Orlistat HEXAL 60 mg Orlistat Hexal for weight loss 60 mg, 84 pcs, Germany

People suffering from obesity are often prescribed special medications that can control the amount of calories and fat they eat. One of these effective drugs is an inhibitor of special enzymes - steapsins (lipases). This drug is called Orlistat. Thanks to its use, it is possible to reduce excess weight.

Composition and release form

"Orlistat" for weight loss is available in the form of dense blue capsules. Inside the capsule there are white granules (pellets). The total weight of all granules is 240 mg. They contain 120 mg of the active substance - orlistat. Additional components have been added to it: povidone K30 (in an amount of 5.04 mg and cellulose (98.64 mg), as well as various sodium compounds: carboxymethyl starch (10.08 mg) and lauryl sulfate (6.24 mg). The capsules are made of gelatin and titanium dioxide, colored with blue dye.

The capsules are packed in dense cells and hidden in a cardboard box. Packages are available with a very different number of tablets: 5, 6 and 10. Sometimes the drug is placed in a glass jar with 20, 21, 30, 40, 42, 50, 80, 84, 100, 120 or 140 capsules each.

Price

The cost of the medication depends on the manufacturer, the number of capsules in the package and the dosage of the active substance:

1. “Orlistat-Akrikhin” 84 capsules (120 mg) – from 1800 rubles.
2. “Orlistat-Canon” 42 capsules (120 mg) – from 440 rubles.

You can buy products in an online pharmacy, as in a regular one, only if you have a prescription.

The price of synonymous products (at the same time they can be considered analogues of Orlistat) also depends on the dosage of the substance itself and the manufacturing company:

1. “Xenical” (Hoffmann La Roche, Switzerland) with a dosage of 120 mg: 21 capsules – from 800 rubles, 42 k. – from 2000 rubles, 84 k. – from 3300 rubles.
2. "Orsoten" (KRKA, Slovenia) with a dosage of 120 mg: 21 capsules - from 700 rubles, 42 capsules - from 1400 rubles, 84 capsules - from 2200 rubles.
3. “Orsoten Slim” (KRKA-Rus, Russia) with a dosage of 60 mg: 42 capsules - from 580 rubles.
4. “Xenalten” (Obolenskoye FP, Russia) with a dosage of 120 mg: 21 capsules – 715 rubles, 42 capsules – 1160 rubles, 84 capsules – 2100 rubles.
5. "Listata" (Izvarino Pharma, Russia) with a dosage of 120 mg: 30 tablets - 980 rubles, 60 tablets - 1800 rubles, 90 tablets - 2400 rubles.
6. "Alli" (GlaxoSmithKline Consumer Healthcare LP, USA) with a dosage of 60 mg: 120 capsules - from 90 rubles.

Effect of the drug

The drug suppresses the activity of intestinal, gastric and pancreatic lipases. It binds to fat droplets and inactivates lipases. Thanks to this effect, triglycerides do not penetrate into the blood. Thus, dietary fats are broken down less well and are less absorbed into the blood. Because of this, a lack of energy occurs in the body, and then fat is released from those reserves that the body “put aside for a rainy day.” Thanks to this, the volume of fat located in the viscero-abdominal region of the body is reduced.

Once in the intestines, Orlistat reduces the number of monoglycerides and free fatty acids. Due to this, cholesterol is less soluble in liquids and penetrates into the blood in smaller quantities. This allows you to cleanse the blood of excess “bad” cholesterol and improve the functioning of blood vessels.

Orlistat normalizes the fat composition of the blood and increases the sensitivity of body tissues to insulin. This allows you to get rid of excess insulin in the blood, which also leads to a decrease in fat mass in the abdominal area.

"Orlistat" is easily absorbed and quickly eliminated from the body without penetrating into the blood. It is broken down in the intestines and completely eliminated 5 days after the last dose.

According to research results, this medicine made it possible to lose 6.2% of excess body weight (from the original) in 52 weeks. Insulin levels decreased by 18% over the same time.

