Orsoten Slim, 60 mg capsules 84 pcs

Pharmacodynamics

Orlistat is a specific, long-acting inhibitor of gastrointestinal lipases. Its therapeutic activity is realized in the lumen of the stomach and small intestine and consists in the formation of a covalent bond with the active serine site of gastric and pancreatic lipases.

The enzyme thus inactivated loses its ability to hydrolyze dietary fat in the form of triglycerides to absorbable free fatty acids and monoglycerides. Undigested triglycerides are not absorbed and the resulting caloric deficit can have a positive effect on body weight control.

Orlistat at a dose of 60 mg three times daily blocks the absorption of approximately 25% of dietary fat. The therapeutic effect of orlistat is realized without its systemic absorption. The effect of orlistat causes the concentration of fat in the intestinal contents to increase 24-48 hours after oral administration. After discontinuation of orlistat, intestinal fat concentration usually returns to baseline in 48-72 hours.

In adults with a BMI (body mass index) ≥ 28 kg/m2, orlistat at a dose of 60 mg three times daily is effective in combination with a low-fat, hypocaloric diet. At the same time, the main weight loss occurs during the first 6 months of treatment.

The weight loss seen with orlistat at a dose of 60 mg three times daily is accompanied by other beneficial effects: decreased total cholesterol, LDL (low-density lipoprotein) cholesterol, and decreased waist circumference.

Pharmacokinetics

Absorption

Studies in normal and overweight volunteers have shown that the degree of absorption of orlistat is minimal. The plasma concentration of unchanged orlistat is below the limit of quantification (below 5 ng/ml) 8 h after oral administration of orlistat at a dose of 360 mg. In general, with therapeutic doses, the determination of unchanged orlistat in plasma is sporadic and its concentration is extremely low (less than 10 ng/mL or 0.02 μmol/L), with no evidence of cumulation, indicating minimal absorption.

Distribution

The amount of distribution cannot be determined because orlistat is minimally absorbed and has no established systemic pharmacokinetics. Orlistat is more than 99% bound to plasma proteins (mainly lipoproteins and albumin). Orlistat can minimally penetrate into erythrocytes.

Metabolism

The metabolism of orlistat occurs mainly in the walls of the stomach and small intestine.

Excretion

Approximately 97% of the dose is excreted through the intestine, 83% of this amount as unchanged orlistat. Cumulative renal excretion of all orlistat-containing substances is less than 2% of the administered dose. The time to reach complete excretion (through the intestine and the kidneys) is 3 to 5 days.

Indications

Weight loss in adults (over 18 years of age) with excess body weight (BMI ≥ 28 kg/m2). Used only in combination with a moderate, low-fat, hypocaloric diet.

Active ingredient

Composition

Active ingredients:

Orsotene semi-finished product – pellets – 112.8 mg, in terms of orlistat – 60 mg (excipient of semi-finished product – pellets microcrystalline cellulose).

Excipients:

Microcrystalline cellulose – 22.20 mg.

Solid gelatin capsules #3:

Capsule shell:

Titanium dioxide (E 171) – 0.58 mg,

Gelatin – 28.22 mg.

Capsule cap:

titanium dioxide (E 171) – 0.19 mg,

iron oxide yellow (E172) – 0.04 mg,

gelatin – 18.97 mg.

How to take, the dosage

Orally, 1 capsule (60 mg) three times daily with water immediately before, during, or within 1 h after each meal.

If a meal is missed or if the meal was fat-free, Orlistat should be skipped.

No more than three 60 mg capsules of Orsoten® Slim can be taken within 24 hours.

The duration of treatment

The course of treatment should not exceed 6 months. If after 12 weeks of using Orsoten® Slim the reduction of body weight has not occurred (not more than 5% of the initial weight), the patient should consult the physician to decide whether further use is advisable.

Diet and exercise are an important component of a weight loss program. It is recommended that a dietary and exercise program be initiated prior to initiating therapy with Orsotene® Slim.

When using Orsothen® Slim, the patient should receive a moderately hypocaloric diet with a balanced content of nutrients, in which approximately 30% are fats (for example, if the caloric content is 2000 kcal per day, the food should not contain more than 67 grams of fat). The daily intake of fats, carbohydrates, and protein should be distributed among the three main meals. The diet and exercise program should be continued even after the use of Orsoten® Slim is discontinued.

Patients in the elderly

There are limited data on the use of Orlistat in the elderly.

