 120 mg t.i.d. or matching placebo capsules. Primary end points were the maintenance of > or = 5% weight loss after 3 years. Additionally, differences in the development of type 2 diabetes between orlistat and placebo were analyzed.. The VLED induced a mean weight loss of 14.4 +/- 2.0 kg among the subsequently randomized patients. The mean weight gain after 3 years was lower with orlistat than with placebo (4.6 +/- 8.6 vs. 7.0 +/- 7.1 kg; P < 0.02). The number of participants who achieved > or =5% weight loss also favored orlistat (67 vs. 56%; P = 0.037). Waist circumference was significantly more reduced in the orlistat group (P < 0.05), but no other differences in the risk factors were observed between the two groups. The incidences of new cases of type 2 diabetes were significantly reduced in the orlistat group (8 cases out of 153 subjects) versus placebo (17 cases out of 156 subjects) (P = 0.041).. The addition of orlistat to lifestyle intervention was associated with maintenance of an extra 2.4 kg weight loss after VLED for up to 3 years in obese subjects. The combination of orlistat and lifestyle intervention was associated with a reduced occurrence of type 2 diabetes.

Topics: Adult; Aged; Anti-Obesity Agents; Body Mass Index; Body Size; Combined Modality Therapy; Diabetes Complications; Diet, Reducing; Female; Glucose Intolerance; Humans; Lactones; Male; Middle Aged; Obesity; Orlistat; Placebos; Weight Gain

To describe the comparative efficacy of orlistat and sibutramine in an obesity management program, with specific attention to compliance and weight regains after noncompliance. We prospectively evaluated 182 obese patients who were randomized to treatment with orlistat (n=98) or sibutramine (n=84) along with the diet and exercise prescriptions. Compliance (or compliant patient) was defined as adherence to scheduled visit times (at 3- month intervals) and following the prescribed drug regimen. A telephone survey was conducted in case of noncompliance. Significant body weights improvements were seen in both treatment groups. Patients lost a mean of 7.6+/-2.8% and 10.5+/-2.9% of initial body weights after a mean drug use of 8.8+/-5.7 and 8.3+/-3.7 months in the orlistat and sibutramine groups, respectively (p<0.05 vs. initial body weight). Patients in the sibutramine group lost more weight than the orlistat group (p<0.05). A total of 102 patients (56%) were compliant (53.1% in the orlistat group and 59.5% in the sibutramine group). Factors associated with compliance included weight reduction of more than 5% in the first 3 months and adherence to physical activity. Higher initial body weight, prior anti-obesity therapy, number of concurrent medications, and comorbidity were associated with noncompliance. Weight regains in noncompliant patient were a mean of 5.2+/-5.1 kg after a mean period of 9.2+/-4.2 months in the orlistat group, and a mean of 6.1+/-3.8 kg after a mean period of 9.1+/-3.9 months in the sibutramine group (p<0.05 vs. last visit for both groups, p>0.05 between groups). Both drugs in an obesity management program can achieve substantial weight loss. However, noncompliance and rebound weight regain after noncompliance are considerable problems.

Topics: Adult; Anti-Obesity Agents; Appetite Depressants; Combined Modality Therapy; Cyclobutanes; Diet, Reducing; Exercise Therapy; Female; Humans; Lactones; Male; Middle Aged; Obesity; Orlistat; Patient Compliance; Prospective Studies; Weight Gain; Weight Loss

To compare the use of meal replacements or medication during weight maintenance subsequent to weight loss using a very low-energy diet (VLED) in overweight or obese adults.. Participants followed a liquid VLED of 2177 kJ for 12 weeks followed by 4 weeks of re-orientation to solid foods. Participants were randomized at week 16 to receive either meal replacements or Orlistat both combined with a structured meal plan containing an energy value calculated to maintain weight loss.. Sixty-four women (age = 49.9 +/- 10 y, weight = 101.6 +/- 17.1 kg, height = 164.9 +/- 6.0 cm, BMI = 36.7 +/- 5.4 kg/m(2)) and 28 men (age = 53.7 +/- 9.6 y, weight = 121.8 +/- 16.0 kg, height = 178.7 +/- 5.6 cm, BMI = 37.8 +/- 4.9 kg/m(2)) completed a 1 year weight management program. Behavioral weight management clinics included topics on lifestyle, physical activity (PA), and nutrition. Participants met for 90 min weekly for 26 weeks, and then biweekly for the remaining 26 weeks.. Minutes of PA, fruits and vegetables (FV), and pedometer steps were recorded on a daily basis and reported at each group meeting. Body weight was obtained at each group meeting.. During VLED, the MR group decreased body weight by 22.8 +/- 6.1 kg and the Orlistat group decreased body weight by 22.3 +/- 6.1 kg. During weight maintenance, there was no significant group by time interaction for body weight, PA, FV consumption, or pedometer steps. At week 16, the meal replacement group had a body weight of 85.4 +/- 14.3 kg that increased to 88.1 +/- 16.5 kg at 52 weeks (p < 0.05). At week 16, the Orlistat group had a body weight of 85.7 +/- 17.9 kg that increased to 88.5 +/- 20.3 kg at 52 weeks (p < 0.05).. Subsequent to weight loss from a VLED, meal replacements and Orlistat treatments were both effective in maintaining weight significantly below baseline levels over a 52 week period of time. Meal replacements may be a viable alternative strategy to medications for weight maintenance.

