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![]() Xenical, Enzyme Blocker for Rapid Weight Loss Xenical, the most widely prescribed brand of the generic drug Orlistat, stands out among today’s most common, most popular weight loss drugs, because it works on digestion rather than appetite. Dr. Patricia Sheldon, an endocrinologist and weight-loss expert, sums-up: “Xenical ought to rank #1 among prescription weight-loss medications, because it is by far the safest and arguably the most effective over the long term.” Background The majority of popular medications for rapid weight-loss work on the Endocannsbinoid System, which scientists believe controls appetite and craving. No substantial psychological or physiological evidence supports their belief, but everyday experience encourages scientists’’ surmises. In many cases, appetite suppressants have won FDA approval and widespread acceptance in spite of biochemists’ inability to explain precisely how they work; they remain on the market because they do little harm. Because clinical trials have shown their effectiveness and reasonably low risk of side effects, physicians continue prescribing medications, earning mega-million dollar profits for pharmaceutical manufacturers. Endocannsbinoid System controllers have earned the FDA’s approval, but they come with extremely strong warnings about interactions with anti-depressants and the risk of drug-dependency. Limiting their prescriptions to patients at least 15% over their ideal weight or Body Mass Index (BMI), physicians typically prescribe Endocannsbinoid System controllers for four weeks or less, boosting a patient’s defenses during the first few weeks of a behavior modification program and a low-calorie diet. Contrast Xenical has nothing in common with its more dangerous rivals, but it remains under-rated and far too seldom used. Especially for patients with high cholesterol and other serious risks of heart disease, Xenical represents a far more appropriate choice than any of the appetite suppressants. In fact, Xenical significantly reduces cholesterol as it contributes to weight loss, because it blocks the enzyme that breaks down fat for digestion. When the body cannot digest fats, it eliminates them. As the body consumes fewer fats, it burns away stored fats for energy. Xenical does not, however, affect the body’s metabolism of carbohydrates and raw sugars, so that patients must comply with their physicians’’ dietary guidelines, and they must stay with their exercise programs. Xenical numbers among the very few weight-loss medications approved for long-term use. Because it carries little risk of biochemical or psychological dependency, and because most people tolerate it well even at maximum dosage, doctors seldom feel reluctant to refill patients’ Xenical prescriptions even after they have reached their ideal weight. About 8% of Xenical users regained the weight they had lost when they stopped taking the medication; most of them, however, went off their diet and exercise programs when they stopped medication, so that the link between Xenical stoppage and subsequent weight gain remains unclear. Behavioral effects Although the drug’s developers did not plan to reinforce proper diet through the drug’s side effects, it works that way. Because Xenical completely blocks break-down and digestion of dietary fats, users at first experience loose, oily stools, and they may pass gas with discharge as their bodies adjust to metabolic changes. Strict compliance with doctors’ low-fat guidelines eliminates this problem; violations exacerbate it. Because the side effects frequently cause substantial discomfort and even greater embarrassment, patients typically “risk it” only once. In the longest Xenical clinical trial, approximately 70% of patients lost 15% of their original body weight and kept the weight off for more than twelve months; compare those figures against approximately 25% of participants on placebo. |
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![]() Orlistat (Xenical). Unlike other weight-loss medication orlistat is an inhibitor of gastrointestinal lipases. Orlistat covalently binds to the active site of the enzyme, inactivating it. This prevents hydrolyzed and the subsequent absorption of fats from food. Reducing income fats reduces energy intake and subsequently to the loss of extra pounds. Since the primary effect of orlistat, sold in the gastrointestinal tract, a very small amount of the drug enters the systemic circulation. Recently published results of three large randomized double-blind, placebo-controlled studies that examined the effectiveness of orlistat. In all three studies during the first year, patients receiving and orlistat and placebo, respect hypocaloric diet. In order for the opportunity to support the result achieved in the second year, all patients were transferred to eucaloric diet. All three studies demonstrated a significant decrease in weight at the end of the first year in the groups receiving orlistat (on average it amounted to 9%) compared with placebo (mean weight loss - 5%). In addition, all studies showed significantly less weight gain during the second year in the groups receiving