Listat 120mg coated film pills N60
Condition: New product
998 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Orlistat
Release form
Pills
Composition
1 tablet contains: active ingredient: orlistat 120 mg adjuvants: sodium lauryl sulfate - 12 mg; acacia gum - 210 mg; ludiflesh (mannitol - 84–92%, crospovidone - 4–6%, polyvinyl acetate - 3.5–6%, povidone - 0.25–0.6%) - 580 mg; copovidone - 20 mg; Crospovidone - 50 mg; magnesium stearate - 8 mg film coating: Opadry II blue (85F205040) (polyvinyl alcohol - 40%, titanium dioxide - 22.48%, macrogol 3350 - 20.2%, talc - 14.8%, aluminum lacquer blue - 2, 28%, iron oxide dye yellow (0.24%) - 34 mg; Silver opadry (63F97546) (polyvinyl alcohol - 47.03%, talc - 27%, macrogol 3350 - 13.27%, pearlescent pigment - 10%, polysorbate 80 - 2.7%) - 6 mg
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 the fat content 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. The clinical efficacy of patients taking orlistat is a greater loss of body weight compared with patients on diet therapy. 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.Approximately half of patients re-gain weight, not more than 25% of the lost, and the other half of the patients do not re-gain weight, or even further decrease it. In patients with overweight or obesity and type 2 diabetes , taking orlistat within 6–12 months, there is 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, there is a decrease in the dose of hypoglycemic agents, insulin concentration, as well as a decrease in insulin resistance. When using orlistat for 4 years, the risk of developing type 2 diabetes mellitus (approximately 37% compared with placebo) is significantly reduced. 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 the mass index is observed body mass (BMI), fat mass, and waist and hip circumference compared with the placebo group. Also in patients treated with orlistat, there was a significant decrease in DAP compared with the placebo group.
Pharmacokinetics
Suction. Volunteers with normal body weight and obesity have minimal systemic exposure to orlistat. After a single oral dose of 360 mg, unchanged orlistat in the blood plasma is not detected, which means that its concentrations are below the limit of quantitative determination (less than 5 ng / ml). In general, after taking therapeutic doses, unchanged orlistat could be detected in the blood plasma only in rare cases, its concentrations were extremely low (less than 10 ng / ml or 0.02 μmol). There are no signs of cumulation, which confirms that the absorption of orlistat is minimal. Distribution. Vd cannot be determined, since orlistat is very poorly absorbed. In vitro, orlistat is more than 99% bound to plasma proteins (mainly lipoproteins and albumin).In minimal quantities, orlistat can penetrate red blood cells. Metabolism. Orlistat is metabolized mainly in the intestinal wall. In patients with obesity, approximately 42% of the minimum fraction of orlistat, which undergoes systemic absorption, accounts for two main metabolites, M1 (a four-membered hydrolyzed lactone ring) and M3 (M1 with split N-formle leucine residue). lactone ring and extremely weakly inhibit lipase (weaker than orlistat, 1000 and 2500 times, respectively). Given such a low inhibitory activity and low plasma concentrations (an average of 26 and 108 ng / ml, respectively) after receiving therapeutic doses, these metabolites are considered pharmacologically inactive. Excretion. In persons with normal and overweight, the main route of elimination is the elimination of non-absorbed orlistat through the intestines. About 97% of the dose taken is excreted through the intestines, with 83% in the form of unchanged orlistat. The total renal excretion of all substances structurally related to orlistat is less than 2% of the dose taken. The time to complete elimination of orlistat from the body (through the intestine and the kidneys) is 3-5 days. The ratio of the ways of removing orlistat in volunteers with normal and overweight turned out to be the same. Both orlistat and the metabolites M1 and M3 can be excreted with bile. Particular groups of patients are children. The concentrations of orlistat and its metabolites (M1 and M3) in the blood plasma in children do not differ from those in adults when comparing the same doses of orlistat. Daily fat excretion with feces is 27% of food intake during therapy with orlistat.
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 overweight or obese type 2 diabetes.
Contraindications
hypersensitivity to orlistat or any other components of the drug, chronic malabsorption syndrome, pregnancy, breastfeeding period, children under 12 years of age.
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, including 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 h after a meal). In combination with hypoglycemic drugs (metformin, sulfonylurea derivatives and / or insulin) and / or a moderately low-calorie diet in patients with diabetes type 2 with overweight or obesity: adults - the recommended dose of the drug Listat - 1 table. (120 mg) with each main meal (during a meal or no later than 1 hour after a meal). If a meal is skipped or food does not contain fat, then you can also take the drug of Listat. The preparation of 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 should be distributed between the 3 main meals. Increasing the dose of Listat over recommended (120 mg 3 times a day) does not increase its therapeutic effect. Particular groups of patientsEfficiency and safety of Listat in patients with impaired liver function and / or kidneys, 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 / 10,000. Side reactions during the use of orlistat arose 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. From the gastrointestinal tract: often - “soft” stools, pain or discomfort in the rectum, fecal incontinence, bloating, defeat teeth, damage to the gums. Other adverse reactions: very often - headache, upper respiratory tract infections, influenza; often, lower respiratory tract infections, urinary tract infections, dysmenorrhea, anxiety, weakness. In patients with type 2 diabetes, the nature and incidence of adverse events were comparable to those in people without diabetes 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 - bloating. 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 was reduced annually over the 4-year period of the drug administration. cases of bullous rash,increased activity of transaminases and alkaline phosphatase, as well as individual, possibly serious, cases of hepatitis (causal relationship with taking orlistat or pathophysiological mechanisms of development have not been established). With simultaneous use of orlistat with indirect anticoagulants, there are cases of decreased prothrombin, an increase in MHO and unbalanced therapy with anticoagulants, which led to a change in hemostatic parameters. Cases of rectal bleeding, diverticulitis, pancreatitis , Cholelithiasis and oxalate nephropathy (frequency of occurrence is unknown) .If simultaneous administration of orlistat and antiepileptic drugs cases of seizure were observed (see. "Interaction").