Topics: Adult; Aged; Anthropometry; Anti-Obesity Agents; Body Composition; Counseling; Cross-Over Studies; Diet, Reducing; Exercise; Female; Food, Formulated; Health Promotion; Humans; Lactones; Male; Middle Aged; Obesity; Orlistat; Treatment Outcome; Weight Gain; Weight Loss

Topics: Adult; Anti-Obesity Agents; Antidepressive Agents; Body Composition; Body Mass Index; Case-Control Studies; Diet, Reducing; Enzyme Inhibitors; Exercise; Female; Humans; Lactones; Male; Orlistat; Pilot Projects; Prospective Studies; Treatment Outcome; Weight Gain

Topics: Anti-Obesity Agents; Body Mass Index; Female; Humans; Lactones; Lipase; Male; Middle Aged; Orlistat; Psychotropic Drugs; Weight Gain

Weight gain is a common side effect associated with antidepressant, anxiolytic, and antipsychotic drug use. Obesity is a risk factor for several other disorders, including hypertension, diabetes, and coronary artery disease. To date, there have been few safe, well-tolerated, and effective pharmacological agents available to alleviate weight gain in general, and virtually no studies specific to psychiatric drug-induced weight gain. This case series looks at the use of orlistat, a reversible inhibitor of lipases approved by the US Food and Drug Administration for obesity management, naturalistically in 13 patients with weight gain secondary to psychotropic drug use. The results showed that orlistat, administered in 3 daily doses with meals, was safe, well-tolerated, and effective, resulting in an average weight loss of 35% during an acute treatment period of about 3 months.

Topics: Enzyme Inhibitors; Humans; Lactones; Obesity; Orlistat; Psychotropic Drugs; Treatment Outcome; Weight Gain

We undertook a randomised controlled trial to assess the efficacy and tolerance of orlistat, a gastrointestinal lipase inhibitor, in promoting weight loss and preventing weight regain in obese patients over a 2-year period.. 743 patients (body-mass index 28-47 kg/m2), recruited at 15 European centres, entered a 4-week, single-blind, placebo lead-in period on a slightly hypocaloric diet (600 kcal/day deficit). 688 patients who completed the lead-in were assigned double-blind treatment with orlistat 120 mg (three times a day) or placebo for 1 year in conjunction with the hypocaloric diet. In a second 52-week double-blind period patients were reassigned orlistat or placebo with a weight maintenance (eucaloric) diet.. From the start of lead-in to the end of year 1, the orlistat group lost, on average, more bodyweight than the placebo group (10.2% [10.3 kg] vs 6.1% [6.1 kg]; LSM difference 3.9 kg [p < 0.001] from randomisation to the end of year 1). During year 2, patients who continued with orlistat regained, on average, half as much weight as those patients switched to placebo (p < 0.001). Patients switched from placebo to orlistat lost an additional 0.9 kg during year 2, compared with a mean regain of 2.5 kg in patients who continued on placebo (p < 0.001). Total cholesterol, low-density lipoprotein (LDL) cholesterol, LDL/high-density lipoprotein ratio, and concentrations of glucose and insulin decreased more in the orlistat group than in the placebo group. Gastrointestinal adverse events were more common in the orlistat group. Other adverse symptoms occurred at a similar frequency during both treatments.. Orlistat taken with an appropriate diet promotes clinically significant weight loss and reduces weight regain in obese patients over a 2-year period. The use of orlistat beyond 2 years needs careful monitoring with respect to efficacy and adverse events.

