Orsoten capsules 120 mg 84 pcs
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Active ingredients
Orlistat
Release form
Capsules
Composition
1 capsule contains: Active substance: Orsoten semi-finished product-granules 112.8 mg Auxiliary substances: MCC 22.2 mg Capsule shell: titanium dioxide (E171) 0.58 mg; gelatin 28.22 mg, iron oxide yellow (E172) 0.04 mg.
Pharmacological effect
A specific inhibitor of gastrointestinal lipases with a long lasting effect. It has a therapeutic effect in the lumen of the stomach and small intestine, forming a covalent bond with the active serine portion of the gastric and intestinal lipases. An enzyme thus inactivated loses its ability to break down edible fats, in the form of triglycerides, into absorbable free fatty acids and monoglycerides. Since unsplit triglycerides are not absorbed, the intake of calories in the body decreases, which leads to a decrease in body weight. The therapeutic effect of the drug is carried out without absorption into the systemic circulation. The action of orlistat leads to an increase in the fat content in the feces after 24-48 hours after taking the drug. After discontinuation of the drug, the fat content in the fecal masses usually returns to the initial level after 48-72 hours.
Pharmacokinetics
Absorption The absorption of orlistat is low. 8 hours after ingestion of the therapeutic dose, unchanged orlistat is practically undetectable in the blood plasma (concentration less than 5 ng / ml). There are no signs of cumulation, which confirms the minimal absorption of the drug. In vitro distribution, orlistat is more than 99% bound to plasma proteins (mainly lipoproteins and albumin). In minimal quantities, orlistat can enter the red blood cells. Metabolism Orlistat is metabolized mainly in the intestinal wall with the formation of pharmacologically inactive metabolites: M1 (hydrolyzed four-membered lactone ring) and M3 (M1 with split N-formyl leucine residue). Withdrawal The main way of elimination is the excretion through the intestines - about 97% of the accepted dose of the drug, of which 83% is unchanged. Cumulative kidney excretion of all substances structurally related to orlistat is less than 2% of the dose of the drug. The time of complete elimination is 3-5 days. Orlistat and metabolites can be excreted with bile.
Indications
Orsoten is indicated for the continued treatment of obese patients with a body mass index (BMI) of> 30 kg / m, or patients with overweight (BMI> 28 kg / m), including those with associated with obesity risk factors, in combination with moderate low-calorie diet. Orsoten can be prescribed in combination with hypoglycemic drugs and / or a moderately low-calorie diet in patients with type 2 diabetes with overweight or obesity.
Contraindications
Chronic malabsorption syndrome; cholestasis; hypersensitivity to orlistat or any other component of the drug; pregnancy and breastfeeding: children under 18 years of age (efficacy and safety have not been studied)
Precautionary measures
Before the appointment of orlistat should eliminate the organic cause of obesity, such as hypothyroidism. At the time of treatment recommend a balanced low-calorie diet, in which fats provide no more than 30% of calories. The likelihood of side effects from the gastrointestinal tract increases with a high content of fat in the diet (more than 30% of daily calories). Daily intake of fats, carbohydrates and proteins should be distributed between the three main meals. Since orlistat reduces the absorption of certain fat-soluble vitamins, patients must take multivitamin preparations that contain fat-soluble vitamins to ensure their adequate intake. In addition, the content of vitamin D and beta-carotene in obese patients may be lower than in non-obese people. Multivitamins should be taken 2 hours before or 2 hours after taking orlistat, for example, before bedtime. Reception of orlistat in doses exceeding 120 mg 3 times a day does not provide an additional effect. Patients taking both orlistat and cyclosporine simultaneously require more frequent monitoring of plasma cyclosporin. Patients who have not received prophylactic vitamin supplements have seen two or more consecutive visits to the doctor during the first and second years of treatment with orlistat. in the following percentage of cases (data in the placebo group are given in parentheses): vitamin A 2.2% (1%), vitamin D 12.0% (6.6%), vitamin E 5.8% (1%), beta -carotene 6.1% (1.7%).In some patients, urinary oxalate levels may increase with orlistat. As with other weight loss drugs, some groups of patients (for example, anorexia nervosa or bulimia nervosa) are likely to misuse orlistat. Orlistat induction may lose weight and improve metabolic control of diabetes, which will require lower doses of oral hypoglycemic agents (derivatives sulfonylurea, metformin, etc.) or insulin.
Use during pregnancy and lactation
According to the results of preclinical studies, teratogenicity and embryotoxicity were not observed when taking orlistat. Clinical data on the use of orlistat during pregnancy are not available, so do not prescribe the drug in this period. Since data on the use in the period of lactation are not available, orlistat should not be prescribed in the period of lactation.
