Xenical capsules 120mg N84
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Active ingredients
Orlistat
Release form
Capsules
Composition
Active ingredient: orlistat (orlistat) Active ingredient concentration (mg): 120
Pharmacological effect
Xenical is a powerful, specific and reversible inhibitor of gastrointestinal lipases, which has 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 discontinuation of the drug, the fat in the feces after 48-72 hours usually returns to the level that occurred prior to the start of therapy. Efficiency Patients with obesity In clinical studies, patients taking orlistat, there was a large loss of body weight compared with patients on diet therapy. The decrease in body weight began already during the first 2 weeks after the start of treatment and lasted from 6 to 12 months even in patients with a negative response to diet therapy. For 2 years, there was a statistically significant improvement in the profile of metabolic risk factors associated with obesity. In addition, compared with taking placebo, there was a significant decrease in body fat. Orlistat is effective in preventing re-gaining body weight. About half of the patients received repeated weight gain of no more than 25% of the lost weight, and half of these patients did not experience repeated weight gain or even further decrease. Patients with obesity and diabetes mellitus type 2 in clinical studies lasting from 6 months to 1 year in patients with overweight or obesity and type 2 diabetes mellitus who take orlistat, there was a large loss of body weight compared with patients treated only with diet therapy. The loss of body weight occurred mainly due to a decrease in the amount of body fat.It should be noted that, prior to the beginning of the study, despite taking hypoglycemic agents, patients often had insufficient glycemic control. However, with orlistat, a statistically and clinically significant improvement in glycemic control was observed. In addition, during the treatment with orlistat, there was a decrease in the doses of hypoglycemic agents, insulin concentration, and a decrease in insulin resistance. Reducing the risk of developing type 2 diabetes in patients with obesity type (about 37% compared with placebo). The degree of risk reduction was even more significant in patients with an initial impairment of glucose tolerance (approximately 45%). In the group of therapy with orlistat, a greater loss of body weight was observed compared with the placebo group. Maintaining body weight at a new level was observed during the entire study period. Moreover, compared with placebo, patients treated with orlistat showed a significant improvement in metabolic risk profile. Pubertal obesity In a 1-year clinical trial in obese adolescents, when taking orlistat, there was a decrease in body mass index compared with the placebo group, where there was even an increase in body mass index. In addition, in the patients in the orlistat group, there was a decrease in fat mass, as well as waist and hip circumference compared with the placebo group. Also in patients treated with orlistat, there was a significant decrease in diastolic blood pressure compared with the placebo group. Preclinical safety data According to preclinical data, no additional risks were identified for patients regarding safety profile, toxicity, genotoxicity, carcinogenicity and reproductive toxicity. In animal studies, no teratogenic effect was also detected. Due to the lack of a teratogenic effect in animals, it is unlikely to be detected in humans.
Pharmacokinetics
Absorption In volunteers with normal body weight and obesity, the systemic effect of the drug is minimal.After a single oral dose of 360 mg, it was not possible to determine unchanged orlistat in plasma, which means that its concentrations are below 5 ng / ml. In general, after taking therapeutic doses, it was possible to detect unchanged orlistat in plasma only in rare cases, In this, its concentrations were extremely low (<10 ng / ml or 0.02 mcmol). There were no signs of cumulation, which confirms that the absorption of the drug is minimal. The distribution of Vd cannot be determined because the drug 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 into erythrocytes. Metabolism Judging from the data obtained in an experiment on animals, the metabolism of orlistat occurs mainly in the intestinal wall. In a study in people with obesity, it was found that about 42% of the minimum fraction of the drug that undergoes systemic absorption falls on the two main metabolites, M1 (four-membered hydrolyzed lactone ring) and M3 (M1 with split N-formle leucine residue). M1 molecules and M3 have an open b-lactone ring and extremely weakly inhibit lipase (respectively, 1000 and 2500 times weaker than orlistat). Given such low inhibitory activity and low plasma concentrations (on average, 26 ng / ml and 108 ng / ml, respectively) after taking therapeutic doses, these metabolites are considered pharmacologically inactive. Examination in people with normal and overweight showed that the main way of elimination is the elimination of non-absorbed drug with feces. About 97% of the accepted dose of the drug was excreted with feces, with 83% of them being in the form of unchanged orlistat. The total renal excretion of all substances structurally related to orlistat is less than 2% of the accepted dose. The time to complete elimination of the drug from the body (with feces and urine) 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 may be excreted with bile. Pharmacokinetics in specific clinical groupsPlasma concentrations of orlistat and its metabolites (M1 and M3) in children do not differ from those in adults when comparing the same doses of the drug. The daily excretion of fat from the feces was 27% of the intake with food during therapy with orlistat and 7% - with placebo.
Contraindications
In combination with hypoglycemic drugs (metformin, sulfonylurea derivatives and / or insulin) or a moderately low-calorie diet in overweight or obese patients with type 2 diabetes: in adults, the recommended dose of orlistat is one 120 mg capsule with each main meal (in eating time or no later than an hour after eating). If a meal is missed or if the food does not contain fat, you can also skip the drug Xenical. The drug should be taken in combination with a balanced, mind Especially hypocaloric diet containing no more than 30% of calories in the form of fat. Daily consumption of fats, carbohydrates and proteins should be divided into three main doses. Increasing the dose of orlistat over the recommended (120 mg 3 times / day) does not increase its therapeutic effect. Efficiency and safety of Xenical in patients with impaired liver and / or kidney function , as well as in patients of elderly and children's age (under 12 years old) have not been studied.
