Xenical and alcohol - their compatibility causes concern among people taking the drug. The drug is recommended to be taken for obesity in order to reduce excess weight. It is consumed over a long period, so there is no protection from various holidays and events that may occur at this time. In our culture, it is customary to celebrate special occasions with alcohol. Therefore, the issue of drug interaction with alcohol worries people planning to begin treatment for obesity. The answer to this can be read in our article.

Xenical - characteristics of the drug

Whether you can take any medication with alcohol depends on the composition of the medicine. Therefore, let’s first consider what components are present in the drug:

1. Orlistat is the main active ingredient, soluble in ethanol, but practically does not interact with water.
2. Primogel or, in other words, sodium carboxymethyl starch. The substance efficiently and quickly adsorbs liquids, increasing in size.
3. Microcrystalline cellulose is a natural polymer. It is a dietary fiber that helps cleanse the body.
4. Polyvinylpyrrolidone, or povidone, is used as a binder for tablets.

Talc and titanium dioxide, gelatin, and indigo carmine for the shell are also used as excipients.

Xenical helps you lose weight due to its ability to block lipase. This is an enzyme that promotes the absorption of fats. The drug simply does not allow the body to absorb them, but removes them. Thanks to this, fats are not absorbed, and weight is reduced.

The drug is available in the form of hard gelatin capsules. You cannot buy it without a doctor's prescription. And this is correct - taking it uncontrollably is dangerous, since the medication has contraindications and side effects.

The effectiveness of the drug in obesity

Xenical underwent clinical trials on overweight patients. As a result, it was revealed:

1. Obese patients lost weight faster during treatment than people undergoing diet therapy. The first results of taking the medication were noted in the middle of the second week.
2. Patients suffering from obesity and type 2 diabetes lost weight more effectively than those who used diet alone. Moreover, they observed an improvement in glycemic indicators, a decrease in insulin resistance and the dosage of hypoglycemic agents.
3. In the case of pubertal obesity, along with weight loss, a decrease in body volume was observed. The subjects' waist and hip circumferences became smaller.

During studies of the effect of Xenical, many patients experienced a decrease in blood pressure and a decrease in metabolic risk factors. The active ingredient of the drug is also effective in preventing re-obesity.

How to take Xenical

The drug can be prescribed to patients with excess body weight. The medication is also recommended for patients with obesity and type 2 diabetes. Prescribed during long-term therapy in conjunction with a moderately hypocaloric diet.

Contraindications for this treatment:

• cholestasis;
• chronic malabsorption syndrome, in which pathology of intestinal functions is observed;
• sensitivity to the components of the drug, including substances included in the shell.

Since no studies have been conducted on the effect of the drug on pregnant women and the fetus, this medicine should not be prescribed to expectant mothers. For the same reason, it is not recommended to take the product during breastfeeding and for children under 12 years of age.

There are a number of side effects caused by the use of Xenical:

The frequency of side effects from the gastrointestinal tract increases with increasing fat content of the diet. Therefore, during therapy you should adhere to a diet. It consists of reducing the fat content in foods. This reduces the risk of unpleasant complications.

Is it possible to combine the drug with alcohol?

The instructions for the medicine contain no contraindications to drinking alcohol during therapy. This means that Xenical does not interact with ethyl alcohol. Alcohol does not affect the effectiveness of the active component, and it, in turn, does not interfere with the absorption of ethanol into the blood. Therefore, drinking alcohol during therapy is not prohibited.

However, there are several points that indicate the undesirable consequences of combining the drug with alcohol consumption:

Everyone decides the issue of combining medicine and alcohol individually. Definitely people who are concerned about their own health will not do this.

Consequences of combining Xenical and alcohol for the gastrointestinal tract

The effect of using the drug for weight loss is similar to the effects of taking laxatives. The most active manifestations can be noticed at the initial stage of treatment. The reaction of the gastrointestinal tract is manifested in the following symptoms:

• loose stools;
• fatty inclusions are observed in the stool;
• pain in the lower back and lower abdomen;
• increased gas formation, accompanied by intestinal secretions;
• irresistible frequent urge to defecate;
• uncontrollable discharge from the anus with fatty inclusions.

When drinking alcohol, ethanol also has an effect on the gastrointestinal tract. Alcohol irritates the walls of the stomach and intestines, increasing the negative effects of the drug. How is it shown:

• strengthening the process of peristalsis;
• producing large amounts of mucus;
• formation of inflammatory processes;
• the appearance of hernia-like formations in the intestines;
• Bleeding may occur in the intestines.

You can notice a direct relationship with the amount of fat consumed while taking the drug with the intensity of oily secretions. Drinking alcohol often causes loose stools. It relaxes muscles, reduces concentration, dulls reflexes and reactions. Usually it is not difficult for a person to restrain himself from the urge to defecate. If you take the drug at the same time, it can be difficult. As a result, you can end up in a very awkward situation.

What happens to metabolic processes

The accumulation of excess weight is largely a consequence of impaired and slow metabolism. At the same time, metabolic processes are inhibited, and the load on the heart and blood vessels increases. Metabolism is expressed in the rate of processing of food entering the body. In this case, many chemical processes occur that ensure human life.

What happens in the body if you take alcohol and Xenical:

1. The use of the drug does not affect metabolism in any way. Its effectiveness is associated with the exclusion of the process of absorption and assimilation of fats.
2. Alcoholic drinks help slow down your metabolism. The rate of ethanol oxidation directly depends on metabolism. Therefore, the breakdown of alcohol in obese people takes much longer.
3. Ethanol is recognized by the human body as a poison, to eliminate which all reserves are mobilized. At the same time, other reactions and processes are suspended, including blocking lipase. Because of this, fat is not removed, but accumulates.

