Listata: a drug for weight loss for obesity of 2-3 degrees

• Description
• Compound
• Pharmacodynamics
• Pharmacokinetics
• Mode of application
• Indications
• Contraindications
• Side effects
• Storage conditions
• Analogs

Proper balanced nutrition and physical activity are the key to health and physiological weight loss.
Sometimes, due to the disease and characteristics of the body, this principle does not help, or the effect is very slow. In this case, the pharmaceutical market joins the fight against obesity. The drug Listata is its prominent representative. Listata is a drug whose pharmacological action is based on the inhibition of gastrointestinal lipases.

Release form and composition

The drug is produced in the form of film-coated tablets: blue, pearlescent, oval, biconvex, with the symbol “f” on one side and a line mark on the other; the core is almost white or white (10 pcs each in blister packs, in a cardboard pack there are 1, 2, 3, 6 or 9 packs and instructions for use of Listata).

1 tablet contains:

• active ingredient: orlistat – 120 mg;
• auxiliary components: sodium lauryl sulfate, acacia gum, mannitol, copovidone, crospovidone, magnesium stearate;
• film shell: Opadry II blue (85F205040) (polyvinyl alcohol, macrogol 3350, titanium dioxide, aluminum blue varnish, yellow iron oxide dye, talc), Opadry silver (63F97546) (polyvinyl alcohol, polysorbate-80, macrogol 3350, pearlescent pigment, talc).

How much do weight loss pills cost?

The price of Listata in pharmacies depends on the dosage and number of capsules in the package. In Moscow, the drug is sold at the following cost:

Pharmacological properties

Pharmacodynamics

Listata is a drug for the treatment of obesity. Its active substance, orlistat, is a strong, specific and reversible inhibitor of gastrointestinal lipases with a long-lasting effect. Orlistat does not enter the systemic circulation; its action is realized in the lumen of the stomach and small intestine by forming a covalent bond with the active serine site of gastric and pancreatic lipases. This leads to inactivation of the enzyme and loss of its ability to break down dietary fats, which come in the form of triglycerides, absorbable free fatty acids and monoglycerides. The reduction in the patient’s body weight is due to a decrease in the intake of calories into the body, since unsplit triglycerides are not absorbed from the digestive tract, but are immediately excreted through the intestines. This is confirmed by the results of a study of stool, where the fat content after taking the drug for two days increases sharply.

After stopping Listata, stool fat levels usually return to previous levels within two to three days.

Compared with dietary therapy, the clinical efficacy of orlistat results in greater weight loss. After starting treatment, a decrease in body weight is observed within the first 14 days. Even in patients with a negative response to dietary therapy, it may last from 180 to 365 days. A statistically significant improvement in the profile of metabolic risk factors associated with obesity was confirmed over two years. In addition, there was a significant decrease in the amount of body fat compared to placebo. Orlistat prevents weight gain. A repeated increase in body weight was noted in approximately half of the patients; it amounted to no more than 1/4 of the lost weight. In 50% of patients, there was no re-gain of body weight or even a further decrease in weight.

In patients with type 2 diabetes mellitus who are obese or overweight, taking Listata for 180–365 days leads to greater weight loss compared to patients who are on diet therapy alone. Losing body weight occurs mainly due to a decrease in the amount of fat in the body. At the same time, there is a statistically and clinically significant improvement in glycemic control, a decrease in the dose of hypoglycemic agents, insulin concentrations and a decrease in insulin resistance.

The use of orlistat for 4 years significantly (by approximately 37%) reduces the risk of developing type 2 diabetes. It should be noted that with initial impaired glucose tolerance, the degree of reduction in this risk is more significant (by approximately 45%).

During the entire period of taking Listata, the new level of body weight is maintained.

In obese adolescents, use of orlistat for 365 days helps reduce body weight index, fat mass, waist and hip circumference.

During orlistat therapy, a significant decrease in diastolic blood pressure (blood pressure) was noted.

Pharmacokinetics

Orlistat has minimal systemic effects, this is confirmed by research results. In obese volunteers with normal body weight, unchanged orlistat was not found in the blood plasma after taking the drug orally at a dose of 360 mg. This means that the absorption of orlistat is minimal, its concentration level is less than 5 ng/ml, that is, it is below the limit of quantitative determination.

