Description
Listat Pharmacodynamics
Orlistat is a potent, specific and reversible inhibitor of gastrointestinal lipases, with long-lasting action. Its therapeutic effect is carried out in the lumen of the stomach and small intestine and consists in formation of a covalent bond with the active serine site of gastric and pancreatic lipases.
The inactivated enzyme loses its ability to break down food fats that come in the form of triglycerides into absorbable free fatty acids and monoglycerides. Since unchecked 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 fecal fat content, the action of orlistat starts 24-48 hours after intake. After withdrawal of orlistat, the fecal fat content usually returns to the pre-therapy level in 48-72 hours.
Indications
Long-term therapy in obese patients with a body mass index (BMI) of 30 kg/m2 or overweight patients with a BMI of 28 kg/m2 or more, including those with obesity-related risk factors, in combination with a moderately hypocaloric diet.
In combination with hypoglycemic agents (metformin, sulfonylurea derivatives and/or insulin) and/or moderately hypocaloric diet in patients with type 2 diabetes mellitus with excess body weight or obesity.
Contraindications
Hypersensitivity to orlistat or any other drug components; chronic malabsorption syndrome; cholestasis; pregnancy, breast-feeding period; children under 12 years of age.
Pregnancy and lactation:
No teratogenic and embryotoxic effects of orlistat were observed in animal reproductive toxicity studies. In the absence of teratogenic effects in animals, similar effects in humans are not expected. Since there are no clinical data on the use of orlistat during pregnancy, the use of Listat in pregnant women is contraindicated.
Since there is no data on excretion of orlistat with breast milk, application of Listat during breast feeding is contraindicated.
Dosage and administration method
- Orally with water.
- Treatment of patients with obesity at BMI of 30 kg/m2 or overweight patients at BMI of 28 kg/m2 or more, including those with obesity-associated risk factors, in combination with a moderately low-calorie diet
- Adults and children over 12 years of age
The recommended dose of Listat is 1 tablet (120 mg) with each main meal (with a meal or at least 1 hour after a meal). - In combination with hypoglycemic agents (metformin, sulfonylurea derivatives and/or insulin) and/or a moderately hypocaloric diet in patients with type 2 diabetes mellitus with excessive body weight or obesity
- Adults
The recommended dose of Listat is 1 tablet (120 mg) with each main meal (with a meal or at least 1 hour after a meal). - If a meal is skipped or if the food does not contain fat, the drug Listat may also be skipped.
- The drug Listat should be taken in conjunction with a balanced, moderately hypocaloric diet containing not more than 30% of calories in the form of fat. The daily intake of fats, carbohydrates and proteins should be distributed between the 3 main meals.
- Increasing the dose of the drug Lystat above the recommended (120 mg 3 times a day) does not lead to increase in its therapeutic effect.
- Efficacy and safety of Listat in patients with hepatic and/or renal dysfunction, as well as in elderly patients and children under 12 years old have not been studied.