Looking at alcoholics, some people don't understand why most of them are thin. It's all about an insufficient diet, which drinkers replace by drinking alcohol. The lack of normal balanced food does not replenish expended energy. However, such thinness only harms your health. Alcohol abuse leads to mental and physical disorders.

A person must decide what is more important: normalizing weight using Xenical or drinking alcohol. If the latter, then you don’t have to start taking the drug. The effect will be either minimal or completely zero.

Xenical is classified as a pharmaceutical drug intended for weight loss, that is, for the treatment of obesity.

Drugs that are designed for weight loss and are designed to control weight or reduce it to normal levels.

Mechanism of action

• weight regulation by reducing appetite;
• activation of general metabolism;
• regulation of calorie absorption.

Orlistat is a white crystalline powder, insoluble in water, easily soluble in methanol and ethanol. Refers to inhibitors of gastrointestinal lipases. It does not penetrate into the bloodstream, therefore it has no systemic effect on the body. Metabolism occurs in the intestine with the formation of inactive metabolites. It is excreted unchanged (up to 83%) in feces (97%). Complete elimination occurs after five days.

Pharmacological group

Refers to gastrointestinal lipase inhibitors

Description of the drug

The dosage form is available in the form of hard gelatin opaque capsules, turquoise with the inscription “XENICAL 120” in black, the “ROCHE” logo on the cap; White pellets are in capsules.

Active substance

Each capsule contains 120 mg orlistat

Excipients – microcrystalline cellulose – 93.6 mg, sodium carboxymethyl starch (Primogel) – 7.2 mg, povidone K-30 – 12 mg, sodium lauryl sulfate – 7.2 mg. – .

pharmachologic effect

Possessing high lipophilicity, the active substance quickly interacts with fat droplets and inactivates lipase centers (pancreatic and gastric). Since lipases are inhibited as a result of entering the body, the ability of triglycerides to penetrate into the bloodstream is lost.

The result is a lack of energy and, as a result, active mobilization of lipids from the depot and a decrease in body weight due to the loss of the viscero-abdominal fat layer.

Reduces the amount of free fatty acids and monoglycerides in the body and the solubility of cholesterol, which cannot properly penetrate into the bloodstream after Orlistat enters the body.

It also helps to normalize the lipid composition of the blood, which significantly increases the sensitivity of tissue cells to insulin. Hyperinsulinemia also leads to a decrease in body fat.

Clinical trials have shown that taking drugs containing Orlistat, in recommended doses, leads to weight loss 52 weeks after the start of regular use. A weight reduction of 6.2% from baseline was reported. At the same time, a decrease in insulin by 18% was observed.

Indications

The main indication is the treatment of obesity.

Clinical trials have confirmed the effectiveness of the drug in the treatment of patients with a body mass index exceeding 30 kg/m2. The presence of a number of concomitant diseases in such patients in the vast majority of cases makes the treatment of obesity problematic.

Obese patients had:

• hyperlipidemia;
• persistent arterial hypertension;
• metabolic syndrome;
• diabetes.

Xenical has shown a therapeutic effect, especially in combination with regular dosed physical activity, selected in the form of special therapeutic exercises.

The medicine is recommended for use as part of complex treatment measures for obese patients, provided they follow a special diet. Nutrition should be balanced, regular, contain a sufficient amount of vitamins, microelements, minerals, but at the same time have low calorie content. The amount of fat supplied with food should not exceed 30%.

For patients suffering from metabolic syndrome (prediabetes) and diabetes mellitus, who are overweight with an index of more than 30 kg/m2, it is possible to use Xenical together with hypoglycemic drugs (metformin), insulin and sulfonylurea derivatives in the dosages that were prescribed by the doctor before treatment.

Important! Obesity is the result of an imbalance in human energy balance. It is possible to balance the energy balance only when the amount of food consumed completely covers the body’s energy needs. Excess body weight appears when the amount of food consumed increases with low physical activity, when energy expenditure is not high.

If little food is eaten, but weight gain still occurs, doctors talk about reducing energy costs. In such cases, it is recommended to increase physical activity.

Contraindications

Like any other medicine, Xenical has its contraindications:

• cholestasis (stagnation of bile);
• chronic absorption disorders (malabsorption);
• increased individual sensitivity to the components of the dosage form.

The use of the drug is not recommended for pregnant and lactating women, elderly and senile patients, and children under 12 years of age. There is currently no information on clinical studies of the safety of the drug for these groups of patients.

Directions for use and doses

The medicine can be used for a long time, orally.

Attention! You do not need to take more than one capsule at a time. You do not need to take more than three capsules per day. Exceeding the dosage will not increase the effectiveness of the drug, will not contribute to greater weight loss and reduce the time of therapy.

Side effects

Most of the side effects that may develop when taking the drug relate to the gastrointestinal tract. This is explained by the mechanism of action of orlistat, which blocks the absorption of fats.

The main side effects include:

• flatulence;
• discharge of oily secretions and fat with feces (steatorrhea);
• increased frequency of bowel movements;
• fecal incontinence;
• discomfort in the epigastric area;
• heaviness in the stomach;
• pain of varying intensity in the abdomen;
• menstrual irregularities in women;
• headache.

In patients with diabetes mellitus, a decrease in blood glucose levels is possible, which is confirmed by laboratory tests.

Attention! When eating fatty and high-calorie foods, the incidence of side effects increases. Side effects often develop at the beginning of treatment; over the next one to two to three months of therapy they gradually decrease. The occurrence of side effects that are not hazardous to health does not serve as a reason to discontinue the drug.

