The medical treatment of obesity is aimed at decreasing appetite,alterating absorption of calories, and increasing thermogenesis. Two agents are available for the long-term treatment of obesity: sibutramine, a centrally acting anorectic agent, and orlistat, which blocks the absorption of fat by inhibiting the enzyme lipase.
Full Answer
How effective is orlistat for weight loss?
In several trials lasting up to 2 years, orlistat was more effective than diet alone for weight reduction and maintenance of lost weight. Orlistat treatment also results in modest improvements in total cholesterol, low-density lipoprotein, blood pressure, and fasting glucose and insulin concentrations.
When are weight loss medications indicated in the treatment of obesity?
Weight-loss medications are recommended, unless contraindicated, for patients who have a BMI ≥ 30 kg/m 2 or > 27 kg/m 2 with obesity-related comorbidities. 4 Medications should be combined with nutrition education, behavioral intervention, an exercise program, and a long-term weight-maintenance plan.
Do weight-loss medications work?
The addition of these lifestyle modifications to weight-loss pharmacology results in greater weight loss and treatment satisfaction. 5 In general, weight-loss medications have a modest effect; this may be because of the complex regulatory system designed to prevent starvation. 6 Weight-loss medications have had a tainted past.
What is the best medication to suppress appetite?
The following FDA-approved medications suppress appetite: Liraglutide (Saxenda™), Naltrexone-Bupropion (Contrave™), Phentermine-Topiramate (Qysmia™), as well as these stimulants: benzphetamine (Didrex™), diethylpropion (Tenuate™), phentermine (Adiphex-P™, ProFast™), and phendimetrazine. Each medicine impacts appetite differently.
Which pharmacologic weight loss treatment works to reduce appetite?
Phentermine (Adipex, Ionamin, Suprenza) and diethylpropion are the oldest medications for weight loss. Phentermine is available in daily doses of 37.5 mg, 30 mg,15 mg, and 8 mg (Lomaira). Phentermine is FDA-approved for short term use, and it is an adrenergic agonist that produces appetite suppression.
Does orlistat work for weight loss?
Orlistat (brand name: alli) is an FDA-approved OTC medication that can help overweight adults lose weight. Orlistat works by blocking fat from being absorbed into the body after it is eaten during a meal. Approximately 5 to 10 pounds may be lost during the first 6 months of orlistat use.
What type of diet drug is orlistat?
Orlistat is in a class of medications called lipase inhibitors. It works by preventing some of the fat in foods eaten from being absorbed in the intestines. This unabsorbed fat is then removed from the body in the stool.
Does orlistat affect appetite?
Orlistat inhibition of intestinal lipase acutely increases appetite and attenuates postprandial glucagon-like peptide-1-(7-36)-amide-1, cholecystokinin, and peptide YY concentrations.
Is orlistat successful?
Does orlistat work? Studies have shown that, on average, orlistat, plus a weight-reducing diet and exercise, causes more weight loss than a weight-reducing diet and exercise alone. Some people lose 10% or more of their body weight within six months with the help of orlistat. In others, it is less effective.
Is orlistat harmful?
More specifically, the use of orlistat has been associated with several mild-to-moderate gastrointestinal adverse effects, such as oily stools, diarrhoea, abdominal pain and faecal spotting.
How does the drug orlistat work?
Orlistat (the active ingredient in Alli) promotes weight loss by decreasing the amount of dietary fat absorbed in your intestines. Lipase, an enzyme found in the digestive tract, helps break down dietary fat into smaller parts, so it can be used or stored for energy. Orlistat blocks the work of lipase.
What is orlistat and how does it work?
Orlistat works by preventing around a third of the fat from the food you eat being absorbed. The undigested fat is not absorbed into your body and is passed out with your poo. This will help you avoid gaining weight, but will not necessarily cause you to lose weight.
What is the brand name of orlistat?
Orlistat is available under the following different brand names: Alli, and Xenical.
How do I get the best results from orlistat?
You must achieve a weight loss of 5% within 3 months of being on orlistat otherwise the treatment may be stopped. It is recommended that you take 1 tablet (120mg) three times per day. The tablet should be taken immediately before, during or up to 1 hour after a meal. If a meal is missed do not take the tablet.
Can orlistat cause weight gain?
Tell your doctor if you experience serious side effects of Xenical including blood in your urine, urinating less than usual or not at all, drowsiness, confusion, mood changes, increased thirst, swelling, weight gain, feeling short of breath, severe pain in your upper stomach spreading to your back, or fast heart rate.
What is orlistat 120 mg used for?