There are no signs of cumulation.

Binding to blood plasma proteins (mainly lipoproteins and albumin) in vitro is more than 99%. Can penetrate in small quantities into red blood cells.

Metabolized primarily in the intestinal wall. In obese patients, about 42% of the orlistat fraction that penetrates the systemic circulation undergoes biotransformation with the formation of two main pharmacologically inactive metabolites: M1 (four-membered hydrolyzed lactone ring), M3 (M1 with a cleaved N-formylleucine residue). The plasma concentration of M1 and M3 molecules is extremely low, averaging 26 ng/ml and 108 ng/ml, respectively. Their inhibitory activity is 1000 and 2500 times weaker than that of orlistat.

Approximately 97% of the dose taken is excreted through the intestines, including 83% unchanged.

Less than 2% of the dose taken is excreted through the kidneys in the form of various substances structurally related to orlistat.

It is completely eliminated from the body within 3–5 days.

The active substance and its metabolites may be excreted in the bile.

When taking the same doses of Listat, the concentration levels of orlistat and its main metabolites in the blood plasma in adults and children are comparable.

During the treatment period, daily excretion of fat in feces is 27% of food intake.

Indications for use

The use of Listata is indicated for the following conditions and diseases:

• obesity with a BMI (body mass index) of at least 30 kg/m2, overweight with a BMI of at least 28 kg/m2 (including patients who have risk factors associated with obesity) - as long-term therapy in combination with a moderately hypocaloric diet;
• type 2 diabetes mellitus in patients with overweight or obesity - in combination with a moderately hypocaloric diet and/or hypoglycemic agents (sulfonylurea derivatives, metformin and/or insulin).

Analogs

Orlistat as the main active ingredient is used in the following medications:

• Xenalten, available in capsules;
• Xenical is a Swedish-made drug;
• Orsoten is a granular weight loss product;
• Alli is a medication used to maintain optimal body weight and get rid of extra pounds.

All these drugs have a similar principle of biochemical action, purpose and dosage regimen with Listata. Reviews about the drug indicate that there is no big difference between analogues, with the exception of price and excipients.

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.

Overdose

In individuals with normal body weight and obese patients, single doses of 800 mg or repeated doses of orlistat 400 mg 3 times a day for 15 days were not accompanied by the occurrence of significant adverse events. In addition, obese patients have experience using orlistat 240 mg 3 times a day for 6 months, which was not accompanied by a significant increase in the incidence of adverse events.

In cases of orlistat overdose, either no adverse events were reported, or the adverse events did not differ from those observed when taking orlistat in therapeutic doses.

In case of severe overdose of orlistat, it is recommended to observe the patient for 24 hours. According to studies in humans and animals, any systemic effects that could be associated with the lipase inhibitory properties of orlistat should be quickly reversible.

Side effects

• from the digestive system: very often (more than 1/10) - discomfort or pain in the abdomen, flatulence, release of gases with some discharge, oily discharge from the rectum, steatorrhea, imperative urge to defecate, loose stools, increased frequency of bowel movements (these side effects reactions occur in the first 3 months of therapy, are mild and transient in nature, their frequency increases with increasing fat content in food); often (more than 1/100, but less than 1/10) - damage to teeth and/or gums, bloating, pain or discomfort in the rectum, soft stools, fecal incontinence; very rarely (less than 1/10,000) - increased activity of liver transaminases and alkaline phosphatase, hepatitis; frequency not established (available data do not allow us to establish the frequency of adverse events) - rectal bleeding, diverticulitis, cholelithiasis, pancreatitis;
• allergic reactions: rarely (more than 1/10,000, but less than 1/1000) – itching, skin rash, urticaria, bronchospasm, angioedema, anaphylaxis; very rarely - bullous rash;
• other: very often - upper respiratory tract infections, headache, flu; often - anxiety, weakness, urinary tract infections, lower respiratory tract infections, dysmenorrhea; frequency not established – oxalate nephropathy.

In addition, hypoglycemic conditions and abdominal bloating were frequently reported during post-marketing surveillance in patients with type 2 diabetes mellitus.

special instructions

The effectiveness of Listata has been confirmed in reducing body weight and preventing its re-gain, reducing the amount of visceral fat, improving the profile of risk factors for the development of diseases associated with obesity, such as impaired glucose tolerance, type 2 diabetes, hyperinsulinemia, hypercholesterolemia, arterial hypertension.

