Xenical - instructions for use, analogs, reviews and release forms (capsules 120 mg) drugs to treat obesity and weight loss in adults, children and pregnancy. Composition
In this article, you can read the instructions for using the drug Xenical. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Xenical in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Xenical with available structural analogues. Use for the treatment of obesity and weight loss, combined with diet in adults, children, as well as during pregnancy and lactation. Composition of the preparation.
Xenical - a powerful, specific and reversible inhibitor of gastrointestinal lipases, which has a long-lasting effect. Its therapeutic effect 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. The inactivated enzyme loses its ability to break down the food fats that come in the form of triglycerides, to sucking free fatty acids and monoglycerides. Since uncleaved triglycerides are not absorbed, the resulting decrease in the intake of calories into the body leads to a decrease in body weight. Thus, the therapeutic effect of the drug is carried out without absorption into the systemic bloodstream.
Judging by the results of fat content in feces, the action of Orlistat (the active substance of the drug Xenical) begins 24-48 hours after ingestion. After the drug is withdrawn, the fat content in the stool after 48-72 hours usually returns to the level that occurred before the start of therapy.
Efficiency
Patients with obesity
In clinical trials, patients taking orlistat had a greater weight loss compared to patients on diet therapy.The decrease in body weight began already within the first 2 weeks after the beginning 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 to taking placebo, there was a significant decrease in the amount of fat in the body. Orlistat is effective in preventing repeated weight gain. A re-set of body weight, no more than 25% of the lost weight, was observed in about half of the patients, and half of these patients did not observe repeated weight gain or even further decrease.
Patients with obesity and type 2 diabetes mellitus
In clinical studies lasting from 6 months to 1 year in patients with overweight or obesity and type 2 diabetes taking orlistat, there was a large loss of body weight compared to patients treated only with diet therapy. The loss of body weight occurred mainly due to a decrease in the amount of fat in the body.It should be noted that before the study, despite the use of hypoglycemic agents, patients often had insufficient glycemic control. However, during the treatment with orlistat, a statistically and clinically significant improvement in glycemic control was observed. In addition, against the background of orlistat therapy, there was a decrease in doses of hypoglycemic agents, insulin concentrations, and a decrease in insulin resistance.
Reducing the risk of developing type 2 diabetes in obese patients
In a 4-year clinical study, orlistat significantly reduced the risk of developing type 2 diabetes (approximately 37% compared with placebo). The degree of risk reduction was even more significant in patients with initial impairment of glucose tolerance (approximately 45%). In the treatment group, orlistat, there was a greater loss of body weight compared to the placebo group. Maintaining the body weight at a new level was observed throughout the study period. Moreover, compared with placebo in patients receiving orlistat therapy, there was a significant improvement in the profile of metabolic risk factors.
Pubertal obesity
In a clinical study of 1 year duration in adolescents with obesity, a decrease in the body mass index was observed with Xenical when compared with the placebo group, where there was even an increase in the body mass index. In addition, patients of the orlistat group had a decrease in fat mass, as well as waist and hip circumference as compared to the placebo group. Also, patients who received orlistat therapy had a significant reduction in diastolic blood pressure compared with the placebo group.
Preclinical safety data
According to the preclinical data, additional risks for patients concerning the safety profile, toxicity, genotoxicity, carcinogenicity and reproductive toxicity were not revealed. In studies on animals, there was also no teratogenic effect. In connection with the lack of a teratogenic effect in animals, it is unlikely to be detected in humans.
Structure of the preparation
Orlistat + excipients + gelatin capsule shell.
Pharmacokinetics
In volunteers with normal body weight and obesity, the systemic effect of the drug is minimal.Judging from the data obtained in the experiment on animals, the metabolism of orlistat occurs mainly in the intestinal wall. Studies in individuals with normal and overweight showed that the main way of elimination is to remove the non-sucking drug with feces. With feces about 97% of the dose of the drug was withdrawn, 83% in the form of unchanged orlistat. The total renal excretion of all substances structurally associated with orlistat is less than 2% of the dose taken. Time to complete elimination of the drug from the body (with feces and urine) is 3-5 days. The ratio of pathways for orlistat in volunteers with normal and overweight was the same.
Indications
- Long-term therapy of obese patients or patients with excessive body weight, incl. associated with obesity risk factors, combined with a moderately hypocaloric diet;
- in combination with hypoglycemic drugs (metformin, derivatives of sulfonylureas and / or insulin) or a moderately hypocaloric diet in patients with type 2 diabetes with excessive body weight or obesity.
Forms of release
Capsules 120 mg.
The drug in the form of tablets or solution currently does not exist, it is possible that Xenical in this form is a fake.
Instructions for use and how to use them
Long-term therapy for obese patients or overweight patients, including those who are associated with obesity risk factors, in combination with a moderately hypocaloric diet in adults and children over 12 years of age, the recommended dose of orlistat is one 120 mg capsule with each major meal time of meal or not later than an hour after a meal).
In combination with hypoglycemic drugs (metformin, derivatives of ulfonylureas and / or insulin) or moderately hypocaloric diet in patients with type 2 diabetes with overweight or obesity: in adults, the recommended dose of orlistat is one 120 mg capsule with each main meal (during meal or not later than an hour after a meal).
If food intake is missed or if the food does not contain fat, Xenical can also be taken.
The drug should be taken in combination with a balanced, moderately hypocaloric diet containing no more than 30% of calories in the form of fats.The daily intake of fats, carbohydrates and proteins must be divided into three main methods.
Increasing the dose of orlistat more than the recommended (120 mg 3 times a day) does not lead to an increase in its therapeutic effect.