Introduction

The rate of obesity spread in both economically developed and developing countries is comparable to the scale of the epidemic. The catastrophic increase in the prevalence of obesity, according to published data from WHO [1], led to the fact that in 2014 more than 1.9 billion adults (18 years and older) were overweight, of which 600 million people were obese. If such trends continue, by 2030 about 60% of the world's population, i.e. 3.3 billion people, may be overweight (2.2 billion) or obese (1.1 billion) [2]. Obesity-associated diseases, such as type 2 diabetes mellitus (T2DM), arterial hypertension (AH), coronary heart disease, etc., represent a global medical problem associated with a significantly increasing risk of morbidity and mortality, a significant increase in health care costs healthcare and significantly worsens the quality of life of patients [1, 3]. WHO lists obesity as one of the top five risk factors for death. Treatment of diseases associated with obesity accounts for about 70% of healthcare costs. The risk of mortality increases significantly with a body mass index (BMI) >30 kg/m2. With a BMI >40 kg/m2, mortality in the age group 35–45 years increases 6 times; In the age group of 25-30 years, mortality is 12 times higher than in people of the same age without obesity.

Since losing body weight can reduce the risk of developing diseases associated with obesity, significantly influence the timing of their manifestation or contribute to their more favorable course [4-7], the issues of conservative treatment of obesity become extremely relevant.

Lifestyle modification, based on dietary correction and increased physical activity, is the cornerstone of treatment for patients with obesity, including morbid obesity. However, not all patients are able to change their deeply ingrained eating and lifestyle habits and achieve positive treatment results.

It is known that patients with obesity complicated by concomitant diseases (DM2, hypertension, atherosclerosis, obstructive sleep apnea syndrome, arthrosis, gout, etc.) find it more difficult to reduce body weight, since such conditions make it difficult to follow medical recommendations on nutrition and physical activity . These difficulties dictate the need to include pharmacological agents in the complex treatment of obesity. Pharmacotherapy makes it possible to achieve more effective weight loss, facilitates the implementation of nutritional recommendations, helps in developing new eating habits, and promotes long-term retention of reduced body weight.

Since obesity is a chronic disease with frequent relapses, requiring long-term lifelong treatment and follow-up, short-term therapy is of little effectiveness.

In patients with complicated obesity, treatment should be continued, even if a slight decrease in body weight is accompanied by an improvement in health status and metabolic parameters.

Therefore, the main goals of pharmacotherapy include achieving effective weight loss (more than 10% of the original), compensation of existing metabolic disorders, improving treatment tolerability and increasing adherence to it, as well as preventing relapses of the disease.

Drugs for the treatment of obesity must have a known mechanism of action, significantly reduce body weight, have a positive effect on metabolic disorders associated with obesity (dyslipidemia, type 2 diabetes, hypertension, etc.), have an acceptable tolerability profile, do not cause dependence, be effective and safe with long-term use.

Modern pharmacotherapy of obesity

Until recently, only two drugs for the treatment of obesity were presented on the Russian pharmaceutical market - orlistat and sibutramine [5-8].

Orlistat

The drug has a peripheral effect, has a therapeutic effect within the gastrointestinal tract (GIT) and does not have a systemic effect. Being a specific, long-acting inhibitor of gastrointestinal lipases, orlistat prevents the breakdown and subsequent absorption of fats from food (about 30%), thereby creating an energy deficit, which leads to weight loss. At the same time, it reduces the amount of free fatty acids and monoglycerides in the intestinal lumen, thus reducing the solubility and subsequent absorption of cholesterol, helping to reduce hypercholesterolemia, regardless of the degree of weight loss. Side effects of the drug include fatty stools, oily rectal discharge, urgency to defecate, increased frequency of bowel movements and fecal incontinence, abdominal pain, and the release of gas with some intestinal secretions.

The severity and duration of side effects directly depend on patient adherence to treatment and compliance with recommendations for limiting fat in food. The side effects of orlistat further encourage patients to follow these recommendations. Adverse events become more frequent with increasing fat content in the diet, occur in the early stages of treatment (the first 3 months), and if fat in the diet is limited, they are mild and transient.

The optimal dose of the drug is 120 mg 3 times a day during meals or no later than an hour after it. Increasing the dose does not increase effectiveness. No dose adjustment is required in elderly patients or with impaired liver or kidney function. The drug is contraindicated in case of exacerbation of pancreatitis and diseases accompanied by diarrhea, malabsorption syndrome, cholestasis, or hypersensitivity to the drug itself or any of its components.

