To suppress a rooted appetite and cure obesity, it is recommended to take the medicine Sibutramine for weight loss. Previously, a characteristic medication was used to treat depressive conditions, but in practice it turned out to be very mediocre. Currently, a unique opportunity has been identified to suppress appetite, to successfully fight extra pounds. Before taking diet pills with sibutramine, you should consult with your dietitian, healthcare professional.

What is Sibutramine

This synthetic medicine in the fight against alimentary obesity is available in the form of tablets, intended for oral administration. Thanks to the active ingredients, the feeling of fullness occurs prematurely, therefore the daily portions are gradually reduced without harm to health. Overweight is also on the decline. Sibutramine hydrochloride monohydrate is a potent drug, the therapeutic effect of which is achieved due to the activity of the active substance of the same name Sibutraminum.

How does it work

The active ingredient of the same name provides anorexigenic effect in the body, that is, it provides enhanced heat exchange, due to which subcutaneous fat is efficiently heated. After using a single dose, beta-adrenergic receptors are stimulated, which are responsible for the release of energy. Due to the moderate inhibitory effect and the action of neurotransmitter hormones in the brain, appetite and daily portions are reduced.

Preparations with sibutramine lower blood cholesterol and contribute to a decrease in the concentration of glycerides, which helps to maintain a new weight for a long period of time without a strict diet. The process of decomposition of synthetic substances is observed in the liver, however, active metabolites are still present in the systemic circulation for 4 days.

What is dangerous

Before you buy a drug at a pharmacy, you need to find out about the potential threat to your own health. For example, a medication can provoke pathologies from the cardiovascular system. Alternatively, it can be attacks of arrhythmias and tachycardia, increased blood pressure. Insofar as medicinal product differs in systemic action in the body, side effects spread to all internal organs of the system, attack in the first days of obesity treatment, weight loss.

Side effects

Patients often complain of severe signs of dyspepsia, constipation, dizziness, nausea, dry mouth and complete lack of appetite. These are abnormal changes in general well-being, which eloquently indicate the presence of side effects. Do not reduce the daily dose of the medication, but it still does not hurt to contact a nutritionist immediately. Perhaps the specialist will recommend a softer analogue for a successful correction. overweight in adulthood.

If you decide to choose such a method of losing weight, it is important to pay attention to such potential anomalies, which in the body after the remedy will be rather temporary in nature:

• headache, paresthesia;
• disturbed sweating, insomnia;
• change in taste;
• more frequent cramps of the limbs;
• depressing effect on the central nervous system;
• thrombocytopenia;
• increased activity of liver enzymes.

Consequences of admission

If side effects have arisen in the body, taking the drug further is categorically contraindicated, and the correction of the daily dose will not provide the desired dietary effect. The doctor offers another way to remove excess pounds at home, to finally solve the problem of excess weight at any age. The unpleasant consequences of oral administration can be as follows:

• violation of cardiac activity;
• blood pressure surges, hypertension;
• tendency to blues, depression;
• sudden mood swings;
• muscle cramps and pain;
• decreased libido;
• inflammation of the intestinal mucosa and stomach.

Why Sibutramine is banned in Russia

Many patients insist that the medication is a narcotic drug, since the consequences of its use resemble an unpleasant phenomenon called "withdrawal from drug addicts." In a losing weight person, already in the middle of the course, a certain dependence appears, and without a new dose, the severity of side effects only increases. Therefore, the authorities decided to ban the sale of medicines in Russian pharmacies, although nothing prevents them from ordering and buying goods in an online pharmacy.

Is it possible to lose weight with Sibutramine

By controlling hunger, the drug promotes productive weight loss. In the absence of medical contraindications, it can be used to correct excess weight in a full course. The drug is not compatible with alcoholic beverages, has drug interactions. Any adjustments to the daily dose are made by the doctor strictly in individually, otherwise, when losing weight, you can worsen general state health.

Indications for use

The drug can be recommended for obese patients when the BMI index is ≥30 kg / m2 or BMI is ≥ 27 kg / m2. The use of pills in a full course helps not only to reduce, but also to stabilize the new weight, to minimize the risk of developing diabetes mellitus. In the presence of the last diagnosis, the use of the drug is not prohibited, since the active components of the drug reduce the glucose level in the blood.

Preparations containing Sibutramine

A detailed description of the specified medication is inspiring, but potential contraindications and side effects should not be ruled out. If it is not possible to lose weight in such a progressive way for medical reasons, in the pharmaceutical industry there are a number of equally worthy analogs that contain similar chemical composition and pharmacological action in a slimming body. Below are the most effective weight regulators from different manufacturers.

This dietary product is available in the form of capsules, which are packed in blisters of 7, 14, 28, 84 pieces. Meridia for weight loss controls the roaming appetite, eliminates the obvious signs of obesity. Here's what you need to know about a typical medication before purchasing and using it:

• manufacturer - pharmaceutical company Abbott GmbH (Germany);
• price - 1,700 rubles (14 capsules, 10 mg each);
• composition - active ingredient: sibutramine monohydrate; auxiliary: colloidal silicone dioxide, microcellulose, magnesium stearate, lactose monohydrate;
• principle of action - suppresses appetite, enhances heat exchange at the cellular level.

