The effect of sibutramine on fat. Sibutramine for weight loss - pros and cons, contraindications, side effects, reviews

The mechanism of action of sibutramine

The substance belongs to the group of appetite regulators. Sibutramine is a white or cream-colored crystalline powder. Release form: capsules for oral administration. The mechanism of action of the main substance is based on the rapid satisfaction of hunger and activation of the feeling of satiety. This leads to a reduction in food intake without effort on the part of the patient. Initially, Sibutramine was developed as a means to correct the psycho-emotional state, and not to reduce body weight.

The process of eating food refers to stimulators of signal transmission between brain neurons. Serotonin and norepinephrine are released into the intercellular space (synapse). Sibutramine blocks the return signal, due to which the concentration of neurotransmitters in the synapse increases. The signal of saturation is more active in postsynaptic cells, and the body does not require additional nutrition.

The molecules of the active substance stimulate thermogenesis - the production of thermal energy. As a result, metabolism accelerates, secondary and primary amines are formed, which independently inhibit the reuptake of norepinephrine, serotonin and the pleasure hormone - dopamine. These processes stimulate rapid saturation, the feeling becomes permanent. The desire to snack disappears, the amount of food is significantly reduced, and the weight begins to go away.

The reduction in body fat when consuming the capsules is complemented by an increase in the level of high-density lipoproteins. At the same time, there is a decrease in the amount of triglycerides, cholesterol, and uric acid. Presumably, Sibutramine is not a mutagen, does not reduce fertility, and does not have a carcinogenic effect. The substance reaches its maximum concentration in plasma after 1-2 hours. Sibutramine is excreted through the kidneys, the half-life is 16 hours.

What is Sibutramine

Sibutramine is a weight loss medication that reduces appetite. Acts through the brain, improves mood and motor activity. It should be taken only in combination with dietary nutrition and physical activity.

Sibutramine - what is this substance?

Sibutramine is the active ingredient in drugs to reduce appetite. Its main characteristics are shown in the table.

It is important to note that there are only two types of medications for weight loss - Sibutramine and Orlistat. Absolutely all other pills that are sold in pharmacies for weight loss are dietary supplements.

How to lose weight with Sibutramine

To lose weight, you need to create a negative calorie balance, that is, your calorie intake must exceed your intake from food. For this, diet and physical activity are prescribed. Since obesity is a disease with hormonal imbalance, attacks of uncontrollable hunger occur. They do not make it possible to adhere to medical recommendations for a long time.

Adipose tissue, once appearing in excess quantities, then protects itself with all its might from reduction. In cases where excess weight not only has a cosmetic defect, but also significantly threatens the patient’s health, Sibutramine is prescribed. Under its influence:

• the amount of food eaten decreases;
• Diet adherence is made easier;
• eating breakdowns are less common;
• consumption of foods in the evening and at night is reduced;
• weight loss faster;
• You can maintain the achieved result for a long time.

If you use Sibutramine, but do not change your diet and physical activity, you will not lose weight. Therefore, the drug is used only in combination with the main methods of losing weight - a lack of calories and increased energy consumption.

Mechanism of action

The peculiarity of Sibutramine is its central mechanism of action, which means it acts through the brain. It inhibits the reuptake of neurotransmitters (serotonin, norepinephrine) by brain cells. As a result, they accumulate at the point of contact between neurons (synapse) and the saturation centers receive a signal that the body has enough food.

At the same time, mood (antidepressive effect) and physical activity improve. Sibutramine also helps burn fat, increases heat production and, accordingly, calorie consumption.

Effect on the body

Under the influence of Sibutramine, fat metabolism is normalized in the body. In patients, the content of “good” cholesterol in the blood increases, which has a protective effect on blood vessels. By reducing triglycerides and low-density lipoproteins, the risk of progression of atherosclerosis and vascular diseases is reduced.

At the same time, tissue sensitivity to insulin is restored and insulin resistance is reduced. This is of great importance for concomitant type 2 diabetes mellitus, metabolic syndrome, and polycystic ovary syndrome. In the latter case, women have an increased chance of successful infertility treatment.

