Sibutramine or ephedrine which is better. Forum for athletes - Power GYM

To suppress the rampant appetite and cure obesity, it is recommended to take Sibutramine for weight loss. Previously, a characteristic medication was used to treat depressive conditions, but in practice it turned out to be very mediocre. At present, a unique opportunity has been revealed to suppress appetite, to successfully fight extra pounds. Before taking diet pills with sibutramine, you need to consult with a nutritionist, your doctor.

What is Sibutramine

This synthetic drug 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, so the volume of daily portions is 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 it works

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

Preparations with sibutramine reduce blood cholesterol and contribute to a decrease in the concentration of glycerides, which helps to maintain your new weight for a long period of time without a strict diet. The process of disintegration 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 in 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 arrhythmia and tachycardia, an increase in blood pressure. Since the drug has a systemic effect 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 pronounced 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 drug, but it still does not hurt to contact a nutritionist immediately. Perhaps the specialist will recommend a milder analogue for successful correction of excess weight in adulthood.

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

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

Consequences of admission

If side effects occur in the body, it is categorically contraindicated to take the drug further, and correction of the daily dose will not provide the desired dietary effect. The doctor suggests another remedy to remove at home overweight, finally solve the problem of overweight at any age. Unpleasant consequences of oral administration can be as follows:

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

Why Sibutramine is banned in Russia

Many patients insist that the drug is a narcotic drug, since the consequences of its use resemble an unpleasant phenomenon called "breakdown in 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 intensifies. Therefore, the authorities decided to ban the sale of medicines in Russian pharmacies, although nothing prevents ordering and buying goods in an online pharmacy.

Is it possible to lose weight with Sibutramine

By controlling the feeling of hunger, the medicine 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 on an individual basis, otherwise, when losing weight, you can worsen general state health.

Indications for use

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

Preparations containing Sibutramine

Detailed description of this 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, the pharmaceutical industry has a number of equally worthy analogues that contain a similar chemical composition and pharmachologic effect in a lean body. Below are the most effective weight regulators from different manufacturers.

This dietary remedy is available in the form of capsules, which are packaged in blisters of 7, 14, 28, 84 pieces. Meridia for weight loss controls rampant appetite, eliminates obvious signs of obesity. Here is what you need to know about the characteristic medication before purchasing and using it:

  • manufacturer - pharmaceutical company Abbott GmbH (Germany);
  • price - 1700 rubles (14 capsules of 10 mg each);
  • composition - active ingredient: sibutramine monohydrate; auxiliary: colloidal silicone dioxide, microcellulose, magnesium stearate, lactose monohydrate;
  • principle of action - suppresses appetite, enhances heat transfer at the cellular level.

Goldline

With the development of obesity, you can lose weight with the help of this medication. Goldline is available in the form of capsules, 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 the 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, sends impulses to the brain about the feeling of satiety.

Lindax

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

  • manufacturer - concern Zentiva (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 dioxide and titanium;
  • principle of action - suppresses appetite, allows you to eat in small portions.

Reduxin

Continuing to study tablets with sibutramine, doctors recommend the anorectic Reduxin, which is also available in the form of capsules. Sales are dominated by packs of 30 and 60 pieces, intended for oral administration before meals. Here is valuable information potential buyer on a note:

  • manufacturer - Ozon (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 the effect of losing weight by stimulating metabolism.

Instructions for use for weight loss

The drug is intended for oral administration, a single dose is shown to be taken with plenty of water. The duration of intensive therapy is 1 year, since even minor changes in the problem figure are not observed immediately. In the first and second months of weight loss, the percentage of subcutaneous fat burning is minimal, as the doctor informs at 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, controlling nutrition. When losing weight, it is important to monitor the blood pressure indicator, which can pathologically increase during the correction of excess weight. The heart rate remains under control, and at the first symptoms of tachycardia, it is indicated to stop taking the medication, and additionally consult with a nutritionist.

Dosage

A single dose of a medicinal product 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 indicated to stop, consult a specialist.

Interaction

The use of Sibutramine for weight loss contributes to the acquisition of ideal forms, an impeccable body. However, it is shown to use it for its intended purpose wisely, not forgetting about drug interactions. For example, in combination with inhibitors of the CYP3A4 isoenzyme, the concentration of metabolites in plasma increases, 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 purchase a typical medicine on the domestic market, even in Moscow and St. Petersburg there are difficulties with buying a medicine. There is no medicine in real pharmacies, it is better to immediately contact an 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 the drug depends on the manufacturer and the number of capsules in one package. Retail prices of domestic pharmacology are more affordable for buyers, but an imported manufacturer often inflates 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

With increased sensitivity of the body to 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;
  • prostatic hyperplasia (for men);
  • pheochromocytoma;
  • drug addiction.

