In combination with a moderately low-calorie diet in the treatment of obese patients, with a body mass index (BMI) equal to or greater than 30 kg / m2 pc. or overweight patients - with a body mass index (BMI) equal to or greater than 28 kg / m2 pc. with simultaneously occurring risk factors. Treatment with orlistat should be discontinued after 12 weeks if patients were unable to reduce weight by at least 5% relative to body weight at the start of treatment.
Composition:
1 capsule contains 120 mg orlistat.
Action:
Orlistat is a potent, specific and long-acting inhibitor of lipases produced in the gastrointestinal tract. It works in the light of the stomach and small intestine after formation of binding to the active serine site of gastric and pancreatic lipase. The enzyme-depleted enzyme does not hydrolyse the fat used in food in the form of triglycerides, absorbing free fatty acids and monoglycerides. The effect of orlistat on increasing fats in stool occurs already 24-48 h after drug application. After discontinuation of the drug, the fat content in the stool returns to the value from before the treatment period after 48-72 hours. The orlistat absorption level is minimal. It is very rarely detected in plasma, and the concentrations achieved are very low, with no evidence of accumulation.In vitro Orlistat binds to plasma proteins in over 99% (mainly with lipoproteins and albumin); minimally penetrates into erythrocytes. It is probably mainly metabolised within the walls of the digestive tract. There were 2 major metabolites with minimal lipase inhibitory activity: M1 (hydrolyzed 4-membered lactone ring) and M3 (M1 with attached N-formyloleucine molecule), representing approximately 42% of total plasma concentration. In people with normal body weight and in obese, elimination of the unabsorbed medication is the main route of elimination. Approx. 97% of the administered dose was excreted in the faeces, 83% as unchanged orlistat. The total elimination time of orlistat (with faeces and urine) is 3-5 days. Orlistat and its metabolites M1 and M3 are excreted in bile.
Contraindications:
Hypersensitivity to orlistat or other ingredients of the preparation. Chronic malabsorption syndrome. Cholestasis. Breastfeeding period.
Precautions:
In clinical studies with orlistat treatment, weight loss was less pronounced in patients with type 2 diabetes compared to non-diabetic patients. In diabetic patients, close monitoring of antidiabetic treatment may be necessary during treatment with orlistat. Co-administration of cyclosporin is not recommended. In patients treated concomitantly with antidiabetic agents, coagulation parameters should be monitored. Orlistat may affect the instability of antiepileptic treatment in patients with epilepsy, by lowering the absorption of antiepileptic drugs, which may lead to epileptic seizures. Caution should be used in patients with renal insufficiency and / or with reduced volume of blood because the use of orlistat may rarely be associated with excessive urinary excretion of oxalate and oxalate nephropathy. In case of severe diarrhea, it is recommended to use additional contraception. In the case of severe, persistent rectal bleeding, detailed diagnostics are recommended. In rare cases, thyroid insufficiency and / or reduced control of hypothyroidism may occur during treatment. the mechanism of this phenomenon may consist in a reduced absorption of Iodine salt and / or levothyroxine. Orlistat may reduce absorption and negatively affect the effectiveness of HIV antiretrovirals. The efficacy of treatment with orlistat has not been studied in patients with impaired hepatic and / or renal function, in children and in elderly patients. Orlistat is not intended for the treatment of children.
Pregnancy and lactation:
There are no studies on the effects of orlistat on pregnancy - caution should be exercised when prescribing pregnant women to orlistat. The drug is contraindicated during breastfeeding.
Side effects:
The possibility of gastrointestinal side effects may increase if orlistat is used together with a high fat diet (eg in the case of a diet with a caloric value of 2000 kcal / day, where more than 30% of energy contains more than 67 g of fat). Very common: headache, upper respiratory tract infections, abdominal pain, discomfort, rectal fat stain, exudate gas, stool pressure, fatty, oily stools, flatulence, liquid stools, fatty spotting, more frequent bowel movements, hypoglycaemia , flu. Common: lower respiratory tract infections, anal pain, discomfort, loose stools, fecal incontinence, spreading sensation, tooth disease, gum disease, urinary tract infection, fatigue, irregular menstruation, anxiety. In addition, the following adverse reactions were observed after the marketing of the drug: increased hepatic transaminases and alkaline phosphatase, decreased prothrombin activity, INR elevation and anticoagulant disorder, rectal bleeding, diverticula, pancreatitis, blisters on the skin, hypersensitivity reactions (eg pruritus , rash, urticaria, angioneurotic edema, bronchospasm, anaphylaxis), cholelithiasis, severe hepatitis (reports of fatal cases or requiring liver transplantation), oxalate nephropathy (may lead to renal failure).
Dosage:
Orally. Adults: the recommended dose is 120 mg (1 capsule) immediately before, during or within 1 h after ingestion of each main meal and with water. If the patient does not eat, or if the meal does not contain fat, the dose should be skipped. A dose greater than 120 mg three times a day does not lead to additional benefits.
(C)
