Orsoten - Instructions For Use Of The Drug, Reviews, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Orsoten

Orsoten: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Orsoten

ATX code: A08AB01

Active ingredient: orlistat (orlistat)

Manufacturer: KRKA-RUS (Russia)

Description and photo updated: 2018-26-11

Prices in pharmacies: from 492 rubles.

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Orsoten is a drug for the treatment of obesity that has an inhibitory effect on gastrointestinal lipases.

Release form and composition

Orsoten is produced in the form of capsules: from white with a yellow tint to white; contents of capsules - microgranules or a mixture of microgranules and powder, almost white or white, possibly the presence of caked agglomerates that easily crumble when pressed (7 pieces in a blister strip, 3, 6 or 12 packs in a cardboard box; 21 pieces in a contour cell packaging, 1, 2 or 4 packages in a cardboard box).

Composition for 1 capsule:

• active substance: orsoten semi-finished granules * - 225.6 mg (equivalent to the active substance orlistat in an amount of 120 mg);
• additional component: microcrystalline cellulose;
• capsule cap and body: hypromellose, water, titanium dioxide (E171).

* 100 mg of semi-finished granules contain: orlistat - 53.1915 mg, microcrystalline cellulose - 46.8085 mg.

Pharmacological properties

Pharmacodynamics

Orlistat is a specific, reversible inhibitor of gastrointestinal lipases with a long-lasting effect. The substance has a therapeutic effect in the lumen of the stomach and small intestine through covalent binding to the active serine residue of gastric and pancreatic lipases. As a result of inactivation, the enzyme cannot break down fats from food in the form of triglycerides, as well as monoglycerides and absorbed free fatty acids. Thanks to the action of orlistat, the undigested triglycerides are not absorbed from the digestive tract, fewer calories enter the body and, as a result, the body weight decreases. The therapeutic effect of Orsoten is carried out without systemic absorption of orlistat.

After 24–48 hours after taking the drug, the fat content in the feces increases, and after stopping the use of the drug - after 48–72 hours - it returns to the initial level.

In the course of clinical studies, obese patients treated with Orsoten showed a more pronounced loss of body weight compared to patients who were prescribed diet therapy. The decrease in body weight was noted already within the first 2 weeks after the start of the course and lasted for 6-12 months, even in those who did not respond to diet therapy. Within 2 years, there was a statistically significant improvement in the profile of metabolic risk factors associated with obesity. In addition, there was a marked reduction in body fat deposits compared to placebo. The drug has also been shown to be effective when used to prevent re-gain in body weight. On average, half of the patients showed a weight gain of no more than 25% of the weight lost,and the other half of these patients did not gain or even experienced further weight loss.

According to the results of clinical studies carried out over 6-12 months, obese or overweight patients with type 2 diabetes mellitus experienced more significant weight loss when compared with patients who were only on diet therapy. The loss of body weight was mainly due to a decrease in body fat. It should be noted that, despite the use of antidiabetic drugs, patients often had insufficient glycemic control before the study began. However, significant improvement in glycemic control was achieved with orlistat. In addition, in patients with type 2 diabetes mellitus during treatment with Orsoten, it was noted the possibility or need to reduce the doses of hypoglycemic drugs (for example, sulfonylurea derivatives),a decrease in plasma insulin levels and a decrease in insulin resistance were also observed.

In a clinical study lasting 4 years, it was demonstrated that orlistat significantly reduces the risk of developing type 2 diabetes mellitus - by about 37% compared to taking a placebo. In the presence of an initial impairment of glucose tolerance, this threat decreased by about 45%.

The orlistat group experienced more significant weight loss compared to the placebo group. The new level of body weight was maintained throughout the 4 years of the study period. The patients treated with orlistat also showed a marked improvement in the metabolic risk factor profile compared with placebo.

In a clinical study lasting 1 year, obese adolescents with orlistat showed a decrease in body mass index (BMI), body fat, and waist and hip circumference compared with the group of adolescents who received placebo. There was a significant decrease in diastolic blood pressure compared with the placebo group.

