» Xenical - Orlistat .Treatment of obesity Ksenikalom
Xenical - Orlistat .Treatment of obesity Ksenikalom
Xenical - Orlistat .Treatment of obesity Ksenikalom
Xenical (orlistat) - a synthetic derivative of lipstatina, product life mold fungus Streptomyces toxytricini, which inhibits most kinds of lipases (enzymes break down fats).
In many studies of Xenical, the drug was administered at low doses (30-60 mg 3 times daily), which are ineffective. Therefore, we only considered data from studies in which orlistat was administered in standard doses - 120 mg 3 times a day. Seven published prospective randomized controlled trials of 1 year or more on evaluating the effectiveness of Xenical for weight loss and maintaining it at an optimal level
In all studies have confirmed the effectiveness of Xenical for weight loss, compared with placebo. Within a year, almost a third of patients taking orlistat, weight decreased by 5% or more of its original value, as opposed to those taking placebo. Nearly twice as many patients than in the placebo group had lost more than 10% of initial weight.
Patients in the study who received primary medical advice and is not held behavioral therapy or consult with a nutritionist, have achieved less success than those who had received a standard course of behavioral therapy and had contact with a specialist in nutrition. In addition, success was more difficult for patients with type 2 diabetes and who had risk factors for cardiovascular disease.
Some studies have focused on evaluating the effectiveness of Xenical in the maintenance of weight at the current level. A number of studies were a continuation of the earlier one-year study. In these studies, which lasted another year, but rather to prevent the re-gaining weight, even more than the achievement of its decline was mitigated by conditions related to the number of calories consumed.
Almost half of the patients participated in the study, which lasted a total of 2 years. After 1 year of weight gain began to patients in both groups, and treated with ksenikalom, and who took a placebo (dummy), but the overall percentage of weight loss by the end of the second year was greater in group therapy ksenikalom. For 2 years 34% of patients treated by behavioral therapy and treatment ksenikalom, lost 10% of initial weight or more, compared with 19% of patients treated with Xenical and only initial consultation with a doctor.
One study was devoted to studying the effectiveness of Xenical for weight maintenance at a level that was reached earlier with the diet. 729 patients with obesity, which lost 8% or more weight after 6 months of therapy, has been appointed maintenance diet and therapy ksenikalom or placebo for 12 months. Compared with patients taking a placebo, patients treated with Xenical, achieved a somewhat higher total weight loss (8.2% of baseline vs. 6.4%) and a smaller increase in body weight in the future (32% of the lost pounds vs. 56%) .
In comparing the results of this study with a similar study which evaluated the efficacy of sibutramine, there is the assumption that Xenical is not as effective in maintaining weight loss achieved by using a diet level as sibutramine. Data from several clinical trials of Xenical suggest that the drug has a positive effect on the level of serum cholesterol, regardless of weight loss.
In patients treated with Xenical, cholesterol concentration in serum low-density decreased to a greater extent than placebo, even with the level of weight loss. The mechanism of this additional effect of the drug to decrease the concentration of lipids, can be explained in terms of its effect on the absorption of cholesterol from food. It was found that taking Xenical reduces the absorption of dietary cholesterol by 25%.
There is a hypothesis that in addition to blocking the absorption of fats Xenical promotes weight loss due to the fact that patients limit their fat intake from food, to avoid the side effects associated with malabsorption (malabsorption) of fats. That is, the reception of Xenical can be another tool for behavioral therapy due to the effect "Antabuse" in relation to fat.
However, according to two prospective studies of therapy ksenikalom, compared with placebo, does not lead to a decrease in fat intake in patients who spelled low-calorie diet low in fat (60 g per day). Moreover, the energy losses associated with malabsorption of fat, are larger than expected for a given weight loss, suggesting that orlistat promotes weight loss only at the expense of fat absorption, excluding the amount of their consumption.
Side effects of Xenical (orlistat)
Major side effects of Xenical are related to its activity against gastrointestinal lipases. According to the 1 - and 2-year studies, about 70-80% of patients treated ksenikalom, against 50-60% of those taking a placebo reported having one or more side effects. Gastrointestinal disorders usually appear early enough (in the first 4 weeks of treatment), mild to moderate, often limited to one or two episodes and disappear on their own, despite the continued taking the drug. Many side effects from the gastrointestinal tract can be prevented by supplementation of gelling fibers (psyllium mucilloid).
Long-term use of Xenical may cause changes in the level of essential fat-soluble vitamins in the body. A study involving healthy volunteers, showed that taking Xenical inhibits the absorption of carotene and vitamin E, with A viamin absorbed normally. Measurement of serum concentrations of fat-soluble vitamins and-carotene for 1 - and 2-year clinical trial found that in the main concentration of these substances remained within normal limits, despite the fact that patients do not receive extra vitamins.
The concentration of vitamins, usually D, E and carotene, fell below the normal range in patients treated with ksenikalom, in a larger number (5%) cases than in the placebo group. These deviations are quickly disappearing as soon as further prescribed vitamins. Thus, all patients who are treated ksenikalom recommended supplementation of multivitamins, and vitamins and Xenical should not be taken simultaneously.
Xenical can significantly impair the absorption of other fat-soluble drugs. That is, Xenical should not be given at least two hours before or after taking these drugs, and, moreover, it is necessary to monitor the extent possible, the concentration of drug in plasma for a possible correction of the dose. The results of pharmacokinetic studies suggest that some drugs are likely to be taken with ksenikalom (glyburide, oral contraceptives, furosemide, captopril, nifedipine, atenolol). There is a theoretical concern that long-term use of Xenical can increase the risk of specific diseases of the gastrointestinal tract: the formation of gallstones and colon cancer.
Xenical can increase the tendency to form stones in the gallbladder, since inhibition of fat digestion process prevents the release of fatty acids in the intestinal lumen, it is necessary to stimulate the reduction of the gallbladder. However, when orlistat is administered together with food, in which the fat content varies, this does not lead to a decrease in motility of the gallbladder.
In addition, there was no case of increasing tendency to form gallstones from thousands of patients who completed participation in the 1 - and 2-year studies on Xenical. Increased intake of fat in the colon causes concern about the increased risk of developing colon cancer. However, the appointment of Xenical volunteers who are obese, does not cause enhanced growth of cells of the colon. However, to confirm these data requires further investigation.