Goldline

With the development of obesity, you can lose weight with the help of the specified medication. Goldline is available in capsule form, where each aluminum foil package can contain 10, 30, 60, 90 pieces. Before starting intensive therapy, it is required to consult a nutritionist to minimize the risk of deterioration in general condition. Here's what you need to know about this tool:

• manufacturer - Ranbaxy Laboratories (India);
• price - 1700-1900 rubles for 60 capsules;
• composition - active ingredient: sibutramine monohydrate; auxiliary elements: lactose, calcium and magnesium stearate, microcrystalline cellulose;
• principle of action - satisfies hunger, directs impulses to the brain about the feeling of satiety.

Lindax

This medicine is available in the form of gelatin capsules for oral administration. One package can contain 10, 30 or 90 capsules, so the duration of intensive care should be determined in advance. Here's what you need to know when purchasing this productive weight loss dietary supplement:

• manufacturer - Zentiva concern (Czech Republic);
• price - 2100-2200 rubles for 30 capsules;
• composition - active ingredient: sibutramine monohydrate; auxiliary elements - gelatin, lactose monohydrate, magnesium stearate, microcellulose, iron oxide, silicon and titanium dioxides;
• principle of action - suppresses appetite, allows you to eat in small portions.

Reduksin

While continuing to study sibutramine tablets, doctors recommend the anorectic Reduxin, which is also available in capsule form. Packages of 30 and 60 pieces prevail on sale, intended for oral administration before meals. Here's some valuable information for a potential buyer to note:

• manufacturer - Ozone (Russia);
• price - from 1600 rubles for 30 capsules;
• composition - active ingredient: sibutramine; auxiliary elements: microcrystalline cellulose, calcium stearate, gelatin, titanium dioxide;
• principle of action - provides a slimming effect by stimulating metabolism.

Instructions for use for weight loss

The drug is intended for oral administration, a single dose is shown to be washed down with plenty of water. The duration of intensive therapy is 1 year, since even minor changes in the problem figure are not immediately observed. In the first and second months of losing weight, the percentage of burning of subcutaneous fat is minimal, as the doctor informs about in an individual consultation. If you maintain a diet, eat low-calorie foods and take the drug, weight loss becomes noticeable only after 4-6 months.

How to use

If the doctor prescribes Sibutramine, he additionally recommends playing sports, monitoring nutrition. When losing weight, it is important to monitor the blood pressure indicator, which can pathologically increase during the correction of excess weight. The frequency of heart contractions remains under control, and at the first symptoms of tachycardia, it is shown to stop taking the medication, in addition to consult a nutritionist.

Dosage

A single dose of a medicine is 10 mg, i.e. one capsule of the drug per day. If there is no dietary effect, it should be increased to 15 mg, further adjusted individually. If, instead of productive weight loss, there is a rapid weight gain, further use of the capsules is shown to be stopped, consult a specialist.

Interaction

The use of Sibutramine for weight loss contributes to the acquisition of ideal forms, a flawless body. However, using it as directed is shown wisely, without forgetting about drug interactions. For example, in combination with inhibitors of the isoenzyme CYP3A4, the concentration of metabolites in the plasma increases, and the QT interval increases. Serotonin syndrome is not excluded if combined with 5-HT1 receptor agonists, opium analgesics, selective serotonin reuptake inhibitors, antitussives.

Where to buy Sibutramine

It is difficult to buy a typical medication on the domestic market, even in Moscow and St. Petersburg there are difficulties with the purchase of a medication. There is no medicine in real pharmacies, it is better to immediately go to the online pharmacy, place an order and receive the goods by mail, by courier. Delivery from virtual resources does not cause problems, while there is a chance to get a discount on capsules.

Price

The cost of a medicine depends on the manufacturer and the number of capsules in one package. Retail prices of domestic pharmacology are more accessible to buyers, but an import manufacturer often overstates prices, but the result is guaranteed. On average, the purchase of Sibutramine for weight loss costs the patient 1,000 rubles for 30 capsules.

Contraindications

At hypersensitivity the body to the active components, the use of the drug is contraindicated, otherwise side effects occur in the form of local, allergic reactions. Other medical contraindications from the instructions are presented below:

• pregnancy;
• glaucoma;
• dysfunction of the liver, kidneys;
• Tourette's syndrome;
• psychical deviations;
• chronic myocardial diseases;
• hyperthyroidism;
• hyperplasia of the prostate (for men);
• pheochromocytoma;
• drug addiction.

Video

Losing weight is difficult - and everyone who tried to get rid of at least a couple of extra pounds knows this. The laws of nature cannot be bypassed: only diet and physical activity can defeat fat accumulation. Losing dozens of extra pounds through diet and fitness takes tremendous willpower. Obese people start looking for miracle pills and diet pills, including medicine sibutramine for weight loss.

