Orlistat-Akrikhin
Orlistat-Akrikhin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews Orlistat-Akrikhin
- 19. Price in pharmacies
Latin name: Orlistat-Akrikhin
ATX code: A08AB01
Active ingredient: orlistat (orlistat)
Producer: Polfarma S. A., Poland Pharmaceutical plant (Poland)
Description and photo update: 28.11.2018
Prices in pharmacies: from 737 rubles.
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Orlistat-Akrikhin is a lipid-lowering drug, an inhibitor of lipases of the gastrointestinal tract.
Release form and composition
The product is produced in the form of capsules: size No. 1, hard gelatinous, blue; the contents of the capsules are white powder or slightly compacted agglomerates (7 or 14 pcs. in a blister, in a cardboard box 3 blisters of 7 pcs., or 3 blisters of 14 pcs., or 6 blisters of 14 pcs. and instructions for use of Orlistat-Akrihin).
1 capsule contains:
- active substance: orlistat - 120 mg;
- additional components: sodium carboxymethyl starch, microcrystalline cellulose, sodium lauryl sulfate, colloidal anhydrous silicon dioxide;
- capsule shell: titanium dioxide (E171), gelatin, indigo carmine (E132).
Pharmacological properties
Pharmacodynamics
Orlistat belongs to long-acting specific inhibitors of gastrointestinal lipases. This substance manifests its effect in the lumen of the stomach and small intestine by forming a covalent bond with the active serine center of gastric and pancreatic lipases. As a result of the influence of a lipid-lowering agent, the inactivated enzyme loses its ability to break down fats in the form of triglycerides (TG) entering with food to monoglycerides and absorbed free fatty acids. Since undigested TGs are not absorbed from the gastrointestinal tract (GIT), fewer calories are supplied to the body, and as a result, body weight is reduced. Thus, the therapeutic effect of the drug is carried out without its absorption into the systemic circulation. Due to the activity of orlistat, the concentration of fat in the feces increases 24–48 hours after oral administration of the drug. Leading to a decrease in fat depot, Orlistat-Akrikhin ensures effective control of body weight.
In clinical trials involving obese patients, the group of patients treated with orlistat showed more pronounced body weight loss compared to patients who were only on diet therapy. Weight loss was observed already within the first 2 weeks after the start of taking Orlistat-Akrikhin and further within 6–12 months, even if there was a negative response to diet therapy.
A statistically significant significant improvement in the profile of obesity-related metabolic risk factors was recorded over two years. In addition, there was a significant reduction in body fat deposits when compared with the placebo group. Orlistat has also been shown to be effective when used to prevent re-gaining body weight. Approximately half of the patients showed no more than 25% weight gain of the weight lost, and the other half of the patients in the study did not regain weight, or even recorded a subsequent weight loss.
In clinical studies that lasted from 6 months to 1 year, patients with overweight or obesity and type 2 diabetes when using orlistat experienced a more significant body weight loss compared to patients who were only on diet therapy. Weight loss occurred mainly as a result of a decrease in the deposition of fat in the body. It should be noted that in the patients involved in the study, before the start of the study, despite the intake of antidiabetic drugs, insufficient glycemic control was often noted. With orlistat, these patients were found to have significantly improved glycemic control. Also, during the use of Orlistat-Akrikhin, there was a decrease in doses of antidiabetic agents, insulin concentration, as well as a decrease in insulin resistance.
According to research data, which lasted 4 years, it was found that with orlistat therapy, the threat of type 2 diabetes mellitus was significantly reduced - by an average of 37% compared with placebo. This threat was reduced by about 45% in patients with an initial impairment of glucose tolerance. The orlistat group experienced a greater reduction in body weight compared to the placebo group, and in addition, a significant improvement in the metabolic risk factor profile. The achieved new level of body weight was maintained throughout the 4 years of the study.
In obese adolescents, a 1-year study with orlistat showed a decrease in body mass index (BMI), as well as a decrease in body fat and waist and hip circumference compared with placebo. Also, during the period of taking Orlistat-Akrikhin in adolescents, there was a significant decrease in diastolic blood pressure (BP) compared with those who received placebo.
Pharmacokinetics
The drug is characterized by low absorption. 8 hours after oral administration, unchanged orlistat is not detected in plasma, since its concentration is not more than 5 ng / ml. No signs of accumulation of the active substance were found, which indicates an extremely low degree of its absorption.
It is impossible to establish the volume of distribution, since the agent is practically not absorbed. In vitro, it binds to plasma proteins almost completely (by 99%), mainly with lipoproteins and albumin. In minimal quantities, the agent is able to penetrate into erythrocytes. The metabolic transformation of orlistat occurs mainly in the intestinal wall with the formation of two metabolites that do not exhibit pharmacological activity - M1 (four-membered hydrolyzed lactone ring) and M3 (M1 with a cleaved N-formylleucine residue).
The substance is excreted mainly through the intestines - about 97% of the dose taken, from this amount in unchanged form - about 83%. The total excretion of all metabolites of orlistat by the kidneys does not exceed 2% of the dose taken. The period of complete elimination of the substance with feces and urine is 3-5 days. The routes of elimination of orlistat in patients with normal body weight and obesity are similar. Also, the active substance and its metabolites can be excreted in the bile.
