Sibutramine - a dangerous medicine for weight loss: instructions, analogues, reviews

Almost every overweight person at least once in his life dreamed of a miracle pill that could make him thin and healthy. Modern medicine has come up with many drugs that can trick the stomach into eating less. These drugs include sibutramine. It really regulates appetite and reduces food cravings, but it’s not as simple as it might seem at first glance. In many countries, the marketing of sibutramine is limited due to its serious side effects.

What is Sibutramine?

Sibutramine is a potent drug. Initially, it was developed and tested as an antidepressant, but scientists noted that it has a powerful anorexigenic effect, that is, it can reduce appetite.

Since 1997, it began to be used in the United States and other countries as an effective means for losing excess weight, prescribed to people with a variety of concomitant diseases. Side effects were not long in coming.

It turned out that sibutramine causes addiction and depression, which can be compared to a drug. In addition, it increased the risk of cardiovascular diseases; many people suffered strokes and heart attacks while taking it. There is anecdotal evidence that the use of sibutramine has led to the death of patients.

At the moment, it is prohibited for use in many countries; in the Russian Federation, its circulation is strictly controlled using special prescription forms on which it is prescribed.

Notes[edit | edit code]

  1. ↑ Sibutramine. European Medicines Agency (15.09.2010). Retrieved August 26, 2014.
  2. ↑ Meridia (sibutramine hydrochloride): Follow-Up to an Early Communication about an Ongoing Safety Review Retrieved August 3, 2012.
  3. ↑ Russian Medicines Register (2012): Sibutramine Archived copy from August 11, 2014 on the Wayback Machine (inaccessible link from 06/14/2016 [1477 days]) Retrieved August 3, 2012.
  4. ↑ Decree of the Government of the Russian Federation of December 29, 2007 N 964. Moscow Retrieved August 2, 2012.
  5. ↑ Decree of the Government of the Russian Federation of December 29, 2007 N 964. “On approval of lists of potent and toxic substances for the purposes of Article 234 and other articles of the Criminal Code of the Russian Federation, as well as large amounts of potent substances for the purposes of Article 234 of the Criminal Code of the Russian Federation” (with changes and additions). Guarantee. Retrieved January 27, 2021. Archived November 12, 2015.
  6. ↑ Order of the Ministry of Health of Russia dated April 22, 2014 N 183n. legalacts.ru. Retrieved October 14, 2021.
  7. Olga Bobrova.
    Drug addiction. Novaya Gazeta, No. 117 (October 21, 2009). Retrieved January 27, 2021. Archived September 3, 2014.
  8. ↑ Potent substance // Arguments of the week No. 30 (168) dated July 29, 2009
  9. ↑ POLIT.RU: Consideration of the complaint in the case of Svetlana Sukhorukova has been postponed to July 30
  10. ↑ REGIONS.RU - Federation news | The court should not violate the law (opinion of parliamentarians)
  11. ↑ World Anti-Doping Code, Prohibited List 2012 Archived copy dated October 26, 2013 on the Wayback Machine “B: Stimulants classified as Specified Substances (examples): ... sibutramine"
  12. ↑ Astakhova A.V., Lepakhin V.K., Pereverzev A.P. Sibutramine: possible side effects and recommendations for their prevention. Archived copy dated August 19, 2014 on the Wayback Machine Drug safety and pharmacovigilance, FC MBLS of Roszdravnadzor, No. 1, 2010, pp. 4-10

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.

sibutramine and amphetamine formula

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.

Properties

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

The thermogenic effect of Sibutramine occurs through the adrenergic system, mainly through 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, body temperature changes upward 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 reduce fat accumulation gradually, sustainably and safely through two basic aspects. Firstly, this drug increases calorie expenditure and speeds up metabolism. Secondly, sibutramine hydrochloride significantly suppresses the feeling of hunger. During the research, it was found that the first time the drug was taken at a dose of 10 mg, metabolism improved by approximately 30% and this effectiveness did not decrease for six hours, and the calorie content of food consumed per day was reduced to 1300 Kcal.

Clinical researches

In 2001, two independent clinical studies were conducted in different countries of the world.

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

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, both in one and another country, patients taking Sibutramine hydrochloride showed positive dynamics in the process of weight loss. More accurate data shows that in China, the average weight loss for 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 original weight of the subjects.

Indications for use

The drug is prescribed only by a doctor and only in cases where safer methods do not bring tangible results:

  • Nutritional obesity. This means that the problem with excess weight arose due to poor nutrition and lack of physical activity. In other words, when the body receives much more calories than it has time to expend. Sibutramine helps only when the body mass index exceeds 30 kg/m2.
  • Nutritional obesity in combination with type 2 diabetes mellitus. BMI must be greater than 27 kg/m2.

helps people with addiction

Sibutramine can ruin your life, and a rehabilitation program will help you cope with the consequences of its use. When choosing a center, we recommend that you consider whether the program takes into account all aspects of drug addiction, what the atmosphere in the center is like and the attitude of the staff, and most importantly, what the results are.