orlistat. After the first year in 30-65% of patients receiving orlistat, there was a weight loss 5% or more against 30-43% of patients receiving placebo. Loss of weight 10% or more have achieved 28-38% receiving orlistat, against 11-24% receiving placebo. After the second year of continued weight loss> = 10% for 18-34% are on orlistat, and a 6-17,5% receiving placebo. In addition to reducing body weight during therapy orlistat, these studies found a significant decrease associated with obesity risk factors such as hypertension, hyperglycemia, hypercholesterolemy and abdominal obesity. In two studies showed a significant decrease in insulin levels in patients taking orlistat for two years, whereas a third study, there were not only a reduction in insulin levels, but also improve the level of fasting blood glucose. Hollander et al. studied the effects of orlistat in combination with a moderately hypocaloric diet in patients with type 2 diabetes. As in previous studies, they also showed statistically significant weight loss in patients taking orlistat. In addition, patients with type 2 diabetes receiving orlistat for 1 year, noted the reduction of fasting blood glucose and improvement in glycated hemoglobin compared with the placebo group. However, significant differences in fasting insulin levels of these two groups were noted. All randomized in this study, patients received therapy second-generation sulfonylureas (glyburide or glipizide). Reducing the dose of sulfonylurea required 43% of patients on orlistat and 28% receiving placebo. In all three studies showed a significant reduction in total cholesterol and LDL on the background of orlistat treatment. It is believed that improvement in lipid metabolism is not due to loss of body weight per se. It is associated with the ability of orlistat to violate the absorption of lipids. Accordingly, reduced their intake to the liver, which ultimately leads to increased receptor sensitivity of hepatocytes to cholesterol - LDL. It should be noted that unlike other drugs for weight reduction, Medicaid recommends that orlistat in the first place, precisely because of its positive impact on the lipid composition of blood, not associated with weight loss. Because orlistat is not absorbed into the systemic circulation, it has no side effects typical of other drugs to reduce body weight. The most common symptoms of gastro-intestinal tract, as well as increased excretion of fat. Side effects such as abdominal pain, fecal incontinence, flatulence, increased frequency and volume of stools, "bold" chair, and others are found in 95% of patients taking orlistat. In most patients, these symtoms held within four weeks, but some can persist up to 6 months or longer. Reduce the manifestations of the intestine may be using a diet low in fat (daily intake of fat should not exceed 30% of the total calories). While receiving orlistat is not recommended for patients with the syndrome of cholestasis, data indicating the possibility of the formation of gallstones in the background of his admission, no. Orlistat is not recommended to patients with malabsorption syndrome. Against the background of treatment orlistat may be violated absorption of fat-soluble vitamins (A, D, E and K) and b-carotene. Therefore it is recommended acceptance of multivitamins during orlistat therapy. And they should be taken 2 hours before or 2 hours after taking orlistat. It is believed that by sharing a orlistat with warfarin pharmacokinetics latter should not be changed. Despite this, due to the fact that orlistat reduces the absorption of vitamin K, with time anticoagulant effect of warfarin may increase. Because, as we know, food fat increases the absorption of cyclosporine, we can expect the opposite effect, resulting in reduction of food fat, caused by taking orlistat. Although there are publications on the research, which studied the interaction of cyclosporine and orlistat, there is evidence that in six patients while taking orlistat in the blood was subtherapeutic levels of cyclosporin. In one small study showed that while taking pravastatin and increased lipid-lowering effect of orlistat, pravastatin and noted a slight increase in levels of pravastatin in the blood. Nevertheless, it is considered that the additive lipid-lowering effect to a greater extent due to the mechanism of action of orlistat, than a change in the pharmacokinetics of pravastatin. In small studies have shown that orlistat does not affect the pharmacokinetics of digoxin, glibutida, nifedipine, oral contraceptives, and phenytoin. In combination with a reduced-calorie diet orlistat is used for long-term treatment of obesity patients with a BMI> = 30 kg/m2 or BMI> = 27, with risk factors. well as to maintain the achieved results. He was taken three times a day to 120 mg during or within 1 hour after meals containing fat. If you skip meals or it does not contain fat, the drug should not be accepted. Patients should be advised multivitamins, which are best taken two hours before or 2 hours after taking orlistat. It is also necessary to remind about the importance of a diet low in fat - in order to avoid side effects. |
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