Side effects that are less common include:

• infectious diseases of the respiratory tract;
• urinary tract infections;
• damage to the mucous membrane of the gums;
• tooth damage;
• increased fatigue and anxiety;
• inflammation of the pancreas (isolated cases);
• diverticulitis (extremely rare);
• hepatitis (isolated cases);
• nephropathy (extremely rare);
• allergic reactions in the form of rash, bronchospasm, laryngeal edema, in rare cases, anaphylactic shock requiring immediate medical attention.

Isolated cases of bleeding from the rectum have been described.

Special instructions for doctors and patients

It is possible to take Xenical simultaneously with:

• with oral contraceptives;
• with statins;
• with cardiac glycosides;
• fibrates;
• warfarin.

Compatible with alcoholic beverages and preparations containing ethanol. Before taking alcohol-containing medications and Xenical, consultation with a doctor is required.

Helps reduce the absorption of fat-soluble multivitamins in the intestines and reduces their therapeutic effect, therefore vitamins must be taken two to three hours after taking the drug, preferably at night.

It should not be taken by patients with epilepsy, since antiepileptic drugs and Xenical increase the incidence of seizures.

For patients with diabetes mellitus who take Xenical to reduce excess body weight, constant monitoring by their physician and laboratory diagnostic measures to control blood glucose levels are recommended. With regular use of the drug in patients with diabetes, blood sugar levels often decrease and this requires a reduction in the dosage of medications that lower glucose.

Xenical is taken only as prescribed by a doctor. Before the course of treatment, a comprehensive examination of the body is recommended in order to clarify the diagnosis, including laboratory and diagnostic studies of the body.

Vacation in the Russian Federation is by doctor's prescription.

Overdose

To date, no cases of overdose have been reported.

Clinical studies have shown that in patients without excess body weight and patients with any degree of obesity, a single dose of 800 mg or taking the drug several times in doses of 400 mg for fifteen days did not cause the development of side effects. Cases have been reported of taking Xenical 240 mg three times a day for six months in obese patients. In these cases, there is also no evidence of any undesirable consequences.

INattention! In case of severe overdose, medical supervision is necessary for 24 hours. According to data obtained from studies in humans and animals, any systemic effect that can be associated with the lipase-inhibitory properties of the drug is quickly reversible.

History of the creation of drugs for weight loss

Attempts to come up with an effective and safe means for losing weight were made in ancient times.

2nd century AD. Documented facts date back to the second century AD and are associated with the Greek physician Soranus of Ephesus, who made an elixir for weight loss. The product contained laxatives and body cleansing components. The complex of treatment procedures, according to the doctor, should have included massage, physical exercise and treatment with high temperatures. Interestingly, this technique was used until 1930.

1920-1930s. To treat obesity, they began to use thyroid hormone, which was used to treat hypothyroidism. The treatment was effective, but was used for people who did not suffer from hypothyroidism, and therefore had a number of side effects related to the functioning of the thyroid gland. After the course of treatment, persistent insomnia and attacks of tachycardia appeared.

1933 The emergence of DNP - dinitrophenol, which had a serious, in addition to some not so dramatic, side effect in the form of an increase in body temperature to high levels and was often fatal. The mechanism of action of dinitrophenol was based on the uncoupling of biological processes (ATP synthesis and oxidative phosphorylation in cellular mitochondria). This produced heat instead of ATP. By the early 1940s, dinitrophenol was no longer used.

Late 1930s Amphetamines for weight loss have appeared on the market under the trade name Benzedrine. The mechanism of action of Benzedrine was to suppress appetite. Many were also impressed by the accompanying pleasant effect of the drug – increased physical activity.

Amphetamines, which were considered very effective for weight loss, became very popular. Benzedrine was used in combination with other drugs, calling the whole set “rainbow-colored pills.” “Rainbow” pills were taken in incredible quantities throughout the day.

Courses of “treatment” prescribed by doctors included taking a wide variety of stimulants: amphetamines, thyroid hormones, various diuretics, digitalis, laxatives, and even barbiturates. The latter were prescribed to reduce the numerous side effects of stimulant components.

1967-1968. The craze for amphetamines and “rainbow-colored pills” did not pass without consequences. Reports of deaths began to emerge, prompting the Senate to decide to investigate. This led to a sharp limitation in the sales of weight loss drugs available at that time.

1979 The US Food and Drug Administration prohibits the use of amphetamine in any pharmacological form intended to treat obesity.

Interestingly, in 1959 the same Office gave permission for the use of phentermine; fenfluramine was approved for use in 1973. Phentermine and fenfluramine did not become widespread until reports of their effectiveness emerged in 1992. It was claimed that when taking the drugs, weight is reduced by 10% with the effect maintaining for more than two years.

The first serious drug for weight loss is Fen-Phen, most often prescribed by doctors.

1990s. The emergence of Dexenfluramine (Redux) as an alternative to fenfluramine. Dexenfluramine had fewer adverse effects.

1996 Obtaining a registration number for Dexfenfluramine. There are reports of a serious side effect - the development of pathologies of the heart valves (up to 30% of those using the drug).

1997 Prohibition of Fen-Phen and Dexfenfluramine.

2004 Ban on the drug Ephedra in the USA. Ephedra caused the development of arterial hypertension, which led to strokes (bleeding in the brain) and death.

Generic research

Generic is a bioequivalent copy of the original drug. In research by scientists A. Schneider, L.A. Wessjohann, conducted in 2009, studied therapeutic equivalence, which is the most important component of the issue of generics.

The task of analytical chemistry is to compare the impurity profiles of the original drug and the generic drug. Such studies always require increased attention, since differences in the composition of the impurities of the original drug and the generic undoubtedly affect the therapeutic qualities.