Topics: Adolescent; Anti-Obesity Agents; Biomarkers; Body Mass Index; Cholesterol; Cholesterol, LDL; Diet, Fat-Restricted; Double-Blind Method; Female; Humans; Lactones; Lipase; Male; Obesity; Orlistat; Secondary Prevention; Weight Gain

Topics: Cardiologists; Cardiovascular Diseases; Expert Testimony; Heart Disease Risk Factors; Humans; Obesity; Orlistat; Weight Gain; Weight Loss

Bariatric surgery is the most efficient treatment for obesity. However, in some cases, weight regain can occur. Currently, it is unknown the best antiobesity medication (AOM) for such clinical situation. This study aims to evaluate the effect of AOM in patients with weight regain after bariatric surgery.. A retrospective cohort study from December 2010 to July 2019 with patients submitted to bariatric surgery that had weight regain and received AOM for at least 2 years.. Of 96 patients that had weight regain in the analyzed period and received AOM, 16 were excluded from the analysis due to non-compliance (n = 7), treatment failure (n = 5), intolerable side effects with all available AOM (n = 2), or interaction with other medications (n = 2). Eighty patients were included in the analysis. The mean age was 59.0 ± 10.1 years, 88.8% were female, 91.2% white, and most of them were submitted to gastric bypass (87.6%). The mean preoperative and nadir weight after surgery were 127.9 ± 25.5 kg and 84.7 ± 22.8 kg, respectively. At the initiation of AOM, the mean baseline weight was 99.4 ± 23.1 kg. After 2 years of follow-up, there was significant weight loss in the groups treated with topiramate-alone (- 3.2 kg), topiramate plus sibutramine (- 6.1kg), and orlistat-alone or in combination (- 3.9kg). No statistical difference was observed in the sibutramine-alone group.. Topiramate (alone or associated with sibutramine) and orlistat (alone or in combination) promoted significant weight loss after 2 years of use in patients submitted to bariatric surgery with weight regain.

Topics: Aged; Anti-Obesity Agents; Bariatric Surgery; Female; Humans; Male; Middle Aged; Obesity, Morbid; Orlistat; Retrospective Studies; Topiramate; Weight Gain; Weight Loss

The aim was to first investigate the efficacy of a preoperative weight management program centered on orlistat, which is mechanistically similar to gastrointestinal bypass procedures in that it restricts dietary fat absorption, and then assess its impact on the results of one-anastomosis gastric bypass (OAGB).. We retrospectively reviewed the clinical data of consecutive patients aged 20-65 years with a body mass index (BMI) ≥ 42.5 kg/m2 who underwent primary OAGB from 2014 to 2020. Eligible patients who adhered to a 10-14 day orlistat regimen as part of a 4-6-week diet/lifestyle modification plan preceding surgery were stratified into weight reduction (Group 1) and weight gain (Group 2) groups post treatment. The correlation between pre- and postoperative weight loss and perioperative outcomes was assessed.. Of 62 eligible patients, 55 met the inclusion criteria and complied with treatment; 35 (64%) patients in Group 1 lost a median of 2.0 kg, and Group 2 had a median weight gain of 2.9 kg. Group 1 had a significantly higher initial BMI (48.9 kg/m2 vs. 44.6 kg/m2; p = 0.003), more females (54% vs. 25%) and a shorter operation time than Group 2 (107 min vs. 140 min; p = 0.109). There was no difference in the incidence of 30-day complications. Weight loss did not differ between the groups at 24 months.. Effective weight control through an orlistat-containing regimen benefitted two-thirds of patients who underwent OAGB; however, further weight loss was not observed at 2 years post-surgery.

Topics: Female; Gastric Bypass; Humans; Obesity, Morbid; Orlistat; Retrospective Studies; Weight Gain; Weight Loss

Topics: Animals; Diet, High-Fat; Diet, Western; Glucose Intolerance; Lipase; Liver; Mice; Mice, Inbred C57BL; Obesity; Orlistat; Phalaris; Seeds; Weight Gain

Chronic diseases, such as obesity, cause great harm to human health. Conventional drugs have promising therapeutic effects but also cause significant side effects. Functional foods are an excellent therapeutic alternative to pharmaceuticals, as they have fewer side effects. However, screening for active ingredients in natural foods is difficult. In this study, a novel pancreatic lipase inhibitor screening strategy, guided by the drug molecule orlistat, was combined with experimental verification. Twenty compounds from natural foods were evaluated based on the characteristics of orlistat interaction with pancreatic lipase. The characteristics of 13 molecules were comparable to those of orlistat. The pancreatic lipase inhibition rates of curcumin and sinensetin were 82.42 ± 0.50% and 81.07 ± 2.05%, respectively, and their IC