Video

The World Health Organization has called obesity the epidemic of the 21st century. Of the 7 billion people on the planet excess weight have 1,700 million, obesity - 500 million. According to disappointing forecasts, by 2025 the number of overweight people will exceed 1 billion! In Russia, 46.5% of men and 51% of women are overweight, and these figures are constantly growing.

According to medical terms, obesity is considered to be an excess of body weight by 30% or more. Weight gain due to the fatty layer, localized mainly in the abdomen and thighs.

In addition to physical and mental discomfort, the main problem excess weight - in complications: the likelihood of developing cardiovascular pathologies, diseases of the musculoskeletal system, arterial hypertension, atherosclerosis, and type 2 diabetes increases.

Not everyone succeeds in normalizing weight in such conditions only with the help of fitness and fashionable diets, so many resort to medication. The principle of action of such drugs is different: some reduce appetite, others block the absorption of carbohydrates and fats, others have a laxative effect that does not allow food to be fully absorbed.

Serious drugs have many contraindications and undesirable consequences. The doctor prescribes them for severe obesity, when it is simply unrealistic to lose a third or even half of your weight in other ways.

Among these potent medicines is Sibutramine (in the Latin prescription - Sibutramine).

An antidepressant developed at the end of the last century American company Abbott Laboratories, did not justify the hopes placed on him, but proved to be a powerful anorectic. The weight loss was so significant that it was prescribed to patients with severe obesity who did not control their appetite.

Why is Sibutramine banned?

Among those who like to solve all problems with a miraculous pill, the medicine has gained worldwide popularity. A drug that stimulates metabolic processes and suppresses an indomitable appetite, WHO predicted a great future.

In addition, Sibutramine caused an addiction close to a drug addiction (the effect of ecstasy or amphetamine). Patients were especially difficult to tolerate treatment. middle age. Until further research, the drug was banned in the USA, Canada, Australia, Europe, and Ukraine. In the domestic pharmacy chain, it can be purchased by prescription.

Anorectic is prescribed for primary obesity of II-III degree, when BMI exceeds 30-35 kg/m² and other treatment methods are ineffective. The therapeutic regimen includes special diet and adequate physical activity.

He was appointed to everyone with or without reason. But soon doctors began to sound the alarm because of side effects: patients had mental disorders, increased cardiovascular risk, and suicides became more frequent.

The drug is also indicated for type 2 diabetes mellitus, hyper- and hyproteinemia. In such cases, the body mass index should be above 27 kg/m². -Complex treatment, including Sibutramine and its analogues, is carried out under medical supervision.

An important aspect of the course is the patient's motivation to modify lifestyle and diet while maintaining the achieved result after treatment. Why Sibutramine is banned in civilized countries, see the TV report on the video:


Pharmacodynamics anorectic

In the head, different brain structures are responsible for the feeling of satiety. The connection between them is carried out due to the activity of neurons, the excitation of which awakens the appetite, calling us to the next snack.

When food enters the stomach, nerve impulses excite the brain structures responsible for the feeling of satiety. But the feeling of hunger does not necessarily have a physiological basis: sometimes you want to have a bite to reduce nervous tension, relax, and enjoy the process.

When there is no control over the balance between satiety and the amount of food ingested, inadequate eating behavior is created.

Sibutramine harmonizes the entire system, affecting neurons. Cells connect using synapses, connections that conduct signals like contacts in electrical wiring. Any activity of a neuron is accompanied by a release into a neurotransmitter - a biologically active compound that connects to the receptors of other neurons. This is how signals pass along their chain. Information about hunger or satiety is also transmitted along this path.

The balance helps to regulate serotonin: if its volume drops, a person experiences hunger. In the process of eating, the neurotransmitter is synthesized, when its amount reaches a certain limit, the body experiences saturation.

The drug prolongs this feeling by maintaining an appropriate level of serotonin in the synaptic gap. Thanks to this effect, healthy eating habits are formed in the patient, night hunger attacks disappear, and the amount of food consumed is reduced.

Anorectic also inhibits the reuptake of norepinephrine, which is produced in the central nervous system, where it plays the same role as a neurotransmitter. An increase in its content in the synoptic gap provokes a surge of energy. One of the features of this substance is the activation of thermogenesis, which releases energy from the liver, adipose and muscle tissues. This helps to reduce body fat and normalize lipid metabolism.

Under the influence of the synthetic appetite regulator Sibutraminum, eating behavior changes, thermogenesis increases. Fat reserves are burned, and the caloric content of the diet does not allow them to be restored. Increased thermogenesis activates β-adrenergic receptors that control energy production. Reduced appetite is associated with inhibition of the reuptake of norepinephrine and serotonin.