Sibutramine was developed as a drug for depression, but trials have shown its ability to effectively suppress appetite. For 13 years in the United States and Europe, doctors prescribed the drug to obese people until serious side effects of this popular weight loss product were discovered. According to American experts, the harm from using sibutramine far outweighs the benefits it has in weight loss. In the United States, this drug has been taken off the market, and in Russia it is included in the list of potent drugs for weight loss, which are bought in a pharmacy strictly according to a doctor's prescription.

So, more than 10 years history of the use of sibutramine in the West has shown that its use is associated with health risks. However, people who are tired of fighting overweight are ready to take any risk in order to achieve real results and see themselves in the mirror looking slimmer. Like all powerful drugs, in addition to the positive effect, the drug has many contraindications.

How justified is the risk of using sibutramine for weight loss, is it not a time bomb that can undermine the body's defenses? To understand this issue, you need to understand the principle of action of the drug, thanks to which it promotes weight loss.

Pharmacological properties of the drug Sibutramine

Chemical compound
IUPAC	(±) -1- (4chlorophenyl) -N, N-dimethyl- Alpha- (2-methylpropyl) cyclobutanemethanamine (as hydrochloride)
Gross- formula	C17H26ClN
Like. weight	279.85 g / mol
CAS	106650-56-0
PubChem	5210
DrugBank	APRD00456
Classification
Farm. group	Appetite regulators
ATX	AO8AA10
ICD-10	E66
Pharmacokinetics
Bioavailability	Adsorption 77% Presumably effect of the first passing
Metabolism	List (CYP3A4- connected)
Period half-life	Sibutramine about 1 hour Metabolite1: 14 hours Metabolite2: 16 hours
Excretion	Bile (sibutramine and active metabolites) kidneys (inactive metabolites)

Sibutramine is used medicinally in the treatment of obesity, this drug affects the production of heat in the body. An increase in the temperature of metabolic processes creates conditions for burning fat reserves. The second property of sibutramine is appetite suppression, it helps to reduce calorie intake while losing weight. Old fat stores are burned, new ones are not formed - there is a rapid decrease in body weight. An increase in temperature during metabolism is due to the fact that sibutramine acts on beta-adrenergic receptors and, like adrenaline, increases the rate of metabolic processes in the body.

Adipose tissue is quickly burned, cholesterol levels in the blood decrease, but at the same time the heart rate increases, the heart's need for oxygen increases, and blood pressure- the body behaves as in a situation of severe stress. Decreased appetite is associated with the selective action of sibutramine on serotonin and norepinephrine - these neurotransmitters in the brain cause a state of happiness, satisfaction, dull hunger, and reduce the need for food.

At the same time, narcotic intoxication occurs and dependence on the drug is formed. After oral administration, sibutramine is absorbed into the bloodstream within 1-2 hours, and absorbed by 77%. In the liver, its transformation takes place, active metabolites are formed, which act in the body for 4 days.

Please note: Sibutramine is a psychotropic drug that makes the vital systems of the body work with increased stress, forms drug addiction and provokes a state of withdrawal.

Indications and application features

There is a small range of indications for which the use of sibutramine tablets as a medicine for weight loss is justified.

• Firstly, this is a severe degree of obesity, when the body mass index (BMI) is equal to or more than 30 kg / m2, and all attempts to reduce weight by other available methods have not been successful.
• Secondly, it is permissible to use drugs with a sibutramine content with a BMI of 27 kg / m2, if obesity is accompanied by complications such as diabetes mellitus and hypertension.

However, even with such indications, it is dangerous to take this medicine for weight loss on your own. Only a doctor who knows the dangers of sibutramine can weigh the pros and cons, assess the patient's condition and make a decision with the least risk to his health. Correction of obesity should be carried out in a comprehensive manner.

Despite the help of a potent medicine, the following are absolutely necessary:

• adherence to a diet;
• balanced physical activity;
• changing lifestyle and eating habits.

The course of therapy with the use of sibutramine lasts at least a year, while it is important to adhere to the doctor's recommendations in everything: do not change the dose of the drug and the frequency of its administration, do not start or end the treatment without permission. It is imperative to consult a doctor before taking other medicines, since sibutramine can interact with their components, enhancing undesirable effects. First of all, these drugs include: antidepressants, narcotic analgesics, and other drugs for obesity.

Contraindications

Perhaps the most important sections that contain instructions for the use of the drug are lists of contraindications and side effects... From the bitter experience of the first years of using sibutramine, it was found that this is far from a harmless drug, and it cannot be prescribed to everyone who wants to lose weight.

The mortality rate from heart attacks and strokes among patients taking the drug was noticeably higher than among those who were not familiar with it. Suicides have become more frequent among people who systematically used the drug. The list of contraindications was compiled on the basis of experimental data and as a result of in-depth study possible consequences the action of the drug in the body.

• Sibutramine is contraindicated in obesity, which is caused by organic pathologies such as endocrine diseases, hormonal imbalance; neoplasms in the brain; violation of metabolism and water balance in the body.
• It is very risky to use this means for losing weight in cardiovascular diseases: ischemia, tachycardia, arrhythmias, heart failure, myocardial defects, vascular disorders.
• It is categorically impossible to use drugs that contain sibutramine for diseases of the central nervous system, mental disorders (including bulimia and anorexia of a nervous nature), for alcohol and drug addiction, after strokes.
• The use of sibutramine is risky for people suffering from glaucoma, pathologies of the liver, kidneys, and prostate gland.
• A special risk group is made up of women during pregnancy and lactation, persons over 65 years of age, those who have an individual intolerance to the drug.