Topics: Animals; Anti-Obesity Agents; Cholesterol; Drug Evaluation, Preclinical; Enzyme Inhibitors; Flavonoids; Functional Food; Lipase; Lipids; Liver; Male; Mice; Mice, Inbred C57BL; Molecular Dynamics Simulation; Obesity; Orlistat; Pancreas; Triglycerides; Weight Gain

To determine the efficacy of Corchorus olitorius (C. olitorius) leaf extract in the prevention of metabolic syndrome induced in rats by high-fat diet (HFD) and compare it with that of orlistat.. Phytochemical analysis was performed. Effect of orlistat and C. olitorius extract on lipase activity and acute food intake were investigated. Body weight, biochemical parameters and histopathological examination were demonstrated.. Corchorus olitorius extract inhibited the pancreatic lipase activity, but orlistat was more potent. Cumulative food intake has not changed by the tested agents. In obese rats, C. olitorius or orlistat significantly decreased weight gain and visceral white adipose tissue. They exhibited a significant reduction in serum glucose, total cholesterol, triglycerides, low density lipoprotein cholesterol, free fatty acids, IL-1β, tumour necrosis factor-α (TNF-α), insulin and leptin levels of obese rat groups while high density lipoprotein cholesterol and adiponectin levels were significantly increased by them. Histopathological examination of the liver revealed that C. olitorius was more effective than orlistat in the alleviating of steatosis and adipocyte hypertrophy shown in obese control rats.. Corchorus olitorius is effective as orlistat in preventing obesity, hyperlipidaemia, steatosis and insulin resistance. These actions may be mediated by inhibiting of lipase activity, TNF-α, IL-1β and leptin resistance along with increasing of adiponectin.

Topics: Adiponectin; Animals; Anti-Obesity Agents; Corchorus; Cytokines; Diet, High-Fat; Hyperlipidemias; Insulin; Insulin Resistance; Leptin; Lipase; Male; Metabolic Syndrome; Obesity; Orlistat; Plant Extracts; Plant Leaves; Rats; Rats, Sprague-Dawley; Weight Gain

The incidence of obesity is rising at an alarming rate throughout the world and is becoming a major public health concern with incalculable social and economic costs.

Topics: Adiposity; AMP-Activated Protein Kinases; Animals; Anti-Obesity Agents; Blood Glucose; Diet, High-Fat; Disease Models, Animal; DNA-Binding Proteins; Gene Expression Regulation; Glucose Tolerance Test; Insulin; Lactones; Male; Mice; Mice, Inbred ICR; Obesity; Organ Size; Orlistat; Plant Extracts; Rhodophyta; Signal Transduction; Transcription Factors; Uncoupling Protein 1; Weight Gain

The increasing rate of obesity in the past years has become a worldwide concern and it causes many diseases. Even though, Orlistat, a synthetic anti-obesity drug approved by FDA, it causes severe side effects. DATS, a natural product from garlic have gained attention in many biological activities. The aim of the study is to determine the impact of Dially trisulpide (DATS) and its combination with Orlistat therapy on obese animals. 30 male Wistar rats (150-180g) were assigned into 5 groups (n=6). Group 1 rats received normal diet and Group 2 fed with high fat diet (HFD) for 14 weeks. Group 3-5 animals fed with HFD for 8 weeks, after that respective drugs were given simultaneously along with HFD for 6 weeks; Group 3: HFD+Orlistat; Group 4: HFD+DATS; Group 5: HFD+Orlistat+DATS. Before and after drug treatment, body weight was measured and blood was collected for assessment of lipid and liver function profiles. After end of the treatment 14 weeks, liver and adipose tissues were collected for antioxidants determination and histological observations. The significantly (p<0.05) increased body weight, serum glucose, total cholesterol, triglycerides, LDL-cholesterol were observed while significantly (p<0.05) decreased HDL-cholesterol and liver function parameters in HFD induced rats when compared to control group. The significantly (p<0.05) decreased activities of SOD, CAT, GPx and GSH levels were observed while significantly (p<0.05) increased LPO in both the tissues of HFD treated group when compared to control. Histopathological changes were observed in both the liver and adipose tissue of HFD treated group. The DATS and its combination with orlistat supplementation restored all the parameters significantly (p<0.05) especially liver function parameters and also retrieved histopathological changes when compared to orlistat alone. DATS and its combination with Orlistat had great effect than Orlistat alone.