The use of orlistat leads to an effective reduction in body weight and BMI in more than 80% of patients. While taking the drug, there is a decrease in risk factors and diseases associated with obesity. The safety of long-term use (up to 4 years of continuous use), as well as the effectiveness of preventing type 2 diabetes, were demonstrated in the XENDOS (Xenical in the Prevention of Diabetes in Obese Subjects) study. Long-term use of the drug in combination with lifestyle changes led to more pronounced weight loss and a statistically significant reduction in the incidence of type 2 diabetes compared to lifestyle changes alone. In addition, the treatment led to a significant and persistent decrease in such cardiovascular risk factors as blood pressure (BP) and the level of atherogenic lipid fractions, and the positive effect on the lipid spectrum was provided not only by a decrease in body weight, but also by a direct, independent of the degree its reduction by the drug’s effect on cholesterol absorption [5]. Data have also been obtained on the positive effect of orlistat on carbohydrate metabolism: treatment with the drug leads to a decrease in the severity of such components of the metabolic syndrome as fasting hyperglycemia, hyperinsulinemia and insulin resistance. S. Heymsfield et al. [7] showed that in the group of patients taking orlistat, impaired glucose tolerance with subsequent development of type 2 diabetes was recorded half as often as in the group receiving placebo (3.0 and 7.6%, respectively). At the same time, the number of patients whose carbohydrate metabolism normalized while taking the drug, on the contrary, turned out to be significantly higher (71.6 and 49.1%, respectively).

Since the mechanism of action of orlistat is to limit the absorption of fats, its long-term use can potentially lead to a deficiency of fat-soluble vitamins, in particular vitamin 25 (OH)D, and, as a result, to impaired calcium metabolism. Some studies have shown that in postmenopausal women, treatment of obesity with orlistat does not change the content of 25 (OH)D, however, with longer use of the drug (12 months), a significant decrease in the vitamin content was observed [8, 9]. Therefore, all patients receiving orlistat treatment, especially postmenopausal women, are advised to take supplemental multivitamins, including calcium and 25 (OH)D, and orlistat and vitamins should not be taken at the same time.

Orlistat increases the likelihood of gallstone formation because inhibition of lipolysis reduces the release of fatty acids into the intestinal lumen, which is necessary to stimulate cholecystokinin secretion and gallbladder contraction. Since orlistat inhibits the breakdown of only 30% of dietary fats, rational consumption of fats does not lead to a decrease in gallbladder motility.

Sibutramine

Sibutramine, a dual-mechanism anti-obesity drug, is a reuptake inhibitor of serotonin, norepinephrine and, to a lesser extent, dopamine at central nervous system synapses. The drug enhances and prolongs the feeling of fullness, thereby reducing the amount of food consumed. On the other hand, sibutramine increases the body's energy expenditure, which collectively leads to a negative energy balance. Thus, the drug makes it easier for patients to follow medical recommendations on nutrition.

While taking sibutramine, 1/3 of patients manage to reduce weight by more than 10% [6].

As an initial dose, sibutramine is prescribed 10 mg in the morning, daily, regardless of meals. If body weight has decreased by less than 2 kg during the first month of treatment, it is recommended to increase the dose to 15 mg, provided the drug is well tolerated. If, after the next month, body weight has decreased by less than 2 kg, or after 3 months of use by less than 5% of the original, treatment is considered ineffective. The maximum period of therapy with sibutramine is 2 years. If type 2 diabetes is present, treatment begins immediately with 15 mg. A loss of less than 2 kg during the first month of therapy does not require discontinuation of the drug, since patients with type 2 diabetes lose weight more slowly. Moreover, even a slight decrease in body weight is accompanied by an improvement in carbohydrate metabolism. As the STORM study showed, about 54% of patients reduced body weight by more than 10% within 6 months of treatment, and the reduced body weight during this period was maintained throughout 2 years of treatment. By positively influencing anthropometric parameters, sibutramine has a beneficial effect on metabolic disorders. Its use is accompanied by a decrease in triglyceride levels by 20% and an increase in high-density lipoprotein levels by 21%, which significantly reduces cardiovascular risk [10].

