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Active ingredients
Orlistat
Release form
Pills
Composition
Orlistat 120 mg. Excipients: sodium lauryl sulfate - 12 mg, acacia gum - 210 mg, mannitol - 580 mg, crospovidone - 50 mg, magnesium stearate - 8 mg. The composition of the shell: opadry II blue (85F205040) - 34 mg, incl. polyvinyl alcohol - 40%, titanium dioxide - 22.48%, macrogol 3350 - 20.20%, talc - 14.8%, aluminium blue varnish - 2.28%, iron dye yellow oxide - 0.24%. silver opadry (63F97546) - 6 mg, incl. polyvinyl alcohol - 47.03%, talc - 27%, macrogol 3350 - 13.27%, pearlescent pigment - 10%, polysorbate-80 - 2.7%.
Pharmacological effect
Orlistat is a potent, specific and reversible inhibitor of gastrointestinal lipases, with a long lasting effect. Its therapeutic action is carried out in the lumen of the stomach and small intestine and consists in the formation of a covalent bond with the active serine portion of the gastric and pancreatic lipases. An inactivated enzyme at the same time loses the ability to break down food fats, coming in the form of triglycerides, into absorbable free fatty acids and monoglycerides. Since unsplit triglycerides are not absorbed, the resulting reduction in calorie intake leads to a decrease in body weight. Thus, the therapeutic effect of the drug is carried out without absorption into the systemic circulation. Judging by the results of fat in the feces, the action of orlistat begins 24–48 hours after ingestion. After the withdrawal of orlistat, the fat content in the feces after 48–72 hours usually returns to the level that occurred before the start of therapy. Clinical efficacy In patients taking orlistat, there is a greater loss of body weight compared with patients on diet. A decrease in body weight begins already during the first 2 weeks after the start of treatment and lasts from 6 to 12 months, even in patients with a negative response to diet therapy. For 2 years, there has been a statistically significant improvement in the profile of metabolic risk factors associated with obesity. In addition, compared with taking placebo, there is a significant decrease in body fat. Orlistat is effective in preventing re-gaining body weight. Repeated weight gain, not more than 25% of the loss, is observed in about half of the patients, and in the other half of the patients, re-weight gain is not observed, or even a further decrease is noted.Patients with overweight or obesity and type 2 diabetes who take orlistat for 6–12 months have a greater loss of body weight compared with patients receiving only diet therapy. Loss of body weight occurs mainly due to a decrease in the amount of fat in the body. During the treatment with orlistat, a statistically and clinically significant improvement in glycemic control is observed. In addition, during the treatment with orlistat, a decrease in the dose of hypoglycemic agents, insulin concentration, as well as a decrease in insulin resistance is observed. When using orlistat for 4 years, the risk of developing type 2 diabetes mellitus is significantly reduced (by about 37% compared with placebo). The degree of risk reduction is even more significant in patients with an initial impaired glucose tolerance (approximately 45%). Maintaining body weight at a new level is observed during the entire period of drug use. When using orlistat for 1 year in adolescents with obesity, a decrease in body mass index (BMI), fat mass, and waist and hip circumference was observed compared with the placebo group. Also in patients treated with orlistat, there was a significant decrease in DAP compared with the placebo group.
Indications
long-term therapy of patients with obesity with a BMI of at least 30 kg / m2 or patients with overweight with a BMI of at least 28 kg / m2, including associated with obesity-associated risk factors in combination with a moderately low-calorie diet. in combination with hypoglycemic drugs (metformin, sulfonylurea derivatives and / or insulin) and / or a moderately low-calorie diet in patients with type 2 diabetes with overweight or obesity.
Contraindications
hypersensitivity to orlistat or any other component of the drug. chronic malabsorption syndrome. pregnancy breastfeeding period. children under 12 years old.
Use during pregnancy and lactation
In animal reproductive toxicity studies, the teratogenic and embryotoxic effect of orlistat was not observed. In the absence of a teratogenic effect in animals, a similar effect in humans is not expected. Since there are no clinical data on the use of orlistat during pregnancy,use of the drug Listat in pregnant women is contraindicated. Due to the fact that there is no data on the allocation of orlistat with breast milk, the use of the drug Listat during breastfeeding is contraindicated.
Dosage and administration
Inside, drinking water. Treatment of patients with obesity with a BMI of at least 30 kg / m2 or patients with overweight with a BMI of at least 28 kg / m2, incl. having associated with obesity risk factors, in combination with a moderately low-calorie diet: adults and children over 12 years old - the recommended dose of the drug Listat - 1 table. (120 mg) with each main meal (with meals or no later than 1 hour after meals). In combination with hypoglycemic drugs (metformin, sulfonylurea derivatives and / or insulin) and / or a moderately low-calorie diet in patients with type 2 diabetes with overweight or obesity: adults - the recommended dose of the drug Listat - 1 tab. (120 mg) with each main meal (with meals or no later than 1 hour after meals). If a meal is skipped or food does not contain fat, then you may also skip taking the drug Listat. The drug Listat should be taken in combination with a balanced, moderately low-calorie diet, containing no more than 30% of calories in the form of fat. Daily intake of fats, carbohydrates and proteins must be distributed between the 3 main meals. Increasing the dose of the drug Listat over the recommended (120 mg 3 times a day) does not lead to an increase in its therapeutic effect. Special groups of patients The efficacy and safety of the drug Listat in patients with impaired liver and / or kidney function, as well as in elderly patients and children under 12 years of age have not been studied.
