Listata

Pharmacodynamics

Orlistat is a potent, specific and reversible inhibitor of gastrointestinal lipases with a long-lasting effect. Its therapeutic effect occurs in the lumen of the stomach and small intestine and consists of the formation of a covalent bond with the active serine site of gastric and pancreatic lipases.

The inactivated enzyme then loses the ability to break down food fats, which come in the form of triglycerides, into absorbable free fatty acids and monoglycerides. Since unsplit triglycerides are not absorbed, the resulting decrease in caloric intake into the body leads to a decrease in body weight. Thus, the therapeutic effect of the drug is carried out without absorption into the systemic circulation.

Based on fecal fat results, the effects of orlistat begin 24 to 48 hours after dosing. After discontinuation of orlistat, fecal fat content usually returns to pre-therapy levels within 48-72 hours.

Clinical effectiveness

Patients taking orlistat experience greater weight loss compared to patients on diet therapy. Body weight loss begins within the first 2 weeks after the start of treatment and continues from 6 to 12 months, even in patients with a negative response to diet therapy. Over the course of 2 years, there was a statistically significant improvement in the profile of metabolic risk factors associated with obesity. In addition, compared to placebo, there was a significant reduction in body fat. Orlistat is effective in preventing weight gain. Re-gain of body weight, no more than 25% of lost, is observed in approximately half of the patients, and in half of these patients, re-gain of body weight is not observed or even a further decrease is observed.

Overweight or obese patients with type 2 diabetes mellitus treated with orlistat for 6 months to 1 year experienced greater weight loss compared with patients receiving dietary therapy alone. Weight loss occurs mainly due to a decrease in the amount of fat in the body. With orlistat therapy, a statistically and clinically significant improvement in glycemic control is observed. In addition, during therapy with orlistat, there is a decrease in the dose of hypoglycemic agents, insulin concentration, as well as a decrease in insulin resistance.

When using orlistat for 4 years, the risk of developing type 2 diabetes mellitus is significantly reduced (by approximately 37% compared to placebo). The degree of risk reduction is even greater in patients with baseline impaired glucose tolerance (approximately 45%).

Maintaining body weight at a new level is observed throughout the entire period of use of the drug.

When orlistat was used for 1 year in obese adolescents, there was a decrease in BMI, a decrease in fat mass, and a decrease in waist and hip circumference compared to the placebo group. Also, patients treated with orlistat showed a significant decrease in diastolic blood pressure compared to the placebo group.

Pharmacokinetics

Suction

In normal weight and obese volunteers, systemic exposure to orlistat is minimal. After a single oral dose of 360 mg, unchanged orlistat is undetectable in plasma, which means that its concentrations are below the limit of quantitation (less than 5 ng/ml).

In general, after taking therapeutic doses, it was possible to detect unchanged orlistat in blood plasma only in rare cases, and its concentrations were extremely low (less than 10 ng/ml or 0.02 μmol). There are no signs of accumulation, which confirms that the absorption of orlistat is minimal.

Distribution

Vd cannot be determined because orlistat is very poorly absorbed. In vitro, orlistat is more than 99% bound to plasma proteins (mainly lipoproteins and albumin). In minimal quantities, orlistat can penetrate red blood cells.

Metabolism

Orlistat is metabolized primarily in the intestinal wall. In obese patients, approximately 42% of the minimal fraction of orlistat that is absorbed systemically is accounted for by two main metabolites - M1 (a four-membered hydrolyzed lactone ring) and M3 (M1 with a cleaved N-formylleucine residue).

Molecules M1 and M3 have an open b-lactone ring and inhibit lipase extremely weakly (1000 and 2500 times weaker, respectively, than orlistat).

Given this low inhibitory activity and low plasma concentrations (average 26 ng/ml and 108 ng/ml, respectively) after therapeutic doses, these metabolites are considered pharmacologically inactive.