At observance of a dosage from side effects more often than others insignificant fluctuations of a blood pressure and a tachycardia were shown. You can see the possibilities of Sibutramine and the mechanism of its action on the video:

Pharmacokinetics of Sibutramine

Up to 80% of the oral drug is rapidly absorbed from the gastrointestinal tract. In the liver, it is transformed into metabolites - monodemethyl- and didemethylsibutramine. The peak concentration of the main active ingredient was recorded 72 minutes after the use of a tablet weighing 0.015 g, metabolites are concentrated over the next 4 hours.

If you take the capsule during the meal, its effectiveness drops by a third, and the time to achieve the maximum result is extended by 3 hours ( total level and distribution remain unchanged). Up to 90% of sibutramine and its metabolites bind to serum albumin and are rapidly distributed to muscle tissues.

Inactive metabolites are excreted in the urine, up to 1% are excreted in the feces. The half-life of sibutramine is about an hour, its metabolites are 14-16 hours.

The possibilities of the drug were studied in pregnant animals. The drug did not affect the ability to conceive, but experimental rabbits showed a teratogenic effect of the drug on the fetus. Abnormal phenomena were observed in the change in appearance and structure of the skeleton.

All analogues of Sibutramine are canceled at the stage of pregnancy planning. At breastfeeding medication is also contraindicated.

The entire period of treatment with Sibutramine and 45 days after it, women of childbearing age should use proven contraceptives. Before deciding to lose weight with the drug, you should think about planning your next pregnancy.

The drug is teratogenic, and although its ability to provoke mutations has not been established, the drug does not have a serious evidence base, and the list of contraindications will be supplemented.

List of contraindications for Sibutramine

For an anorectic, there are, first of all, age limits: the drug is not prescribed for children and adults (after 65 years). There are other contraindications for Sibutramine:


When prescribing Sibutramine, special attention should be paid to hypertensive patients, patients with blood flow disorders, with complaints of convulsions, with a history of coronary insufficiency, with epilepsy, liver or kidney dysfunctions, glaucoma, cholecystitis, hemorrhages, tics, as well as patients who use medications that affect blood clotting.


Unwanted Consequences

Sibutramine is a serious medicine, and like any serious medicine it has side effects, it is no coincidence that official medicine prohibits it in many countries. The simplest is allergic reactions. Not anaphylactic shock, of course, but skin rashes are quite possible. The rash passes on its own when the drug is discontinued or after adaptation.

A more serious side effect is addiction. They drink anorectic for 1-2 years, but many are not able to stop, strengthening drug addiction, comparable to drug addiction. How sensitive your body will be to Sibutramine cannot be determined in advance.

The effect of dependence can be observed already on the 3rd month of regular use.

Weaning should be gradual. A condition similar to "withdrawal" is a migraine, a lack of coordination, bad dream, a constant feeling of anxiety, high excitability, alternating with apathy and suicidal thoughts.

The drug interferes with the work of the "holy of holies" - the human brain and nervous system. It is not always possible to influence the brain and central nervous system without consequences for the psyche. The first attempts at treatment ended in severe addiction, suicide, mental disorders, and death from heart and brain attacks.

A modern medication undergoes high-quality purification, the dosage is significantly reduced, but unforeseen effects are not excluded. Regarding participation in road traffic and control of complex mechanisms, work at height, in any other conditions that require a quick reaction and increased attention, is prohibited during treatment with Sibutramine.

On Sibutramine, the instructions for use assure that most of the symptoms (tachycardia, hyperemia, hypertension, lack of appetite, changes in taste, defecation rhythm disturbances, hemorrhoids, dyspeptic disorders, sweating, anxiety, isomnia) disappear after discontinuation of the drug.

Study on Sibutramine in Europe - expert opinion

The SCOUT study, which was initiated by the relevant EU authorities after analyzing the sad medical statistics, involved volunteers with a high excess of body mass index and the risk of developing cardiovascular pathologies.

The results of the experiment are impressive: the likelihood of non-fatal strokes and heart attacks after taking Sibutramine increases by 16% compared with the control group who received placebo.

Among other undesirable phenomena, allergic reactions of varying severity, deterioration in blood composition (decrease in platelet levels), autoimmune damage to the vascular walls, and mental abnormalities were recorded.

The nervous system gave out reactions in the form of muscle spasms, memory lapses. Some participants had pain in their ears, back, head, vision and hearing deteriorated. Gastrointestinal disorders were also observed. The report concluded by noting that withdrawal symptoms can cause headaches and uncontrolled appetite.

Read more about how Sibutramine burns fat and improves mood - in the video

How to use anorectic

The tablet is taken once. The time of eating does not affect the result. At the beginning of the course, it is recommended to drink one capsule weighing 0.01 g. It is swallowed whole and washed down with water.