Overdose
In patients with normal body weight and in obese patients, taking single doses of 800 mg or repeated administration of orlistat 400 mg 3 times a day for 15 days was not accompanied by the appearance of significant adverse events. In addition, patients with obesity have experience of using orlistat 240 mg 3 times a day for 6 months, which was not accompanied by a significant increase in the incidence of adverse events. In cases of overdose of orlistat, either no adverse events were reported or adverse events did not differ from those , which are observed when taking orlistat in therapeutic doses. In case of severe overdose of orlistat, it is recommended to observe the patient for 24 hours. According to research data in humans and animals, any systemic effects Those that could be associated with the lipase-inhibiting properties of orlistat should be rapidly reversible.
Interaction with other drugs
There was no interaction between orlistat and amitriptyline, atorvastatin, biguanides, digoxin, fibrates, fluxetine, losartan, phenytoin, oral contraceptives, peeters, pravastatin, warfarin, nifedipine GITS (gastrointestinal therapy, n, and ny, and the ny, and the ny; based on research on drug interactions). However, it is necessary to monitor the indicators of MHO with simultaneous therapy with warfarin or other indirect anticoagulants. When taken simultaneously with orlistat, a decrease in the absorption of vitamins D, E and beta-carotene was noted.If multivitamins are recommended, they should be taken at least 2 hours after taking orlistat or before going to bed. While taking orlistat and cyclosporine, there was a decrease in plasma cyclosporine concentration, therefore more frequent determination of plasma cyclosporine and cyclosporine and orlistat was recommended . When ingesting amiodarone during therapy with orlistat, there was a decrease in systemic exposure of amiodarone and deethylamidarone (by 25–30%), however, due to difficult pharmacology. kinetics of amiodarone, the clinical significance of this phenomenon is unclear. Adding orlistat to long-term treatment with amiodarone may lead to a decrease in the therapeutic effect of amiodarone (no studies have been conducted). Simultaneous administration of orlistat and acarbose should be avoided due to the lack of pharmacokinetic studies. Concurrent seizures have been observed with orlistat and antiepileptic drugs. The causal relationship between the development of seizures and therapy with orlistat has not been established. However, patients should be monitored for possible changes in the frequency and / or severity of the convulsive syndrome.
special instructions
The drug Listata is effective in terms of long-term control of body weight (weight loss and its maintenance, preventing re-gaining body weight). Treatment with Listat leads to an improvement in the profile of risk factors and diseases associated with obesity, including hypercholesterolemia, diabetes mellitus type 2, impaired glucose tolerance, hyperinsulinemia, hypertension, and a decrease in visceral fat. When used in combination with hypoglycemic drugs such as metformin , sulfonylurea derivatives and / or insulin, in patients with type 2 diabetes mellitus with an overweight (BMI of at least 28 kg / m2) or obesity (BMI of at least 30 kg / m2), preparations At Listat in combination with a moderately low-calorie diet helps to further improve the compensation of carbohydrate metabolism. In clinical studies in most patients, the concentration of vitamins A, D, E, K and beta-carotene during four years of therapy with orlistat remained within the normal range.To ensure adequate intake of all minerals, multivitamins can be used. A patient should receive a balanced, moderately low-calorie diet containing no more than 30% of calories in the form of fat. Food rich in fruits and vegetables is recommended. Daily consumption of fats, carbohydrates and proteins should be divided into three main steps. The likelihood of adverse reactions from the gastrointestinal tract can be increased if the preparation of Listat is taken with a diet rich in fats (for example, 2000 kcal / day, more than 30% of them in the form of equal to about 67 grams of fat). If Listat is taken with food that is very rich in fat, the likelihood of gastrointestinal reactions increases. In patients with type 2 diabetes, weight loss during treatment with Listat is accompanied by improved compensation of carbohydrate metabolism, which may allow or require a reduction in the dose of hypoglycemic drugs ( sulfonylureas). Influence on ability to steer vehicles and work with mechanisms. The drug Listat does not affect the ability to drive vehicles and mechanisms. Patients with diabetes mellitus type 2, using the drug Listat in combination with hypoglycemic drugs, should be careful when driving vehicles and mechanisms in connection with the possible development of hypoglycemia, accompanied by dizziness, visual impairment.