Schneider and L.A. Wessjohann examined the impurity profiles of Xenical, manufactured by F. Hoffmann-La Roche Ltd., Switzerland, and two generics - CobeseTM, Ranbaxy Laboratories Limited, manufactured in India and Orsoten, KRKA, manufactured in Russia - Slovenia. The study was carried out using high-performance liquid chromatography and tandem mass spectrometry. Impurities were removed after dissolving the sample in ethanol, and the study showed:

Preparations Kobesa and Orsoten. The impurity profiles are similar to each other.

Preparations Kobesa and Orsoten and Xenical. The impurity profiles of Kobesa and Orsoten are very different from the original Xenical.

The number of impurities in the original drug and generics. Xenical had three impurities, Kobes – 14, Orsotena – 13.

Conclusion: even a slight difference between the original drug greatly changes three qualities:

• pharmacokinetics;
• bioavailability;
• safety.

A change in the three components can cause an allergic reaction and manifestations of intoxication.

Researchers have discovered oxidation products in generics. This indicates a difference in production technology in the manufacture of dosage forms.

In our case, we are talking about the so-called semi-enzymatic method in the manufacture of generics. This technology indicates problems with drug stability (eg storage).

Information on the research was presented in December 2009 in Moscow, at the All-Russian conference “Modern methods of chemical analytical control of pharmaceutical products.”

Manufacturer

Xenical ® , F.Hoffmann-La Roche Ltd. (Switzerland)

Main analogues

• Alay, Germany
• Xenistat, India, UK
• Orlikel, India
• Orlip, Georgia
• Orlistat, Syria
• Orsoten, Russia
• Symmetra, India

Trials of the drug and its prevalence in Europe and the USA

Xenical (Orlistat), as a weight loss agent, was first introduced by Swiss pharmacists. The entire development was undertaken by the oldest reputable company F.Hoffmann-LaRoche Ltd.

The company set itself a difficult goal back in the second half of the last century - to study the problems of safe weight loss and create a drug that would successfully treat obesity, have a minimum of side effects and contraindications, and have a lasting effect.

For a long time, Swiss pharmacologists have been studying in practice the process of metabolism and redistribution of fats in the human body.

It was decided to suppress certain enzymes that help absorb fat, which in turn leads to a reduction in the viscero-abdominal fat layer.

In 1985, with the help of the microorganism Streptomyces toxytricini, scientists were able to isolate the so-called lipstatin, and then synthetic tetrahydrolipstatin. The new drug was given the name Orlistat, or Xenical - from the name of the brand.

The anti-obesity drug trial was very serious. During the study, the effects of Xenical were tested on over four thousand people. This drug is still considered one of the most studied and safest to use.

In the initial period of its production, Orlistat was dispensed only as prescribed by doctors after a thorough examination of the patient. This drug group is now available without a prescription in the United States. In Russia, a prescription is still required to purchase Xenican.

Dear visitors of the Farmamir website. This article does not constitute medical advice and should not serve as a substitute for consultation with a physician.

21 pcs in a blister, 1, 2 or 4 blisters in a cardboard pack.

Description of the dosage form

Capsules: hard gelatin capsules No. 1, opaque, turquoise. On the body there is the inscription “Xenical 120”, on the cap - “ROCHE”, black.

Capsule contents: pellets are white or almost white.

pharmachologic effect

Pharmacodynamics

Xenical is a specific 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 the drug, the fat content in feces usually returns to the level before the start of therapy within 48-72 hours.

Pharmacokinetics

Suction

In volunteers with normal body weight and obesity, systemic exposure to the drug is minimal. 8 hours after oral administration of the drug, unchanged orlistat could not be determined in plasma, which means that its concentrations are below the level of 5 ng/ml.

In general, after taking therapeutic doses, it was possible to detect unchanged orlistat in plasma only in rare cases, and its concentrations were extremely low (<10 нг/мл или 0,02 мкмоль). Признаки кумуляции отсутствовали, это подтверждает, что всасывание препарата минимально.

Distribution

The volume of distribution cannot be determined because the drug 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

Based on animal data, orlistat is metabolized primarily in the intestinal wall. In a study in obese individuals, it was found that approximately 42% of the minimal fraction of the drug that is subject to systemic absorption 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 β-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 and 108 ng/ml, respectively) after therapeutic doses, these metabolites are considered pharmacologically inactive.

Removal

Studies in individuals with normal and overweight have shown that the main route of elimination is excretion of unabsorbed drug in the feces. About 97% of the administered dose of the drug was excreted in the feces, 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 the drug is completely eliminated from the body (with feces and urine) is 3-5 days. The ratio of orlistat elimination routes in volunteers with normal and overweight was the same. Both orlistat and metabolites M1 and M3 can be excreted in 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 the drug. Daily fecal fat excretion was 27% of dietary intake with orlistat and 7% with placebo.

Indications for the drug Xenical ®

long-term therapy for obese or overweight patients, incl.

having risk factors associated with obesity, in combination with a moderately hypocaloric diet;

in combination with hypoglycemic drugs (metformin, sulfonylureas and/or insulin) or a moderately hypocaloric diet in patients with type 2 diabetes mellitus who are overweight or obese.

Contraindications

hypersensitivity to the drug or any other components contained in the capsule;

chronic malabsorption syndrome;

cholestasis.

In animal reproductive toxicity studies, no teratogenic or embryotoxic effects of the drug were observed. In the absence of a teratogenic effect in animals, a similar effect in humans should not be expected. However, due to the lack of clinical data, Xenical should not be prescribed to pregnant women.