If in the first month the weight has gone within 2 kg and the medicine is tolerated normally, you can increase the rate to 0.015 g. If during the next month weight loss is recorded by less than 2 kg, the medication is canceled, since it is dangerous to adjust the dose further.

Interrupt the course of treatment and in the following cases:

  1. If less than 5% of the initial mass is lost in 3 months;
  2. If the process of losing weight has stopped at rates up to 5% of the initial mass;
  3. The patient began to gain weight again (after losing weight).

For more information about Sibutramine, see the video instruction on the video:

Overdose

Non-compliance with recommendations, increasing doses increases the risk of overdose. The results of such consequences have not been studied enough, so an antidote has not been developed. As part of emergency care for such symptoms, the victim is washed with a stomach, they are offered enterosorbents if no more than an hour has passed after using Sibutramine.

It is necessary to observe changes in the condition of the victim during the day. If signs of side effects appear, symptomatic therapy is carried out. The most common symptoms are high blood pressure and an increased heart rate. Such symptoms are treated with β-blockers.

The use of an "artificial kidney" apparatus in case of an overdose of Sibutramine is not justified, since the metabolites of the drug are not eliminated by hemodialysis.

Options for the interaction of Sibutramine with other medicines


Sibutramine is not compatible with alcohol. Tablets based appetite regulator pharmacodynamics oral contraceptives do not change.

Terms of purchase and storage

Despite the fact that in many countries Sibutramine is prohibited in the official pharmacy network, the Internet is full of such offers. So you can buy anorectic without a prescription. True, the consequences in this case will have to be taken care of personally. The price of Sibutramine (about 2 thousand rubles) will also not suit everyone.

The rules for storing the medicine are standard: room temperature (up to 25 ° C), control of the expiration date (up to 3 years, according to the instructions) and children's access. Tablets are best kept in their original packaging.

Sibutramine - analogues

The largest evidence base (but not the lowest cost) is Xenical, a drug with a similar pharmacological effect used in alimentary obesity. In the trading network there is a synonym for Orlistat. The active ingredient blocks the absorption of fats by the intestinal walls and removes them naturally. The full effect (higher by 20%) is manifested only if the diet is followed.

Side effects are observed in the form of violations of the rhythm of defecation, flatulence. The severity of symptoms directly depends on the calorie content of the diet: the fatter the foods, the stronger the intestinal disorders.

The differences between Sibutramine and Xenical are in pharmacological capabilities: if the first reduces appetite by acting on the brain and nerve centers, then the second removes fats, binding to them and forcing the body to spend its own fat reserves to compensate for energy costs. Through the central nervous system, Sibutramine affects all organs of the system, Xenical does not enter the circulatory system and does not affect organs and systems.

Fenfluramine is a serotonergic analogue from the group of amphetamine derivatives. It has a mechanism of action similar to Sibutramine and is just as banned on free sale as a narcotic substance.

Fluoxetine, an antidepressant that inhibits serotonin reuptake, also has anorexic potential.

The list can be supplemented, but all anorexigenic drugs, like the original, have many side effects and can seriously harm health. The original has no full-fledged analogues, appetite regulators of the Indian manufacturer are more or less known - Slimia, Gold Line, Redews. It’s not worth talking about Chinese dietary supplements - 100% pig in a poke.


Reduxin Light - dietary supplement based on oxytriptan, which has nothing to do with sibutramine, has sedative capabilities, depresses appetite. Are there analogues for Sibutramine cheaper? Available dietary supplements Listat and Gold Line Light have a different composition, but the packaging design is very similar to the original Sibutramine. Such a marketing trick certainly does not affect the quality of the supplement.

Opinions of losing weight and doctors

About Sibutramine, some reviews are alarming, the victims and their relatives are intimidated by irreversible side effects, they call for quitting treatment. But those who survived the adaptation period and did not quit the course note noticeable progress.

Andrey, 37 years old. I have been taking Sibutramine for only a week so far, but it really helps me overcome hunger. The fear of novelty and the threats of "well-wishers" is gradually disappearing. The first two days the head was heavy, now there is still dryness in the mouth. Loss of strength and, moreover, the desire to kill myself, I did not have. I eat twice a day, but you can also once a day: I eat up from one small portion. I take one fat burner capsule with meals. Before that, he did not leave the refrigerator at night. So far, my weight is 119 kg with a height of 190 cm. There is enough energy to climb the horizontal bar. If anyone cares about the issue of sex, then that's all right.

