Orlistat-Acrihin, 120 mg capsules 84 pcs

Orlistat refers to specific inhibitors of long-acting gastrointestinal lipases. This substance shows 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 effect of hypolipidemic agent inactivated enzyme loses the ability to break down fats coming with food in the form of triglycerides (TG) to monoglycerides and absorbable free fatty acids.

Since unreplenished TGs are not absorbed from the gastrointestinal tract (GIT), fewer calories are fed into 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 bloodstream. Due to the activity of orlistat 24-48 hours after oral administration of the drug, the concentration of fat in stools increases.

Leading to a decrease in fat depot, Orlistat-Acrichin provides effective body weight control. In clinical studies involving obese patients, more pronounced weight loss was observed in the group of patients receiving Orlistat compared to patients on diet therapy alone. Weight loss was already observed within the first 2 weeks of starting Orlistat-Acrychin and for 6-12 months thereafter, even if there was a negative response to diet therapy.

Statistically significant significant improvement in the profile of obesity-related metabolic risk factors was recorded for two years. In addition, there was a significant reduction in body fat deposits when compared to the placebo group. Orlistat such patients were found to have a significant improvement in glycemic control. Also during the use of Orlistat-Acrihin a decrease in doses of antidiabetic drugs, insulin concentration, as well as a decrease in insulin resistance was observed. According to 4-year studies, orlistat therapy was found to significantly reduce the threat of type 2 diabetes, by an average of 37% compared to placebo use. This threat was reduced by about 45% in patients with initial impaired glucose tolerance.

In the group receiving Orlistat, there was a greater reduction in body weight compared with the placebo group, and in addition, a significant improvement in the profile of metabolic risk factors. The new body weight level achieved was maintained for all 4 years of the study. In adolescents with obesity in a 1-year study during treatment with orlistat a decrease in body mass index (BMI) was registered, as well as a decrease in fat deposits and waist and hip circumference compared to the placebo group. Also during the period of taking Orlistat-Acrychin a significant decrease in diastolic blood pressure (BP) was observed in adolescents compared to those who received placebo.

Indications

Orlistat-Acrichin is recommended for long-term therapy in obese patients with BMI ≥ 30 kg/m² or in overweight patients with BMI ≥ 28 kg/m² who have obesity-related risk factors on a moderately restricted low-calorie diet.

Also Orlistat-Acrychin is indicated for administration in patients with type 2 diabetes mellitus with excess body weight or obesity in combination with moderately restricted hypocaloric diet and/or hypoglycemic drugs (insulin and/or sulfonylurea derivatives, metformin).

Active ingredient

Orlistat

Composition

In 1 capsule contains:


Active substance:

orlistat – 120 mg;

Additional Components:

sodium carboxymethyl starch,

microcrystalline cellulose,

Kapplet cover:

titanium dioxide (E171),

gelatin,

indigo carmine (E132).

Interaction

– antiepileptic drugs – absorption of these drugs decreases, which may cause the development of convulsions;

– cyclosporine – its level in the blood plasma may decrease, which may lead to weakening of the immunosuppressive effectiveness of the drug; this combination is not recommended; in case it is necessary to perform frequent monitoring of cyclosporine plasma concentration both during concomitant administration of orlistat and after it;

– warfarin and other anticoagulants – prothrombin concentration decrease and increase of international normalized ratio (INR) are possible that can lead to changes in hemostatic parameters; In case of this combination it is necessary to monitor INR;

– fat-soluble vitamins A, D, E, K and beta-carotene – absorption of these substances decreases; in combined use they should be taken before sleep or not earlier than 2 hours after Orlistat administration;

– acarbose – it is recommended to avoid combined use due to absence of pharmacokinetic interaction studies;

– levothyroxine sodium – possible development of hypothyroidism and/or decrease of its control due to decreased absorption of levothyroxine sodium and/or inorganic iodine;

– oral contraceptives – the risk of decreased contraceptive effect is increased, which in some cases increases the likelihood of unplanned pregnancy; additional contraceptive methods should be resorted to, including the occurrence of severe contraception.

– antiretroviral drugs for the treatment of human immunodeficiency virus (HIV), neuroleptics (including
– antiretroviral drugs for treatment of human immunodeficiency virus (HIV), neuroleptics (including lithium preparations), antidepressants, benzodiazepines – therapeutic effect of these drugs may weaken, therapy with orlistat should be started in such patients after careful assessment of expected benefits from this treatment and possible risk;

– fibrates, atorvastatin, digoxin, amitriptyline, biguanides, losartan, pravastatin, fluoxetine, phentermine, sibutramine, nifedipine, phenytoin, ethanol – no interaction with these drugs was observed.

Directions for use

Orlistat-Acrichin is used orally with each main meal (with a meal, immediately before a meal or not later than 1 hour after a meal). The capsules should be washed down with water.