Side effects and overdose

Sibutramine has an impressive list of side effects, so its use is possible only after consultation with a nutritionist and under the supervision of a physician. Undesirable effects are most pronounced during the first month of using the drug, then they weaken and come to naught. Only a doctor can determine the potential danger of these manifestations and make a decision: to continue treatment, reduce the dosage or abandon sibutramine in favor of its analogues.

According to doctors, the most common side effect of the drug is the addictive effect and withdrawal symptoms. (withdrawal) with its sudden cancellation. Without the usual dose of the drug, the patient experiences anxiety, depression, insomnia, and suicidal thoughts. A restless state of consciousness is accompanied by general weakness, rapid heart rate, hand tremors, migraines and fainting. The table below shows the percentage of adverse symptoms in the control group (persons who lost weight with sibutramine) and in the placebo group.

Back pain, joint pain, rhinitis, sinusitis, tonsillitis, indigestion - this is not a complete list of side effects of sibutramine. When taken in patients, blood pressure rises, heart rate increases, chronic fatigue syndrome develops. An overdose of the drug can increase unwanted effects and pose a health hazard. It is recommended to take activated charcoal, see a doctor or poison control center.

Sibutramine instructions for use

According to doctors' reviews, sibutramine is very effective remedy for weight loss, which can help people suffering from advanced form of alimentary obesity as a result of unhealthy eating habits. Pathologically heavy weight (BMI ˃ 30) provokes deadly diseases: diabetes, oncology, strokes and heart attacks.

The use of a powerful weight loss drug that suppresses appetite is justified in the event of a real threat of the development of such diseases. The instructions indicate the basic rules for using the drug.

• The initial daily dose is 10 mg.
• The optimal time for admission is the first half of the day.
• Tablets and capsules containing sibutramine are swallowed without chewing, washed down with a glass of water.
• If one or more doses of the medicine have been missed, you cannot increase the dose, you should continue taking the pills as usual.
• The expected effect of using the drug during the first month is a weight loss of 2 kg.
• In the absence of side effects, the dose can be increased to 15 mg / day, but this dosage is a limited course.
• If within 3 months it is not possible to reduce the weight by 5%, then you should switch to an analogue containing another active ingredient.
• Treatment with drugs containing sibutramine should not be continued for more than a year; taking the drug is stopped under the supervision of a physician.

An effective course of treatment allows you to reduce weight within 10-12 months by no less than 10%. You can save the results obtained only with the help of diet and physical activity.

Sibutramine price in Russia

Since 2008, sibutramine and all drugs based on it (Reduxin, Goldline - Russian production) have been included in the list of potent substances prohibited for free sale in the pharmacy network. You can buy medicine only with a prescription from a nutritionist and endocrinologist.

Price for a package of 30 capsules ( monthly rate) - from 900 rubles. for 30 capsules Goldline and from 1500 for the same package of Reduksin. When used under medical supervision, the drug helps many obese people change their dietary habits and lose weight. This is evidenced by the reviews of losing weight about sibutramine.

A drug Sibutramine belongs to the pharmacotherapeutic group of centrally acting appetite regulators that act directly on the brain, in particular, the saturation center. Increases the concentration of neurotransmitters: serotonin, norepinephrine and dopamine due to inhibition of their reuptake by neurons in the brain.
An agent for the treatment of obesity of central action. The mechanism of action is due to the selective inhibition of the reuptake of serotonin and norepinephrine, to a lesser extent - dopamine. Accelerates the onset and prolongs the feeling of fullness, which leads to a decrease in food intake. Increases energy expenditure by stimulating thermogenesis by indirect activation of β3-adrenergic receptors. Acts on both sides of the energy balance and contributes to weight loss.
Sibutramine and its metabolites do not release monoamines and are not MAO inhibitors, have no affinity for serotonergic, adrenergic, dopaminergic, muscarinic, histamine, benzodiazepine and NMDA receptors.

Indications for use:
Complex supportive therapy of overweight patients with alimentary obesity with a body mass index of 30 kg / m2 or more or with a body mass index of 27 kg / m2 or more, but in the presence of other risk factors due to overweight (type diabetes mellitus 2, dyslipoproteinemia).

Mode of application:
A drug Sibutramine used orally, once a day (in the morning), the initial dose is 10 mg (with poor tolerance, 5 mg may be taken); in case of insufficient effectiveness, after 4 weeks, the dose is increased to 15 mg / day. The duration of treatment is 1 year.