Topics: Adipose Tissue; Allyl Compounds; Animals; Anti-Obesity Agents; Antioxidants; Body Mass Index; Body Weight; Cholesterol; Diet, High-Fat; Garlic; Lactones; Liver; Male; Obesity; Orlistat; Phytotherapy; Plant Extracts; Protective Agents; Rats; Rats, Wistar; Sulfides; Triglycerides; Weight Gain

The prevalence of obesity is increasing worldwide, with high fat diet (HFD) as one of the main contributing factors. Obesity increases the predisposition to other diseases such as diabetes through various metabolic pathways. Limited availability of antiobesity drugs and the popularity of complementary medicine have encouraged research in finding phytochemical strategies to this multifaceted disease. HFD induced obese Sprague-Dawley rats were treated with an extract of Morinda citrifolia L. leaves (MLE 60). After 9 weeks of treatment, positive effects were observed on adiposity, fecal fat content, plasma lipids, and insulin and leptin levels. The inducement of obesity and treatment with MLE 60 on metabolic alterations were then further elucidated using a (1)H NMR based metabolomics approach. Discriminating metabolites involved were products of various metabolic pathways, including glucose metabolism and TCA cycle (lactate, 2-oxoglutarate, citrate, succinate, pyruvate, and acetate), amino acid metabolism (alanine, 2-hydroxybutyrate), choline metabolism (betaine), creatinine metabolism (creatinine), and gut microbiome metabolism (hippurate, phenylacetylglycine, dimethylamine, and trigonelline). Treatment with MLE 60 resulted in significant improvement in the metabolic perturbations caused obesity as demonstrated by the proximity of the treated group to the normal group in the OPLS-DA score plot and the change in trajectory movement of the diseased group towards the healthy group upon treatment.

Topics: Adiposity; Animals; Anti-Obesity Agents; Biomarkers; Diet, High-Fat; Disease Models, Animal; Feces; Lactones; Male; Metabolomics; Morinda; Obesity; Orlistat; Phytotherapy; Plant Extracts; Plant Leaves; Plants, Medicinal; Proton Magnetic Resonance Spectroscopy; Rats, Sprague-Dawley; Time Factors; Weight Gain

Orlistat is currently the only prescribed form of pharmacological management for obesity and functions by reducing the amount of fat absorbed from food eaten. Although frequently prescribed, there is marked variability in outcomes. A total of 10 participants' experiences of gaining weight after taking orlistat were analysed using thematic analysis. Participants attributed their failed weight loss to mechanisms of the medication, emphasised a medical model of obesity with barriers to their weight loss and other weight-loss methods which had also failed. Overall, their weight gain was considered an inevitable part of their self-identity, reflecting their self-fulfilling prophecy of being a perpetual dieter.

Topics: Adult; Aged; Anti-Obesity Agents; Diet; Female; Follow-Up Studies; Humans; Interviews as Topic; Lactones; Male; Medication Adherence; Middle Aged; Obesity; Orlistat; Qualitative Research; Self Concept; Treatment Failure; Weight Gain

Drug treatments for obesity have proven efficacy from randomized trials, but their effectiveness in routine clinical practice is unknown. We assessed the effects on weight and body mass index (BMI) of orlistat and sibutramine when delivered in routine primary care.. We used United Kingdom data from the Clinical Practice Research Datalink to estimate the effects of orlistat or sibutramine on weight and BMI over 3 years following treatment initiation. For comparison, we matched each patient with up to five obese patients receiving neither drug. Mixed effects linear regression with splines was used to model change in weight and BMI. Mean change with 95% confidence intervals (CI) was estimated.. We identified 100 701 patients receiving orlistat, 15 355 receiving sibutramine and 508 140 non-intervention patients, with body mass index of 37.2, 36.6 and 33.2 kg m(-2) , respectively. Patients receiving orlistat lost, on average, 0.94 kg month(-1) (0.93 to 0.95) over the first 4 months. Weight gain then occurred, although weight remained slightly below baseline at 3 years. Patients receiving sibutramine lost, 1.28 kg month(-1) (1.26 to 1.30) over the first 4 months, but by 3 years had exceeded baseline weight. Non-intervention patients had slight increases in weight throughout the 3 year period, with gains ranging between 0.01 and 0.06 kg month(-1) .. Orlistat and sibutramine had early effects on weight loss, not sustained over 3 years. As new treatments for obesity are approved, their effectiveness should be measured in routine clinical practice, as effectiveness may be considerably less than seen in randomized trials.

