Orlistat - instructions for use, doses, side effects, contraindications

hard gelatin capsules of light blue color. The size of capsules number 3. The contents of the capsules are white powder or slightly compacted agglomerates.

Pharmacotherapeutic group:Lipase inhibitor of the gastrointestinal tract.

ATX: & nbsp

A.08.A.B.01 Orlistat

Pharmacodynamics:

Orlistat is a specific inhibitor of long-acting gastrointestinal lipases. It acts in the lumen of the stomach and small intestine, forming a covalent bond with the active serine portion of the gastric and pancreatic lipases. The inactivated enzyme is not able to break down the food fats coming in the form of triglycerides, up to the absorbed free fatty acids and monoglycerides. Undivided triglycerides are not absorbed, in connection with which, 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 bloodstream. Increases fat concentration in fecal masses after 24-48 hours after administration. Provides effective control of body weight, reducing the proportion of fat.

In adults with a body mass index (BMI)> 28 kg / m² orlistat in a dose of 60 mg three times a day is effective in combination with a low-fat hypocaloric diet. In this case, the main weight loss occurs during the first 6 months of treatment. The decrease in body weight, caused by the use of orlistat at a dose of 60 mg three times a day, is accompanied by another beneficial effect: a decrease in the concentration of total cholesterol, LDL cholesterol, and a decrease in the waist circumference.

Pharmacokinetics:

Suction

Absorption is low. After 8 hours after ingestion of the therapeutic dose, the unchanged orlistat in blood plasma is practically not determined (concentration <5 ng / ml). Signs of cumulation are absent, which is consistent with the minimum absorption of the drug.

Distribution

The volume of distribution can not be established, since orlistat is practically not absorbed and does not have established systemic pharmacokinetics. Orlistat more than 99% associated with blood plasma proteins in vitro (mainly with lipoproteins and albumin). Orlistat in minimal amounts can penetrate into the red blood cells. Metabolism

Metabolism of orlistat is carried out, mainly, in the intestinal wall with the formation of pharmacologically inactive metabolites: M1 (four-membered hydrolyzed lactone ring) and M3 (M1 with a split residue N- formylleucine).

Excretion

The main way of excretion is the excretion through the intestine - approximately 97% of the dose, 83% of which is unchanged orlistat. Total excretion by the kidneys of all metabolites of orlistat is <2% of the accepted dose of orlistat. The time of complete excretion (through the intestine and kidneys) is 3-5 days. The ratio of pathways for orlistat in individuals with normal body weight and obesity was similar. Orlistat and metabolites can also be excreted with bile.

Indications:Reduction of excess body weight (BMI> 28 kg / m²) when used in conjunction with a moderately hypocaloric diet with a low fat content.

Contraindications:

- Hypersensitivity to any of the components of the drug;

- Syndrome of chronic malabsorption;

- Cholestasis;

- Concomitant therapy with warfarin or other oral anticoagulants;

- Concomitant therapy with cyclosporine;

- Pregnancy and lactation;

- Children under 18 years.

Pregnancy and lactation:

Preclinical studies did not reveal a teratogenic and embryotoxic effect of orlistat. However, due to the lack of clinical data on the use in pregnant women, orlistat contraindicated in pregnancy.

Since it is not known whether the orlistat in breast milk, it is contraindicated in the period of breastfeeding.

Dosing and Administration:

Inside, with water, at the recommended dose of 60 mg before each main meal, together with food or not later than one hour after ingestion. If food intake is skipped or food is fat-free, you can also skip orlistat. Within 24 hours, do not take more than 3 capsules of 60 mg.

If no weight loss occurs after 12 weeks of therapy, orlistat should be discontinued. Treatment should not exceed 6 months.

In elderly patients, patients with impaired liver and kidney function, dose adjustment is not required.

Orlistat should not be used in children and adolescents under 18 due to insufficient safety and efficacy data.

Side effects:

Adverse events were noted when taking orlistat mainly from the gastrointestinal tract and were driven by higher amounts of fat in the feces. With prolonged therapy with orlistat, the incidence of adverse events decreases.

The following side effects are given according to the following gradations of their frequency: very often (> 1/10); often (> 1/100, <1/10); sometimes (> 1/1 LLC, <1/100); rarely (> 1/10 LLC, <1/1 LLC) and very rarely (<1/10 LLC).

From the gastrointestinal tract. Often: oily discharge from the rectum; gases with a certain amount of detachable; imperative urges for defecation; steatorrhea; flatulence; unformed chair. Often: stomach ache; fecal incontinence; loose stools; increased frequency of stools.

Other. Often: anxiety.

The following side effects are reported in the postmarketing period (frequency unknown):

From the gastrointestinal tract: minor bleeding from the rectum; diverticulitis; pancreatitis.