The excretion of orlistat into breast milk has not been studied and should not be taken during breastfeeding.

Side effects

The following categories are used to describe the frequency of adverse reactions: very often (≥1/10), often (≥1/100,<1/10), нечасто (≥1/1000, <1/100), редко (≥1/10000, <1/1000) и очень редко (<1/10000), включая отдельные случаи.

Adverse reactions to orlistat occurred mainly from the gastrointestinal tract and were due to the pharmacological effect of the drug, which interferes with the absorption of dietary fats. Very often, phenomena such as oily discharge from the rectum, the release of gases with some discharge, an imperative urge to defecate, steatorrhea, increased frequency of bowel movements, loose stools, flatulence, pain or discomfort in the abdomen were noted.

Their frequency increases with increasing fat content in food. Patients should be informed of the possibility of gastrointestinal adverse reactions and taught how to manage them through better diet, especially regarding the amount of fat contained in the diet. Adopting a low-fat diet reduces the likelihood of gastrointestinal side effects and thereby helps patients control and regulate their fat intake.

As a rule, these adverse reactions are mild and transient. They occurred in the early stages of treatment (in the first 3 months), and most patients had no more than one episode of such reactions.

When treated with Xenical, the following adverse events from the gastrointestinal tract often occur: “soft” stools, pain or discomfort in the rectum, fecal incontinence, bloating, dental damage, gum damage.

Also noted very often were headaches, upper respiratory tract infections, flu; often - lower respiratory tract infections, urinary tract infections, dysmenorrhea, anxiety, weakness.

Rare cases of allergic reactions have been described, the main clinical symptoms of which were itching, rash, urticaria, angioedema, bronchospasm and anaphylaxis.

Very rare cases of bullous rash, increased activity of transaminases and alkaline phosphatase, as well as isolated, possibly serious, cases of hepatitis have been described (a cause-and-effect relationship with taking Xenical or pathophysiological mechanisms of development have not been established).

With the simultaneous administration of Xenical and anticoagulants, cases of decreased prothrombin and increased INR have been reported.

Cases of rectal bleeding, diverticulitis, pancreatitis and cholelithiasis have been reported (incidence unknown).

In patients with type 2 diabetes mellitus, the nature and frequency of adverse events were comparable to those in individuals without diabetes mellitus with overweight and obesity. The only new adverse effects occurring at an incidence of >2% and ≥1% compared with placebo were hypoglycemic conditions (which may have resulted from improved carbohydrate compensation) and abdominal bloating.

Interaction

No interaction detected with amitriptyline, atorvastatin, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, pravastatin, warfarin, nifedipine GITS (gastrointestinal therapeutic system) and nifedipine slow release, sibutramine or alcohol(based on drug interaction studies). However, it is necessary to monitor INR values ​​during concomitant therapy with warfarin or other oral anticoagulants.

When taken simultaneously with Xenical, a decrease in absorption was noted vitamins A, D, E, K and beta-carotene. If multivitamins are recommended, they should be taken at least 2 hours after taking Xenical or before bedtime.

When taking Xenical and cyclosporine a decrease in plasma concentrations of cyclosporine was noted, therefore, more frequent determination of plasma concentrations of cyclosporine is recommended when taking cyclosporine and Xenical simultaneously.

Upon appointment amiodarone During therapy with Xenical, a decrease in the systemic exposure of amiodarone and desethylamiodarone was noted (by 25-30%), however, due to the complex pharmacokinetics of amiodarone, the clinical significance of this phenomenon is not clear. The addition of Xenical to long-term amiodarone therapy may result in a decrease in the therapeutic effect of amiodarone.

Avoid simultaneous use of Xenical and acarbose due to lack of pharmacokinetic study data.

Directions for use and doses

Inside, adults - 1 capsule. (120 mg) with each main meal (during or no later than 1 hour after meals). If a meal is skipped or the food does not contain fat, then the drug can also be skipped.

Dose adjustments in patients elderly not required.

Dose adjustments with impaired liver or kidney function not required.

Safety and effectiveness of Xenical in children under 18 years of age not installed.

Overdose

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

Symptoms: in cases of overdose, either the absence of adverse events was reported, or the adverse events did not differ from those observed when taking the drug in therapeutic doses.

Treatment: in case of severe overdose of Xenical, it is recommended to observe the patient for 24 hours.

Based on human and animal studies, any systemic effects that could be attributed to the lipase inhibitory properties of orlistat should be rapidly reversible.

special instructions

Xenical is effective in terms of long-term control of body weight (loss of body weight and its maintenance at a new level, prevention of re-gain of body weight). Treatment with Xenical leads to an improvement in the profile of risk factors and diseases associated with obesity, including hypercholesterolemia, type 2 diabetes mellitus (NIDDM), impaired glucose tolerance, hyperinsulinemia, arterial hypertension, and a decrease in the amount of visceral fat.

When used in combination with hypoglycemic drugs such as metformin, sulfonylurea derivatives and/or insulin in patients with type 2 diabetes mellitus with overweight (BMI≥28 kg/m2) or obesity (BMI≥30 kg/m2) Xenical, in combination with a moderately hypocaloric diet, provides an additional improvement in the compensation of carbohydrate metabolism.

In clinical studies, the majority of patients had concentrations of vitamins A, D, E, K and beta-carotene within the normal range during two full years of orlistat therapy. A multivitamin may be prescribed to ensure adequate intake of all nutrients.

The patient should receive a balanced, moderately hypocaloric diet containing no more than 30% of the nutritional value in the form of fat. A diet rich in fruits and vegetables is recommended. The daily intake of fats, carbohydrates and proteins should be divided into three main meals.