Patients with impaired hepatic and renal function

The effects of orlistat in persons with impaired hepatic and/or renal function have not been studied, but given that the absorption of orlistat is minimal, no dose adjustment is required in the elderly and in persons with impaired hepatic and/or renal function.

Interaction

Cyclosporine

Concomitant use of cyclosporine and orlistat leads to decreased plasma concentrations of cyclosporine, which may be accompanied by a decrease in its immunosuppressive activity.

The simultaneous use of Orsotene and cyclosporine is contraindicated.

Peroral anticoagulants

The concomitant use of warfarin or other oral anticoagulants and orlistat may change the International Normalized Ratio (INR).

Fat-soluble vitamins

The use of orlistat may impair absorption of fat-soluble vitamins (A, D, E and K).

Acarbose

In the absence of data on pharmacokinetic interactions, it is not recommended to use orlistat concomitantly with acarbose.

Amiodarone

Concomitant use with orlistat has resulted in decreased plasma concentrations of amiodarone after a single use. The clinical significance of this effect in patients taking amiodarone is unclear. Concomitant use of orlistat and amiodarone is possible only under the recommendation of a physician.

Orlistat does not interact with amitriptyline, phenytoin, fluoxetine, sibutramine, phentermine; atorvastatin, pravastatin, fibrates; biguanides; digoxin, nifedipine, losartan; oral contraceptives and ethanol.

Special Instructions

Patients should be advised to follow the dietary recommendations they receive. The likelihood of gastrointestinal side effects is higher if a single meal or the diet as a whole is high in fat.

The treatment with Orsothen® Slim may lead to impair the absorption of fat-soluble vitamins (A, D, E and K). For this reason multivitamins should be taken before going to bed.

As weight loss may be accompanied by improved metabolic control in patients with diabetes mellitus, those who are taking hypoglycemic drugs should consult a physician before starting Orsothen® Slim and, if necessary, adjust the dose of hypoglycemic agents.

The decrease in body weight may be accompanied by an improvement in blood pressure and a decrease in cholesterol concentrations.

Patients taking medications for arterial hypertension or hypercholesterolemia should consult a physician when using Orsotene® Slim and adjust the dose of these medications, if necessary. Patients taking amiodarone should consult a physician before starting therapy with Orsotene® Slim.

In patients using Orlistat, cases of rectal bleeding have been described. If this occurs, the patient should consult a physician.

The use of an additional contraceptive method is recommended to prevent possible failure of oral contraceptives if severe diarrhea occurs.

Impact on ability to drive vehicles and other mechanisms requiring increased concentration

The drug Orsothen® Slim has no effect on driving vehicles and operating technical devices requiring increased concentration and rapid psychomotor reaction.

Contraindications

Side effects

The frequency of side effects (WHO):

Adverse reactions when using orlistat are usually gastrointestinal in nature and are related to its pharmacological effects.

Digestive system disorders: very common: oily discharge from the rectum, gas discharge with some discharge, urgent defecation urges, steatorrhea; common: abdominal pain, fecal incontinence, liquid stools, increased frequency of defecation.

The following adverse reactions (frequency unknown) have been noted during post-marketing use of orlistat:

Hematopoietic system: decreased prothrombin concentration; increased International Normalized Ratio (INR) in patients taking orlistat concomitantly with anticoagulants.

Digestive system disorders: minor rectal bleeding, diverticulitis, hepatitis, cholelithiasis, increased hepatic transaminases and alkaline phosphatase activity.

Skin disorders: bullous rash.

Allergic reactions: itching, rash, urticaria, angioedema, bronchospasm, anaphylaxis.

Overdose

Symptoms: no significant adverse reactions were found in both normal weight and obese patients when orlistat was administered in a dose of 800 mg once and up to 400 mg three times a day, daily, for 15 days. When using orlistat 240 mg three times daily for 6 months, no increase in the incidence of adverse reactions was noted.

The majority of reports of orlistat overdose in the post-marketing period either lack specific adverse reactions or describe adverse reactions that do not differ from those observed with the recommended doses of orlistat.

Treatment: In case of overdose, medical consultation is necessary. In case of a significant overdose of orlistat it is recommended to monitor the patient for 24 hours. Based on data from human and animal studies, all systemic effects of orlistat due to lipase inhibition are usually quickly reversible.

Pregnancy use

There are no clinical data on the use of Orlistat during pregnancy, therefore Orsothen® Slim should not be used during pregnancy.

If it is unknown whether orlistat is excreted into the breast milk, Orsothen® Slim should not be used during breastfeeding.

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