Removal

In individuals with normal and overweight, the main route of elimination is the elimination of unabsorbed orlistat through the intestines. About 97% of the dose taken is excreted through the intestines, with 83% as unchanged orlistat.

The cumulative renal excretion of all substances structurally related to orlistat is less than 2% of the administered dose. The time until orlistat is completely eliminated from the body (through the intestines and kidneys) is 3-5 days. The ratio of orlistat elimination routes in volunteers with normal and overweight was the same. Both orlistat and the metabolites M1 and M3 can be excreted in the bile.

Pharmacokinetics in special clinical groups

Plasma concentrations of orlistat and its metabolites (M1 and M3) in children do not differ from those in adults when comparing the same doses of orlistat. Daily excretion of fat in feces is 27% of dietary intake during orlistat therapy.

Application

The drug is taken in strict compliance with the regimen specified by the nutritionist and in the doses prescribed by him. The standard daily concentration of orlistat in the body of an adult is 360 mg.
A typical dosage regimen is 3 times a day, 1 tablet with meals or no later than an hour after meals. In combination with a course of treatment with Listata, diet correction is necessary.
Food should contain no more than 30% of calories in the form of lipid compounds and fatty acids. Weight loss improves metabolism and restores the functions of the gastrointestinal tract and endocrine glands.
The drug is washed down with plenty of water (at least 1/2 glass) to facilitate absorption of the active ingredients. You should not take diet pills separately from food.
The best therapeutic effect is achieved with an even distribution of calories received by the body throughout the day. It is recommended to combine Listata with protein and vegetable dishes and a fruit diet.

For children under 18 years old

The drug interferes with the absorption of fat-soluble vitamin compounds of groups A, E, D. The drug is combined with multivitamin complexes. The medication is prescribed to children from 12 years of age.

Listata (reviews of the drug confirm this) improves the appetite of adolescents, facilitates hormonal changes in the body, and improves immunity. Children who regularly undergo such therapy are less likely to get ARVI.

The maximum single dose for patients 12-18 years of age is 60 mg orlistat. Tablets are taken 3 times a day with food. During this period, the body is in a phase of active growth. Therefore, to restore the vitamin and mineral balance disturbed as a result of the action of orlistat, special complex preparations are prescribed.

Rating of the best of them:

"Vitrum Junior" . It has a balanced composition, does not cause allergic reactions, and combines well with the active ingredients of Listata. Available in the form of chewable tablets in various fruit flavors.
"Pikovit Forte" . A rich multivitamin complex that replenishes nutritional deficiencies, allowing you to cope with mental stress and physical activity.
"Complivit Active" . Contains 12 vitamins and 10 mineral compounds. The drug combines well with orlistat, increases resistance to stress, and strengthens the immune system.
"Centrum" . Activates the body's protective functions. As a result of taking it, energy increases and mood improves. Contains 13 vitamins and 11 mineral compounds.

Any of these drugs or an analogue must be supplemented with the course of treatment with Listata in order to avoid inhibition of the important functions of the growing body.

For adults

The nutritionist calculates the dosage individually based on the observed clinical picture. For diabetes mellitus, Listata is taken in combination with compatible hypoglycemic drugs.

Often, as part of complex therapy, the following are prescribed:

Metformin is a tableted drug that reduces blood glucose levels, suppresses the oxidative capacity of fatty acids, and relieves hyperinsulinemia;
Siofor is a biguanide drug that enhances the utilization of glucose by muscle fibers, causing a significant decrease in body weight in patients with type 2 diabetes mellitus;
Galvus is a stimulator of the islet system of the pancreas, a selective inhibitor of the enzyme dipeptidyl peptidase-4, complements the therapeutic effect of orlistat;
Victoza is a biochemical recombinant with hypoglycemic action that affects the physiological regulator of appetite and absorption of consumed calories.

The duration of taking Listata and related medications is determined individually by the attending physician. The daily concentration of the active substance in the body of adult patients, according to the decision of a nutritionist, can be increased from 360 mg to 480.