The likelihood of adverse reactions from the gastrointestinal tract may increase if Xenical is taken on a diet rich in fat (for example, 2000 kcal/day, of which more than 30% is in the form of fat, which equals approximately 67 g of fat). Daily fat intake should be divided into three main meals. If Xenical is taken with food very rich in fat, the likelihood of gastrointestinal reactions increases.

In patients with type 2 diabetes mellitus, a decrease in body weight during treatment with Xenical is accompanied by an improvement in the compensation of carbohydrate metabolism, which may allow or require a reduction in the dose of hypoglycemic drugs.

Storage conditions for the drug Xenical ®

Keep out of the reach of children.

One tablet contains Xenical ( capsules ) includes: 120 mg (in the form of pellets - 240 mg) and talc as an excipient.

One pellet contains: 120 mg orlistat , MCC, Primogel (Na carboxymethyl starch), povidone K-30, Na lauryl sulfate.

Indigo carmine, gelatin, and titanium dioxide are used in the manufacture of capsule shells.

Release form

Capsules .

The capsules are hard, gelatinous, turquoise in color. The body is marked with the inscription “XENICAL 120”, and the inscription “ROCHE” is printed on the cap.

Capsules are packaged in blisters of 21 pcs., pack. No. 21, No. 42, No. 84.

pharmachologic effect

Gastrointestinal lipase inhibitor.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

The drug has a specific, powerful and reversible effect on the gastrointestinal tract (helping to fractionate, dissolve and digest fats). Characterized by long-lasting action.

The action of the drug is carried out in the lumen of the stomach and small intestine. The therapeutic effects are due to the ability of orlistat to form a covalent bond with the active serine site of pancreatic and gastric lipases.

After inactivation, the enzyme is not able to break down dietary fats in the form of triglycerides into monoglycerides and non-esterified (free) fatty acids.

Unsplit triglycerides in the body are not absorbed, as a result of which the intake of calories decreases and body weight decreases.

Thus, the drug acts without being absorbed into the systemic circulation.

Based on the results of tests that determine the concentration of fat in feces, it can be seen that the effects of orlistat begin to appear 1-2 days after taking the capsules.

After discontinuation of Xenical, the concentration of fat in feces returns to the level that occurred before the start of therapy after 2-3 days.

Pharmacokinetics

Systemic exposure to the substance is minimal both in individuals with normal body weight and in obese individuals. After a single dose of three 120 mg capsules, the substance in unchanged form is not detected in plasma, which indicates that its plasma concentration does not exceed 5 ng/ml.

After taking therapeutic doses of Xenical, it was extremely rare to detect an unchanged substance, and its content was negligible.

Due to poor absorption orlistat Its volume of distribution cannot be determined. In vitro, more than 99% of the substance is in states associated with plasma proteins (connection mainly with And lipoproteins ). In minimal concentrations it can penetrate into.

Animal experiments have shown that orlistat biotransformed mainly in the intestinal wall. Studies in a group of obese patients have established that about 42% of the fraction of the substance exposed to systemic absorption is 2 - M1 and M3.

The metabolite molecules have an open b-oriented lactone ring and very weakly inhibit lipase (1 and 2.5 thousand weaker than orlistat, respectively). Low plasma concentration and low inhibitory activity of M1 and M3 allow the products to be considered orlistat as pharmacologically inactive.

In both normal-weight and obese individuals, the drug is eliminated primarily by eliminating unabsorbed drug from the intestinal contents (approximately 97% of the dose taken). Of these, 83% are in the form orlistat unchanged.

No more than 2% of all structurally related orlistat substances.

The drug is completely eliminated from the body (with feces and urine) within 3-5 days. The ratio of excretion routes between obese and normal weight people is the same.

AND orlistat , and the products of its metabolism can be excreted in bile.

Indications for use

The drug is intended for long-term use in overweight and obese patients, as well as in persons with risk factors associated with obesity.

Xenical is prescribed in combination with hypocaloric, to patients non-insulin-dependent diabetes with obesity or overweight - with moderately restricted or glucose-lowering medications.

in combination with hypoglycemic drugs (metformin, sulfonylureas and/or insulin) or a moderately hypocaloric diet in patients with type 2 diabetes mellitus who are overweight or obese.

The instructions list the following contraindications for the use of Xenical:

• cholestatic syndrome ;
• malabsorption syndrome ;
• intolerance to any of the components of the capsules.

Side effects

It was found that the most common (incidence ³1/10) side effects of the drug are reactions from the gastrointestinal tract. Their cause is pharmacological action orlistat , preventing the absorption of fats entering the body with food.

These side effects manifested themselves in the form of:

• imperative (urgent) urge to defecate;
• release of gases (flatulence) with evacuation of some intestinal contents;
• loose stools;
• oily discharge from the anus;
• steatorrhea;
• increased frequency of bowel movements;
• discomfort and/or abdominal pain.

The incidence of these symptoms increases with increasing fat content in the diet. Patients should be informed of the possibility of developing such reactions and taught how to take the drug correctly to minimize or eliminate them.

When treating with Xenical, it is very important to follow the prescribed diet as best as possible and monitor the fat content in the diet with particular care.

Following a low-fat diet reduces the risk of gastrointestinal disorders and thus helps control and regulate the intake of fatty foods.

In most cases, the side effects listed above were mild and transient in nature. They occurred mainly in the first three months of treatment, and almost all patients experienced no more than one episode of such reactions.

Somewhat less frequently (with a frequency of ³1/100,<1/10) фиксировались:

• discomfort and/or pain in the rectum;
• bloating;
• "a soft chair;
• fecal incontinence;
• damage to the gums and/or teeth.