Side effects:
From the side nervous system and sensory organs:> 10% - insomnia; 1-10% - headache, dizziness, anxiety, paresthesia, change in taste; in isolated cases - convulsive seizures (0.1%); acute psychosis (in one patient with schizoaffective disorder).
From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): 1-10% - tachycardia, palpitations, increased blood pressure, vasodilation (skin hyperemia with a feeling of warmth); in isolated cases - Shenlein-Henoch disease, thrombocytopenia.
From the digestive tract:> 10% - dry mouth, loss of appetite, constipation, diarrhea; 1-10% - nausea, exacerbation of hemorrhoids.
From the side genitourinary system: in isolated cases - acute interstitial nephritis, mesangiocapillary glomerulonephritis.
Others: 1-10% - sweating; an increase in serum concentrations of AST, ALT, gamma-glutamyltransferase, LDH, alkaline phosphatase, bilirubin (less than 1.6% of cases).

Contraindications:
Hypersensitivity, the presence of organic causes of obesity, neurotic anorexia, bulimia, mental illness, Gilles de la Tourette's syndrome, coronary heart disease, decompensated heart failure, congenital heart disease, occlusive peripheral arterial disease, tachycardia, arrhythmia, cerebrovascular diseases (stroke, circulatory system), arterial hypertension (BP> 145/90 mm Hg), hyperthyroidism, severe liver or kidney dysfunction, benign prostatic hyperplasia, accompanied by the presence of residual urine, pheochromocytoma, glaucoma, established pharmacological, drug and alcohol dependence, simultaneous taking or for a period of less than 2 weeks after discontinuation of MAO inhibitors or others.

drugs acting on the central nervous system (including antidepressants, neuroleptics, tryptophan), as well as other drugs to reduce body weight, pregnancy, breastfeeding.
Epilepsy, motor-verbal tic (involuntary muscle contractions, impaired articulation), children and elderly age(safety and efficacy of use in children under 18 and in people over 65 have not been determined).

Interaction with other medicinal products:
Inhibitors of microsomal oxidation, incl. inhibitors of P450 3A4 (ketoconazole, erythromycin, cyclosporine, etc.) lower the Cl of sibutramine. Drugs with serotonergic activity increase the risk of developing serotonin syndrome (agitation, sweating, diarrhea, fever, arrhythmia, convulsions, etc.).

Pregnancy:
A drug Sibutramine contraindicated (adequate controlled studies in women have not been conducted).

Overdose:
Symptoms: increased severity of side effects.
Treatment: reception activated carbon, symptomatic therapy, monitoring of vital functions, with an increase in blood pressure and tachycardia - the appointment of beta-blockers.

Additionally:
It is necessary to control the level of blood pressure and pulse rate every 2 weeks in the first 2 months of treatment and then once a month. In patients with arterial hypertension with blood pressure< 145/90 мм рт.ст. контроль должен осуществляться тщательнее и чаще, а в случае дважды зарегистрированного подъема АД >145/90 mm Hg treatment should be discontinued. The appearance during therapy of chest pain, progressive dyspnea (breathing disorder) and edema of the lower extremities may indicate the development of pulmonary hypertension (in this case, it is imperative to consult a doctor).
It is not recommended to take simultaneously drugs that increase the QT interval (astemizole, terfenadine, antiarrhythmic drugs, etc.), drugs containing ephedrine, phenylpropanolamine, pseudoephedrine, etc. (risk of increasing blood pressure and increasing heart rate), as well as other anorexigenic drugs with a central mechanism actions. With caution should be prescribed against the background of hypokalemia and hypomagnesemia, with impaired liver and kidney function of mild and moderate severity.
It should be borne in mind that sibutramine can reduce salivation and promote the development of tooth decay, periodontal disease, candidiasis and oral discomfort. It is recommended to limit alcohol consumption during the treatment period. It should not be used during work by drivers of vehicles and people whose profession is associated with increased concentration of attention. Women of childbearing age should use adequate contraception during treatment.
Application is possible only in cases where all other measures aimed at reducing body weight are ineffective. Treatment should be carried out under the supervision of a physician who has experience in correcting obesity as part of complex therapy (diet, changes in eating habits and lifestyle, increasing physical activity). The period of taking a dose of 15 mg should be limited in time.

Gross formula

C 17 H 26 ClN

Pharmacological group of the substance Sibutramine

Nosological classification (ICD-10)

CAS code

106650-56-0

Characteristics of the substance Sibutramine

Sibutramine hydrochloride monohydrate is a white to creamy crystalline powder. Solubility in water: 2.9 mg / ml at pH 5.2. Partition coefficient (octanol / water): 30.9 (pH 5.0). Molecular weight 334.33.

Pharmacology

pharmachologic effect- anorexigenic.

Inhibits the reuptake of neurotransmitters - serotonin and norepinephrine from the synaptic cleft, potentiates the synergistic interactions of the central norepinephrine and serotonergic systems. Reduces appetite and the amount of food consumed (enhances the feeling of satiety), increases thermogenesis (due to the indirect activation of beta 3 -adrenergic receptors), affects brown adipose tissue. It forms active metabolites (primary and secondary amines) in the body that are significantly superior to sibutramine in their ability to inhibit the reuptake of serotonin and norepinephrine. In research in vitro active metabolites also block the reuptake of dopamine, but 3 times weaker than 5-HT and norepinephrine. Neither sibutramine nor its active metabolites affect the release of monoamines and MAO activity, do not interact with neurotransmitter receptors, including serotonergic, adrenergic, dopaminergic, benzodiazepine and glutamate (NMDA), do not have anticholinergic and antihistaminic effects. Inhibits the uptake of 5-HT by platelets and can alter platelet function.