In patients with type 2 diabetes mellitus with obesity (BMI not less than 30 kg/m2) or overweight (BMI not less than 28 kg/m2), combination therapy with hypoglycemic drugs and orlistat in combination with a moderately hypocaloric diet further improves the compensation of carbohydrate metabolism. A dose reduction of hypoglycemic agents may be required.

To ensure adequate intake of vitamins A, D, E, K, beta-carotene and other minerals into the body, the use of multivitamins is indicated.

It should be taken into account that foods very rich in fat increase the likelihood of developing gastrointestinal reactions.

Impact on the ability to drive vehicles and complex mechanisms

The use of the drug Listata does not have a negative effect on the ability of patients to drive vehicles and complex mechanisms. Caution is recommended for patients with type 2 diabetes mellitus who take tablets in combination with hypoglycemic agents. This is due to the fact that against the background of this combination, hypoglycemia may develop, which often causes blurred vision and dizziness.

Contraindications

A medical ban on taking Listata is associated with impaired renal and gastrointestinal function.

The drug is not prescribed in the following cases:

• cholestasis is a pathological disorder in which there is no or insignificant release of steapsins, triglycerides, bile secretions due to blockage of the excretory ducts;
• chronic malabsorption syndrome - hereditary or acquired dysfunction of the parietal breakdown of food in the small intestine, due to which;
• individual intolerance;
• renal failure or anatomical deformation of the organ.

In some cases, on the recommendation of a nutritionist, the daily dose is reduced and additional medications are prescribed to minimize pathological symptoms.

Drug interactions

• amitriptyline, atorvastatin, digoxin, fibrates, biguanides, fluoxetine, losartan, phenytoin, phentermine, pravastatin, nifedipine slow release, nifedipine GITS (gastrointestinal therapeutic system), sibutramine, oral contraceptives, ethanol: the combination of orlistat with any of these drugs does not cause drug interactions;
• indirect-acting anticoagulants (including warfarin): against the background of concomitant therapy with indirect-acting anticoagulants, a decrease in prothrombin, an increase in INR values ​​(international normalized ratio), and changes in hemostatic parameters are possible;
• antiepileptic drugs: there is a risk of developing seizures in patients taking anticonvulsants;
• acarbose: it is recommended to avoid combination with Listata;
• beta-carotene, vitamins D and E: absorption of these vitamins is reduced with orlistat, so they should be taken before bed or 2 hours after taking the drug;
• cyclosporine: a decrease in its concentration in the blood plasma is possible;
• amiodarone (oral dosage form): a 25–30% decrease in the systemic exposure of amiodarone and desethylamiodarone is observed, and its clinical effect may be reduced.

Pharmacodynamics

The active ingredients of the drug quickly penetrate the gastrointestinal tract and are concentrated in the blood plasma. The pharmacodynamic characteristics of the drug are determined by the ability of orlistat to block steapsins, preventing the fermentation of lipid compounds.

Listata (reviews of the drug state that visible results occur a few weeks after the start of systematic use) effectively inhibits gastric lipases. Orlistat has a reversible and prolonged effect.

The breakdown of mono-, triglycerides and lipids continues for another 48 hours after completion of the therapeutic course. To increase the effectiveness of the drug, it is necessary to ensure a minimum intake of calories into the gastrointestinal tract.

The main pharmacodynamic action of Listata occurs outside the circulatory system. Therefore, internal organs and the brain are not affected. Orlistat stops the process of converting fat-soluble vitamins into heat energy.

Additionally, a gastric lipase inhibitor disrupts the synthesis of cholesterol and low-density lipoproteins. As a result, the risk of blockage of blood vessels and blood clots is reduced. Systematic use of orlistat reduces the likelihood of developing diabetes mellitus.

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.

About the features

It is important to understand that using the drug under study alone is not enough for significant weight loss. The thing is that Listata allows you to limit only 30% of incoming fat. For maximum efficiency you will have to:

• give up fatty foods;
• to live an active lifestyle;
• follow all recommendations of a nutritionist;
• avoid stress.

Only in this case can one hope for a good result from treatment with Listata.