During long-term therapy in patients with obesity (BMI ≥ 30 kg/m²) or overweight persons (BMI ≥ 28 kg/m²) with obesity-related risk factors, aged 12 years and older while following a moderately restricted low-calorie diet should be taken Orlistat-Acrihin at a dose of 120 mg orlistat (1 capsule) 3 times daily.

If the preparation is administered to adults with diabetes mellitus type 2 with obesity or overweight when combined with hypoglycemic agents and/or following a moderately restricted 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 capsule in the case if the meal does not contain fat or if the meal was missed.

During the therapy it is required to stick to a balanced moderately restricted hypocaloric diet containing no more than 30% of calories in the form of fat, it is also recommended to include fruits and vegetables in the daily diet. The total amount of carbohydrates, fats and proteins consumed per day should be distributed into three main meals. When using orlistat in doses greater than 3 capsules a day no increase in the therapeutic effect was observed.

Study of safety and efficacy of taking Orlistat-Acrihin in patients with liver and/or kidney functional disorders was not conducted.

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Special Instructions

Orlistat-Acrichine is recommended for long-term body weight control (including body weight loss, maintaining it at the desired achieved level and preventing weight gain again). In patients with type 2 diabetes as a result of weight loss when using the drug increases the likelihood of improved carbohydrate metabolism, against which a reduction in the dose of hypoglycemic drugs may be required.

Therapy with Orlistatom-Acrihin should not last more than 2 years. If after 12 weeks after the course start it was not possible to achieve weight reduction of at least 5%, the drug should be discontinued. In case of occurrence of such symptoms as fatigability, weakness, fever, darkened urine and jaundice during the course of therapy it is required to consult the attending physician in order to exclude possible liver function disturbances.

During the drug treatment mainly in patients with concomitant chronic kidney disease and/or dehydration the development of hyperoxaluria and oxalate nephropathy is possible, which in some cases may lead to renal failure.

Synopsis

Available in capsule form: size 1, hard gelatin, blue color, the contents of capsules – white powder or slightly compacted agglomerates.

Features

The drug is characterized by low absorption. In 8 hours after oral administration unchanged orlistat is not detected in plasma, because its concentration is not more than 5 ng/ml. No signs of cumulation of the active substance are found, which indicates an extremely low degree of absorption. It is impossible to establish the volume of distribution, because the drug is practically not absorbed.

In vitro it is almost fully bound with plasma proteins (99%), mainly with lipoproteins and albumin. The drug is able to penetrate into erythrocytes in minimal amounts. Metabolic transformation of orlistat proceeds mainly in intestinal wall with formation of two metabolites without pharmacological activity – M1 (four-membered hydrolyzed lactone ring) and M3 (M1 with detached N-formylleucine residue). The substance is excreted mainly through the intestine – about 97% of the dose taken, about 83% of this amount is taken unchanged.

Total excretion of all orlistat metabolites by kidneys does not exceed 2% of the drug dose. Period of complete elimination of the substance with feces and urine is 3-5 days. Excretion routes of orlistat in patients with normal body weight and obesity are similar. Also the active substance and its metabolites may be excreted with bile.

Contraindications

Absolute:

– cholestasis;

– chronic malabsorption syndrome;

– age less than 12 years;

– Pregnancy and lactation;

– Hypersensitivity to any of the constituents of Orlistat-Acrihin.

With extreme caution the drug should be treated with concomitant use of cyclosporine, warfarin or other oral anticoagulants.

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Side effects

Undesirable effects caused by taking orlistat appeared in most cases on the gastrointestinal tract and were associated with the pharmacological action of the drug, which blocks the absorption of food fats.

The following disorders may occur while taking Orlistat-Acrihin:

– metabolism and eating 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;

– genital organs and mammary gland: often – irregular menstruation;

– kidneys and urinary tract: often – urinary tract infections;

– GI tract: very common – oily discharge from the rectum, abdominal discomfort/pain, gas discharge with some discharge, flatulence, liquid stools, imperative urges to defecate, frequent defecation, steatorrhea; common – rectal discomfort/pain, fecal incontinence, soft stools, bloating, dental lesions, gum lesions;

– general disturbances: often – weakness.

The nature and frequency of adverse effects in patients with type 2 diabetes were similar to those in patients without diabetes who were overweight and obese. Against the background of treatment, the incidence of adverse reactions from the gastrointestinal tract increased with an increase in the amount of fat in the consumed food. 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 occurrence was noted mainly in the first 3 months of therapy and usually not more than one episode. Against the background of long-term use of Orlistat-Acrihin the incidence of these phenomena decreased.

Overdose

No cases of drug overdose have been described.

No adverse effects were observed while taking single (800 mg) and multiple doses (for 15 days up to 400 mg three times a day) of orlistat in subjects with normal body weight/obesity. When orlistat was administered to 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 significant overdose of Orlistat-Acrihin the patient should be observed for 24 hours. According to clinical and preclinical studies, the systemic effects associated with lipase-inhibitory properties of orlistat should be rapidly reversible.

Similarities

Xenical, Orsotene, Orsotene Slim, Listata, Listata Mini, Orlistat