Side effects
Clinical research data Side effects of the drug are systematized relative to each of the organ systems, depending on the frequency of occurrence, using the following classification: very often - more than 1/10. often more than 1/100, less than 1/10. infrequently - more than 1/1000, less than 1/100. rarely more than 1/10000, less than 1/1000. very rarely, including single messages - less than 1/10000. Adverse reactions in the use of orlistat occurred mainly from the gastrointestinal tract and were caused by the pharmacological action of orlistat, which prevents the absorption of food fats.Very often such phenomena as oily discharge from the rectum, gas with some discharge, imperative urge to defecate, steatorrhea, increased bowel movements, loose stools, flatulence, pain or abdominal discomfort were noted. Their frequency increases with increasing fat content in food. Patients should be informed about the possibility of adverse reactions from the gastrointestinal tract and should be taught how to eliminate them by following the diet, especially with regard to the amount of fat contained in it. The use of a diet low in fat reduces the likelihood of side effects from the gastrointestinal tract and thus helps patients to control and regulate fat intake. As a rule, these side reactions are mild and transient. They occur in the early stages of treatment (in the first 3 months), and most patients had no more than one episode of such reactions. On the part of the gastrointestinal tract: often - "soft" stools, pain or discomfort in the rectum, fecal incontinence, abdominal distension, tooth damage, gum damage. Other adverse reactions: very often - headache, upper respiratory tract infections, flu. often - lower respiratory tract infections, urinary tract infections, dysmenorrhea, anxiety, weakness. In patients with type 2 diabetes, the nature and frequency of adverse events were comparable to those in people without diabetes mellitus with overweight and obesity. The only additional side effects in patients with type 2 diabetes were hypoglycemic conditions that occurred with a frequency of more than 2% and an incidence of at least 1% compared with placebo (which could result from improved compensation of carbohydrate metabolism), and often - abdominal distension. In a 4-year clinical study, the overall safety profile did not differ from that obtained in 1- and 2-year studies. At the same time, the overall incidence of adverse events from the gastrointestinal tract annually decreased over the 4-year period of taking the drug. Post-Marketing Surveillance Rare cases of allergic reactions have been described, the main clinical manifestations of which were skin rash, pruritus, urticaria, angioedema, bronchospasm, and anaphylaxis.Very rare cases of bullous rash, increased transaminase and alkaline phosphatase, as well as individual, possibly serious, cases of hepatitis are described (causal relationship with taking orlistat or pathophysiological mechanisms of development have not been established). With the simultaneous use of orlistat with indirect anticoagulants, there have been cases of a decrease in prothrombin, an increase in the values of MHO and unbalanced therapy with anticoagulants, which led to a change in hemostatic parameters. Cases of rectal bleeding, diverticulitis, pancreatitis, cholelithiasis, and oxalate nephropathy have been reported (the incidence is unknown). While taking orlistat and antiepileptic drugs at the same time, there were cases of seizures (see "Interaction").
special instructions
Clinical research data Side effects of the drug are systematized relative to each of the organ systems, depending on the frequency of occurrence, using the following classification: very often - more than 1/10. often more than 1/100, less than 1/10. infrequently - more than 1/1000, less than 1/100. rarely more than 1/10000, less than 1/1000. very rarely, including single messages - less than 1/10000. Adverse reactions in the use of orlistat occurred mainly from the gastrointestinal tract and were caused by the pharmacological action of orlistat, which prevents the absorption of food fats. Very often such phenomena as oily discharge from the rectum, gas with some discharge, imperative urge to defecate, steatorrhea, increased bowel movements, loose stools, flatulence, pain or abdominal discomfort were noted. Their frequency increases with increasing fat content in food. Patients should be informed about the possibility of adverse reactions from the gastrointestinal tract and should be taught how to eliminate them by following the diet, especially with regard to the amount of fat contained in it. The use of a diet low in fat reduces the likelihood of side effects from the gastrointestinal tract and thus helps patients to control and regulate fat intake. As a rule, these side reactions are mild and transient. They occur in the early stages of treatment (in the first 3 months), and most patients had no more than one episode of such reactions.On the part of the gastrointestinal tract: often - "soft" stools, pain or discomfort in the rectum, fecal incontinence, abdominal distension, tooth damage, gum damage. Other adverse reactions: very often - headache, upper respiratory tract infections, flu. often - lower respiratory tract infections, urinary tract infections, dysmenorrhea, anxiety, weakness. In patients with type 2 diabetes, the nature and frequency of adverse events were comparable to those in people without diabetes mellitus with overweight and obesity. The only additional side effects in patients with type 2 diabetes were hypoglycemic conditions that occurred with a frequency of more than 2% and an incidence of at least 1% compared with placebo (which could result from improved compensation of carbohydrate metabolism), and often - abdominal distension. In a 4-year clinical study, the overall safety profile did not differ from that obtained in 1- and 2-year studies. At the same time, the overall incidence of adverse events from the gastrointestinal tract annually decreased over the 4-year period of taking the drug. Post-Marketing Surveillance Rare cases of allergic reactions have been described, the main clinical manifestations of which were skin rash, pruritus, urticaria, angioedema, bronchospasm, and anaphylaxis. Very rare cases of bullous rash, increased transaminase and alkaline phosphatase, as well as individual, possibly serious, cases of hepatitis are described (causal relationship with taking orlistat or pathophysiological mechanisms of development have not been established). With the simultaneous use of orlistat with indirect anticoagulants, there have been cases of a decrease in prothrombin, an increase in the values of MHO and unbalanced therapy with anticoagulants, which led to a change in hemostatic parameters. Cases of rectal bleeding, diverticulitis, pancreatitis, cholelithiasis, and oxalate nephropathy have been reported (the incidence is unknown). While taking orlistat and antiepileptic drugs at the same time, there were cases of seizures (see "Interaction").