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

The process of losing weight can be so difficult that any aids in it become good. This also applies to medications. Sibutramine and its analogues have earned special respect among those losing weight. This drug was previously distributed in the Russian Federation and was sold by prescription, as the instructions for using Sibutramine clearly indicate. But at present, a drug with this name cannot be found in pharmacies. There are only analogues that contain sibutramine as an active ingredient.

"Breakthrough" in dietetics

At the moment, sibutramine in medications is dosed at 10 and 15 mg. During drug trials, dosages were used that were significantly higher than modern ones. The result was that weight loss was easy and rapid. The patient almost completely lost his appetite, and fat depots were consumed twice as actively, because the body’s energy needs require constant satisfaction.

Sibutramine turned out to be effective against pathological excess weight, when the body mass index went off scale at more than 30. The research could be called a real revolution in dietetics, if not for the side effects of the drug. The use of huge dosages was accompanied by multiple side effects, including:

heart attacks and strokes;
heart rhythm disturbances;
lesions of the gastrointestinal mucosa;
migraine pain;
mental disorders.

Therefore, at that stage they could not launch the drug into mass use. Having found the minimum therapeutic doses, scientists have achieved positive dynamics in reducing the incidence of side effects, which made it possible to register the drug as a drug for the treatment of obesity.

Many pharmaceutical companies began producing the formula and its analogues. However, this did not turn out to be a particularly successful undertaking, as reports of new undesirable effects continued to arrive. As a result, since 2010, America and the European Union have included sibutramine in the list of prohibited medicinal substances. Some countries, for example, Russia, have included it in the list of potent prescription drugs, significantly limiting the possibilities of self-medication with it.

Mechanism of weight loss

"Sibutramine" or its analogues are prescribed by nutritionists or psychiatrists to people with alimentary obesity and eating disorders. Often, the appointment occurs when other methods of losing weight have been exhausted. Sibutramine acts on the body as follows:

blocks the uptake of the neurotransmitter serotonin;
blocks the uptake of the neurotransmitter norepinephrine;
inhibits dopamine uptake to a much lesser extent.

Violation of the consumption and transformation of mediators in the central nervous system leads to the development of similar mechanisms in all organs and tissues. The consequences of taking sibutramine are as follows:

appetite - the patient’s feeling of hunger is significantly dulled, he may not experience it at all, even if he has not had a single meal in a day;
metabolism - due to the effect on vascular tone, heat exchange increases, the body is forced to consume more energy, using its reserves from the depot;
fat burning - based on the previous effect, since the supply of energy from outside is significantly reduced;
satiety - due to dulling of appetite, the patient feels full almost immediately after starting a meal;
digestion - noticeably improves due to an increase in serotonin concentration in the mucous membranes of the gastrointestinal tract (GIT), peristalsis and juice production improves;
mood - improves due to an increase in the level of “happiness hormones”, the patient feels happy even in the case of food addiction;
activity - increases due to increased excitability of the central nervous system, the patient feels a surge of strength, vigor, and is ready for active actions during the day.

A number of changes in brain function, which are provoked by the use of sibutramine, facilitate weight loss at all levels: physical, emotional, hormonal. A special feature of the drug is its ability to activate the burning of “brown fat”. Although these accumulations are found in the human body in small quantities, they play a vital role in the process of thermoregulation. And their breakdown activates the consumption of “white fat,” the excess of which accompanies obesity.

Sibutramine also tends to regulate fat balance in the body. In particular, the drug activates the production and secretion of bile. For this reason, indications for use of the drug include obesity in type 2 diabetes mellitus and lipid metabolism disorders. The condition for prescribing sibutramine in these cases is that the body mass index exceeds 27.

Use abroad

Sibutramine and similar drugs are actively used not only in Russia. For example, in the United States such products are marketed under the Meridia brand and are sold only as prescribed by a doctor. Local specialists, who conducted many experiments on volunteers with different degrees of obesity, resulted in a minimal number of deaths. For this reason, they only allow healthy patients who do not have any health problems, especially those with the cardiovascular system, to take the pills.

In the European Union, the production of Sibutramine was stopped. The reason for this was the discovery by specialists of a negative effect on the functioning of the heart and blood vessels. To find out this, various studies were carried out on people suffering from diseases of these organs, where the results were not at all reassuring.

Instructions for use of sibutramine

Sibutramine belongs to the group of drugs for excess weight, intended “as a last resort.” The use of the drug must be coordinated with a doctor to make sure that all available methods for correcting body weight have been exhausted. This approach is necessary because of the enormous health risks that come with interfering with the functioning of the nervous system.

Often, treatment begins with a minimum dose of 10 mg. A tablet of the appropriate dosage is taken once per knock, with a sufficient amount of liquid. Taking the drug does not depend on the time of the meal, but doctors recommend taking the tablets in the morning on an empty stomach after waking up to ensure maximum concentrations of the drug in the blood in the first half of the day.