Valeria, 54 years old. Sibutramine is a strong medicine, I lost 15 kg in six months. Given that I have diabetes, this victory is doubly credited to me. At first, there were side effects from Sibutramine - the stomach was upset, the body itched, and the head ached. I even thought about quitting the course, but the doctor prescribed me vitamins, sedatives, something for the liver and kidneys. Gradually, everything went away, now I only take Sibutramine 1 tablet and my own Metformin. I feel good - my sleep and mood have improved.

About Sibutramine, the doctors' reviews are more restrained: doctors do not deny the high effectiveness of Sibutramine, they remind of the exact observance of the prescription and regular monitoring of those who are losing weight. They warn about the dangers of self-medication, since the drug is very serious and no one is immune from side effects.

According to statistics, at least 50% of those who lose weight with Sibutramine face at least one of the undesirable effects. After all, it is no coincidence that in most economically developed countries the drug is banned, and in Russia it is included in the list of potent drugs.

Losing weight is difficult - and everyone who has tried to get rid of at least a couple of extra pounds knows this. You can’t get around the laws of nature: only diet and physical activity can defeat fat accumulation. To lose dozens of extra pounds through diet and fitness, you need remarkable willpower. Obese people are beginning to look for miracle pills and diet pills, among them is the drug sibutramine for weight loss.

Sibutramine was created as a cure for depression, but during the trials it was found to be an effective appetite suppressant. For 13 years in the US and Europe, doctors prescribed the drug to people suffering from obesity, until serious side effects of this popular weight loss remedy were discovered. According to American experts, the harm from the use of sibutramine far outweighs the benefits it provides for weight loss. In the United States, this drug has been withdrawn from sale, and in Russia it is included in the list of potent weight loss drugs that are bought at a pharmacy strictly on prescription.

So, more than 10 years of history of sibutramine use 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 built in the mirror. Like all potent 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 a time bomb that can undermine the body's defenses? To understand this issue, it is necessary to understand the principle of the drug, thanks to which it contributes to weight loss.

Pharmacological properties of the drug Sibutramine (Sibutramine)

Chemical compound
IUPAC (±)-1-(4chlorophenyl)-N, N-dimethyl-
Alpha-(2-methylpropyl)
cyclobutanemethanamine
(as hydrochloride)
Gross-
formula
C17H26ClN
Mol.
weight
279.85 g/mol
CAS 106650-56-0
PubChem 5210
drug bank APRD00456
Classification
Pharm.
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 in medicine 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 the burning of fat reserves. The second property of sibutramine is appetite suppression, it helps to reduce the calorie intake during weight loss. Old fat reserves 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, the level of cholesterol in the blood decreases, but at the same time the heart rate increases, the heart's need for oxygen increases, blood pressure rises - the body behaves as in a situation of severe stress. Reduced appetite is associated with the selective action of sibutramine on serotonin and norepinephrine - these brain neurotransmitters cause a state of happiness, satisfaction, dull the feeling of hunger, and reduce the need for food.

At the same time, drug intoxication occurs and dependence on the drug is formed. After oral administration, sibutramine is absorbed into the blood within 1-2 hours, and absorbed by 77%. In the liver, its transformation occurs, 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 in which the use of sibutramine tablets as a weight loss drug is justified.

  • Firstly, it is a severe degree of obesity, when the body mass index (BMI) is equal to or greater 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 containing sibutramine with a BMI equal to 27 kg / m2, if obesity is accompanied by complications in the form of diabetes mellitus, hypertension.

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

Despite the help of a potent drug, the following remain absolutely necessary:

  • dieting;
  • balanced physical activity;
  • changing lifestyle and eating habits.

The course of therapy with the use of sibutramine lasts not less than a year, while it is important to follow the doctor's recommendations in everything: do not change the dose of the medicine and the frequency of its administration, do not start and end the treatment without permission. It is mandatory 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, other anti-obesity drugs.

Contraindications

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

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

  • Sibutramine is contraindicated in obesity, caused by organic pathologies - such as endocrine diseases, hormonal failure; neoplasms in the brain; violation of metabolism and water balance in the body.
  • It is very risky to use this remedy for weight loss in cardiovascular diseases: ischemia, tachycardia, arrhythmia, heart failure, myocardial defects, vascular disorders.
  • It is strictly forbidden to use drugs containing 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, liver, kidney, and prostate pathologies.
  • A special risk group is women during pregnancy and lactation, people over 65 years of age, those who have found 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 consulting a nutritionist and under the supervision of a doctor. Undesirable effects are most pronounced during the first month of using the drug, then they weaken and disappear. Only a doctor can determine potential danger 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 effect of addiction and withdrawal symptoms. (breaking) with its sudden cancellation. Without the usual dose of medication, the patient experiences anxiety, depression, insomnia, and suicidal thoughts. The restless state of consciousness is accompanied by general weakness, rapid pulse, hand tremors, migraines and fainting. The table below shows the percentage of occurrence 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 it is taken, patients experience increased blood pressure, increased heart rate, and chronic fatigue syndrome develops. An overdose of the drug may increase unwanted effects and pose a threat to health. It is recommended to take Activated carbon, contact a doctor or poison control center.