We recommend reading about drugs for the treatment of obesity. From the article you will learn about when drugs are prescribed for obesity, their mechanism of action, drugs for the treatment of 1st, 2nd and 3rd degree obesity. And here is more information about what powerful weight loss products you can purchase.

Is sibutramine a drug?

Sibutramine does not have a direct narcotic effect, but, nevertheless, there are examples where patients did not comply with the recommendations for duration of use and dosage. This drug initially causes a surge of energy and inhibits appetite. It is easier to lose weight with it, and when withdrawn, the brain is deprived of stimulating support, withdrawal syndrome occurs - depressed mood, general weakness, and even mental disorders have been described.

Another feature is addiction. It does not stop acting at the molecular level, but the feeling of vigor gradually fades away. This leads to the fact that patients tend to compensate for this decrease in effect by increasing the daily dose. It does not provide greater weight loss, but provokes the development of severe adverse reactions. Therefore, independent uncontrolled use and changing the treatment regimen are strictly prohibited.

Official study

The drug Sibutramine has a complex and interesting history:

• invented as an antidepressant, then found to reduce appetite and weight;
• approved for the treatment of obesity based on a study of 20,000 people, proven effectiveness;
• after the start of use, reports of death from heart attack and stroke appeared (49 deaths in patients under 50 years of age);
• there was a demand for withdrawal from the market;
• the manufacturing company decided to more carefully determine contraindications (SCOUT study in 10 thousand people over 55 years old), the risk was proven for elderly patients and those with heart disease;
• since 2010 it has been banned in the European Union, Ukraine, India, Hong Kong and China.

The drugs Reduxin and Goldline, which contain not pure sibutramine, but its combination with methylcellulose, are registered in Russia. This limits the possibility of its use as a psychostimulant and narcotic drug, but increases its effectiveness in reducing appetite.

Goldline

Reduxin

In 2011-2012, the “Spring” study was conducted among 34,000 obese people. It gave the following results:

• the diagnosis was removed in 44%;
• weight decreased by 11-13% in 16,000;
• ideal weight achieved at 3500;
• indicators of fat and carbohydrate metabolism have improved;
• after normalization of the mass, blood pressure decreased by 2-3 mmHg. Art., pulse 3 beats per minute;
• side effects occurred in 921 people;
• there were no serious complications.

A larger study was of Reduxin called PrimaVera in 100,000 people. The drug was taken for 6 months. The diagnosis of obesity was removed in 51%, and adverse reactions were recorded in 2.8%.

Watch this video about how Reduxin works, its use and contraindications:

Indications for use

Sibutramine is indicated for obese patients if the body mass index (weight/height square in meters) is above 30. Against the background of excess weight, there may be concomitant metabolic diseases:

• diabetes,
• metabolic syndrome,
• polycystic ovary syndrome,
• elevated blood cholesterol.

For such patients, as well as for those with a family history, Sibutramine is recommended even with a lower index (from 27). The drug can be used if diet and physical activity are ineffective after 3 months of compliance, or it can be prescribed by an endocrinologist from the very beginning of obesity treatment.

Indications for use

Medicines containing sibutramine are potent drugs. It is necessary to understand that self-medication is strictly prohibited. It is important to take Sibutramine only after consulting a specialist. The course of treatment must be carried out under the supervision of a doctor. Indications for the use of the drug are the following conditions:

• Primary nutritional obesity, in which the body mass index is more than 30–35 kg/m². An important condition for prescribing is the ineffectiveness of other treatment methods.
• Insulin-dependent diabetes (type 2) with a body mass index of 27 kg/m² or more.
• Dislipoproteinemia is a metabolic pathology characterized by a violation of the quantitative and qualitative parameters of lipoproteins in plasma.