Taking into account, however, such possible side effects of the drug as an increase in blood pressure by 1-3 mm Hg. and increased heart rate by 3-7 beats. per minute, the drug can be prescribed to patients with obesity and often accompanying hypertension only after correction of the latter. The drug should not be prescribed to patients with uncontrolled hypertension, coronary heart disease, decompensated heart failure, cardiac arrhythmias, cerebrovascular diseases (stroke, transient cerebrovascular accidents), severe liver and kidney damage, as well as when taken simultaneously or earlier than 2 weeks after withdrawal of monoamine oxidase inhibitors or other drugs acting on the central nervous system (including antidepressants).

Side effects such as nausea, loss of appetite, constipation, dry mouth, changes in taste, insomnia, headache, agitation, sweating are usually mild, noted only at the beginning of treatment and, as a rule, do not require discontinuation of therapy.

When treating with sibutramine, medical supervision is necessary. Control A.D. and the pulse follows in all patients before the start of treatment, then from the 1st to the 3rd month of treatment every 2 weeks, from the 4th to 6th month - monthly, from the 6th to 12th month - every 3 months .

The drug is discontinued if the heart rate increases by more than 10 beats/min, the blood pressure increases by more than 10 mm Hg, and also if the blood pressure is >140/90 mm Hg. in persons with previously compensated hypertension, with progression of shortness of breath, the appearance of chest pain or swelling of the joints.

A predictor of successful reduction and long-term retention of body weight is a loss of more than 2 kg in the first months of treatment or more than 5% of the initial weight in 3 months. In women, especially young women, treatment success is recorded more often than in men. The higher your initial BMI, the more intense weight loss you can expect. The presence of diseases concomitant with obesity predetermines slow weight loss.

Of interest is the prematurely completed SCOUT study [11], the first prospective study of the association between weight loss during long-term pharmacotherapy for obesity (sibutramine) and cardiovascular outcomes (cardiovascular death, angina, myocardial infarction, stroke). The results of a randomized, double-blind, placebo-controlled trial involving 10,744 overweight or obese people (mean age 63 years) at 300 centers in 17 countries showed that patients with existing cardiovascular disease who used sibutramine long-term had an increased risk of non-fatal myocardial infarction and nonfatal stroke, but not cardiovascular or all-cause mortality. These results led to the recall of the drug sibutramine in the European Union and the United States.

The drug has not currently been recalled in Russia; it remains an approved treatment for obesity. Since January 2008, sibutramine has been included in the government-approved list of potent drugs, which means it is available by prescription only.

Liraglutide 3 mg

The availability in our country of only two drugs for the treatment of obesity, with the need for strict adherence to indications and contraindications for their use, extremely limited the possibility of treating this condition. In the spring of 2021, the first glucagon-like peptide-1 (GLP-1) analogue for the treatment of obesity was registered in Russia - liraglutide

at a dose of 3 mg (Saxenda). Previously, liraglutide at doses of 1.2 and 1.8 mg per day was used under the name Victoza for the treatment of type 2 diabetes. GLP-1 is a physiological regulator of appetite and food intake. Liraglutide at the level of the hypothalamus activates GLP-1 receptors, increasing satiety signals and weakening hunger signals, which promotes weight loss. In addition, liraglutide stimulates glucose-dependent insulin secretion and reduces paradoxical hyperglucagonemia (characteristic of patients with impaired carbohydrate metabolism), and also helps maintain a functioning pool of ß-cells.

The efficacy and safety of liraglutide at a dose of 3 mg per day in the treatment of obese patients was investigated in a series of randomized, double-blind, placebo-controlled studies that were part of the SCALE program (the Satiety and Clinical Adiposity - Liraglutide Evidence in nondiabetic and diabetic individuals). This program, which covered more than 5,000 patients, provided the evidence base that allowed the drug to be registered in the USA, Europe and Russia. The program included 4 studies - “SCALE, obesity and prediabetes”, “SCALE, diabetes”, “SCALE, weight maintenance” and “SCALE, sleep apnea”.

The 56-week SCALE Obesity and Prediabetes Study was conducted at 191 clinical centers in 27 countries and included 3,731 obese or overweight patients with dyslipidemia and/or hypertension. In Russia, 160 patients participated. All patients were randomized 2:1 to receive liraglutide 3 mg ( n

=2487) or placebo (
n
=1244) as an addition to diet therapy and physical activity. Equivalent endpoints were change in body weight and the proportion of patients whose body weight decreased by ≥5%. After 56 weeks, the mean weight loss in the liraglutide group was 8.0 ± 6.7% (8.4 ± 7.3 kg) compared with 2.6 ± 5.7% (2.8 ± 6.5 kg) in the placebo group.