The efficacy and safety of Xenical in patients with impaired liver and / or kidney function, as well as in elderly and children (under 12 years) have not been studied, so taking this medication is not recommended for these categories of individuals.
Side effect
- oily discharge from the rectum;
- the emission of gases with a certain amount of detachable;
- imperative urges for defecation;
- steatorrhea;
- more bowel movements;
- loose stools;
- flatulence;
- pain or discomfort in the abdomen.
Their frequency increases with an increase in the fat content in the diet. Patients should be informed about the possibility of occurrence of adverse reactions from the gastrointestinal tract and teach how to eliminate them by better adherence to the diet, especially regarding the amount of fat contained in it. The use of a low-fat diet reduces the likelihood of side effects on the part of the gastrointestinal tract and thereby helps patients to monitor and regulate the consumption of fats.
As a rule, these adverse reactions are mild and transient. They appeared at early stages of treatment (in the first 3 months), and in most patients there was not more than one episode of such reactions.
When treating with Xenical, the following undesirable effects also occur:
- "a soft chair;
- pain or discomfort in the rectum;
- fecal incontinence;
- bloating;
- damage to teeth;
- defeat of gums;
- headache;
- upper respiratory tract infection;
- infections of the lower respiratory tract;
- urinary tract infections;
- dysmenorrhea;
- anxiety;
- weakness;
- hypoglycemic conditions;
- itching;
- rash;
- hives;
- angioedema;
- bronchospasm;
- anaphylaxis;
- rectal bleeding;
- diverticulitis;
- pancreatitis.
Contraindications
- syndrome of chronic malabsorption;
- cholestasis;
- hypersensitivity to the drug or any other components contained in the capsule.
Application in pregnancy and lactation
The drug category B.
In studies of reproductive toxicity in animals, the teratogenic and embryotoxic effect of the drug was not observed. In the absence of a teratogenic effect in animals, one should not expect a similar effect in humans.However, due to the lack of clinical data, Xenical should not be given to pregnant women.
Excretion of Xenical with breast milk has not been studied, so it should not be taken during breastfeeding.
special instructions
Xenical is effective in terms of long-term control of body weight (reduction in body weight and its maintenance at a new level, prevention of repeated weight gain). Treatment with Xenical leads to an improvement in the profile of risk factors and diseases associated with obesity, including hypercholesterolemia, type 2 diabetes, impaired glucose tolerance, hyperinsulinemia, arterial hypertension, and a reduction in visceral fat.
When used in combination with such hypoglycemic drugs as metformin, sulfonylureas and / or insulin in patients with type 2 diabetes who are overweight (body mass index (BMI) ≥28 kg / m2) or obese (BMI ≥30 kg / m2 ), Xenical in combination with a moderately hypocaloric diet provides an additional improvement in the compensation of carbohydrate metabolism.
In clinical studies in most patients, concentrations of Vitamins A, D, E,K and betakaren for four years of orlistat therapy remained within the normal range. To ensure adequate intake of all nutrients, multivitamins can be prescribed.
The patient should receive a balanced, moderately hypocaloric diet containing no more than 30% of calories in the form of fats. We recommend eating rich in fruits and vegetables. The daily intake of fats, carbohydrates and proteins must be divided into three main methods.
The likelihood of GI adverse reactions may increase if Xenical is taken amid a diet rich in fats (for example, 2000 kcal / day, of which more than 30% is fat, which is about 67 g of fat). Daily intake of fat should be divided into three main methods. If Xenical is taken with food, very rich in fat, the likelihood of gastrointestinal reactions increases.
In patients with type 2 diabetes mellitus, a decrease in body weight when treated with Xenical is accompanied by an improvement in the compensation of carbohydrate metabolism, which may or may require a reduction in the dose of hypoglycemic drugs (for example, sulfonylurea derivatives).
Drug Interactions
No interaction with amitriptyline, atorvastatin, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, pravastatin, warfarin, Nifedipine GITS (gastrointestinal therapeutic system) and slow release nifedipine, Sibutramine or alcohol (based on studies of interactions between drugs). However, it is necessary to monitor the rates of MNO with concomitant therapy with Warfarin or other oral anticoagulants.
With simultaneous admission with the drug Xenical, there was a decrease in absorption of vitamins D, E and beta-carotene. If multivitamins are recommended, they should be taken no less than 2 hours after taking Xenical or before bedtime.
With the simultaneous administration of the drug Xenical and cyclosporine, a decrease in plasma concentrations of cyclosporine was noted, therefore, a more frequent determination of the concentrations of cyclosporine in plasma with simultaneous administration of cyclosporine and Xenical is recommended.
With oral administration of Amiodarone during therapy with Xenical, the systemic exposure of amiodarone and desethylamiodarone decreased by 25-30%However, in connection with the complex pharmacokinetics of amiodarone, the clinical significance of this phenomenon is not clear. Addition of Xenical to prolonged therapy with amiodarone may lead to a decrease in the therapeutic effect of amiodarone (no studies have been performed).
It is necessary to avoid simultaneous administration of Xenical and acarbose, due to the lack of pharmacokinetic data.
With the simultaneous administration of orlistat and antiepileptic drugs, cases of seizures developed. Causal relationship between the development of seizures and orlistat therapy is not established. However, patients should be monitored for possible changes in the frequency and / or severity of the convulsive syndrome.
Analogues of the drug Xenical
Structural analogs for the active substance:
- Allie;
- Xenalten;
- Orlimax;
- Orlistat;
- Orsotene;
- Orsoten Slim.
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