The Narconon program is a comprehensive rehabilitation program during which a person copes with both the causes and consequences of drug addiction. An important step of the program is non-medical detoxification, due to which toxic substances (medicines, alcohol or drugs) that have accumulated during use are removed from the body. They, too, these deposits, cause cravings and a desire to use again and again. To get effective help to start living a normal and healthy life, call us right now!

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Haloperidol

Contraindications and side effects

Conditions when taking sibutramine is prohibited:

  • allergic reactions and intolerance to any of the components in the composition;
  • cases when excess weight is due to the presence of any organic causes (for example, a long-term and persistent lack of thyroid hormones - hypothyroidism);
  • excessive production of thyroid hormones;
  • anorexia nervosa and bulimia;
  • mental illness;
  • Tourette's syndrome (a central nervous system disorder characterized by multiple uncontrollable tics and behavioral disturbances);

    drug addiction

  • simultaneous use of antidepressants, antipsychotics and other drugs acting on the central nervous system, as well as when any of these drugs were used 2 weeks before the prescription of sibutramine;
  • known drug, alcohol and drug addiction;
  • disorders of the cardiovascular system (CVS): coronary heart disease, chronic failure, congenital defects, tachycardia, arrhythmia, stroke, cerebrovascular accidents;
  • high blood pressure that cannot be treated;
  • severe disorders of the liver and kidneys;
  • benign growth of part of the prostate gland;
  • age under 18 and after 65;
  • period of pregnancy and breastfeeding.

Side effects colorfully explain why sibutramine is released strictly according to the prescription.

  1. CNS. Quite often, patients note insomnia, headaches, restlessness and changes in taste, in addition to this they usually experience dry mouth.
  2. SSS. Much less common, but still occurring, is an increase in heart rate, an increase in blood pressure, and dilation of blood vessels, resulting in redness of the skin and a local feeling of warmth.
  3. Gastrointestinal tract. Loss of appetite, bowel movements, nausea and vomiting, and even worsening hemorrhoids - these symptoms are as common as insomnia.
  4. Leather. Excessive sweating can occur at any time of the year, but fortunately this side effect is rare.
  5. Allergy. It can occur either in the form of a small rash on a small area of ​​the body or in the form of anaphylactic shock, in which case you should urgently seek help from a doctor.

Typically, all side effects are observed within 1 month after taking the drug, have a mild course and go away on their own.

In isolated cases, the following unpleasant effects of sibutramine have been officially recorded:

  • painful menstrual bleeding;
  • swelling;
  • pain in the back and abdominal area;
  • itchy skin;
  • a condition similar to the flu;
  • unexpected and sudden increase in appetite and thirst;
  • depression;
  • severe drowsiness;
  • sudden mood swings;
  • convulsions;
  • a decrease in the number of platelets, which causes bleeding;
  • acute psychosis (if the person already had serious mental disorders).

Precautions[edit | edit code]

It is necessary to monitor blood pressure and pulse rate every 2 weeks in the first 2 months of treatment and then once a month. In patients with arterial hypertension with a blood pressure level >145/90 mm Hg. Art. monitoring should be carried out more carefully and more often, and in the case of a twice registered rise in blood pressure >140/90 mm Hg. Art. treatment should be stopped. The appearance of chest pain, progressive dyspnea (breathing difficulty) and swelling of the lower extremities during therapy may indicate the development of pulmonary hypertension (in this case, you must consult a doctor). The simultaneous use of drugs that increase the QT interval (astemizole, terfenadine, antiarrhythmic and other drugs), drugs containing ephedrine, phenylpropanolamine, pseudoephedrine, etc. (risk of increased blood pressure and increased heart rate), as well as other anorexigenic drugs with a central mechanism of action is not recommended. Caution should be prescribed against the background of hypokalium and hypomagnesemia, and in cases of mild to moderate impairment of liver and kidney function. Women of childbearing age should use adequate contraception during treatment. It should be kept in mind that sibutramine may reduce salivation and contribute to the development of caries, periodontal disease, candidiasis and oral discomfort. During treatment, it is recommended to limit alcohol consumption. Should not be used during work by vehicle drivers and people whose profession involves increased concentration of attention.

Mode of application

The dosage is selected only by a doctor and only after carefully weighing all the risks and benefits. Under no circumstances should you take the drug yourself! In addition, sibutramine is sold from pharmacies strictly according to a prescription!

It is prescribed once a day, preferably in the morning. The initial dose of the drug is 10 mg , but if a person does not tolerate it well, it is reduced to 5 mg. The capsule should be washed down with a glass of clean water, but it is not recommended to chew it and pour the contents out of the shell. You can take it on an empty stomach or during breakfast.

If during the first month there are no proper changes in body weight, the dosage of sibutramine is increased to 15 mg. Therapy is always combined with proper physical activity and a special diet, which is selected individually for each person by an experienced doctor.

Guide to choosing medications Anti-obesity pills

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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:

  1. Combination medications containing ephedrine, pseudoephedrine, etc. increase blood pressure and pulse numbers.
  2. 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.
  3. Some antibiotics (macrolide group), phenobarbital, carbamazepine accelerate the breakdown and absorption of sibutramine.
  4. 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.