Pharmacokinetics

Orsoten is characterized by minimal systemic action. 8 hours after a single oral administration of the agent in a dose of 360 mg, unchanged orlistat could not be detected in the blood plasma, which confirms that its level is below 5 ng / ml. After using therapeutic doses of the drug, it was possible to detect unchanged orlistat in plasma only in some cases, and its concentrations were less than 10 ng / ml or 0.02 μmol. No signs of cumulation were found, which confirms the extremely low absorption of Orsoten.

The volume of distribution cannot be established, since the active substance is very poorly absorbed. Orlistat binds to plasma proteins (mainly albumin and lipoproteins) by more than 99% in vitro. The drug can penetrate into erythrocytes in minimal quantities.

Orlistat is metabolized according to data obtained in an experiment on animals, mostly in the intestinal wall. When conducting studies with the participation of obese people, it was found that about 42% of the minimum fraction of the active substance undergoing systemic absorption is accounted for by 2 main metabolites: M1 (four-membered hydrolyzed lactone ring) and M3 (M1 with a cleaved N-formylleucine residue) …

Molecules М1 and МЗ have an open β-lactone ring and suppress lipase to a very insignificant extent (weaker than orlistat by 1000 and 2500 times, respectively). After using therapeutic doses of Orsoten, these metabolic products are considered pharmacologically inactive due to their extremely weak inhibitory effect and low plasma concentrations (approximately 26 and 108 ng / ml, respectively).

Approximately 97% of the oral dose of orlistat is excreted through the intestines, with 83% in unchanged form.

The cumulative renal excretion of all substances structurally related to orlistat is less than 2% of the dose taken. The period required for complete elimination of the drug by the kidneys and through the intestine can vary from 3 to 5 days. In volunteers with normal and overweight bodies, the ratio of drug excretion routes was the same. Orlistat and its two main metabolites can be excreted in the bile.

Indications for use

According to the instructions, Orsoten is recommended for long-term treatment of obese patients with BMI ≥ 30 kg / m2, or patients with overweight (BMI ≥ 28 kg / m2) in the presence of risk factors associated with obesity, in combination with moderate hypocaloric diet.

The drug Orsoten can be prescribed to patients with type 2 diabetes mellitus with obesity or overweight in combination with hypoglycemic agents and / or a moderately low-calorie diet.

Contraindications

• cholestasis;
• chronic malabsorption syndrome;
• pregnancy and breastfeeding;
• age up to 18 years;
• hypersensitivity to orlistat or any other component of the drug.

Orsoten should be used with caution during therapy with cyclosporine and oral anticoagulants (including warfarin).

Instructions for the use of Orsoten: method and dosage

Orsoten is taken orally.

The recommended single dose is 1 capsule (120 mg of orlistat). Capsules should be taken immediately before each main meal, during or after it, but no later than 1 hour after its completion. In the event that there was no meal or the meal did not contain fat, you can skip the capsule intake. The duration of treatment is no more than 2 years.

When using the drug more than 3 times a day, 120 mg, its therapeutic effect is not enhanced.

Reception of Orsoten should be combined with a balanced, moderately hypocaloric diet, including in the form of fats not more than 30% of the total calorie intake. The daily intake of protein, carbohydrates and fat should be spread over 3 main meals. It is recommended to include fruits and vegetables in the diet daily.

Side effects

According to clinical studies, the following side effects of Orsoten have been identified:

• kidneys and urinary tract: often - urinary tract infections;
• Gastrointestinal tract: very often - discomfort / pain in the abdomen, flatulence, gas with some discharge, oily discharge from the rectum, urge to defecate, increased frequency of bowel movements, steatorrhea (inclusions of fat in the stool), loose stools; often - discomfort / pain in the rectum, fecal incontinence, bloating, soft stools, gum / tooth damage;
• infectious and parasitic diseases: very often - flu;
• nervous system: very often - headache;
• mental disorders: often - anxiety;
• metabolism: very often - hypoglycemia;
• genitals and mammary gland: often - irregular menstruation;
• respiratory system, chest and mediastinal organs: very often - upper respiratory tract infections; often - lower respiratory tract infections;
• general disorders: often - weakness.

While taking Orsoten, undesirable effects occurred mainly from the digestive tract and were caused by an excessive amount of fat in the feces. The likelihood of developing these effects decreased with a low-fat diet.