The decrease in body weight is accompanied by an increase in the concentration of HDL in the blood serum and a decrease in the amount of triglycerides, total cholesterol, LDL and uric acid.

During treatment, there is a slight rise in blood pressure at rest (by 1-3 mm Hg) and a moderate increase in heart rate (by 3-7 beats / min), but in isolated cases, more pronounced changes are possible. With simultaneous use with inhibitors of microsomal oxidation, the heart rate increases (by 2.5 beats / min) and the QT interval is lengthened (by 9.5 ms).

In 2-year studies in rats and mice, using doses that resulted in the administration of which the observed total area under the concentration-time curves (AUCs) for the two active metabolites exceeded that when taking MRDC by 0.5-21 times, increased the incidence of benign tumors testicular interstitial tissue predominantly in male rats. No carcinogenic effect was found in mice and female rats. Has no mutagenic effect, does not affect fertility. When rats were administered doses for which AUCs of both active metabolites were 43 times higher than that observed when taking MRDC, no teratogenic effect was revealed. However, in studies carried out on Dutch Belted rabbits under conditions when the AUCs of active metabolites of sibutramine were 5 times higher than when using MRDC, abnormalities of physical development were found in the offspring (changes in the shape or size of the muzzle, auricle, tail, bone thickness ).

After oral administration, it is rapidly absorbed from the gastrointestinal tract by at least 77%. At the "first pass" through the liver, it undergoes biotransformation under the influence of the isoenzyme CYP3A4 of cytochrome P450 with the formation of two active metabolites (mono- and didesmethylsibutramine). After taking a single dose of 15 mg, C max of monodesmethylsibutramine is 4 ng / ml (3.2-4.8 ng / ml), didesmethylsibutramine - 6.4 ng / ml (5.6-7.2 ng / ml). C max is achieved after 1.2 hours (sibutramine), 3-4 hours (active metabolites). Simultaneous food intake lowers the C max of metabolites by 30% and increases the time to reach it by 3 hours without changing the AUC. Distributes quickly to tissues. Protein binding is 97% (sibutramine) and 94% (mono- and didesmethylsibutramine). The equilibrium concentration of active metabolites in the blood is reached within 4 days after the start of treatment and is approximately 2 times higher than the plasma level after taking a single dose. T 1/2 of sibutramine - 1.1 hours, monodesmethylsibutramine - 14 hours, didesmethylsibutramine - 16 hours. Active metabolites undergo hydroxylation and conjugation with the formation of inactive metabolites, which are excreted mainly by the kidneys.

Use of the substance Sibutramine

Complex maintenance therapy of overweight patients with alimentary obesity with a body mass index of 30 kg / m 2 or more or with a body mass index of 27 kg / m 2 or more, but in the presence of other risk factors due to overweight (sugar type 2 diabetes, dyslipoproteinemia).

Contraindications

Hypersensitivity, organic causes of obesity, anorexia nervosa or bulimia nervosa, mental illness, Gilles de la Tourette's syndrome, coronary heart disease, decompensated heart failure, congenital heart disease, occlusive peripheral arterial disease, tachycardia, arrhythmia, transient cerebrovascular disease (stroke cerebral circulation), arterial hypertension (BP> 145/90 mm Hg), hyperthyroidism, severe liver or kidney dysfunction, benign prostatic hyperplasia, accompanied by residual urine, pheochromocytoma, glaucoma, established pharmacological, drug and alcohol dependence, simultaneous administration or a period of less than 2 weeks after the withdrawal of MAO inhibitors or other drugs acting on the central nervous system (including antidepressants, antipsychotics, tryptophan), as well as other drugs to reduce body weight.

Restrictions on use

Epilepsy, motor-verbal tic (involuntary muscle contractions, impaired articulation), children and old age (safety and efficacy of use in children under 18 and in people over 65 have not been determined).

Application during pregnancy and lactation

It is not known whether sibutramine and its metabolites penetrate into breast milk... During the period breastfeeding application is not recommended.

Side effects of the substance Sibutramine

In placebo-controlled studies, 9% of patients receiving sibutramine (n = 2068) and 7% of patients receiving placebo (n = 884) discontinued treatment due to side effects.

In placebo-controlled studies, the most common side effects were dry mouth, anorexia, insomnia, constipation, and headache.

The following are side effects that were observed in patients taking sibutramine, with a frequency of ≥1% or more often than in the placebo group. Next to the name is the frequency of occurrence of this side effect in the group taking sibutramine, in brackets - similar data in the placebo group.

The organism as a whole: headache - 30.3% (18.6%), back pain - 8.2% (5.5%), flu-like syndrome - 8.2% (5.8%), accidental injury - 5.9% (4.1%), asthenia - 5.9% (5.3%), abdominal pain - 4.5% (3.6%), chest pain - 1.8% (1.2%), pain in the neck - 1.6% (1.1%), allergic reactions — 1,5% (0,8%).