Orlistat blocks some of the fat that you eat, keeping it from being absorbed by your body. Orlistat is used to aid in weight loss, or to help reduce the risk of regaining weight already lost. This medicine must be used together with a reduced-calorie diet. Orlistat is for use only in adults.
What are the differences between OTC and prescription weight loss medications?
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Which weight loss medications are known for suppressing appetite?
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Weight-Loss Medications
Weight-loss medications have had a tainted past. Among the first medications to be used for weight loss were thyroid hormone (1893) and digoxin (1940s), with disastrous results. 7 The most infamous weight-loss medication is fenfluramine (part of the phentermine-fenfluramine combination known as “phen-fen”), which was pulled from the U.S.
Appetite-Altering Drugs
Several categories of medications alter appetite, including the sympathomimetics, serotonergics, endocannaboid antagonists, and others. When discussing appetite, it is important to appreciate two distinct concepts of hunger. The first—satiety—refers to the sensation of feeling full when eating.
Absorption-Altering Drugs
A parallel to decreasing caloric intake is to reduce the absorption of nutrients in the gastrointestinal system. The two most common drugs that alter absorption are orlistat and acarbose. Orlistat is a lipase inhibitor that reversibly inhibits human gastrointestinal lipases and is FDA-approved for the long-term treatment of obesity.
Thermogenesis-Increasing Drugs
No agent that specifically increases thermogenesis (basal metabolic rate)is available. However, several agents display thermogenic properties. The mechanism of weight loss with sibutramine is often proposed to be by both decreasing appetite and increasing energy expenditure through thermogenesis.
Agents on the Horizon
Several new agents are under investigation for weight loss. Some are drugs that are already FDA-approved for other indications; the manufacturers of many of these are seeking additional FDA-approved indications for weight loss. The U.S.
Summary
Obesity is a common disease with a substantial burden on both individuals and the U.S. health care system as a whole. 61 The medical treatment of obesity has been confounded by worrisome adverse events and modest efficacy. However, many overweight and obese patients benefit from modest weight loss.
How much weight did Orlistat lose?
After 57 weeks of treatment, patients who received orlistat had substantially more weight loss from baseline (6.19 vs 4.31 kg, p<0.001), with 48.8% losing 5% or more of baseline weight, compared with 22.6% for those receiving placebo (p<0.001). Fasting blood glucose remained relatively constant at the end of 57 weeks (0.36 mg/dl decrease) in the orlistat group, whereas patients in the placebo group had a mean increase of 9.7 mg/dl (p<0.001). Orlistat-treated patients with baseline blood glucose concentrations greater than 140 mg/dl experienced the greatest benefit (mean decrease 8.4 mg/dl). They also had significantly greater reductions in HbA1cconcentrations (mean decrease 0.28% vs 0.18%, p<0.001), with patients having baseline HbA1cconcentrations above 8% showing the greatest benefit (mean decrease 0.53%). The average dosages of glyburide and glipizide also decreased by 23% in orlistat-treated patients compared with 9% in the placebo group (p=0.0019).29
How much did total cholesterol decrease with orlistat?
Total and LDL cholesterol significantly decreased by 7.7% and 8.9% , respectively, in all orlistat-treated groups combined compared with no change with placebo. Total and LDL cholesterol returned to baseline values after 2-wk placebo follow-up.
How many patients were in the placebo group when they were on Orlistat?
Overall withdrawal rates were larger in the placebo group (83 patients) than in the orlistat group (61 patients). However, withdrawals due to gastrointestinal adverse events were more common with orlistat-treated patients (3.5% vs 0.6%). In general, adverse effects and vitamin replacement requirements were similar to those reported in the United States trial.
What is the best treatment for obesity?
However, it was recognized that pharmacologic agents approved for long-term therapy may be useful adjuncts to diet and exercise for patients with a body mass index (BMI) of 30 kg/m2or more, and for those with a BMI above 27 kg/m2who have concomitant obesity-related risk factors or diseases.7Two drugs, orlistat and sibutramine, are approved by the Food and Drug Administration (FDA) for long-term therapy of obesity.8Orlistat (Xenical; Roche Pharmaceuticals, Nutley NJ), was granted approval in March 1999 for obesity management, including weight loss and weight maintenance.9This agent has a novel gastrointestinal mechanism of action and is the first available antiobesity agent that does not primarily alter neurotransmitter concentrations in the central nervous system.
Where does orlistat metabolite occur?
