Sibutramine: effects, use and risks

25/02/2024

Sibutramin

Sibutramine 15mg is a serotonin and noradrenaline reuptake inhibitor. It works by affecting the reuptake of the neurotransmitters 5-hydroxytryptamine (called serotonin) and norepinephrine into nerve cells in the brain. Neurotransmitters are chemicals that allow nerve cells to communicate with each other. By blocking their reuptake, sibutramine increases the amount of these neurotransmitters in the brain. Increased levels of neurotransmitters in the brain help patients feel fuller after eating and help reduce their food intake.

Sibutramine was voluntarily withdrawn by the manufacturer from the European and American markets in 2010 (it was used in the treatment of obesity for 13 years). By its mechanism of action, it dampened food intake and at the same time increased energy expenditure. It was withdrawn due to the long-term study SCOUT (Sibutramine Cardiovascular Outcomes Trial), which showed a higher incidence of non-fatal myocardial infarctions and strokes in the intervention group compared to the placebo. These drugs should not be used primarily by patients with coronary artery disease, congestive heart failure, ischemic disease of peripheral arteries, arrhythmias or cerebrovascular diseases (stroke or TIA). All patients had to be regularly checked due to the possibility of an increase in blood pressure or pulse. Patients who did not lose at least 5% of their body weight during 3 months of taking sibutramine should discontinue treatment. The maximum duration of treatment should not exceed one year.

Sibutramine contains Serotonin and Norepinephrine (both substances are very effective, noropinephrine puts the body under stress and thus pushes for fat loss, serotonin, on the contrary, calms down and thus tries to suppress hunger). It is a medicine for obese patients who have no history of cardiovascular disease and are unable to reduce their weight with diet and exercise. It acts centrally, in the brain, where the hunger signal is generated. It has no addictive or psychostimulant properties.

Why has sibutramine been reviewed?

Sibutramine was originally reviewed by the Agency in 1999 and 2002 after concerns about its safety, particularly for adverse cardiovascular effects (increased blood pressure and heart rate). At that time, the CHMP concluded that the benefits of sibutramine in the treatment of obesity and overweight outweighed its risks. However, the committee also asked the company that makes Meridia, Abbott Laboratories, to begin a study of sibutramine in patients with cardiovascular risk factors, particularly with regard to the drug's safety. The committee also asked the company to provide a six-month update on the progress of this study.

As a result, the company started the Sibutramine Cardiovascular OUTcome Trial (SCOUT) in 2002 to determine the effect of weight loss after sibutramine on cardiovascular problems in a large group of overweight and obese patients at high cardiovascular risk. The study compared sibutramine to a placebo (a blinded sample) and observed not only how much weight the patients lost, but also the incidence of cardiovascular events such as myocardial infarction, stroke and cardiac arrest. In total, about 9,800 patients were followed for six years.

Although the overall data from the SCOUT trial have not yet been analyzed, the Data Safety Monitoring Board (a body of independent experts designated to regularly review the results of clinical trials) informed the Agency in October 2009 of preliminary data showing that sibutramine is associated with more cardiovascular problems.

Based on these data, the German Medicines Agency (BfArM) launched a review under Article 107 of Directive 2001/83/EC. They asked the CHMP to assess the impact of the new data on the benefit-risk balance of sibutramine and prepare an opinion on whether the marketing authorization decision for sibutramine-containing products should be maintained, changed, suspended or withdrawn across the EU.

Structural formula of Sibutramine

The CHMP noted that the SCOUT study showed an increased risk of serious cardiovascular events (such as myocardial infarction or stroke) in patients with known cardiovascular disease who took sibutramine.

Most patients in the SCOUT study would not normally have received sibutramine, as sibutramine is contraindicated in patients with cardiovascular disease. However, the committee considered that the increased risk may also apply to patients who may be prescribed sibutramine, as obese and overweight patients are more likely to be at risk of cardiovascular disease.

Finally, taking into account all studies of sibutramine in the treatment of obesity, the CHMP noted that the weight loss achieved with sibutramine treatment was modest compared to placebo-treated patients, with patients losing an average of two to four kilograms more than placebo. The committee also noted that it is not clear whether this weight loss effect can be maintained after treatment with sibutramine is stopped.

Based on the currently available data and the scientific discussion in the committee, the CHMP concluded that the benefits of sibutramine-containing medicines do not outweigh their risks and therefore recommended that the marketing authorizations for sibutramine-containing medicines be suspended throughout the EU. The suspension will remain in effect until the company provides data sufficient to identify a patient population for whom the benefits of sibutramine clearly outweigh its risks.

Scheme of reuptake inhibition of the neurotransmitters serotonin and noradrenaline

Adverse effects

Originally, sibutramine was marketed as a suitable alternative to other classic anorexic drugs. An increased risk of cardiovascular events (heart attack or stroke) has been reported due to the increase in heart rate and blood pressure caused by sibutramine. Another disadvantage of this drug was that if obese patients lost weight, they started to gain weight again very quickly after stopping it. Adverse effects occur mainly at the beginning of treatment during the first 4 weeks. Their frequency decreases over time. As a rule, they are not serious, do not lead to interruption of treatment and are transient.

increase in blood pressure
heart beat
dry mouth
traffic jam
Headache
sleep problems
fast heart rate
hot flushes
anxiety
dizziness

In general, they are usually not severe and do not lead to discontinuation of treatment. Their frequency disappears within the first 4 weeks.