For pregnant

Listata (reviews of the drug from women characterize its effect positively) has no reproductive toxicity and does not affect the process of bearing a child and breastfeeding.

During studies on experimental animals, teratogenic disorders of embryonic development were not recorded. The use of the drug during pregnancy is not contraindicated. A preliminary consultation with a doctor is required.

There are no clinical data on the effects of orlistat on the body during pregnancy. There is no clinical data and the release of the active substance into breast milk. During lactation it is advisable to refrain from taking the drug.

For the elderly

There is no reliable information about the effect of the active ingredients of Listata on the body of elderly patients.

Older people should take the drug only after:

consultations with a nutritionist;
visits to specialists of other profiles;
taking tests;
conducting instrumental research.

The maximum daily concentration of orlistat in elderly patients should not exceed 240 mg.

Contraindications and side effects

The list is far from complete; please read the instructions carefully. In it you will also find information about contraindications to taking the drug, incl. intolerance to the components of the drug, impaired absorption in the intestine, congestion in the gallbladder, pregnancy and lactation, childhood. In addition, caution should be exercised when taking certain medications in parallel; for example, the effectiveness of oral contraceptives and fat-soluble vitamins is reduced. Here are some quite numerous and extremely unpleasant side effects:

loose stools;
involuntary oily discharge;
frequent urge to defecate;
flatulence;
pain and bloating in the abdomen;
bleeding from the rectum;
cholelithiasis;
inflammatory processes of the respiratory tract;
allergic reactions, itching, urticaria;
headache;
depressed state.

Reviews about Listat

Reviews about Listat are contradictory. Patients who give a positive assessment of the effectiveness of the drug report fairly good tolerability, noticeable weight loss and the need to follow a low-calorie diet during the treatment period. Some of them experienced adverse events from the digestive system (including frequent and/or loose stools, flatulence) in the first days of taking orlistat.

At the same time, there are often reviews in which patients indicate the absence of any therapeutic effect of Listata, the appearance of side effects in the form of headache, diarrhea, nausea, and vomiting.

What is the difference between the regular form and the “mini” one?

The only difference between Listata and Listata mini is the amount of the main active ingredient. In the classic version of the drug for weight loss it is 120 mg, in the “mini” version it is 60 mg. The principle of action of the tablets, as well as the dosage regimen and side effects, are no different. Therefore, even such “lightweight” weight loss should be carried out under the supervision of a doctor.

Listata, instructions for use: method and dosage

Listat tablets are taken orally during each main meal (but no later than 1 hour after meals), with water.

In cases where a meal is skipped or does not contain fat, the tablet may not be taken.

You should follow a balanced, moderately hypocaloric diet that contains no more than 30% of calories in the form of fat. The daily intake of fats, carbohydrates and proteins must be divided between three main meals. When prescribing Listata, the doctor must inform the patient about the possible occurrence of side effects from the gastrointestinal tract (GIT) and how to eliminate them by following a diet. A low-fat diet helps reduce the risk of developing adverse reactions from the gastrointestinal tract.

Recommended dosage: 1 pc. 3 times a day.

It should be borne in mind that increasing the single dose does not lead to an increase in the therapeutic effect of Listata.

Where to buy and at what price

"Listata" can only be purchased with a doctor's prescription. But its mini format is sometimes available for free sale, but it is still better to get medical advice first - we are talking about your health. And, despite the lower dosage of orlistat, side effects when using this drug are present in full. You can buy tablets in a pharmacy chain or order them from an online pharmacy. The cost depends on the volume of packaging. The price range is approximately this:

Listata No. 30 from 730 to 1000 rubles;
Listata No. 60 from 1300 to 1500 rubles;
Listata No. 90 from 2000 to 2400 rubles;
Listata mini No. 30 from 600 to 800 rubles;
Listata mini No. 60 from 1000 to 1500 rubles;
Listata mini No. 90 from 1600 to 2000 rubles.