From the liver and bile ducts: increased activity of "liver" transaminases and alkaline phosphatase, hepatitis, cholelithiasis.

Other: decrease in the concentration of prothrombin,

normalized ratio (INR) in patients taking orlistat together with anticoagulants; bullous rash; hypersensitivity reactions (pruritus, rash, hives, angioedema, bronchospasm and anaphylaxis); oxalate nephropathy.

Overdose:

In individuals with normal body weight and obesity, the administration of single doses of orlistat (800 mg) and multiple doses (up to 400 mg of orlistat 3 times a day for 15 days) did not cause undesirable effects. In addition, in patients with obesity, taking orlistat at a dose of 240 mg 3 times a day for 6 months was not accompanied by an increase in adverse events.

Most reports of cases of overdose of orlistat indicated the absence of adverse reactions, or unwanted reactions were similar to those observed with orlistat at recommended doses.

In case of a significant overdose of orlistat, it is recommended to observe the patient for 24 hours.According to preclinical and clinical studies, systemic effects associated with the lipaspptive properties of orlistat should be rapidly reversible.

Interaction:

With the simultaneous use of orlistat and cyclosporine, a decrease in the concentration of cyclosporine in the blood plasma is possible, and therefore it is necessary to monitor the content of cyclosporine in the blood plasma. The simultaneous use of orlistat and cyclosporine is contraindicated.

With the simultaneous use of orlistat with amiodarone, clinical observation and monitoring of the ECG is recommended, since it is possible to reduce the concentration of amiodarone in the blood plasma.

With the simultaneous administration of orlistat and warfarin or other anticoagulants, there may be a decrease in the concentration of prothrombin and an increase in INR, which leads to a change in haemostatic parameters. The simultaneous use of orlistat and warfarin and other oral anticoagulants is contraindicated.

Orlistat may reduce the absorption of fat-soluble vitamins A, D, E, K and beta-carotene. If the reception of multivitamins is indicated, they should be taken no earlier than 2 hours after taking orlistat or before bedtime.

Orlistat may reduce the absorption of antiepileptic drugs, which can lead to seizures.

Given the lack of studies of pharmacokinetic interaction, the co-administration of orlistat and acarbose should be avoided.

In some cases orlistat can indirectly reduce the bioavailability of oral contraceptives. In the case of severe diarrhea, the use of an additional contraceptive method is recommended.

When taking with sodium levothyroxine concurrently, in connection with a decrease in absorption of inorganic iodine and / or levothyroxine sodium, hypothyroidism and / or a decrease in the control of hypothyroidism may develop.

There was no drug interaction with amitriptyline, atorvastatin, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, phentermine, pravastatin, nifedipine, sibutramine and ethanol.

Special instructions:

Diet and exercise are important components of the slimming program. It is recommended to begin the diet program and physical exercises before the start of orlistat therapy. The patient should receive a moderately hypocaloric diet containing no more than 30% of calories in the form of fats (for example, at a caloric value of 2000 kcal / day the food should contain no more than 67 g of fat).Daily intake of fat should be distributed among the three main meals.

A diet low in fat reduces the likelihood of developing adverse events from the gastrointestinal tract.

Patients taking antiepileptic drugs should consult a doctor before starting to use orlistat, as it is possible to change the frequency and severity of seizures. In these cases, you can consider taking orlistat and antiepileptic drugs at different times.

By reducing body weight against the background of orlistat, it is possible to improve carbohydrate metabolism in patients with type 2 diabetes mellitus, and therefore it is necessary to consult a doctor and, if necessary, reduce the dose of hypoglycemic drugs.

Decreased body weight may be accompanied by a decrease in blood pressure and cholesterol concentration. Patients taking antihypertensive and hypolipidemic drugs should consult a physician before taking orlistat, and, if necessary, adjust the dose of these drugs.

If symptoms such as weakness, fatigue, fever, jaundice and darkening of the urine occur, you should consult your doctor to rule out liver damage.

Effect on the ability to drive transp. cf. and fur:

No adverse effect of orlistat on the ability to drive vehicles and mechanisms has been identified.

Form release / dosage:

Capsules 60 mg.

Packaging:

For 14 or 15 capsules in a foil blister Al /RVC / RVDFROM.

3 blisters of 14 capsules or 4 blisters of 15 capsules, or 6 blisters of 14 capsules, or 6 blisters of 15 capsules (42 or 60 or 84, or 90 capsules, respectively) along with the instructions for use are placed in a cardboard box.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-002322

Date of registration:09.12.2013

Expiration Date:09.12.2018

The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia

Manufacturer: & nbsp

AKRIKHIN HFK, JSC Russia

Information update date: & nbsp09.12.2013

Illustrated instructions

Instructions

Orlistat (Orlistat)