Indications for use
Orlistat-Akrikhin is recommended for long-term therapy of obese patients with a BMI ≥ 30 kg / m2 or overweight patients with a BMI ≥ 28 kg / m2, who have obesity-related risk factors, while following a moderately restricted low-calorie diet.
Orlistat-Akrihin is also indicated for use in patients with type 2 diabetes mellitus with overweight or obesity in combination with a moderately limited hypocaloric diet and / or taking hypoglycemic drugs (insulin and / or sulfonylurea derivatives, metformin).
Contraindications
Absolute:
- cholestasis;
- chronic malabsorption syndrome;
- age up to 12 years;
- pregnancy and lactation;
- hypersensitivity to any of the constituents of Orlistat-Akrikhin.
With extreme caution, treatment with the drug should be carried out with the concomitant administration of cyclosporine, warfarin or other oral anticoagulants.
Orlistat-Akrikhin, instructions for use: method and dosage
Orlistat-Akrikhin is used orally with each main meal (during meals, immediately before meals or not later than 1 hour after meals). The capsules should be taken with water.
For prolonged therapy, obese patients (BMI ≥ 30 kg / m2) or overweight (BMI ≥ 28 kg / m2) with obesity-related risk factors, aged 12 years and older, on a moderately restricted low-calorie diet should take Orlistat-Akrikhin at a dose of 120 mg orlistat (1 capsule) 3 times a day.
When prescribing the drug to adult patients with type 2 diabetes mellitus with obesity or overweight with combined intake of hypoglycemic agents and / or following a moderately limited hypocaloric diet, it is recommended to take 120 mg of orlistat (1 capsule) 3 times a day.
It is allowed to skip the next intake of the capsule if the food does not contain fat or the meal was skipped.
During the period of therapy, it is required to adhere to a balanced, moderately limited hypocaloric diet containing no more than 30% of calories in the form of fats; it is also recommended to include fruits and vegetables in the daily diet. The total amount of carbohydrates, fats and proteins consumed per day must be divided into three main doses.
When using orlistat in doses exceeding 3 capsules per day, there was no increase in the therapeutic effect.
A study of the safety and efficacy of taking Orlistat-Akrikhin in patients with functional impairment of the liver and / or kidneys has not been conducted.
Side effects
The undesirable effects caused by taking orlistat appeared in most cases from the gastrointestinal tract and were associated with the pharmacological action of a drug that blocks the absorption of food fats.
During the period of taking Orlistat-Akrikhin, the following violations may occur:
- metabolism and nutritional disorders: very often - hypoglycemia;
- infectious and parasitic lesions: very often - flu;
- nervous system: very often - headache;
- mental disorders: often - anxiety;
- respiratory system, chest and mediastinal organs: very often - upper respiratory tract infections; often - lower respiratory tract infections;
- genitals and mammary gland: often - irregular menstruation;
- kidneys and urinary tract: often - urinary tract infections;
- Gastrointestinal tract: very often - oily discharge from the rectum, discomfort / pain in the abdomen, gas with a certain amount of discharge, flatulence, loose stools, urge to defecate, increased frequency of bowel movements, steatorrhea; often - discomfort / pain in the rectum, fecal incontinence, soft stools, bloating, tooth damage, gum disease;
- general disorders: often - weakness.
The nature and frequency of side effects in patients with type 2 diabetes mellitus were similar to those in patients without diabetes mellitus, overweight and obesity.
During treatment, the incidence of gastrointestinal adverse reactions increased with an increase in the amount of fat in food intake. It is possible to eliminate or reduce the severity of these disorders by following a low-fat diet. In most cases, the above effects were transient and mild, their appearance was noted mainly in the first 3 months of therapy and, as a rule, no more than one episode. Against the background of prolonged use of Orlistat-Akrikhin, the incidence of these phenomena decreased.
Overdose
Cases of drug overdose are not described.
When taking single (800 mg) and multiple doses (for 15 days up to 400 mg three times a day) of orlistat in persons with normal body weight / obesity, there were no undesirable effects. When taking orlistat in obese patients for 6 months at a dose of 240 mg three times a day, no increase in the incidence of adverse reactions was observed.
In case of a significant overdose of Orlistat-Akrikhin, the patient should be observed for 24 hours. According to clinical and preclinical studies, systemic effects associated with the lipase-inhibiting properties of orlistat should be rapidly reversible.
special instructions
Orlistat-Akrikhin is recommended for long-term control of body weight (including reducing body weight, maintaining it at the desired achieved level and preventing re-weight gain).
In patients with type 2 diabetes mellitus, as a result of weight loss when using the drug, the likelihood of an improvement in carbohydrate metabolism increases, against which a decrease in the dose of hypoglycemic drugs may be required.
Orlistat-Akrikhin therapy should not last more than 2 years. If after 12 weeks after the start of the course it was not possible to achieve a weight loss of at least 5%, the use of the drug must be discontinued.
