Orlimax - instructions for use, dose, side effects, contraindications

cellulose microcrystalline - 57,10; sodium carboxymethyl starch - 41.50; silicon dioxide colloidal anhydrous - 9,10; sodium lauryl sulfate - 2.30. shell capsules: hard gelatin capsule number 1: gelatin - 75.14; titanium dioxide (E171) - 0.76; indigo carmine (E132) - 0.10.

Description:hard gelatin capsules in blue. Size of capsules №1. The contents of the capsules are white powder or slightly compacted agglomerates.

Pharmacotherapeutic group:an inhibitor of the 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 is not able to break down the food fats coming in the form of triglycerides, up to the absorbed free fatty acids and monoglycerides. Undisintegrated triglycerides are not absorbed, and therefore 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 the concentration of fat in the stool after 24-48 hours after ingestion. Provides effective control of body weight, reduction of fat depot.

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:

Long-term therapy of patients with obesity (body mass index> 30 kg / m²) or patients with overweight (body mass index> 28 kg / m²), who are associated with obesity risk factors, in combination with a moderately hypocaloric diet.

Orlimax can be prescribed in combination with hypoglycemic drugs and / or a moderately low-calorie diet for patients with type 2 diabetes mellitus with excessive body weight or obesity.

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 120 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. Doses of orlistat, exceeding 120 mg 3 times a day, do not enhance its therapeutic effect.

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

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 (> 1/1 000, <1/100); rarely (> 1/10 000, <1/1 000) and very rarely (<1/10 000).

From the gastrointestinal tract. Often: pain / discomfort in the abdomen; oily discharge from the rectum; flatulence and the evolution of gases; imperative urges for defecation; steatorrhea; loose stools; increased frequency of stools; Often: a soft chair; fecal incontinence; bloating; damage to teeth and gums.

Other. Often: headache; upper respiratory tract infection; hypoglycemia in patients with type 2 diabetes mellitus; flu; Often: urinary tract infections; weakness; violation of the menstrual cycle; anxiety.

Below are the side effects registered in the postmarketing period.

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

Overdose:

Cases of overdose are not described.

In individuals with normal body weight and obesity, the administration of single (800 mg) and multiple doses of orlistat (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 three times a day for 6 months was not accompanied by an increase in adverse events.

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:

Orlistat is used for long-term monitoring of body weight (reduction in body weight, maintaining it at an appropriate level and preventing repeated weight gain).

By reducing body weight against the background of taking orlistat, it is possible to improve carbohydrate metabolism in patients with type 2 diabetes that can reduce the dose of hypoglycemic drugs.

The patient should be on a balanced moderately low-calorie diet, containing no more than 30% of calories in the form of fats. It is recommended that such a diet is rich in fruits and vegetables. 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. If after 12 weeks of therapy there was no decrease in body weight, at least 5%, orlistat should be stopped.

Treatment should not last more than 2 years.

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

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 120 mg.

Packaging:

7 or 14 capsules in a foil blister AI/RVC / RVDFROM.

3 blisters for 7, 14 capsules or 6 blisters for 14 capsules together with instructions for use in a cardboard box.

Storage conditions:

In a dry, the dark 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:On prescription

Registration number:LP-001455

Date of registration:25.01.2012

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

Manufacturer: & nbsp

AKRIKHIN HFK, JSC Russia

Information update date: & nbsp25.01.2012

Illustrated instructions

Instructions

Orlimax (Orlimax)