On the part of the cardiovascular system and blood (hematopoiesis, hemostasis): tachycardia - 2.6% (0.6%), vasodilation (flushing of the skin with a feeling of warmth) - 2.4% (0.9%), migraine - 2.4% (2.0%), hypertension / increased blood pressure - 2.1% (0.9%), heart rate - 2.0% (0.8%).

From the digestive tract: anorexia - 13.0% (3.5%), constipation - 11.5% (6.0%), increased appetite - 8.7% (2.7%), nausea - 5.9% (2.8 %), dyspepsia - 5.0% (2.6%), gastritis - 1.7% (1.2%), thirst - 1.7% (0.9%), vomiting - 1.5% (1 , 4%), exacerbation of hemorrhoids - 1.2% (0.5%).

From the side of the musculoskeletal system: arthralgia - 5.9% (5.0%), myalgia - 1.9% (1.1%), tenosynovitis - 1.2% (0.5%), joint diseases - 1.1% (0.6 %).

From the nervous system and sensory organs: dry mouth - 17.2% (4.2%), insomnia - 10.7% (4.5%), dizziness - 7.0% (3.4%), nervousness - 5.2% (2, 9%), anxiety - 4.5% (3.4%), depression - 4.3% (2.5%), paresthesia - 2.0% (0.5%), drowsiness - 1.7% ( 0.9%), arousal - 1.5% (0.5%), emotional lability - 1.3% (0.6%), taste change - 2.2% (0.8%), ear diseases - 1.7% (0.9%), ear pain - 1.1% (0.7%).

From the respiratory system: rhinitis - 10.2% (7.1%), pharyngitis - 10.0% (8.4%), sinusitis - 5.0% (2.6%), increased cough - 3.8% (3.3 %), laryngitis - 1.3% (0.9%).

From the side of the skin: rash - 3.8% (2.5%), sweating - 2.5% (0.9%), Herpes simplex- 1.3% (1.0%), acne - 1.0% (0.8%).

From the genitourinary system: dysmenorrhea - 3.5% (1.4%), urinary tract infections - 2.3% (2.0%), vaginal candidiasis - 1.2% (0.5%), metrorrhagia - 1.0% (0 ,eight%).

Others: generalized edema - 1.2% (0.8%).

Interaction

Inhibitors of microsomal oxidation, incl. inhibitors of CYP3A4 cytochrome P450 (ketoconazole, erythromycin, cyclosporine, etc.) reduce the clearance of sibutramine. Drugs with serotonergic activity increase the risk of developing serotonin syndrome (agitation, sweating, diarrhea, fever, arrhythmia, convulsions, etc.).

Overdose

Symptoms: increased severity of side effects, most often - tachycardia, increased blood pressure, headache and dizziness.

Treatment: taking activated carbon, symptomatic therapy, monitoring vital functions, with an increase in blood pressure and tachycardia - the appointment of beta-blockers.

Route of administration

Inside.

Precautions for the substance Sibutramine

It is necessary to control the level of blood pressure and pulse rate every 2 weeks in the first 2 months of treatment and then once a month. In patients with arterial hypertension with blood pressure> 145/90 mm Hg. control should be carried out more thoroughly and more often, and in the case of twice registered increase in blood pressure> 145/90 mm Hg. treatment should be discontinued. The appearance during therapy of chest pain, progressive dyspnea (breathing disorder) and edema of the lower extremities may indicate the development of pulmonary hypertension (in this case, it is imperative to consult a doctor).

It is not recommended to take simultaneously drugs that increase the QT interval (astemizole, terfenadine, antiarrhythmic and other drugs), drugs containing ephedrine, phenylpropanolamine, pseudoephedrine, etc. (risk of increasing blood pressure and increasing heart rate), as well as other anorexigenic drugs with a central mechanism of action. With caution should be prescribed against the background of hypokalemia and hypomagnesemia, with impaired liver and kidney function of mild and moderate severity.

Women of childbearing age should use adequate contraception during treatment.

It should be borne in mind that sibutramine can reduce salivation and promote the development of tooth decay, periodontal disease, candidiasis and oral discomfort. It is recommended to limit alcohol consumption during the treatment period.

Sibutramine INN

International name: Sibutramine

Dosage form: capsules

Pharmachologic effect:

Anorexigenic agent that enhances the feeling of fullness. In vivo, it manifests its action due to metabolites (primary and secondary amines) that suppress the reuptake of monoamines (serotonin (5-HT) and norepinephrine). An increase in the content of neurotransmitters in synapses increases the activity of central 5HT-serotonite and adrenergic receptors, which contributes to a decrease in appetite and an increase in thermal production. Indirectly stimulating beta3-adrenergic receptors, it acts on brown adipose tissue. Sibutramine and its metabolites do not affect the release of monoamines, do not inhibit MAO; do not have an affinity for a large number of neurotransmitter receptors, including serotonin (5-HT1-, 5-HT1A-, 5-HT1B-, 5-HT2A-, 5-HT2C), adrenergic (beta1-, beta2-, beta3-, alpha1- , alpha2-), dopamine (D1-, D2-), choline-, histamine (H1-), benzodiazepine and NMDA receptors.