Other side effects:

• very common - upper respiratory tract infections;
• common - lower respiratory tract infections, anxiety, dysmenorrhea, urinary tract infections, weakness.

In patients with non-insulin-dependent diabetes the frequency and nature of adverse reactions were comparable to those in overweight and obese patients, but without . The only new side effects they had were hypoglycemic conditions and bloating.

Hypoglycemic conditions occurred in more than 2% of patients diabetes . Their incidence in comparison with placebo is ³1% (the reason, most likely, is the improvement in compensation of carbohydrate metabolism).

Four-year clinical studies showed that the safety profile of Xenical did not differ from that obtained in one- and two-year studies. The overall incidence of adverse effects from the gastrointestinal tract decreased annually over the four-year period of drug use.

Post-marketing observations

To date, there are descriptions of cases of the development of hypersensitivity reactions, the main clinical manifestations of which were , bronchospasm , skin rashes, , anaphylaxis .

In rare cases, increased activity of alkaline phosphatase and transaminases and a bullous rash were recorded. Isolated (probably serious) cases of the disease have also been described hepatitis during treatment with the drug (neither the pathophysiological mechanisms of development nor the cause-and-effect relationship with the use of Xenical have been established).

Use of the drug in combination with anticoagulants led to a decrease prothrombin and change hemostatic parameters .

Other side effects recorded during post-marketing observations:

• oxalate nephropathy;
• diverticulitis ;
• cholelithiasis ;
• pancreatitis ;
• rectal bleeding.

When taking the drug with antiepileptic drugs There have been cases of seizures.

Xenical tablets, instructions for use

Long-term treatment of overweight/obese patients (including patients with predisposing factors for obesity) is carried out with the use of 120 mg for each of the main meals. The capsule is taken during or within an hour (but not later!) after a meal.

Patients with non-insulin-dependent diabetes the drug is prescribed in a standard dosage - 1 capsule with each meal. If the food consumed does not contain fat or the patient skips meals, Xenical may not be taken.

How to take the drug to lose weight?

As an adjunct to therapy, the patient should adhere to a balanced, low-calorie diet, in which calories in the form of fat do not exceed 30%. The daily dose of proteins, fats and carbohydrates should be divided into three main doses. The diet should be dominated by vegetables and fruits.

The instructions for use of Xenical indicate that increasing the recommended dose (360 mg/day) does not lead to an increase in its therapeutic effect.

Overdose

It is reliably known that neither a single dose of 0.8 g of Xenical, nor multiple doses of the drug 0.4 g 3 times a day for 15 days cause significant side effects.

In addition, there is experience in the treatment of obesity using a dose of 720 mg/day. for six months. The therapy was not accompanied by a significant increase in the incidence of adverse reactions.

In case of an overdose of Xenical, undesirable symptoms are either absent altogether or do not differ from those observed when taking a therapeutic dose.

In case of severe overdose, the patient should be monitored for 24 hours.

Animal and human studies have shown that any associated pharmacological properties orlistat systemic effects should be quickly reversible.

Interaction

Drug interaction studies have shown that orlistat does not interact with Atorvastatite , alcohol, biguanides , fibrates , oral contraceptives , Pravastatin , Phentermine , Nifedipine (long-acting or GITS), .

However, with concomitant therapy anticoagulants in oral dosage form (in particular, Warfarin ) you need to monitor your INR levels.

When taken simultaneously with orlistat absorption decreases (according to Wikipedia, by 30%) fat-soluble (β-carotene , α-tocopherol , vitamin K ).

Patients prescribed multivitamins should take them at least 2 hours after taking the capsules or before bedtime.

Orlistat helps reduce plasma concentrations, and therefore, when taking drugs in combination, it is recommended to more often determine the concentration of the latter in plasma.

Orlistat reduces systemic exposure by about a third And Desethylamiodarone while taking capsules with Amiodarone in oral dosage form. However, since Amiodarone has rather complex pharmacokinetics; the clinical significance of this phenomenon could not be established.

Reception orlistat against the background of long-term therapy A miodarone, will most likely lead to a decrease in the effectiveness of the latter (no studies have been conducted).

Since pharmacokinetic interaction studies orlistat in with Acarbose have not been conducted, it is recommended to avoid the use of these drugs in combination.

When using the drug simultaneously with anticonvulsants There have been cases of seizures.

The cause-and-effect relationship of therapy with this phenomenon has not been established. However, patients should be carefully monitored for possible changes in the severity and/or frequency of seizures.

Terms of sale

On prescription.

Storage conditions

Capsules should be stored at temperatures below 25°C.

Best before date

Three years.

special instructions

The effectiveness and safety of the drug in patients with functional disorders of the kidneys and/or liver, as well as in the elderly, have not been studied.

The product is effective when long-term weight control is necessary: ​​Xenical helps to lose weight and maintain it at a new level, and also prevents weight gain.

Treatment leads to an improvement in the profile of predisposing factors and pathologies associated with obesity, including non-insulin dependent diabetes , hypercholesterolemia , hypertension, hyperinsulinemia, impaired glucose tolerance, and helps reduce the amount of visceral fat.

Using a weight loss product in combination with sulfonylurea derivatives, and/or in patients with non-insulin-dependent diabetes with BMI, if they are overweight or obese, and also in combination with a moderately restricted low-calorie diet, it is possible to further improve the compensation of carbohydrate metabolism and reduce the need for hypoglycemic drugs .

A four-year study found that most patients had concentrations beta carotene , and , TO remained within normal limits. To ensure an adequate supply of all essential nutrients? Treatment can be supplemented with taking multivitamins.