The frequency and nature of adverse reactions in patients with type 2 diabetes mellitus were comparable to those in patients with overweight and obesity who did not have this disease. Recorded disturbances, as a rule, were mild and transient; their occurrence was noted at an early stage of therapy during the first three months, but not more than one episode. With prolonged use of Orsoten, the frequency of occurrence of its side effects decreased.

Adverse reactions registered with spontaneous post-registration messages (frequency unknown):

• liver and biliary tract: cholelithiasis, isolated cases of liver damage, sometimes severe, leading to the need for its transplantation or death;
• digestive system: diverticulitis, rectal bleeding (if severe and / or persistent symptoms occur, additional examination is necessary), pancreatitis;
• kidneys and urinary tract: oxalate nephropathy with possible development of renal failure (aggravation of the risk of this complication was observed in patients with chronic renal failure and / or dehydration);
• immune system: hypersensitivity reactions (skin rash, itching, urticaria, bronchospasm, angioedema, anaphylaxis);
• skin and subcutaneous tissue: bullous rash;
• laboratory data: increased activity of hepatic transaminases and alkaline phosphatase, a decrease in the plasma concentration of prothrombin, an increase in the international normalized ratio (INR) and cases of unbalanced treatment with anticoagulants, causing a change in hemostatic parameters, hyperoxaluria.

Overdose

When orlistat was taken in a single dose of 800 mg or when used 3 times a day, 400 mg for 15 days, no pronounced adverse effects were observed. In addition, when Orsoten was prescribed to obese patients for 6 months 3 times a day at 240 mg, there was no significant increase in the frequency of side effects.

In case of an overdose of orlistat, adverse reactions were either absent, or they did not differ from those that were recorded when using Orsoten in therapeutic doses. In case of overdose, it is recommended to monitor the patient for 24 hours.

special instructions

If, over 12 weeks of treatment with Orsoten, it was not possible to achieve a decrease in body weight by at least 5% compared to the initial weight, the drug should be discontinued.

According to clinical studies, the use of Orsoten in patients with type 2 diabetes mellitus resulted in less weight loss when compared with the results of taking the drug in patients without diabetes mellitus.

Orsoten demonstrates effectiveness in long-term control of body weight - it reduces body weight, maintains it at the achieved level, and prevents re-weight gain. The drug therapy helps to improve the profile of risk factors and diseases associated with obesity, such as hypercholesterolemia, hyperinsulinemia, type 2 diabetes mellitus, impaired glucose tolerance, arterial hypertension. Orlistat helps to reduce the amount of visceral fat, and also in patients with type 2 diabetes leads to an additional improvement in the compensation of carbohydrate metabolism, allowing a decrease in the dose of hypoglycemic agents.

In the overwhelming number of patients while using Orsoten, according to clinical studies, the levels of vitamins D, A, E, K and beta-carotene did not go beyond the normal range. To ensure adequate intake of all nutrients in the body during the period of therapy, you can take multivitamins.

When using Orsoten, in rare cases, the development of hypothyroidism and / or a violation of its control was observed. The mechanism of this phenomenon is unclear, but may be associated with a decrease in the absorption of iodized salt and / or sodium levothyroxine.

Influence on the ability to drive vehicles and complex mechanisms

Orsoten does not affect the ability to drive vehicles and control other complex and potentially dangerous equipment.

Application during pregnancy and lactation

In the course of studies of reproductive toxicity in animals, the embryotoxic and teratogenic effects of orlistat were not revealed. However, there is no reliable clinical data regarding the use of Orsoten in pregnant women, therefore, its use during pregnancy is contraindicated.

Whether orlistat is excreted in breast milk has not been established, for this reason, treatment with Orsoten during breastfeeding is contraindicated.

Pediatric use

There is no information confirming the efficacy and safety of therapy with orlistat in children under 18 years of age; therefore, Orsoten is contraindicated in patients of this age category.

With impaired renal function

In the presence of functional renal impairment, dose adjustment of Orsoten is not required.

For violations of liver function

In the presence of functional disorders of the liver, dose adjustment of Orsoten is not required.

Use in the elderly

When using Orsoten in elderly patients, there is no need for dose adjustment.

