Orlistat Mini - instructions for use, dose, side effects, contraindications

Opaprai II blue (85F30720) 34.8 mg (polyvinyl alcohol 40.00%, titanium dioxide 21.40%, macrogol 3350-20.20%, talc 14.80%, indigocarmine 3.50%, lacquer aluminum quinoline yellow-0.10%).

Rip off silvery (63F97546) 5.2 mg (polyvinyl alcohol 47.03%, talc 27.00%, macrogol 3350 13.27%, pearlescent pigment 10.00%, polysorbate 80 80% 2.70% ).

Description:The tablets are oval, biconcave, covered with a film shell of light blue color with pearlescent effect, with a risk on one side and engraving "f" - another. On the cross section - the core is white or almost white.

Pharmacotherapeutic group:Inhibitor of gastrointestinal tract lipases

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 loses the ability to break down food fats that act as triglycerides, up to 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.

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.

The action of orlistat leads to an increase in the fat content in feces after 24-48 hours after taking the drug. After the drug is withdrawn, the fat content in the stools usually returns to the initial level after 48-72 hours.

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-formleleucine).

Excretion

About 97% of the administered dose is excreted through the intestine, 83%) of this amount - in unchanged form. The excretion of orlistat and its metabolites by the kidneys is less than 2% of the dose taken. The drug is completely eliminated after 3-5 days. The excretion of orlistat in individuals with normal body weight and obese patients is similar.

Indications:

Reduction of excess body weight (body mass index 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;

- simultaneous use with indirect anticoagulants (warfarin) or other oral anticoagulants;

- simultaneous application with cyclosporine;

- period of pregnancy and lactation;

- children's age till 18 years.

Pregnancy and lactation:

In connection with the lack of clinical data on the use in pregnant women, orlistat contraindicated in pregnancy.

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

Dosing and Administration:

The drug is taken orally. The recommended dose is 60 mg 3 times a day with each main meal in combination with a moderately hypocaloric diet with a low fat content. The tablet should be taken immediately before meals, during meals or no later than 1 hour after meals, washed down with water. If food intake is missed or food is fat-free, Orlistat Mini should be taken.

During the day you can take no more than 3 tablets of 60 mg.

Treatment is recommended not more than 6 months. If after 12 weeks of therapy there is no decrease in body weight (ie, a decrease in body weight is less than 5% of the baseline), a doctor's consultation is needed to resolve the issue of continued use of the drug.

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

Orlistat Mini is not recommended for use in children and adolescents under 18 years due to insufficient safety and efficacy data.

Side effects:

Adverse events with orlistat are observed, mainly, from the gastrointestinal tract and are caused by the pharmacological action of the drug.

Side effects recorded during clinical trials.

The frequency of side effects is as follows: Often (≥ 1/10); often (≥ 1/100, <1/10); infrequently (≥ 1/1 000, <1/100); rarely (≥ 1/10 000, <1/1 000) and very rarely (<1/10 000), including individual messages.

From the gastrointestinal tract. Very often: oily discharge from the rectum; the escaping of gases with a certain amount of detachable, imperative desires for defecation, steatorrhea. Often: abdominal pain, fecal incontinence, loose stools; increased frequency of stools.

Side effects recorded in the postmarketing period (frequency unknown).

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

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

From the skin and subcutaneous tissue: Bullous rash.

From the immune system: hypersensitivity reactions (pruritus, rash, hives, angioedema, bronchospasm and anaphylaxis).

Other: a decrease in the prothrombin concentration, an increase in the International Normalized Ratio (INR) in patients taking orlistat together with indirect anticoagulants.

Overdose:

In the application of orlistat 800 mg once and at a dose of up to 400 mg 3 times daily for 15 days, both in individuals with normal body weight and in obese patients, no significant adverse events have been identified. When using orlistat at a dose of 240 mg 3 times a day for 6 months in patients with obesity, an increase in dose-related side effects was not observed.

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

In the event of a significant overdose of orlistat, it is recommended that the patient be monitored for 24 hours. According to preclinical and clinical studies, the systemic effects associated with the lipase-inhibiting 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, in connection with which it is necessary to monitor the content of cyclosporine in the blood plasma. Simultaneous use of the drug Orlistat Mini and cyclosporine is contraindicated.

With the simultaneous use of orlistat with amiodarone, a decrease in the concentration of amiodarone in the blood plasma is possible. The clinical significance of this effect is not clear. With the simultaneous administration of orlistat and warfarin or other oral anticoagulants, a decrease in prothrombin concentration and an increase in INR may occur. Simultaneous use of the drug Orlistat Mini and warfarin or 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.

Because of the lack of studies of pharmacokinetic interaction, joint use of orlistat and acarbose is not recommended.

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 programs to reduce body weight.It is recommended to start the diet program and physical exercises before the start of therapy with Orlistat Mini. 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 the drug Orlistat Mini, since 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.

Patients with kidney disease should consult with a physician, since possibly the development of hyperoxaluria and nephropathy.

By reducing body weight against the background of taking the drug Orlistat Mini, it is possible to improve the carbohydrate metabolism in patients with type 2 diabetes mellitus, in connection with which it is necessary to consult the attending physician and, if necessary, to 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:

Orlistat does not affect the ability to drive vehicles and mechanisms.

Form release / dosage:

Film-coated tablets are 60 mg.

Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

On 20 tablets in a glass jar for storage of medicines of type BTS with a triangular aureole, ukuporennuju a cover of the polyethylene pulled. Each jar or 1, 2, 3, 6, and 9 contour cell packs, together with instructions for medical use, are placed in a pack of cardboard boxes.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 of the year.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Obsolete name of the trade product: & nbspListata Mini

Date renamed: & nbsp20.11.15

Registration number:LP-002353

Date of registration:28.01.2014 / 07.04.2017

Expiration Date:28.01.2019

The owner of the registration certificate:IZVARINO PHARMA, LLC IZVARINO PHARMA, LLC Russia

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Representation: & nbspPROMO-MED LLC PROMO-MED LLC Russia

Information update date: & nbsp11.04.2018

Illustrated instructions

Instructions

Orlistat Mini (Orlistat Mini)