Metabolism of the agent appears to occur in the gastrointestinal wall. 9Based on data from studies of radiolabeled orlistat in obese patients, two major metabolites were identified, M1, with a hydrolyzed 4-member lactone ring, and M3, M1 with the N-formal leucine moiety cleaved.15These metabolites accounted for approximately 42% of total radioactivity in plasma, with mean concentrations of 26 ng/ml and 108 ng/ml for M1 and M3, respectively, 2–4 hours after drug administration. The primary metabolite, M1, has a relatively short half-life of approximately 3 hours; the half-life of M3 is approximately13 hours.9, 15Both M1 and M3 contain an open β-lactone ring in their chemical structures. Due to their very low plasma concentrations, and given data indicating that the β-lactone ring is required for lipase inhibition, they are considered to be pharmacologically inactive.9, 15, 17
What is the new lipase inhibitor?
Orlistat, a New Lipase Inhibitor for the Management of Obesity
How many people dropped out of Orlistat?
In the United States trial, 4.9% of patients in the placebo group dropped out during the first year due to “treatment failure,” whereas only 0.9% of orlistat-treated patients withdrew for this reason. The drug’s long-term health benefits are unclear, as are benefits accrued from modest reductions in weight.
How long does it take to lose weight on orlistat?
Monitor weight loss & BMI. Most weight loss occurs in first 6 months of therapy, but as patients continue to take orlistat, they can maintain the weight reduction. The metabolic improvements of weight loss are very beneficial for people w/ obesity-related health problems (diabetes, dyslipidemia, HTN, & metabolic syndrome).
How do drugs promote weight gain?
Mechanisms by which the drugs promote weight gain are unclear but may involve stimulation of appetite &/or a slowed metabolic rate.
What is the name of the lipase inhibitor?
Orlistat (Xenical, Alli) is the prototype of the lipase inhibitors.
Which group has the highest obesity rate?
Generally, more women than men are obese, whereas more men than women are over-weight. African American women & Mexican American men & women have the highest rates of overweight & obesity in the US.
Why is o use recommended for older adults?
o Use in older adults: Recommendations advise conservative use & lower dosages, because older adults often have decreased renal, cardiac, & hepatic function.
Why is drug therapy problematic?
Drug therapy has a problematic history, mainly because of serious adverse effects & rapid weight regain stopped. o The FDA took some drugs & a component of many over-the-counter and herbal weight loss products (ephedra & ma huang) off the market because of adverse effects.
Why do obese people collapse their upper airways?
Commonly occurs in obese persons. Due to enlargement of soft tissue in the upper airways that leads to collapse of the upper airways w/ inspiration during sleep.
How long can you take orlistat?
Dosing and contraindications: Patients can use orlistat for up to 4 years in the treatment of obesity. If therapy is to continue for more than four years, a discussion with the patient is to inform then of the lack of more extended studies. The recommended dose is 120 mg three times daily, along with each meal.
What are the goals of obesity medication therapy?
Treatment should focus on short-term as well as long-term weight reduction, avoidance of weight gain, improvement of health parameters, and management of side effects.
What is lifestyle intervention?
Lifestyle intervention - Before the initiation of weight loss drug therapy, it is important to have established a lifestyle intervention program, ideally with close monitoring by a dietitian, and long term follow-up as performed in long term trials. [11] [12] Discussion of these different ways of lifestyle intervention is beyond the scope of this article, which focuses on medication therapy; however, pharmacologic therapy should be a consideration after all these non-pharmacologic approaches are optimized.
How does behavioral therapy help with obesity?
The main therapy for obesity includes weight loss promotion by behavioral therapy, including diet, and a healthy lifestyle with regular physical activity. Weight loss produces a significant reduction in cardiovascular risk factors, prevention of disease, and improvements in self-esteem and function. Greater weight loss produces benefits in overall ...
What is the BMI of a person with obesity?
A BMI greater than 30 kg/m^2 is considered diagnostic for obesity and it is further subclassified into class 1 (30 to 34.9 kg/m^2), class 2 (35 to 39.9kg/m^2), and class 3 or morbid obesity (≥ 40kg/m^2). The main therapy for obesity includes weight loss promotion by behavioral therapy, including diet, and a healthy lifestyle with regular physical ...
How is obesity measured?
Epidemiologic studies have defined obesity by the body mass index (BMI), which is calculated by dividing a person’s weight in kilograms by the square of their height in meters. That helps to stratify obesity-related health risks at a population level.
Is naltrexone a good med for obesity?
Therefore it is not recommended as first-line pharmacologic therapy for obesity management. A naltrexone-bupropion combination is a good option; however, for smokers who desire to pursue a combined therapy to quit smoking and mitigate the weight gain, usually following that.