Topics: Adult; Anti-Obesity Agents; Appetite Depressants; Body Mass Index; Case-Control Studies; Cyclobutanes; Databases, Factual; Female; Humans; Lactones; Linear Models; Longitudinal Studies; Male; Middle Aged; Obesity; Orlistat; Primary Health Care; Time Factors; Treatment Outcome; United Kingdom; Weight Gain; Weight Loss

This study investigated the inhibitory effect of aqueous extract of Trigonella foenum-graecum seeds (AqE-TFG) on fat accumulation and dyslipidemia in high fat diet- (HFD-) induced obese rats. Female Wistar rats were fed with HFD ad libitum, and the rats on HFD were treated orally with AqE-TFG or orlistat ((HFD for 28 days+AqE-TFG (0.5 and 1.0 g/kg) or orlistat (10 mg/kg) from day 8 to 28), respectively. Treatment with AqE-TFG produced significant reduction in body weight gain, body mass index (BMI), white adipose tissue (WAT) weights, blood glucose, serum insulin, lipids, leptin, lipase, and apolipoprotein-B levels and elevation in adiponectin levels. AqE-TFG improved serum aspartate amino transferase (AST), alanine amino transferase (ALT), and lactate dehydrogenase (LDH) levels. AqE-TFG treatment reduced the hepatic and cardiac thiobarbituric acid reactive substances (TBARS) and elevated the antioxidant enzyme (glutathione (GSH), superoxide dismutase (SOD), and catalase (CAT)) levels. In addition, liver and uterine WAT lipogenic enzyme (fatty acid synthetase (FAS) and glucose-6-phosphate dehydrogenase (G6PD)) activities were restored towards normal levels. These findings demonstrated the preventive effect of AqE-TFG on fat accumulation and dyslipidemia, due to inhibition of impaired lipid digestion and absorption, in addition to improvement in glucose and lipid metabolism, enhancement of insulin sensitivity, increased antioxidant defense, and downregulation of lipogenic enzymes.

Topics: Adipose Tissue, White; Amino Acids; Animals; Anthropometry; Antioxidants; Body Mass Index; Body Weight; Diet, High-Fat; Disease Models, Animal; Dyslipidemias; Female; Homeostasis; Lactones; Obesity; Orlistat; Oxidative Stress; Plant Extracts; Rats; Rats, Wistar; Seeds; Trigonella; Weight Gain

Obesity is a disease involving body weight gain. Several synthetic drugs of better efficacy are being introduced in the modern system of medicine. Orlistat is a pharmacological agent promoting weight loss in obese subjects via inhibiting of gastric and pancreatic lipase. Ginger (Zingiber officinale Roscoe, Zingiberacae) is one of the most commonly used spices around the world; it has long been used in traditional medicine as a cure for some diseases.. To evaluate the effect of ginger and orlistat on rats fed high fat diet.. Forty male Albino rats were either not treated (control), or fed high fat diet, or fed high fat diet with dietary orlistat supplementation (200 mg/kg diet), or fed high fat diet supplemented with 5% ginger powder. After four weeks of treatment, final body weight and food intake were determined. Blood samples were collected, lipid parameters, total bilirubin, pancreatic lipase were determined. Liver peroxisomes were isolated from rat livers and peroxisomal catalase activity was determined.. Treatment with both ginger and orlistat had significant effect in reducing body weight, besides, supplementing diet with orlistat increase food intake. Both ginger and orlistat had the ability to reduce lipid profile, ginger had great effect in increasing HDL-cholesterol than orlistat. When compared to the control group, ginger treatment did not alter either total bilirubin or pancreatic lipase activity while orlistat clearly reduced their concentration. Orlistat supplementation induced a significant reduction in peroxisomal catalase level, while ginger has been reported to interfere with enzyme activity increasing its level.. Ginger has a great ability to reduce body weight without inhibiting pancreatic lipase level, or affecting bilirubin concentration, with positive effect on increasing peroxisomal catalase level and HDL-cholesterol.