Pharmacokinetics:

Absorption is rapid after oral administration. It is almost completely metabolized in the liver with the participation of isoenzymes of the cytochrome CYP3A4 system with the formation of mono- (desmethylsibutramine) and di-desmethyl (di-desmethylsibutramine) forms of active metabolites (M1 and M2), as well as by hydroxylation and conjugation with the formation of inactive metabolites. TCmax of sibutramine - 1.2 h, M1 and M2 - 3-4 h. Cmax of M1 and M2 after a single oral administration of sibutramine at a dose of 15 mg - 4 ng / ml (3.2-4.8 ng / ml) and 6.4 ng / ml (5.6-7.2 ng / ml), respectively. Food intake increases TCmax and decreases Cmax of desmethyl metabolites by 3 hours and 30%, respectively; does not affect the AUC value of desmethyl metabolites. It is quickly and well distributed in tissues. Communication with proteins: sibutramine - 97%, M1 and M2 - 94%. T1 / 2 of sibutramine - 1.1 hours, M1 - 14 hours, M2 - 16 hours. It is excreted mainly by the kidneys in the form of inactive metabolites. In renal failure, the main pharmacokinetic parameters (Cmax, T1 / 2, AUC) of sibutramine and its active metabolites do not change significantly.

Indications:

Alimentary obesity with a body mass index of 30 or more; alimentary obesity with a body mass index of 27 or more, with risk factors caused by overweight (type 2 diabetes mellitus, dyslipoproteinemia).

Contraindications:

Hypersensitivity, mental anorexia, uncontrolled arterial hypertension, concomitant use of MAO inhibitors, pregnancy, lactation. With caution. Arrhythmia (including history), CHF (including history), coronary artery disease (including history), stroke (including history), drug or drug abuse dependence, cholelithiasis, angle-closure glaucoma, severe renal / hepatic failure, arterial hypertension (controlled and in history), neurological disorders, including mental retardation and seizures (including in history), childhood (up to 16 years - effectiveness and security not established).

Dosing regimen:

Inside, 10 mg in the morning, without chewing and drinking 200 ml of water; in case of ineffectiveness (decrease in body weight by less than 2 kg / month), the dose is increased to 15 mg / day. In patients who are poorly responsive to taking 15 mg (weight loss less than 2 kg in 4 weeks), further treatment should be discontinued. The course of treatment is no more than 3 months in patients who do not respond well to therapy (it is not possible to achieve a 5% level of weight loss from the initial one; treatment should not be continued if, after the achieved weight loss, with further therapy, the patient regains 3 kg or more ). The duration of treatment is 1 year.

Side effects:

Dysmenorrhea, edema, flu-like syndrome, itchy skin; tachycardia, palpitations, increased blood pressure, flushing of the skin; backache; abdominal pain, increased appetite, thirst, taste perversion, constipation or diarrhea, nausea, exacerbation of hemorrhoids; dryness of the oral mucosa, rhinitis; depression, insomnia, drowsiness, headache, dizziness, anxiety, irritability, nervousness, emotional lability; paresthesia of the skin; increased sweating; acute interstitial nephritis, mesangiocapillary glomerulonephritis; Shenlein-Henoch disease, convulsions; thrombocytopenia, bleeding; transient increase in the activity of "hepatic" transaminases. Overdose. Treatment: beta-blockers with an increase in blood pressure and tachycardia, control of vital functions (CVS, respiratory system), consultation with a psychiatrist. The effectiveness of forced diuresis or hemodialysis has not been established.

Special instructions:

Patients need to change their lifestyle and habits as part of drug therapy. (diet and increased physical activity) to ensure that the achieved weight loss is maintained after completion of treatment. Failure to comply with these requirements will lead to a repeated increase in body weight. Treatment is carried out only in cases where all other measures aimed at reducing body weight are ineffective. Women of childbearing age should use contraceptive drugs. During the period of treatment, it is necessary to refrain from using ethanol. During the period of treatment, it is necessary to control the level of blood pressure, heart rate in the first 2 months of treatment (every 14 days), and then monthly; concentration of serum lipids, uric acid, indicators of liver function. If the drug is missed, then continue taking it according to the prescribed scheme. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Interaction:

An increase in the concentration and toxicity of sibutramine (slowing down the metabolism) with the simultaneous use of inhibitors of microsomal oxidation (ketoconazole, erythromycin, toleandomycin, cyclosporine, cimetidine). Microsomal oxidation inducers reduce efficiency. Drugs that increase the concentration of serotonin in the blood (sumatriptan, dihydroergotamine, pentazocine, fentanyl, dextromethorphan) increase the risk of developing "serotonin syndrome" (due to selective blocking of serotonin reuptake). Drugs that increase blood pressure and / or heart rate (ephedrine, phenylpropanolamine, pseudoephedrine, as well as combined drugs for the treatment of "colds" containing these drugs) increase the risk of increased blood pressure and heart rate. The interval between taking MAO inhibitors (including furazolidone, procarbazine, selegiline) and sibutramine should be at least 2 weeks.