The action develops as follows:

80% of the contents of the tablet are absorbed in the small intestine;
active metabolites of sibutramine - released into the blood and bind to its proteins;
concentration in the blood reaches a maximum three to four hours after administration;
metabolites of the drug - spread throughout the body, accumulating in synaptic joints;
after taking the fourth tablet , a stable therapeutic concentration of the drug is achieved in the tissues.

It is not advisable to combine the intake with food. The fact is that the absorption of the drug from the food bolus is worse - it decreases by a third. The substance is excreted from the body by the kidneys. Fragments of metabolites remain in tissues for about a month, but their concentrations after the end of administration do not have therapeutic significance.

Sibutramine tablets for weight loss could be taken for up to a year. Now they drink analogues the same way. If the minimum dosage of 10 mg shows satisfactory effectiveness, it is maintained until the end of the course of treatment. The need to increase the dosage arises if, within two to three months after the start of treatment, the patient’s “plumb line” amounted to up to 3% of the total body weight. Then sibutramine is prescribed at a dose of 15 mg. If the plumb line remains minimal, the drug is discontinued due to ineffectiveness. All decisions regarding dosage and timing of treatment are made by the doctor.

Pharmacological action of the drug

Sibutramine itself is a so-called prodrug, that is, in order for it to act, the drug must “decompose” into active components after passing through the liver. The maximum concentration of metabolites in the blood is achieved after 3-4 hours.

If taken simultaneously with food, then its concentration decreases by 30% and reaches its maximum after 6-7 hours. After 4 days of regular use, its amount in the blood becomes constant. The longest period for half of the drug to leave the body is about 16 hours.

The principle of action of the substance is based on the fact that it can increase the production of heat by the body, suppress the desire to eat and increase the feeling of satiety. When the desired temperature is consistently maintained, the body does not need to store fat reserves for future use, and the existing ones are “burned” faster.

There is a decrease in cholesterol and fats in the blood, while at the same time the content of “good” cholesterol increases. All this allows you to lose weight quickly and maintain the new weight for a long time after stopping sibutramine, but subject to maintaining a diet.

Facts about harm

Considering the complex assistance of the drug in the process of losing weight, the question arises: “What will you have to pay for such tangible support on the path to slimness?” The answer lies in the results of studies of the substance, which clearly list its side effects. But based on the reviews of those losing weight, we can say that the drug is often well tolerated. Some undesirable effects that occur at the beginning of therapy lose intensity or disappear altogether if sibutramine is taken correctly. The most common side effects:

feeling of dry mouth;
bowel dysfunction;
exacerbation of hemorrhoids;
headache;
increased heart rate;
insomnia;
complete lack of appetite;
slight increase in blood pressure.

Side effects of sibutramine, like other medications, include the possibility of an allergic reaction, manifested by hives and itchy skin. In this case, the drug is discontinued.

More serious adverse effects of the drug include addiction and withdrawal symptoms. Drug dependence does not occur, however, during the first time after cessation of treatment, the patient’s psycho-emotional state may deteriorate, which may provoke a return to old eating habits. To reduce the intensity of these effects, doctors recommend stopping treatment by gradually reducing the dosage of the drug.

Dangerous undesirable effects include:

psychological disorders (up to suicidal ideation);
eating disorders (bulimia, anorexia);
increased risk of heart attacks;
insomnia;
critical increase in blood pressure;
tachycardia;
fainting;
peripheral circulatory disorder.

Given the fact that previously sibutramine could be purchased without a prescription, some side effects may not be registered by the manufacturer and not displayed in the instructions. Doctors focus the attention of those losing weight on the need for professional prescription of the product. This is the only way to reduce the possibility of side effects.

Contraindications

If the body is hypersensitive to the active components, the use of the drug is contraindicated, otherwise side effects may 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.

Who is prohibited from taking the drug?

Sibutramine-based drugs have an impressive list of serious contraindications. The main ones are considered to be disturbances in the functioning of the heart, liver and kidneys, since the substance creates the main burden on these organs.

The harm of the drug is more significant if obesity is not of nutritional origin, but is secondary. Most often it is caused by metabolic disorders and internal organs. Medical practice confirms the ineffectiveness of sibutramine in such situations. Other contraindications for taking the drug:

up to 18 years old;
after 65 years;
for bulimia;
with anorexia;
mental disorders;
teak;
hyperthyroidism;
arterial hypertension;
BPH;
glaucoma;
substance abuse;
drug addiction;
alcoholism.

Particular caution is required when prescribing sibutramine to epileptics and people prone to seizures, as well as those with hematopoiesis or blood clotting disorders.

Given the increased risk of overdose and complications, you should completely abstain from alcohol during treatment. To remove a drug from the body that has been overdosed intentionally or accidentally, you should perform a gastric lavage, take an adsorbent, and be sure to call an ambulance.