Dosage and administration
The recommended single dose of orlistat is one 120 mg capsule, which is taken orally, with water, immediately before each main meal, during a meal, or no later than an hour after a meal. If a meal is missed, or if the food does not contain fat, then the intake of orlistat can be skipped. Doses of orlistat over 120 mg 3 times a day do not enhance its therapeutic effect. Duration of therapy no more than 2 years. Dose adjustment is not required for elderly patients or patients with impaired liver or kidney function.
Side effects
Adverse reactions were mainly observed on the part of the gastrointestinal tract and were due to an increased amount of fat in the feces. Commonly observed adverse reactions are mild and transient. The appearance of these reactions was observed at the initial stage of treatment during the first 3 months. (but no more than one case). With prolonged use of orlistat, the number of adverse events decreases. On the part of the digestive system: flatulence, accompanied by discharge from the rectum, urge to stool, fatty / oily stools, oily discharge from the rectum, loose stools, soft stools, fat in the feces (steatorrhea), pain / discomfort in the abdomen, more frequent bowel movements, pain / discomfort in the rectum, imperative urge to have a bowel movement, fecal incontinence, damage to the teeth and gums, hypoglycemia in patients with type 2 diabetes; very rarely - diverticulitis, cholelithiasis, hepatitis, possibly severe, elevated levels of liver transaminases and alkaline phosphatase.From the side of the central nervous system: headache, anxiety. Allergic reactions: itching, rash, urticaria, angioedema, bronchospasm, anaphylaxis; very rarely - bullous rash. Other: flu-like syndrome, fatigue, upper respiratory tract infections, urinary tract infections, dysmenorrhea.
Overdose
Cases of overdose are not described. The administration of a single dose of orlistat 800 mg or multiple doses up to 400 mg 3 times / day for 15 days was not accompanied by significant adverse reactions. In addition, the dose of 240 mg 3 times / day, prescribed to patients with obesity for 6 months, did not cause a significant increase in adverse reactions. In case of an overdose of orlistat, it is recommended to monitor the patient for 24 hours.
Interaction with other drugs
In patients receiving warfarin or other anticoagulants and orlistat. there may be a decrease in the level of prothrombin, an increase in the international normalization factor (INR), which leads to changes in hemostatic parameters. Interaction with amitriptyline, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, nifedipine GITS, sustained-release nifedipine, sibutramine, furosemide, captoprilum, hypotelemoleosylmoleoyl chloride, dehydroxylmoleoyl hypophenolol, frothymide, captoprilum, nyliphenol Increases the bioavailability and hypolipidemic effect of pravastatin, increasing its plasma concentration by 30%. A decrease in body weight can improve the metabolism in diabetic patients, as a result of which it is necessary to reduce the dose of oral hypoglycemic agents. Treatment with orlistat potentially disrupts the absorption of fat-soluble vitamins (A, D, E. K). If taking multivitamins is recommended, they should be taken no earlier than 2 hours after taking orlistat or before going to bed. With the simultaneous use of orlistat and cyclosporine, a decrease in plasma plasma levels of cyclosporine was noted, therefore it is recommended to determine the plasma levels of cyclosporine more frequently. In patients receiving amiodarone, clinical observation and monitoring of ECG should be carried out more thoroughly, since Cases of a decrease in the concentration level of amiodarone in the blood plasma
special instructions
Orlistat is effective for long-term control of body weight (weight loss, maintaining it at an appropriate level and preventing re-gaining body weight). Treatment with orlistat leads to an improvement in the profile of risk factors and diseases associated with obesity (including hypercholesterolemia, impaired glucose tolerance, hyperinsulinemia, arterial hypertension, type 2 diabetes mellitus), and a decrease in visceral fat. A decrease in body weight during treatment with orlistat may be accompanied by an improvement in the compensation of carbohydrate metabolism in patients with type 2 diabetes, which may reduce the dose of hypoglycemic drugs. To ensure adequate nutrition of patients, it is recommended to take multivitamin preparations. Patients should follow dietary guidelines. They should receive a balanced, moderately low-calorie diet, containing no more than 30% of calories in the form of fat. Daily fat intake should be divided into three main meals. The likelihood of adverse reactions from the gastrointestinal tract may increase if orlistat is taken on a diet rich in fats (for example, 2000 kcal / day,> 30% of daily calorie intake comes in the form of fat, which is approximately 67 g of fat). Patients should be aware that the more accurately they follow a diet (especially with regard to the amount of fat permitted), the less likely it is that adverse reactions will develop. A low-fat diet reduces the likelihood of adverse gastrointestinal reactions and helps patients monitor and regulate fat intake. If after 12 weeks of therapy there is no decrease in body weight by at least 5%, the use of orlistat should be discontinued.