If symptoms such as fatigue, weakness, fever, dark urine and jaundice occur during therapy, it is necessary to seek the advice of your doctor in order to exclude possible liver dysfunctions.
During the period of drug treatment, mainly in patients with concomitant chronic kidney damage and / or dehydration, hyperoxaluria and oxalate nephropathy may develop, which in some cases can lead to renal failure.
Influence on the ability to drive vehicles and complex mechanisms
Orlistat-Akrikhin does not adversely affect the ability to drive vehicles or other complex mechanisms.
Application during pregnancy and lactation
During pregnancy and lactation, drug treatment is contraindicated.
Pediatric use
The efficacy and safety of using orlistat in children under 12 years of age have not been studied, and therefore, taking Orlistat-Akrikhin in patients of this age group is contraindicated.
With impaired renal function
The efficacy and safety of drug treatment in persons with impaired renal function have not been studied.
In the presence of impaired renal function, there is no need to change the dose of Orlistat-Akrikhin.
For violations of liver function
The efficacy and safety of drug treatment in persons with impaired hepatic function have not been studied.
With existing violations of the liver, it is not required to change the dose of Orlistat-Akrikhin.
The presence of cholestasis is a contraindication for taking the drug.
Use in the elderly
The efficacy and safety of drug treatment in the elderly have not been studied. There is no need to adjust the dose in elderly patients.
Drug interactions
- amiodarone - there may be a decrease in the level of this substance in the blood plasma, clinical observation and monitoring of ECG indicators should be carried out;
- antiepileptic drugs - the absorption of these drugs decreases, which can cause seizures;
- cyclosporine - the level of its content in the blood plasma decreases, which may lead to a weakening of the immunosuppressive efficacy of the drug; this combination is not recommended, if necessary, its implementation requires frequent monitoring of the plasma concentration of cyclosporine, both with concomitant administration of orlistat, and after its completion;
- warfarin and other anticoagulants - a decrease in the concentration of prothrombin and an increase in the international normalized ratio (INR) is possible, which can lead to a change in hemostatic parameters; with this combination, it is necessary to monitor INR indicators;
- fat-soluble vitamins A, D, E, K and beta-carotene - absorption of these substances is weakened; with combined use, they must be taken before bedtime or no earlier than 2 hours after taking orlistat;
- acarbose - it is recommended to avoid combined use due to the lack of pharmacokinetic interaction studies;
- levothyroxine sodium - hypothyroidism may develop and / or a decrease in its control due to a decrease in the absorption of levothyroxine sodium and / or inorganic iodine;
- oral contraceptives - the risk of a decrease in the contraceptive effect is aggravated, which in some cases increases the likelihood of an unplanned pregnancy; you should resort to additional methods of contraception, including in the event of severe diarrhea;
- antiretroviral drugs for the treatment of the human immunodeficiency virus (HIV), antipsychotics (including lithium preparations), antidepressants, benzodiazepines - the therapeutic effect of these drugs may be weakened; starting therapy with orlistat in such patients should be after a careful assessment of the expected benefit from this treatment and the possible risk;
- fibrates, atorvastatin, digoxin, amitriptyline, biguanides, losartan, pravastatin, fluoxetine, phentermine, sibutramine, nifedipine, phenytoin, ethanol - no interaction with these drugs was observed.
Analogs
Orlistat-Akrikhin analogs are: Orsoten, Listata, Orsoten Slim, Orlistat, Xenical, Orliksen 120, Orlistat Canon, Alli, Ksenalten Light, Xsenalten Logo.
Terms and conditions of storage
Store in its original packaging in a place protected from light and out of the reach of children, at a temperature not exceeding 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Orlistat-Akrihin
Reviews about Orlistat-Akrikhin are very diverse. Many patients respond positively to the drug, reporting that thanks to its action, they were able to lose about 5 kg of excess weight in 3 months. After that, body weight steadily decreased, but not so quickly. In patients with a slower metabolism, the process of weight loss was slightly longer. At the same time, patients note that in order to achieve effective treatment results, it is necessary to adjust nutrition and habitual lifestyle - adhere to an appropriate diet that allows you to reduce the number of calories in the diet, perform regular feasible physical activity, move as much as possible, and so on.
The disadvantages of Orlistat-Akrikhin include, in most cases, the occurrence of side reactions in the form of flatulence, loose stools, diarrhea, and an urge to defecate. But, as a rule, these violations are noted during the first months of the course of therapy and then go away on their own. Rarely are reviews that indicate a very weak effect of drug treatment.
Price for Orlistat-Akrikhin in pharmacies
The price for Orlistat-Akrikhin (capsules of 120 mg) can be: 950-1250 rubles for 42 pcs., 1850-2050 rubles for 84 pcs. packaged.
Orlistat-Akrikhin: prices in online pharmacies
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Drug name Price Pharmacy |
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Orlistat-Akrikhin 120 mg capsules 42 pcs. 737 RUB Buy |
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Orlistat-Akrikhin capsules 120mg 42 pcs. 1196 RUB Buy |
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Orlistat-Akrikhin 120 mg capsules 84 pcs. 1641 RUB Buy |
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Orlistat-Akrihin capsules 120mg 84 pcs. 1973 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