Topics: Animals; Anti-Obesity Agents; Bilirubin; Catalase; Lactones; Lipase; Lipids; Liver; Male; Obesity; Orlistat; Pancreas; Peroxisomes; Rats; Rats, Wistar; Weight Gain; Zingiber officinale

1. The aim of the present study was to determine whether the addition of a subeffective dose of rimonabant (1 mg/kg) to orlistat would be beneficial in the treatment of diet-induced obesity in rats compared with orlistat monotherapy. 2. Male rats were divided into five groups: (i) rats fed a low-fat diet for 4 months; (ii) rats fed a high-fat diet (HFD) for 4 months and treated daily with vehicle (0.2% Tween-80 solution); (iii) orlistat (10 mg/kg per day)-treated HFD-fed rats; (iv) rimonabant (1 mg/kg per day)-treated HFD-fed rats; and (v) HFD-fed rats treated with a combination of orlistat plus rimonabant. Fasting blood glucose, serum insulin, leptin and adiponectin levels were measured. Liver and adiposity indices were calculated and liver and adipose tissues were processed for histological examination. 3. Over the 4 months of the study, vehicle-treated HFD-fed rats exhibited increased cumulative food intake, bodyweight and liver and adiposity indices. Moreover, vehicle-treated HFD-fed rats exhibited a deterioration in liver function and an abnormal lipid profile. Insulin resistance and serum leptin were increased in this group, whereas serum adiponectin levels were decreased. Orlistat monotherapy or combination therapy with orlistat plus rimonabant improved all these parameters. 4. The addition of the low subeffective dose of rimonabant to orlistat therapy ameliorated HFD-induced obesity to a much greater extent than orlistat monotherapy. This combination showed better weight control and metabolic profile compared with orlistat alone. Therefore, the results of the present study encourage reassessment of the use of a low dose of rimonabant to potentiate the effect of orlistat in the clinical management of obesity if proper clinical safety data are available.

Topics: Adiposity; Animals; Anti-Obesity Agents; Body Weight; Diet, High-Fat; Dose-Response Relationship, Drug; Drug Therapy, Combination; Lactones; Male; Obesity; Orlistat; Piperidines; Pyrazoles; Rats; Rats, Wistar; Rimonabant; Weight Gain

This study evaluated the anti-obesity effects of Phellinus baumii extract (PBE) in high-fat diet (HFD)-fed mice. Male 8-week-old C57BL/6 mice were randomly divided into four groups: control, normal chow diet plus vehicle; HFD-control, high-fat plus vehicle; HFD plus orlistat (Xenical(®), Roche, Basel, Switzerland) (50 mg/kg); and HFD plus PBE (500 mg/kg). PBE was administered daily by oral gavage for 12 weeks. Oral administration of PBE (500 mg/kg) significantly reduced body weight gain, hepatic lipid concentrations, and fat accumulation in epididymal adipocytes compared with mice fed HFD alone (P < .05). mRNA expression of genes related to triglyceride (TG) synthesis was suppressed in the PBE groups, and fatty acid synthase activity was also significantly inhibited (P < .05). Furthermore, we evaluated the effect of PBE on TG absorption and detected marked reduction in TG absorption in Xenical- and PBE-treated mice compared with the control group (P < .05). To determine the active compound of PBE, fractionation was conducted, and interfungin A, davallialactone, and hypholomine B were identified as the main compounds. Among the three identified compounds, as a representative compound, davallialactone was also shown to suppress fat accumulation in an in vitro model system. These anti-obesity and hypolipidemic effects appear to be partly mediated by suppressing plasma and hepatic fat accumulation through the inhibition of enzymes associated with hepatic and intestinal lipid absorption and synthesis.

Topics: Adipocytes; Adipose Tissue; Animals; Anti-Obesity Agents; Basidiomycota; Biological Products; Dietary Fats; Epididymis; Fatty Acid Synthases; Intestinal Absorption; Lactones; Lipid Metabolism; Liver; Male; Mice; Mice, Inbred C57BL; Obesity; Orlistat; Phytotherapy; Random Allocation; RNA, Messenger; Triglycerides; Weight Gain