Drug interactions

• amitriptyline, digoxin, biguanides, atorvastatin, fibrates, fluoxetine, phenytoin, losartan, oral contraceptives, pravastatin, phentermine, slow-release nifedipine and nifedipine GITS (gastrointestinal drug interactions - no data, ethanolamine), sibanol
• oral anticoagulants (including warfarin) - the level of prothrombin decreases and the INR indicator increases, which can cause changes in hemostatic parameters (monitoring of the INR indicator is necessary);
• cyclosporine - the plasma concentration of this substance decreases, which can provoke a decrease in its immunosuppressive efficacy; if necessary, this combination requires frequent monitoring of the level of cyclosporin in plasma during concomitant therapy with orlistat, as well as after its completion;
• beta-carotene, vitamins D and E - absorption of these biologically active substances is weakened, with combined use they should be used no earlier than 2 hours after taking Orsoten or before bedtime;
• amiodarone - when taken orally, a decrease in the level of its content in blood plasma is possible, and therefore requires clinical observation and ECG monitoring;
• antidepressants, antipsychotics (including lithium preparations), antiretroviral drugs for the treatment of HIV - the effect of these drugs may decrease; before starting treatment with Orsoten, a careful assessment of the potential risk of exposure to orlistat on such patients is necessary;
• acarbose - simultaneous administration should be avoided due to the lack of pharmacokinetic interaction studies;
• antiepileptic drugs - seizures may develop; the causal relationship between the appearance of this complication and the administration of orlistat has not been established, but, despite this, the patients' condition should be monitored for possible changes in the severity and frequency of seizures;
• oral contraceptives - there is a possibility of deterioration in their effectiveness due to the indirect effect of Orsoten, which increases the risk of developing an unplanned pregnancy; additional methods of contraception should be used, especially if severe diarrhea occurs.

Analogs

Orsoten's analogs are: Xsenalten, Alli, Xenalten Light, Xenical, Listata, Xsenalten Slim, Listata Mini, Orlimax, Orliksen 60, Orliksen 120, Orlistat.

Terms and conditions of storage

Keep out of the reach of children. Store at a temperature not exceeding 25 ° C.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Orsoten

There are many reviews about Orsoten on medical websites and they are quite diverse. Most patients and doctors consider the drug to be an effective drug for reducing volume and body weight to 5–7 kg in one month (depending on the degree of obesity). At the same time, all positive reviews indicate that in order to achieve the desired therapeutic effect, it is necessary to combine Orsoten's intake with a low-calorie diet and an expansion of the motor regime. Many doctors consider the advantage of the drug that it does not accumulate in the body and practically does not enter the systemic circulation.

The disadvantages of Orsoten include the appearance of side effects, usually from the gastrointestinal tract, such as loose stools, stomach discomfort after taking capsules, increased gas formation, and involuntary defecation. To reduce the severity of these disorders, patients recommend not to abuse fatty foods. There are also reviews in which dissatisfaction with the drug treatment is expressed, since after its prima it was not possible to reduce weight. It is sometimes noted that by adjusting your diet and reducing the usual intake of fats and carbohydrates, you can reduce excess weight without resorting to medication.

Price for Orsoten in pharmacies

The price for Orsoten (capsules 120 mg) can be for a package containing 21 pieces, 640–840 rubles, 42 pieces. - 1280-1700 rubles, 84 pcs. - 2299–2580 rubles.

Orsoten: prices in online pharmacies

Drug name Price Pharmacy

Orsoten Slim 60 mg capsules 42 pcs. 492 r Buy

Reviews Orsoten Slim 492 r Buy

Orsoten Slim Caps. 60mg n42 669 r Buy

Orsoten 120 mg capsules 21 pcs. RUB 682 Buy

Orsoten capsules 120mg 21 pcs. 774 RUB Buy

Orsoten Slim 60 mg capsule 84 pcs. 868 RUB Buy

Orsoten 120 mg capsules 42 pcs. RUB 980 Buy

Orsoten Slim capsules 60mg 84 pcs. 1194 RUB Buy

Orsoten capsules 120mg 42 pcs. 1306 RUB Buy

Orsoten 120 mg capsules 84 pcs. 2296 RUB Buy

Orsoten capsules 120mg 84 pcs. 2315 RUB Buy

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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!