It has been confirmed that there are no additional risks regarding toxicity, reproductive toxicity, carcinogenicity, genotoxicity and the safety profile of the drug. Animal studies also did not reveal teratogenic effects.

Since the teratogenic effect of the drug has not been detected in experimental animals, it can be assumed that it is unlikely to occur in humans.

Xenical's analogs

Structural analogues of the drug are: , Orlistat Canon , , , Orlimax , Orsoten slim .

The price of Xenical analogues is from 404 rubles. The most inexpensive substitute for the drug is Orsoten Slim (capsules 60 mg pack No. 42 cost an average of 450 rubles).

For children

The safety and effectiveness of Xenical in patients under the age of twelve years have not been studied.

Xenical and alcohol

Alcohol and orlistat do not interact, which was confirmed in drug interaction studies of Xenical.

Xenical for weight loss

Diet pills Xenical: effectiveness in obese patients

In clinical studies in recipients orlistat patients experienced significant weight loss compared to patients who were prescribed diet therapy.

Body weight began to decrease within the first two weeks of treatment and continued to decrease over the next 6-12 months (including in patients with a negative response to diet treatment).

Over the course of 24 months, there was a statistically significant improvement in the profile of metabolic risk factors associated with obesity. Body fat was also significantly reduced compared to placebo.

Xenical effectively prevents weight gain: weight gain not exceeding ¼ of what was lost was observed in approximately 50% of patients, while in half of the patients weight gain was not observed, and in some cases weight continued to decrease.

The use of a drug for weight loss in patients with non-insulin-dependent diabetes

Studies lasting from six months to a year in patients with a BMI more than 28 kg/m2 showed that in individuals receiving therapy orlistat , there is significantly greater weight loss compared to patients who were prescribed only a therapeutic diet.

Weight loss occurs mainly by reducing the percentage of body fat.

It must be emphasized that before the start of the study, despite taking hypoglycemic agents , patients often had insufficient control hypoglycemia .

However, during treatment with the drug, a clinically and statistically significant improvement in control was observed hypoglycemia , decrease insulin resistance , as well as a decrease in concentration and the patient's needs for hypoglycemic agents .

In addition, four-year clinical studies have shown that the use of Xenical can significantly (by approximately 37% compared to placebo) reduce the risk of developing non-insulin dependent diabetes . However, in patients with impaired glucose tolerance, the degree of risk reduction was even more significant (45%).

Maintaining weight and improving the profile of predisposing factors to a new level was noted throughout the entire study period.

Efficacy of Xenical for pubertal obesity

In a group of obese adolescents, studies were conducted over a year. In all patients under observation, BMI decreased more significantly than in patients taking placebo.

Patients taking the drug had a noticeable reduction in body fat percentage and diastolic blood pressure, and a noticeable reduction in body circumference (hips, waist) compared to control group patients who received a placebo.

The modern pharmaceutical market provides a large number of weight loss products, but Xenical is considered one of the most common, effective and safe. It blocks the breakdown of fats, reduces fat deposits, and does not have a negative effect on the functionality of internal organs. You can get acquainted with the drug, its properties, indications, from the instructions for use.

Composition and release form of the drug

Active ingredient of the drug: orlistat, 1 capsule contains 120 milligrams of the active substance, also excipients: sodium carboxymethyl starch, povidone K-30, microcrystalline cellulose, sodium lauryl sulfate. Available in cardboard packaging in blister No. 21, the package contains 4 blisters.

Pharmacological properties

After taking the drug, the active substance suppresses gastric and pancreatic lipases, which are responsible for the absorption and breakdown of fats in the intestines, as a result of which lipases lose their properties when digesting food. Fats that come with food are not absorbed by the intestines and are excreted from the body during bowel movements. Blocking fats prevents them from being absorbed by the body, which leads to a lack of fat deposits and a decrease in body weight.

Studies have shown that the activity of Xenical does not change, regardless of food intake. Also, after taking it, the absorption of fats is quickly normalized, which does not lead to disruption of the digestive system. The mechanical effect of the drug is well tolerated, without having any chemical effects on the body.

Xenical is not absorbed into the lymph and systemic blood flow, and also does not accumulate in the body, but is excreted along with feces. The therapeutic effect is observed 1-2 days after taking the first tablet and stops within 2-3 days after the course of treatment.

Indications for use

Xenical is recommended to be taken for weight loss in case of obesity or overweight; it is also prescribed for various concomitant diseases caused by obesity: hypertension, diabetes, metabolic disorders. For overweight people who take hypoglycemic drugs, Xenical is taken as part of complex therapy.

Contraindications for use

Taking Xenical is contraindicated for patients with chronic diseases of the biliary tract, with impaired functional absorption of active substances in the intestine, or with individual intolerance to the composition of the drug. Not suitable for children and pregnant women.

Mode of application

You need to take the drug after consulting a doctor, the results of the examination, and the collected medical history. Usually the doctor prescribes 1 capsule 1-3 times a day during meals or 1 hour after meals. It is not recommended to exceed the recommended dose, as this may lead to side effects.

To enhance the therapeutic effect, the drug can be taken for a long time. While taking Xenical, you need to monitor your diet, exercise, and lead an active lifestyle. The result after taking Xenical is observed within a few days, weight loss sometimes reaches from 6 to 15 kilograms.

Possible side effects

Usually the drug is well tolerated, but sometimes, if fat absorption is impaired, side effects from the digestive system occur: diarrhea, heaviness in the stomach, nausea, increased frequency or incontinence of stools that have oily discharge. Menstrual irregularities, vomiting, headaches, and allergic reactions are less common.

Most often, side effects are observed when the recommended dose is exceeded or after consuming fatty foods.

Video

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