This study evaluated the hypolipidemic and antiobesity effects of phloroacetophenone (2',4',6'-trihydroxyacetophenone, THA) isolated from Myrcia multiflora and their relationship with triglyceride (TG) intestinal absorption and pancreatic lipase activity inhibition. The hypolipidemic effect of THA was evaluated by acute (Triton WR-1339 treatment) and chronic assay (high-fat diet treatment), the antiobesity effect was evaluated by chronic assay (high-fat diet treatment), while the inhibition of enzymatic activity of pancreatic lipase was measured in the intestinal tissue of mice treated with high olive oil concentration. In the acute assay, THA caused greater total cholesterol (37 %) and triglyceride (46 %) serum level reduction than lovastatin (32 and 1 %), a HMG-CoA reductase inhibitor or orlistat (26 and 34 %), a gastrointestinal lipase inhibitor. In addition, in the chronic assay with a high-fat diet, THA reduced cholesterol and triglyceride levels (32 and 61 %, respectively) while lovastatin showed a decrease of 35 and 49 %, respectively. THA also caused a reduction in weight gain very similar to orlistat (40 and 38 %, respectively) when the animals were submitted to a high-fat diet. Moreover, THA showed a stronger and continuous pancreatic lipase inhibitory activity when compared with orlistat, causing inhibition of this enzyme during 6 hours associated to a significant reduction of triglyceride serum levels. The IN VIVO antiobesity and hypolipidemic effects of THA may be partly mediated by delaying the intestinal absorption of dietary fat by inhibiting pancreatic lipase activity.

Topics: Acetophenones; Animals; Anti-Obesity Agents; Cholesterol; Diet, High-Fat; Glucosides; Hypolipidemic Agents; Intestinal Absorption; Lactones; Lipase; Lipids; Lovastatin; Male; Mice; Myrica; Obesity; Orlistat; Pancreas; Plant Extracts; Rats; Rats, Wistar; Triglycerides; Weight Gain

To assess the efficacy of a specific long-term programme for weight loss maintenance using a new 'on/off' Orlistat approach in obese subjects who previously lost more than 10% of their body weight.. 50 patients were followed up during 4 years; 34 completed the study. Subjects were followed up by physicians trained in obesity management. Anthropometrical, biological and psychological parameters were measured. Insulin sensitivity was evaluated by euglycaemic insulin clamp. Orlistat was given in case of weight relapse more than 2.5%. Subjects could take Orlistat on a voluntary basis for special occasions.. The BMI of completers remained stable (29.5 ± 0.9 vs. 30.6 ± 1.0 kg/m(2)). 73% of completers maintained 10% or more of their weight loss. Subjects from the no-regain group improved most of their parameters while the regain group did not. Insulin sensitivity was negatively linked to body weight during the follow up (p < 0.01, r(2) = 0.20). A negative relationship has been found between extent of the previous weight loss and the evolution of body weight during the 4 years follow-up (p < 0.01, r(2) = 0.26). Orlistat intake showed a body fat lowering effect (p < 0.05).. 73% of subjects maintained more than 10% of their weight loss. Subject with a large weight loss amount are at high risk for weight regain. The Orlistat 'on/off' intake regarding his lowering body fat mass effect seems to be efficient.

Topics: Adipose Tissue; Adult; Anti-Obesity Agents; Body Mass Index; Female; Follow-Up Studies; Humans; Insulin Resistance; Lactones; Male; Obesity; Orlistat; Recurrence; Treatment Outcome; Weight Gain; Weight Loss

Weight gain induced by long-term psychopharmacotherapy has emerged as a relevant clinical issue because it is a major problem affecting compliance and long-term outcome. The novel antiobesity drug orlistat inhibits gastrointestinal lipases, thus lowering the absorption of dietary fat and raising the possibility of decreased absorption of fat-soluble vitamins and certain concomitantly administered drugs in some individuals. We monitored plasma levels of several psychotropic agents in eight psychiatric patients receiving orlistat to determine the potential influence of orlistat on the bioavailability of these drugs. We found no clinically relevant changes in plasma concentrations of haloperidol, clozapine, clomipramine, desipramine, or carbamazepine over an 8-week period in orlistat recipients. We therefore consider orlistat to be compatible with use during long-term pharmacotherapy. Our preliminary findings suggest that orlistat may offer a pharmacological treatment option to support dietary efforts in obese and overweight psychiatric patients. However, so far no data about the potential influence of orlistat on pharmacokinetics of psychotropics have been published; therefore, plasma level monitoring is recommended.

Topics: Adult; Anti-Obesity Agents; Biological Availability; Drug Interactions; Drug Monitoring; Drug Therapy, Combination; Female; Humans; Lactones; Long-Term Care; Male; Middle Aged; Orlistat; Psychotropic Drugs; Weight Gain

Topics: Adolescent; Anti-Obesity Agents; Diabetes Mellitus; Diabetes Mellitus, Type 1; Diabetic Ketoacidosis; Diet, Reducing; Female; Humans; Lactones; Obesity; Orlistat; Weight Gain

Topics: Adult; Anti-Obesity Agents; Female; Humans; Lactones; Mental Disorders; Middle Aged; Orlistat; Psychotropic Drugs; Weight Gain