Sibutramine instructions for use

According to doctors, sibutramine is very effective tool for weight loss, which can help people suffering from an advanced form of alimentary obesity as a result of bad eating habits. Pathologically large weight (BMI ˃ 30) provokes fatal dangerous diseases: diabetes mellitus, 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 the use of 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 were missed, the dose cannot be increased, you should continue taking the tablets as usual.
  • The expected effect from the use of 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 weight by 5%, then you should switch to an analogue containing another active substance.
  • Treatment with drugs containing sibutramine should not be continued for longer than a year; the drug is stopped under the supervision of a doctor.

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 medicines based on it (Reduxin, Goldline - Russian-made) 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.

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

Many people who want to lose weight know that doing this is not at all easy. After all, you need to have great willpower to follow a diet. And after you managed to lose those extra pounds, you need to moderate your appetite in every possible way so that you don’t return at a double speed. Very often, those who want to lose weight resort to the help of medications. These drugs, at least many of them, contain a chemical called sibutramine. It is about him that will be discussed in this article.

What is Sibutramine?

If several attempts to lose weight do not bring any results, and many effective methods have already been used to lose weight, people's self-esteem is greatly reduced in connection with this. And this can serve as a starting point in the development of deep psychological complexes and severe depression. Perhaps that is why many people who are losing weight believe that it is possible to lose extra pounds with the use of drugs, for example, a drug such as Sibutramine. What is it? An unconditional good that will eradicate the root of evil, or a time bomb that can finally undermine human health?

It is important to understand that Sibutramine is a potent medical drug, and not a harmless substance. And therefore it has, like any medicine, some contraindications, side effects and has negative effects on the body.

In this regard, it is necessary, before starting to take this drug, consult a doctor about the use of this medicine. But after all, people really lost weight by taking Sibutramine, the reviews of those who are losing weight confirm this in every possible way, you say. But at what cost did this happen and what side effects did they have after taking Sibutramine? This article will try to answer these and other questions.

Description

It is a centrally acting drug for the adjunctive treatment of obesity. It must be used in conjunction with a strictly controlled diet and increased physical activity. After taking the drug "Sibutramine" (tablets or capsules), a feeling of fullness occurs. That is, even a small portion of food gives a person a feeling of satiety. And this leads to a decrease in food intake. By suppressing the reuptake of serotonin, the drug "Sibutramine" affects the center of the brain responsible for appetite.

special instructions

The use of the drug is possible only when all other measures aimed at weight loss are ineffective. Therefore, only in these exceptional cases should Sibutramine be used. Reviews of those who are losing weight mainly contain information that energy is increasing. Therapy should be carried out under the strict supervision of a physician who has experience in correcting obesity as part of a complex treatment, such as:

  1. Diet.
  2. Changing eating habits and lifestyle.
  3. Increasing physical activity.

Contraindications

As mentioned above, everything related to medicines, causes side effects and is not always and not suitable for everyone for medical reasons. This also applies to such a drug as Sibutramine. Instructions for the use of this medication has such an important point as contraindications. List of diseases in which the use of "Sibutramine" is prohibited:

  1. Hypersensitivity of the body.
  2. The presence of organic causes of obesity.
  3. Mental illness.
  4. hearts.
  5. Heart failure.
  6. Congenital heart defects.
  7. Tachycardia.
  8. Arrhythmia.
  9. Stroke.
  10. Cerebral circulation disorders.
  11. Severe violations of the liver and kidneys.
  12. Drug and alcohol addiction.
  13. Pregnancy.
  14. lactation period.
  15. Glaucoma etc.

Side effects

Reading numerous reviews, especially those that describe side effects after taking this drug, you involuntarily think that many simply attribute their sores to this medicine. Indeed, even a simple and well-known "Analgin" causes almost similar phenomena after its adoption. Still, it is better, before taking Sibutramine, reviews of doctors, to study the side effects very carefully. Possible:

  1. Headache and dizziness.
  2. Insomnia.
  3. Feelings of fear and excitement.
  4. Jumps in blood pressure.
  5. Tachycardia.
  6. Arrhythmia.
  7. Chills.
  8. Chair problems.
  9. Dry mouth.
  10. Nausea and vomiting.
  11. Sweating.
  12. Changing the psyche and behavior.
  13. Change
  14. Back pain.
  15. Allergic reactions.
  16. flu-like syndrome.
  17. Urinary tract infections.
  18. Laryngitis.
  19. Increased cough.
  20. Drug addiction effect.