Treatment before, during and after pregnancy

Sometimes obesity causes hormonal imbalances in women and prevents them from becoming pregnant, carrying and giving birth to a healthy baby. The situation requires nutritional and medical intervention. If other methods of weight correction are ineffective, sibutramine can be prescribed before pregnancy. It is important to consider that the drug has a teratogenic effect, that is, it can provoke fetal development abnormalities.

For the entire period of treatment, the woman must provide reliable contraception. At least two months must pass from the end of the course of treatment to the moment of conception. During this period, the body will get rid of the remaining drug substance. Treatment with the drug during pregnancy and breastfeeding is strictly prohibited.

Contraindications

The medicine has a large list of contraindications. They are the following states:

• secondary obesity due to organic reasons (diseases of the endocrine system, central nervous system);
• eating disorders (anorexia, bulimia);
• toxic goiter;
• disturbance of blood flow in parts of the brain and peripheral vessels;
• generalized tic (Tourette's syndrome);
• heart disease (ischemia, arrhythmia, stroke, congenital heart disease);
• severe pathologies of the kidneys and liver;
• allergy to the active substance;
• mental pathologies;
• arterial hypertension (high blood pressure);
• hormonally active tumor of the adrenal glands or another location (pheochromocytoma);
• prostate adenoma;
• reduction or complete absence of the lactase enzyme (hypolactasia);
• angle-closure glaucoma;
• pregnancy and breastfeeding;
• alcohol, drug, pharmaceutical addiction.

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There is a list of diseases for which diet pills with sibutramine are prescribed with extreme caution. These are the states:

• age under 18 and over 65 years;
• epilepsy;
• hypertension;
• coronary insufficiency;
• cholelithiasis;
• muscle spasms;
• hemorrhage (pathological bleeding in various parts of the body);
• bleeding disorders;
• increased levels of magnesium and potassium in the blood;
• kidney or liver dysfunction.

Precautionary measures

It is necessary to understand that the effect of the medicine will be noticeable only in combination with a diet. The weight loss product Sibutramine, described in the previous section, should be used with some 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. These are the conditions and precautions, the observance of which will not lead to unpleasant consequences:

1. Old age of the patient.
2. Driving a car.
3. Working with mechanisms.
4. Simultaneous use of medication and alcoholic beverages. Sibutramine enhances the sedative effect of alcohol.

Side effects

Studies have revealed the risk of adverse events when taking the drug. Side effects include:

• headache;
• dry mouth, nausea;
• anxiety, insomnia, acute psychosis;
• sweating, cramps;
• anorexia;
• constipation, hemorrhoids;
• overflow of blood vessels (hyperemia);
• increased bleeding due to a decrease in platelet count (thrombocytopenia);
• increased blood pressure;
• increased heart rate, tachycardia;
• loss of appetite;
• jade, purple;
• increased activity of liver enzymes.

Patient reviews

Reading only laudatory reviews on various forums about Sibutramine and others, you should remember that in order to increase sales, many manufacturers themselves write only about the positive aspects of their product. When choosing “Sibutramine” for weight loss, what kind of medicine this is has already been written in this article, you must first of all follow the recommendations of your doctor. Opinions on the Internet and advice from friends and acquaintances can play a bad joke on you. Of course, you need to read patient stories online, but you shouldn’t believe 100% everything that is written there.

Patient reviews of this drug are very heterogeneous. Some people do not notice any positive changes at all in such a matter as getting rid of excess pounds. Someone notes that they have become depressed. The mood changes very often, even to the point of aggressiveness. Many people experience palpitations, dry mouth, and excessive sweating after taking Sibutramine. The properties of this drug contribute to the occurrence of these side effects. It is important to remember that these unpleasant symptoms should subside within 1-2 months after starting to take the drug.

You need to be very careful about your blood pressure. After all, some patients note its jumps. This is very dangerous for your health. Therefore, doctors recommend that, along with a pack of medications, you also purchase a tonometer to measure blood pressure.