Precautionary measures
chronic malabsorption syndrome; cholestasis; hypersensitivity to the drug or any other components contained in the capsule.
Use during pregnancy and lactation
Xenical is effective in terms of long-term control of body weight (weight loss and maintaining it at a new level, preventing re-gaining body weight). Treatment with Xenical improves the profile of risk factors and diseases associated with obesity, including hypercholesterolemia, type 2 diabetes, 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 overweight (body mass index (BMI) ≥28 kg / m2) or obesity (BMI ≥30 kg / m2), Xenical combined with a moderately low-calorie diet provides an additional improvement in carbohydrate metabolism compensation. In clinical studies in most patients, the concentrations 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 nutrients, multivitamins can be prescribed. 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 probability of adverse reactions from the gastrointestinal tract may increase if Xenical is taken on a diet rich in fats (for example, 2000 kcal / day, more than 30% of them in the form of fats, which equal to about 67 grams of fat). Daily fat intake should be divided into three main methods. If Xenical 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 Xenical is accompanied by improved compensation of carbohydrate metabolism, which may allow or require a reduction in the dose of hypoglycemic drugs (for example, sulfonylurea derivatives ).
Dosage and administration
Indications for useLong-term therapy for patients with obesity or overweight patients, incl. having obesity-associated risk factors in combination with a moderately low-calorie diet; in combination with hypoglycemic drugs (metformin, sulfonylurea derivatives and / or insulin) or a moderately low-calorie diet in patients with type 2 diabetes with overweight or obesity.
Side effects
No interaction was found with amitriptyline, atorvastatin, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, pravastatin, warfarin, nifedipine GITS (gastrointestinal therapeutic system), and in the case of the same i'yo, i'yo, i'yo, i'm using ipitine, heparin, pyroxetine, phenocarcinoma research on drug interactions). However, it is necessary to monitor the performance of MNO with concomitant therapy with warfarin or other oral anticoagulants. When administered concurrently with Xenical, a decrease in the absorption of vitamins D, E and beta carotene was noted. If a multivitamin is recommended,they should be taken at least 2 hours after taking Xenical or before bedtime. When Xenical and cyclosporine were taken simultaneously, there was a decrease in plasma concentrations of cyclosporine, therefore more frequent determination of cyclosporine concentrations in plasma while taking cyclosporine and Xenical was recommended. For oral administration of amiodarone during therapy with Xenical, there was a decrease in systemic exposure of amiodarone and dezethylamidarone (by 25-30%), however, due to the complex armokinetics of amiodarone, the clinical significance of this phenomenon is not clear. Adding the drug Xenical to long-term therapy with amiodarone may lead to a decrease in the therapeutic effect of amiodarone (no studies have been conducted). Simultaneous administration of Xenical and acarbose should be avoided due to the lack of pharmacokinetic studies. Concurrent cases of orlistat and antiepileptic drugs have been observed. 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.
Overdose
The following categories are used to describe the frequency of adverse reactions: very often (≥1 / 10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10000 , <1/1000) and very rarely (<1/10000), including some cases. Adverse reactions to orlistat arose mainly from the gastrointestinal tract and were due to the pharmacological action of the drug, 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 the diet. Patients should be informed about the possibility of adverse reactions from the gastrointestinal tract and should be taught how to eliminate them by better following the diet, especially with regard to the amount of fat contained in it.Using a low-fat diet reduces the likelihood of side effects from the gastrointestinal tract and thereby helps patients control and regulate fat intake. As a rule, these side reactions are mild and transient. They occurred in the early stages of treatment (in the first 3 months), and most patients had no more than one episode of such reactions. The following undesirable effects on the gastrointestinal tract often occur during treatment with Xenical: “soft” stools, pain or discomfort in the rectum, fecal incontinence, abdominal distension, damage to the teeth, and gum damage. It was also noted very often: headaches, 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 frequency of adverse events were comparable to those in patients without diabetes mellitus with overweight and obesity. The only new side effects in patients with type 2 diabetes were hypoglycemic conditions that occurred with a frequency of> 2% and an incidence of ≥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 decreased annually during the 4-year period of taking the drug.
Interaction with other drugs
Do not exceed recommended doses.
special instructions
In clinical studies in individuals with normal body weight and obesity, taking single doses of 800 mg or repeated intake of the drug 400 mg 3 times / day for 15 days was not accompanied by the appearance of significant adverse events. In addition, patients with obesity have experience with orlistat 240 mg 3 times / day for 6 months, which was not accompanied by a significant increase in the incidence of adverse events. In cases of overdose of Xenical, either no adverse events were reported or adverse events did not differ from those , which are observed when taking the drug in therapeutic doses. In case of severe overdose of the drug Xenical, it is recommended to observe the patient for 24 hours.According to studies in humans and animals, any systemic effects that could be associated with the lipase-inhibiting properties of orlistat should be quickly reversible.