Overdose

There are cases when there is an increase in the severity of side effects. This may be when an overdose of a drug has accidentally or deliberately occurred, including one such as Sibutramine. Reviews of doctors in this case agree that the patient needs:

  1. Take activated charcoal.
  2. Call a doctor or medical help.
  3. Contact the nearest poison control center.

Application

How to use this effective weight loss remedy called "Sibutramine"? Instructions for use quite clearly explains what the daily intake of this medication is. The initial dose of the drug per day is 10 mg. The capsules are taken in the morning. It is necessary, without chewing, to drink large quantity water (at least 250 ml) Sibutramine tablets. Instructions for use (the database of tablets is described in this manual) will help you use the product correctly.

If the effect is not observed at this dosage (weight loss within 4 weeks - 2 kg), then with good tolerance of the drug, the rate can be increased to 15 mg per day. If positive dynamics is not observed, the use of "Sibutramine" should be discontinued. The period of taking the drug at a dose of 15 mg is limited in time.

It is necessary to take Sibutramine (tablets) within 1 year. It is not recommended to use it for a longer period, since there is no data on the effectiveness and safety of a longer course of medication. If the patient fails to lose at least 5% of the total weight within 3 months, then the drug should be stopped.

Regularly taking "Sibutramine", reviews of losing weight confirm this information, patients manage to lose overweight within 6 months. The result is maintained throughout the course of treatment. If the daily dose of the medicine was missed, then doubling the dose the next day is not recommended. It is necessary to return to the usual scheme of taking pills. It is necessary to stop taking medications after consulting with your doctor.

Precautionary measures

It must be understood that the effect of the drug will be noticeable only in combination with a diet. It is necessary to use the Sibutramine weight loss agent, which was described in the previous section, with some degree of caution. After all, some of its effects on the human body are already known.

It is also necessary to adhere to certain conditions for those people who use this medicine. Here are the conditions and precautions that should not lead to unpleasant consequences:

  1. The advanced age of the patient.
  2. Driving.
  3. Working with mechanisms.
  4. Simultaneous medication and alcoholic beverages. "Sibutramine" enhances the sedative effect of alcohol.

This drug was developed by Abbott Laboratories. Most often it can be purchased under the name Reductil, and in the United States of America as Meridia. FDA approved.

Chemical composition

Sibutramine is an anorexigenic medicine that increases the feeling of fullness in the body. It is a centrally acting serotonin and norepinephrine reuptake inhibitor, very similar in structure to amphetamine. This drug is a racemic mixture of (+) and (-) enantiomers of 1 - (4-chlorophenyl)-N, N-dimethyl-alpha-(2-methylpropyl) - methylamine cyclobutane, formula C17H26ClN, molecular weight 279.85 g / mol. Sibutramine is one of the drugs that is recommended for use in a complex of maintenance therapy aimed at combating obesity.

In 2010, the United States Food and Drug Administration recommended that people with a history of cardiovascular problems should not use this drug. And the British Health and Medicines Regulatory Agency has said that any drug that contains sibutramine is harmful to a person and his health.

Properties

Sibutramine hydrochloride is a selective serotonin and norepinephrine reuptake inhibitor used in the treatment of overweight patients. It helps to gradually reduce excess body fat, that is, it is a long-term drug. Sibutramine hydrochloride is recommended to be used in addition to a diet in which the amount of calories consumed is gradually reduced.

The thermogenic action of Sibutramine is carried out through the adrenergic system, mainly by indirect activation of beta-3-adrenergic receptors. The use of this drug sharply increases the content of thermogenesis in brown adipose tissue, during this process the body temperature changes upwards by about 1 degree. But this is one of the main actions of clenbuterol, so in this case, the change in body temperature shows that the process is happening correctly.

Sibutramine helps to gradually, sustainably and safely reduce fat accumulation through two basic aspects. First, this drug increases calorie expenditure and speeds up metabolism. Secondly, sibutramine hydrochloride significantly suppresses the feeling of hunger. During the studies, it was found that at the first dose of the drug at a dose of 10 mg, the metabolism improved by about 30% and this efficiency does not decrease for six hours, and the calorie content of the food consumed per day was reduced to 1300 Kcal.

Clinical researches

In 2001, two independent clinical trials were conducted in different countries peace.

The first one took place in the USA, Kansas, Institute of Clinical Pharmacology. A group of people took part in it, which included 322 people of different ages, gender and with varying degrees of obesity.

The second was conducted in China by the Department of Endocrinology. Here, 120 people with the same problems took part in the study.