Sibutramine is a drug that can cause overdose

Sibutramine has all the signs of poison. Any narcotic substance and alcohol, as well as some medications, are poisons that poison, disrupt the functioning of the body and can kill. Some stimulants cause a person to lose appetite, but it is wrong to use them for weight loss.

Poisons have a negative effect on the body. They destroy vitamins and minerals, are deposited in fatty tissues and, like a Trojan horse, negatively affect mental and physical health. They also gradually reduce a person’s mood. Slowly but surely they kill a person. Or they kill quickly, which depends on the dose.

An overdose of sibutramine increases side effects in humans. Most often it is expressed in an accelerated heartbeat, high blood pressure, headache and dizziness. To help, you need to call an ambulance.

Why is sibutramine prohibited and why is it dangerous?

Since 2010, the substance has been restricted for distribution in a number of countries: the USA, Australia, many European countries, Canada. In Russia, its turnover is strictly controlled by government organizations. The drug can only be prescribed on a prescription form with all the necessary stamps. It is impossible to buy it legally without a prescription.

Sibutramine was banned in India, China, and New Zealand. What led him to the ban were side effects that were similar to drug withdrawal: insomnia, sudden anxiety, an increasing state of depression and thoughts of suicide. Several people committed suicide due to its use. Many patients with cardiovascular problems died from heart attacks and strokes.

Dangerous diet pills - Stay alive! Season 4. Issue 30 from 04/18/17

People with mental disorders are strictly prohibited from taking it! Many were overtaken by anorexia and bulimia, acute psychoses and changes in consciousness occurred. This medicine not only suppresses appetite, but also literally affects the head.

Legal status[edit | edit code]

Since January 24, 2008, sibutramine has been included in the list of potent drugs approved by the Russian government[4][5]. Subject-quantitative accounting is subject only in its own form, but is not subject to the common combination of sibutramine + MCC (for example, in the drug “Reduxin”) [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 2400 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.

Official drug study

The original drug sibutramine (Meridia) was released by a German company. It was approved for use in the United States in 1997, and in the European Union in 1999. To confirm its effectiveness, many studies were cited in which over 20 thousand people took part, the result was positive.

After some time, reports of deaths began to arrive, but the drug was in no hurry to ban it.

In 2002, it was decided to conduct the SCOUT study to identify which population groups are at greatest risk of side effects. This experiment was a double-blind, placebo-controlled study. 17 countries took part in it. The relationship between weight loss during sibutramine therapy and problems with the cardiovascular system was studied.

By the end of 2009, preliminary results were announced:

  • Long-term treatment with Meridia in overweight elderly people with existing heart and vascular problems increased the risk of heart attacks and strokes by 16%. But no deaths were recorded.
  • There was no difference in death between the placebo group and the main group.

It has become clear that people with cardiovascular disease are at greater risk than everyone else. But it was not possible to find out which groups of patients can take the drug with the least damage to health.

Only in 2010, old age (over 65 years) was included in the official instructions as a contraindication, as well as: tachycardia, heart failure, coronary disease, etc. On October 8, 2010, the manufacturer voluntarily recalled its drug from the pharmaceutical market until all the circumstances were clarified .

The company is still waiting for additional studies that will show which groups of patients the drug will bring more benefit and less harm.

In 2011-2012, Russia conducted its own study under the code name “SPRING”. Adverse effects were recorded in 2.8% of volunteers; no serious side effects that might require discontinuation of sibutramine were identified. Over 34 thousand people aged from 18 to 60 took part. They took the drug Reduxin at the prescribed dose for six months.

Since 2012, the second study, PrimaVera, was conducted; the difference was the period of use of the drug - more than 6 months of continuous therapy.

Chemical composition

Sibutramine is an anorexigenic drug 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) - cyclobutane methylamine, 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 said that any medicines that contain sibutramine are harmful to humans and their health.

Analogs for weight loss

Sibutramine is available under the following names:

  • Goldline;
  • Goldline Plus;
  • Reduxin;
  • Reduxin Met;
  • Slymia;
  • Lindax;
  • Meridia (registration is currently revoked).


sibutramine analoguesSome of these drugs have a combination composition.
For example, Goldline Plus additionally includes microcrystalline cellulose, and the Reduxin Met package contains 2 medications at the same time - sibutramine along with MCC, in separate blisters - metformin (a drug for lowering sugar levels in type 2 diabetes). At the same time, Reduxin Light does not contain sibutramine at all, and it is not even a drug.

How to replace sibutramine

Weight loss drugs:

Name Active substance Pharmacotherapeutic group
FluoxetineFluoxetineAntidepressants
OrsotenOrlistatDrugs for the treatment of obesity
VictozaLiraglutideHypoglycemic drugs
XenicalOrlistatDrugs for the treatment of obesity
GlucophageMetforminAntidiabetic drugs

Reviews of those losing weight

People's opinions about sibutramine:

sibutramine review

Maria. I want to share my experience in using it. After giving birth I gained a lot of weight and wanted to lose weight quickly. On the Internet I came across the drug Lida, it contains sibutramine. I took 30 mg per day and lost weight quickly. A week after stopping the drug, health problems began and she went to the hospital. There I was diagnosed with chronic renal failure.

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