Mode of application

Sibutramine tablets and capsules should be taken on an empty stomach. It is better to do this in the morning, before breakfast. You need to drink 1 capsule. The instructions indicate that the daily dosage of the medication is 10 mg. If weight loss is slow (less than 2 kg in 30 days), it is allowed to increase the drug intake to 15 mg per day. Ineffectiveness of the maximum dosage leads to discontinuation of the drug. If the patient's response to treatment is inadequate (loss of less than 5% of body weight in 90 days), the medicine should not be taken for more than 3 months.

The occurrence of side effects and poor tolerability of the components of the drug does not mean immediate discontinuation of Sibutramine. Its dosage is reduced to a minimum level of 5 mg. The deterioration of the patient's health indicates the need to terminate therapy. The course of treatment can last up to 12 months. This is the maximum duration of use of the drug.

Links[edit | edit code]

1. "Top obesity drug sibutramine being suspended." 2010-01-22.
2. https://base.garant.ru/12158202/#block_3000
3. Heal, D.J.; Aspley; Prow; Jackson; Martin; Cheetham (1998). “Sibutramine: a novel anti-obesity drug. A review of the pharmacological evidence to differentiate it from d-amphetamine and d-fenfluramine". International journal of obesity and related metabolic disorders : journal of the International Association for the Study of Obesity 22 Suppl 1: S18–28; discussion S29.
4. Colman E. Anorectics on trial: a half century of federal regulation of prescription appetite suppressants. Ann. Intern. Med. 2005;143(5):380-385.
5. Araujo JR, Martel F. Sibutramine effects on central mechanisms regulating energy homeostasis. Curr Neuropharmacol. 2012 Mar;10(1):49-52.
6. "Meridia (sibutramine hydrochloride): Follow-Up to an Early Communication about an Ongoing Safety Review"
7. Bruce Japsen (13 March 2005). “FDA weighs decision on Meridia; Health advisory likely for Abbott obesity drug." Chicago Tribune. Chicago, Illinois. pp. 1.
8. Padwal RS, Majumdar SR Drug treatments for obesity: orlistat, sibutramine, and rimonabant //The Lancet. – 2007. – T. 369. – No. 9555. – pp. 71-77.
9. Fernstrom JD, Choi SJ The development of tolerance to drugs that suppress food intake //Pharmacology & therapeutics. – 2008. – T. 117. – No. 1. – pp. 105-122.
10. price from 100 rub.
11. Decree of the Government of the Russian Federation of December 29, 2007 N 964. Moscow Retrieved August 2, 2012.
12. https://doctorpiter.ru/articles/10100/

special instructions

Reactions to Sibutramine withdrawal are rare. The use of the medicine is justified if the result of treating obesity is a weight loss of 5 kg or less in 3 months. It is recommended to correct nutrition, increase physical activity, and maintain a healthy lifestyle. All this will enhance the pharmacodynamic effect of sibutramine. Particular attention should be paid to your condition, monitor the appearance of pain in the sternum, swelling, and progressive shortness of breath.

Taking Sibutramine for weight loss requires constant monitoring of heart rate and blood pressure. If its values ​​exceed 145/90 mmHg, then treatment should be stopped. It is strictly forbidden to combine taking capsules with alcohol, because it enhances the effect of the drug. This increases the risk of side effects and cases of overdose.

What to replace it with?

Other weight loss products:

Drug interactions

The medicine is not recommended to be combined with certain groups of drugs. These include:

1. Selective serotonin reuptake inhibitors (citalopram, fluoxetine, sertraline, paroxetine), opioids, antitussives, ergot alkaloid derivatives increase the risk of serotonin syndrome.
2. Isoenzyme inhibitors (erythromycin, ketoconazole, cyclosporine, troleandomycin) - the QT interval may increase due to an increase in the concentration of sibutramine in the blood.
3. Macrolide antibiotics, dexamethasone, phenobarbital, rifampicin, phenytoin, carbamazepine - the risk of accelerating the metabolism of sibutramine increases.

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How do Sibutramine and alcohol combine?