As a result of these studies, which lasted for 168 days, and in one and another country, patients taking Sibutramine hydrochloride showed a positive trend in the process of weight loss. More accurate data show that in China, the average weight loss of all subjects was almost 7 kg over this period of time, and in the United States, over the same period, the average weight loss was from 5% to 10% of the initial weight of the subjects.

pharmachologic effect

Pharmacological action - anorexigenic. Inhibits the reuptake of neurotransmitters - serotonin and norepinephrine from the synaptic cleft, potentiates the synergistic interactions of the central norepinephrine and serotonergic systems. Sibutramine suppresses hunger, increases thermogenesis (due to mediated activation of beta3-adrenergic receptors), affects adipose tissue. Forms active metabolites in the body that are superior to sibutramine hydrochloride in the ability to inhibit the reuptake of serotonin and norepinephrine. These active metabolites also block the reuptake of dopamine, but 3 times weaker than 5-HT and norepinephrine. Sibutramine does not affect the release of monoamines and MAO activity, does not interact with neurotransmitter receptors, including serotonergic, adrenergic, dopaminergic, benzodiazepine and glutamate (NMDA), does not have anticholinergic and antihistamine effects, inhibits the uptake of 5-HT by platelets and may alter platelet function.

Weight loss due to a decrease in fat mass is accompanied by a decrease in the amount of triglycerides, cholesterol, LDL and uric acid and an increase in the concentration of HDL in the blood serum. When using this drug, there is an increase in blood pressure at rest (by 1-3 mm Hg) and an increase in heart rate (by 3-7 beats / min), such changes are considered insignificant, but in rare cases they are more pronounced. In the case of simultaneous use with inhibitors of microsomal oxidation, the heart rate increases (by 2.5 beats / min) and the QT interval lengthens (by 9.5 ms).

In a 24-month study in laboratory rats, at doses at which the observed total area under the concentration-time curves (AUCs) for 2 metabolites was 0.5-21-fold greater than that of the MRDH. The frequency of formation of benign tumors of the interstitial tissue of the testicles, mainly in males, has increased. No carcinogenic effect was found in females, as well as in mice of both sexes. Does not affect fertility and does not have a mutagenic effect. During the administration of doses to rats, the AUCs of both active metabolites for which were 43 times higher than those observed when taking MRDH, no teratogenic effect was detected. But when conducting a study in rabbits in conditions where the AUCs of active metabolites of sibutramine was 5 times greater than when using MRDH. In subsequent descendants, minor changes in physical development were found. In some individuals of the offspring, changes in the thickness of the bones were revealed and the tail, muzzle and auricles slightly changed in shape and size.

Application

The initial dose should be 10 mg 1 time per day, but after 4 weeks, if weight loss is insignificant, it is recommended to increase the dose to 15 mg. Further increase in the dose is not recommended. The dosage is the same for both men and women.

Side effects

Side effects may occur during the first month of taking the drug, but over time, the frequency of their manifestation should weaken.

For the digestive system, loss of appetite, constipation, a feeling of dry mouth, nausea, and a transient increase in liver enzymes are possible.

The consequences for the central and peripheral nervous system can be: the occurrence of insomnia, headaches, dizziness, feelings of anxiety, paresthesia, increased sweating, changes in taste, periodic convulsions. A single case was also recorded when a patient's schizoaffective disorder developed into acute psychosis.

As consequences for the cardiovascular system, there may be: tachycardia, an increase in blood pressure (a slight rise in blood pressure at rest by 1-3 mm Hg and a slight increase in heart rate by 3-7 beats / min), vasodilation (the skin turns red, feels warm), hemorrhoids may aggravate. In rare cases, a more pronounced increase in blood pressure and heart rate, a feeling of palpitations is possible.

There are isolated cases of acute interstitial nephritis, mesangiocapillary glomerulonephritis in the urinary system.

For the circulatory system, thrombocytopenia, Shenlein-Genoch purpura, may occur.

Indications for use

With alimentary obesity with a body mass index of 27 kg / m2 or more, in the presence of risk factors that are caused by overweight, incl. type 2 diabetes mellitus or hyperlipidemia. It is recommended to use Sibutramine in complex therapy for patients with severe overweight.

Contraindications

It is contraindicated to use during pregnancy and lactation, as well as in case of mental illness, Tourette's syndrome, coronary artery disease, congenital heart defects, chronic heart failure, peripheral arterial occlusive diseases, tachycardia, arrhythmias, cerebrovascular accidents, arterial hypertension, impaired renal or hepatic function, hyperthyroidism, benign prostatic hyperplasia with residual urine formation, pheochromocytoma, glaucoma, anorexia, bulimia, drug, alcohol or pharmacological dependence, organic cause of obesity, concomitant use or up to 14 days after discontinuation of MAO inhibitors or other medicines, which have a depressant effect on the central nervous system, during the use of other drugs that contribute to weight loss, hypersensitivity to Sibutramine hydrochloride.