A reduction in body weight of 5% or more was achieved in 63.2% of patients in the liraglutide group and in 27.1% of patients in the placebo group; a 10% decrease in body weight was observed in 33.1 and 10.6% of patients, respectively ( p

<0.001).
The prevalence of prediabetes among patients with an initial diagnosis after 56 weeks in the liraglutide group decreased by half (from 61.4 to 30.8%), while in the placebo group it increased (from 60.9 to 67.3%) [12] . After 56 weeks, patients with baseline prediabetes remained in the study for up to 3 years and were re-randomized in a 2:1 ratio to receive liraglutide 3 mg ( n
=1505) or placebo (
n
=749). Over 3 years, type 2 diabetes was reported in 26 (2%) people receiving liraglutide 3 mg and 46 (6%) in the placebo group. In addition, the time to manifestation of type 2 diabetes in patients receiving liraglutide was 2.7 times longer than in the placebo group, indicating a significant reduction in the risk of developing type 2 diabetes while taking liraglutide - by 80% (OR = 0.21 ; 95% CI 0.13—0.34). Over 3 years, weight loss in patients receiving liraglutide 3 mg and placebo was 6.1 and 1.9% of baseline, respectively [13].

The SCALE Obesity and Prediabetes study also assessed the dynamics of cardiometabolic risk factors during weight loss. After 56 weeks of therapy, systolic blood pressure decreased in the liraglutide 3 mg group by 4.2 ± 12.2 mm Hg, which was significantly greater than in the placebo group (1.5 ± 12.4 mm Hg). In addition, in the liraglutide group there was a more pronounced improvement in cardiometabolic parameters such as blood lipids, high-sensitivity C-reactive protein, plasminogen activator inhibitor-1 and adiponectin compared to placebo.

The 56-week SCALE Weight Maintenance study, conducted at 36 study sites and involving 422 patients, assessed the effectiveness of liraglutide 3 mg in maintaining weight after weight loss with a low-calorie diet in patients with obesity or overweight in combination. with dyslipidemia and/or hypertension. During the introductory period lasting from 4 to 12 weeks, diet therapy was administered (daily calorie intake 1200-1400 kcal) and increased physical activity was recommended (fast walking for at least 150 minutes per week). After a run-in period, patients achieving a weight loss of 5% or more were randomized 1:1 to receive liraglutide 3 mg or placebo for 56 weeks. With the use of liraglutide at a dose of 3 mg, the additional reduction in body weight averaged 6.2% (0.2% with placebo). Among those receiving liraglutide 3 mg, the proportion of participants who maintained their 5% or more weight loss during the run-in period was significantly higher (81.4%) than in the placebo group (48.9%). After completing the study for 12 weeks, in the group of patients receiving liraglutide 3 mg, the achieved reduction in body weight was maintained (by 4.1%), while among patients receiving placebo, weight gain was observed (+0.3%) [14] . Thus, the effectiveness of liraglutide at a dose of 3 mg 1 time per day in combination with lifestyle changes was confirmed in relation to the long-term maintenance of clinically significant weight loss. In addition, liraglutide 3 mg reduced some cardiovascular risk factors (waist circumference, fasting plasma glucose, blood pressure, etc.).

The 56-week SCALE Diabetes study, conducted at 126 clinical sites in 9 countries and involving 846 patients, assessed the effectiveness of different doses of liraglutide (3 and 1.8 mg) on ​​weight loss in patients with type 2 diabetes. At the end of the study, the decrease in body weight was 6.1% at a dose of 3 mg, 4.7% at a dose of 1.8 mg, and 1.9% at placebo. The number of patients achieving weight loss of 5% or more was also significantly higher in the group of patients taking liraglutide 3 mg. The proportion of patients who achieved an HbA1c level of <7% during treatment with liraglutide 3 mg was 69.2% (compared to 27.2% on placebo) [15].

In the SCALE Sleep Apnea Study, a 32-week study conducted at 40 clinical sites, 359 obese patients with moderate to severe obstructive sleep apnea were randomized 1:1 to receive either liraglutide 3 mg or liraglutide 3 mg. or placebo. In the main group, along with a more significant reduction in body weight (by 5.7% from the initial level compared to 1.6% on placebo), it was possible to achieve a more significant reduction in the apnea/hypopnea index (-12.2 episodes/hour compared to –6.1 episodes/hour on placebo) [16].