Sibutramine and alcohol are incompatible, as the risk of side effects from the nervous system increases, and alcoholic beverages are not compatible with dietary nutrition. Caution is also required when using other medications simultaneously.

Compatibility with other drugs

Drug interactions can have the following consequences:

• impaired conduction of cardiac impulses in the myocardium, increased QT on the ECG, tachycardia - Nizoral, Erythromycin, Cyclosporine;
• acceleration of Sibutramine metabolism and excretion from the body - Finlepsin, Dexamethasone, Macropen, Rifampicin;
• agitation, sweating, diarrhea – Fluoxetine, Tramadol, Codeine, Antimigraine.

Preparations with sibutramine

Diet pills with sibutramine as a dietary supplement are commercially available. As a medicine, such drugs are available only with a prescription. Examples of fat burners and dietary supplements containing sibutramine hydrochloride monohydrate:

Legal status

Since January 24, 2008, sibutramine has been included in the list of potent drugs approved by the Russian government[4][5]. This means that the sale of sibutramine-containing drugs is allowed only in pharmacies with a special prescription, it is subject to special registration[6].

Despite the fact that in 2007 sibutramine was not included in this list (it did not yet exist and there was a PKKN list with an unclear legal status), Svetlana Sukhorukova was arrested in October 2007 and in January 2008 she was sentenced for selling sibutramine in 2007 to 5 years according to Art. 234 of the Criminal Code of the Russian Federation - illegal trafficking of potent substances[7][8][9][10].

Sibutramine is also included in the Prohibited List of the World Anti-Doping Agency (2010) and is classified as a substance prohibited during competitions[11].

Measures restricting the free sale of drugs containing sibutramine took place in 2008-2010 not only in Russia. Campaigns to suspend sales were launched in the United States, a number of European Union countries and Israel[12]. This measure was applied after receiving the results of a study, where long-term use (several years) of 15 mg of sibutramine in patients with hypertension who had suffered a heart attack and stroke revealed a number of severe side effects. The revocation of documents giving the right to trade in pharmacies, according to the wording of the regulatory authorities, is temporary, until special circumstances are clarified. In Ukraine, this ban does not apply to dietary supplements containing sibutramine in a higher dose (35-50 mg), due to the lack of legal procedures for proving the presence of this component in a weight loss product. There are studies suggesting that side effects are associated with the presence of the S-isomer in racemic sibutramine. On the contrary, R-sibutramine has a 2-fold lower risk of developing undesirable consequences [ source not specified 1779 days

]. The presence of an optically pure dosage form containing R-sibutramine could, with a sufficient evidence base, have a positive impact on the current situation.

Sibutramine price

Russian pharmacists dispense tablets with sibutramine only with a prescription. The drug is banned for use in a number of developed countries. There are many dietary supplements that contain the active ingredient sibutramine, but this is not indicated on the packaging. Such products are positioned as food additives, although they have a psychotropic effect on the body.

Sibutramine is overpriced due to its inaccessibility. Foreign analogs are expensive due to transportation costs. Mostly, the medicine is purchased through an online pharmacy or supplement store. Price range in Moscow:

Effect on the body

The use of the drug is possible in cases where other methods for weight loss do not provide effect. It is advisable to use Sibutramine in combination with diet or physical activity. This way it will bring greater results:

• Dulled appetite;
• Active breakdown of fat deposits;
• Activation of serotonin production, which helps to have a positive mood;
• Reduces salivation and the ability to develop caries;
• If the effect is positive, weight loss is from 7 to 15 kg per month.

General recommendations

Diet pills "Sibutramine" are a drug. And therefore its use is dictated by the presence of various indications. The only situation in which the manufacturer recommends the use of this drug is severe obesity, when there is no effect from various measures related to weight loss.

You should consult your doctor before you start taking Sibutramine. The database of tablets is replete with various weight loss products. Self-medication is unacceptable, and a doctor’s recommendation is necessary throughout the entire course of therapy, which is a very long period (12 months). You need to periodically visit the doctor to assess your physical condition.