Weight loss, recently this word has been popping up more and more often on television and flashing in advertising newspaper clippings.
And all because modern fashion trends dictate to us the ideals of beauty that are practically not natural to humans. This includes a wasp waist, which practically fits in the hands of an adult man. These “unnatural” indicators also include voluminous, toned breasts and plump lips. If some aspects related to the body can be corrected, for example, giving elasticity to the butt and tightening the breasts a little, then some can only be corrected surgically. Especially often we can see how adult women worry about their bodies. Of course, they can no longer boast of elastic skin and a bright appearance, but they have mature sexuality, grace and femininity in their arsenal. But they will not appear if the body is shrouded in a veil of fat. Therefore, losing weight is increasingly popping up in your life and not only young girls who dream of making their body perfect, but also adult women who want to give themselves their former confidence and sexuality are turning to it.

But here comes a new problem - losing weight takes a lot of time, but even if you manage to find it, the most important part comes up - the lack of willpower. It is she who encourages a person to get off the couch and finally take care of his appearance. But what to do if willpower is not so pronounced or is absent at all, but you still want to lose weight. In this case, many turn to the help of medications, many of which include a substance such as sibutramine.

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.

Analogs

The following drugs are complete analogues of Sibutramine:

"Goldline";
"Reduxin";
Lindax.

They contain sibutramine hydrochloride monohydrate salt and are available in two dosages, like the original drug.

Improved forms of Sibutramine are the drugs Goldline Plus and Reduxin Met. In addition to the active substance, they contain microcrystalline cellulose, which reinforces the anorexigenic effect of sibutramine. Reduxin Met also includes metformin, a stimulator of the sensitivity of body cells to insulin.

All analogue drugs are dangerous in the same way that sibutramine is dangerous; they have the same contraindications and side effects. The Goldline Light dietary supplement does not contain sibutramine, and therefore cannot be compared with the original drug.

Among safe substitutes for sibutramine, Xenical is the most popular. Its active ingredient, orlistat, is by far the most studied drug for weight loss with proven safety and effectiveness. The substance acts only in the intestinal lumen, blocking the absorption of fats, and has no effect on the central nervous system.

Reviews of Sibutramine tablets are very varied. Some people have successfully lost weight, completely changed their diet and eating habits, without feeling anything more uncomfortable than dry mouth. In other cases, taking the drug resulted in long-term treatment for psychological disorders. One way or another, sibutramine therapy requires strict medical supervision. When using the drug independently, the risk of severe consequences increases.

Interaction with other drugs

Before taking sibutramine, you should discuss with your doctor all medications that are taken on an ongoing basis or periodically. Not all medications are compatible with sibutramine:

Combination medications containing ephedrine, pseudoephedrine, etc. increase blood pressure and pulse numbers.
Medicines involved in increasing serotonin in the blood, such as drugs for the treatment of depression, anti-migraines, and painkillers, can in rare cases cause “serotonin syndrome.” He is deadly.
Some antibiotics (macrolide group), phenobarbital, carbamazepine accelerate the breakdown and absorption of sibutramine.
Certain antifungals (ketoconazole), immunosuppressants (cyclosporine), erythromycin can increase the concentration of broken down sibutramine along with an increase in heart rate.

The combination of alcohol and the drug does not have a negative effect on the body in terms of their absorption, but strong drinks are prohibited for those who adhere to a special diet and seek to lose excess weight.

Reviews: “The effect was short-lived”

I took Reduxin 10 mg for 3 months and was very pleased with the results. Weight was 78 kg with a height of 152 cm; on Reduxin she lost weight to 61 kg. Of course, the first 2 weeks were a little uncomfortable - I was plagued by thirst and insomnia, but I had a lot more energy, and my productivity at work increased significantly (I work as a teacher). Among the unexpected positive effects, I can note the disappearance of menopause symptoms (hot flashes, profuse sweating) and normalization of blood sugar levels. If we compare it with a similar drug “Goldline”, then I will give preference to “Reduxin” - the side effects are milder and the result is better. Of course, it is still better to take it under the supervision of a doctor; I consulted with a local therapist.
Irina S. , https://protabletky.ru/reduxin/#otzivi

I took these capsules to lose weight. I bought it myself, and I also made the decision to drink it myself. For which I really reproach myself. Yes, I lost weight on it, and dramatically by 11 kilograms. But the effect was short-lived. Literally 4 months later everything came back. I lost 11 kilograms and gained back 19 kilograms. The appetite from these capsules drops immediately, you don’t want to eat at all. I ate much less and drank a lot of water. But this did not save me from the onset of migraines, tachycardia, and constipation. I had a constant headache, and I also had insomnia every night. Keep in mind that there are a huge number of contraindications for this drug, and I personally experienced most of the side effects. And in addition, after finishing the treatment, all my kilograms came back to me. The price of the drug is expensive, it is better to go to the gym for this money. The bottom line is that I regret that I started taking these capsules. I don't recommend them to anyone.
Olga T. , https://protabletky.ru/reduxin/#otzivi