Thus, these clinical research programs demonstrated the high effectiveness of liraglutide at a dose of 3 mg in relation to weight loss and retention of achieved results in obese and overweight individuals, regardless of the presence of type 2 diabetes and other concomitant diseases. This was accompanied by a significant reduction in cardiovascular risk with a good tolerability and safety profile.

According to the instructions, the drug is administered subcutaneously once a day at any time, regardless of food intake, in the abdomen, thigh or shoulder. The initial dose is 0.6 mg per day. The dose is increased by 0.6 mg at intervals of at least one week to improve gastrointestinal tolerability until a therapeutic dose of 3 mg per day is achieved. If there is no reduction in body weight by 5% of the initial value within 12 weeks, treatment is stopped. Side effects include primarily dyspeptic symptoms (decreased appetite, nausea, vomiting, constipation, diarrhea), which usually occur in the first weeks of treatment and in most cases are transient in nature, without requiring discontinuation of therapy.

Because liraglutide may induce medullary thyroid cancer in rodents, the drug is contraindicated in patients with a history of medullary thyroid cancer or multiple endocrine neoplasia syndrome type 2. In case of obesity and in cases of pronounced loss of body weight, the concentration of cholesterol in the bile increases and the contractile function of the gallbladder decreases (which increases the risk of gallstone formation); patients with a history of cholelithiasis should be prescribed liraglutide with caution.

Drugs not registered on the Russian pharmaceutical market

In Europe and the USA, other drugs are used to treat obesity, which are not currently registered in Russia.

Lorcaserin

- agonist of 5HT2c serotonin receptors, reducing appetite. The drug is approved for use in the USA, rejected in the European Union. The effectiveness and safety of the drug was assessed in the BLOOM, BLOOM-DM and BLOSSOM studies, which showed a decrease in body weight after a year of treatment by an average of 3.6% and an improvement in metabolic parameters. There were no statistically significant differences in the incidence of cardiac valvulopathy between the placebo and lorcaserin groups. The most common side effects of lorcaserin were decreased vision, dizziness, drowsiness, headache, and gastrointestinal disorders. Results from the ongoing CAMELLIA TIMI 61 cardiovascular outcomes study will determine the role of lorcaserin in the primary prevention of type 2 diabetes in overweight or obese individuals and the feasibility of this drug in those at high cardiovascular risk [17].

Combination of phentermine and topiramate

used to achieve an effect with less toxicity of drugs. Phentermine, being an atypical amphetamine analogue and sympathomimetic, suppresses appetite at the central nervous system level. Topiramate is an anticonvulsant whose mechanism of action on appetite may involve reducing carbanhydrase activity or modifying the effect of gamma-aminobutyric acid. The efficacy and safety of the combination drug were assessed in the EQUIP, CONQUER, SEQUEL and EQUATE studies. Average weight loss ranged from 6.6% to 8.6% over 1 year. Adverse effects included dry mouth, constipation, insomnia, palpitations, dizziness, paresthesia, disturbances in attention, metabolic acidosis and kidney stones, headache, taste disturbances, alopecia and hypokalemia. Treatment is contraindicated during pregnancy due to possible teratogenic effects [17].

In combination with bupropion

with
naltrexone,
the first agent is a selective norepinephrine and dopamine reuptake inhibitor used in the treatment of depression and nicotine addiction. Naltrexone, an opioid receptor antagonist, is widely used in the treatment of alcohol and opiate addiction. The anorexigenic effect of the bupropion/naltrexone combination may be a consequence of the activation of neurons in the arcuate nucleus of the hypothalamus and the release of α-melanocyte-stimulating hormone. The effectiveness and safety of the drug were assessed in the COR-I, COR-II, COR-BMOD and COR-DM studies. The average weight loss over 1 year of therapy was 4.8%. The most common side effects when taking the combination drug were nausea, vomiting, headache, dizziness, and insomnia [17].

Indications

This drug has a very limited list of indications. It is prescribed for certain conditions:

• overweight;
• obesity;
• metabolic syndrome.

Orlistat is also taken to consolidate the achieved result after losing a little weight. The medicine does not allow the extra pounds to return.

This drug can be taken by patients who are strictly following a moderate calorie diet. Due to excessively high-calorie foods in the diet, the medicine may not work.

Side effects

Orlistat causes many side symptoms from different organs and systems:

• frequent bowel movements;
• fat in stool;
• flatulence;
• oily discharge from the anus;
• urgency and fecal incontinence;
• seizures (in patients with epilepsy);
• symptoms of hypothyroidism;
• dizziness;
• insomnia or increased sleepiness;
• headache;
• anxiety;
• skin rash;
• abdominal pain;
• pancreatitis;
• renal failure;
• allergy.

Additional medications may be needed to manage side effects. During the course of taking the drug, it is advisable to wear absorbent pads or diapers for adults.

Contraindications

The drug is contraindicated in patients suffering from certain diseases:

• impaired absorption of certain substances - malabsorption syndrome;
• excessive sensitivity to components;
• calcium oxalate kidney stones (nephrolithiasis);
• excess oxalates in the urine (hyperoxaluria);
• stagnation of bile (cholestasis);
• periods of pregnancy and lactation;
• age less than 18 years.

It is prohibited to take Orlistat simultaneously with anticoagulants, including warfarin, as well as sitagliptin and cyclosporine.

This substance should be taken with great caution by patients with kidney, liver and gallbladder diseases.

In case of an overdose, you need to temporarily stop drinking this drug, then the body will quickly return to normal. The patient should be monitored during the first 24 hours after overdose symptoms, which manifest themselves in the form of gastrointestinal disturbances.

Interaction with other drugs

This drug reduces the effectiveness of many other medications. The absorption of the following substances is reduced:

• vitamin K (by 30%);
• vitamin E (α-tocopherol);
• vitamin A (β-carotene);
• fat-soluble vitamin D;
• antiepileptic drugs;
• contraceptives;
• iodine;
• levothyroxine sodium.

As a last resort, you can take a multivitamin complex before bed or no earlier than 2 hours after Orlistat.

This medicine should not be taken together with cyclosporine, warfarin, or amiodarone. It suppresses the effect of antipsychotics, antidepressants and antiretroviral drugs against HIV infection.

Additional Information

Conflict of interest.

The authors declare that there are no obvious or potential conflicts of interest related to the publication of this article.

Author contributions:

E.A. Troshina - development of the concept of the manuscript, analysis of foreign and Russian literature, editing of the manuscript; E.V. Ershova - analysis of foreign and Russian literature, writing a draft of the manuscript, preparing the final version of the manuscript.

Information about authors

* Ershova Ekaterina Vladimirovna

, Ph.D. ; address: Russia, 117036, Moscow, Dm street. Ulyanova, 11 [address: 11 Dm. Ulyanova street, Moscow, 117036, Russia]; ORCID: https://orcid.org/0000-0002-6220-4397; eLibrary SPIN: 6728-3764; e-mail

Troshina Ekaterina Anatolevna

, Doctor of Medical Sciences, Corresponding Member. RAS, professor; ORCID: https://orcid.org/0000-0002-8520-8702; eLibrary SPIN: 8821-8990; e-mail

Can pregnant women take it?

These capsules should not be taken by pregnant or nursing mothers. Because of this drug, the amount of fat-soluble vitamins in the body decreases, and this can have an extremely negative impact on the health of the unborn child. It is during pregnancy that it is vital to take enough vitamins. This primarily concerns B vitamins, especially folic acid (B9). They are necessary for the formation of the child’s nervous system. You should also not take Orlistat while breastfeeding.

Instructions for use

A leaflet is included with each Orlistat package. Strict adherence to the manufacturer's dosage recommendations allows you to reduce the risk of developing a negative reaction from the body and achieve good results in terms of weight loss. It is equally important to follow the advice of doctors regarding increasing the effectiveness of excess weight therapy with the drug.

Reception scheme

The medicine is intended for oral administration. The rules of use are as follows:

• A single dose for an adult is 120 mg.
• It is recommended to take 3 capsules of 120 mg per day.
• Capsules are consumed during meals or an hour after, with plenty of water.
• Do not chew or open capsules.

Important! You can skip taking the medication if the daily menu contains a critically small amount of fat, since the effect of the active substance begins only in the presence of enzymes in the digestive tract.

If for any reason a meal was missed, you do not need to drink the capsule of the medicinal product. It is not advisable to increase the dosage at the next dose, since this will not lead to an increase in the effect, but may have a negative impact on well-being.

The optimal duration of a weight loss course is about three months (any shorter duration is likely to be a waste of time). However, doctors draw the attention of those losing weight to the fact that better results can be achieved by taking the drug for a period of 6 to 12 months. The maximum duration of the course is 2 years.

If a medication has not shown its effectiveness for several months, losing weight with its help is considered pointless.

Nutrition

Better results can be achieved by combining Orlistat with a low-calorie diet. For women, the daily calorie intake should not exceed 1300 kcal, for men – 1500 kcal. With a simultaneous increase in physical activity, the indicators can be raised to 1500 and 1700, respectively.

The following products should be present in the diet:

• low-fat varieties of fish and meat (up to 150 grams daily);
• vegetables with a low glycemic index (celery, cucumbers, cabbage, bell peppers, beets);
• cereals (especially pearl barley and buckwheat);
• low-fat fermented milk and dairy products (can be consumed in their pure form or used for preparing dietary dishes);
• sweet and sour berries and fruits;
• bran bread or wholemeal bread;
• drinks in the form of unsweetened tea, compote (from homemade fruit, without sugar), water (at least 2 liters per day).

Salt should be limited throughout the entire period of weight loss. To improve efficiency, you will also have to abstain from alcohol.

Important! Orlistat affects the absorption of fat-soluble vitamins, therefore, while taking it, it is advisable to take multivitamin complexes with vitamins A, D, E, etc. Vitamins should be taken before taking medicinal capsules, preferably several hours before.

Side effects and complications

Capsules have a direct effect on the functioning of the stomach. Since treatment takes place over a long period, general well-being often suffers. The most likely side effects when taking Orlistat are:

• increased gas formation;
• greasy stools (greasy stains on underwear);
• inability to control the urge to defecate.

It is not difficult to explain their development - the problem is poor absorption of fats. Typically, such side effects go away on their own as soon as the body gets used to the drug. However, there are more complex cases. So, the following symptoms require immediate medical attention:

• headache and fever;
• sore throat, cough;
• chills;
• runny nose and nasal congestion;
• dental caries, bleeding gums;
• urinary tract infections;
• signs of liver damage: loss of appetite, dark urine, yellowing of the skin and eyes, nausea, weakness, light-colored stools, excessive fatigue for no apparent reason.

Signs that can be attributed to complications of losing weight on medication require an immediate call to the ambulance:

• allergic rash, urticaria;
• labored breathing;
• swelling of the face, throat, lips or tongue.

In fact, complications during therapy with the drug are very rare, so we can say that the benefits of its use outweigh the risks. However, if side effects persist for a long time and cause serious discomfort, you should consult your doctor. Perhaps the drug product is being taken in the wrong dosage or it is better to use another remedy.

Contraindications

Losing weight with this medication product is not recommended in the following cases:

• hypersensitivity to components;
• age up to 16 years;
• chronic malabsorption syndrome (impaired absorption in the digestive system);
• nephrolithiasis;
• hyperoxaluria;
• cholestasis (stagnation of bile).

Pregnant and breastfeeding women should also avoid taking the drug, especially without a doctor's prescription. This can be dangerous for the child!

Drug interactions

Orlistat affects not only the absorption of vitamins - the situation is similar with beta-carotene from dietary supplements. The simultaneous use of the drug with Cyclosporine, levothyroxine sodium (hypothyroidism may develop), Warfarin and Acarbose is not recommended. The time interval between the use of these agents and Orlistat should be from 2 to 4 hours.

Women who are simultaneously losing weight on anti-obesity medication and taking birth control pills should consider additional methods of contraception. Since the drug causes diarrhea, the concentration of hormonal contraceptives in the blood is likely to decrease.

Important! Orlistat does not react with alcohol, which makes it possible not to impose a strict ban on the use of the latter (this is necessary solely for more rapid weight loss), and does not affect concentration, due to which it can be used when driving a vehicle.

Storage conditions

The instructions for use of Orlistat say that it is recommended to store capsules in a cool, dry place, and, equally important, out of the reach of children. After the expiration date stated on the packaging, the capsules cannot be taken.