Sibutramine has been withdrawn from the market due to an increased risk of cardiovascular complications

The medicine must not be taken

pregnancy and breastfeeding
drug, medication or alcohol addiction
glaucoma
tumor of the adrenal medulla (phaeochromocytoma)
prostate enlargement with urinary retention
severe renal impairment
severe liver dysfunction
high blood pressure (more than 145/90 mm)
increased activity of the thyroid gland (hyperthyroidism)
diseases of the heart and blood vessels
simultaneous use of preparations for the treatment of sleep disorders, drugs for reducing
body weight, antidepressants and antipsychotics
certain mental or nervous diseases (e.g. Gilles de la Tourette's syndrome)
obesity caused by a cause other than overeating (organic causes)
serious eating disorders (anorexia or bulimia)
hypersensitivity to sibutramine or another component of the drug

Sibutramine and sports

Sibutramine is a synthetic halogen compound similar to amphetamine, which was formerly an ingredient in prescription drugs intended to treat obesity. Medicines containing it have been available in Slovakia since 2000. After concerns about the safety of sibutramine, especially in terms of side effects on the cardiovascular system, the European Medicines Agency (EMA) ended a six-year review of its safety and effectiveness in 2010.

Specified substances are more likely to be consumed by athletes for purposes other than enhancing athletic performance. In such cases, after explaining and proving the use of sibutramine with the absence of intent to support performance, a reduction of the sentence is possible.

Running

Sibutramine as doping

Although it is not a performance-enhancing substance, due to scientific evidence that the use of sibutramine poses a real health risk, the World Anti-Doping Agency (WADA) placed it on the S6 List of Prohibited Substances in 2006. Stimulants (substances prohibited during the competition).

Although medicines containing sibutramine have been withdrawn from the Slovak market, medicines that were delivered for sale outside the EU are illegally imported into Europe. Even according to the State Institute for Drug Control, slimming drugs are among the most frequently offered illegally. Thus, "diet pills" containing sibutramine are widely sold on the Internet. Consumption of these products can lead not only to serious health problems (e.g. heart arrhythmia, high blood pressure, stroke, myocardial infarction), but also to unintentional use of a prohibited substance and a positive doping test.

What are the recommendations for prescribers and patients?

patients should contact their doctor or pharmacist with additional questions
patients taking sibutramine-containing weight loss medications should be informed at their next doctor's visit about other methods of weight loss and discuss alternative treatments with their doctor
doctors should not prescribe medicines containing sibutramine to overweight or obese patients

Sibutramine

Prohibited medicines with sibutramine in Slovakia

In the Slovak Republic, all medicines where it is the main ingredient have been withdrawn from the market. These are Reductil, Lindax, Sibutral or Sibutramin-Teva. So, if you come across any of these drugs, avoid them as much as possible, it is an illegal sale. At the time of writing this review, I came across several websites that offered Sibutramine. Most often under the name MEGA Sibutramine, or Sibutramine 20 mg. In most cases, not only the manufacturer was missing, but also the exact composition, country of origin and other important information. Taking such drugs can cause you serious health complications. For this reason, avoid them.

User experience

I have to admit, I was very pleasantly surprised by the positive reviews of users praising the effects of Sibutramine. However, I also came across a relatively large number of posts regarding the above-mentioned side effects, which selected individuals only confirmed. The most common was stomach upset, dry mouth, but I also registered more serious complications related to kidney problems.

Source: friderika96, modrykonik.sk/forum

Source: 15832, omlazeni.cz/sibutramin

Source: Euphory, omlazeni.cz/sibutramin

As you can see, Sibutramine is not exactly a safe way to lose weight. So, if you care about your health, try using food supplements that contain purely natural substances.

Medicines for weight loss, like Sibutramine, are attractive to many, but their side effects should not be forgotten. Therefore, if you are thinking about something similar, visit your doctor first and discuss with him all the options you have.

If you are only worried about a few extra kilos, a small adjustment of your diet and the inclusion of physical activities will suffice. However, high overweight and obesity mean not only limitations in everyday life, but also health problems.

If someone promises you quick weight loss without any effort, beware and check everything carefully. Yes, it is of course a tempting idea, but losing weight is not that simple.

Physical activity

It is one part of a complex lifestyle change aimed at achieving weight loss. However, it is especially important for people with sedentary jobs, who are recommended to exercise daily for at least 30 minutes. Of the individual activities, it turns out to be the most effective to combine strength training with aerobic activity, as a result of which you will not lose muscle mass, but fat reserves. In addition, if you supplement your physical activity with the adjustment of your eating habits, you are well on your way to success.

Physical activity

Food diary

Adjusting the diet to minimize the intake of refined sugars, i.e. sweet treats or white bread, is certainly important, but meal planning, including control of portion sizes, is also important. So, if you are serious about losing weight, set up a food diary or install one of the applications on your mobile phone (I recommend Calorie Tables) where you will write down individual foods and also physical activity. A review study published in the Journal of the Academy of Nutrition and Dietetics confirms the link between consistently recording meals and weight loss. Yes, at first it is time-consuming and "annoying", but the desired weight loss will be the well-deserved reward.

Good sleep and mental well-being

One of the factors increasing the risk of obesity is insufficient sleep. As a result, metabolism slows down, insulin and cortisol levels increase, which contribute to fat storage. The effect of sufficient sleep on weight loss is proven by the results of a study in the American Journal of Epidemiology, in which 83,377 men and women participated. In people who slept 5-6 hours a day, there was a higher weight gain, which also increased the risk of obesity. Stressful situations also lead to an increase in body weight. Hand on heart, surely you too have fought stress with a bar of chocolate at least once. No wonder, since stress triggers the release of cortisol. The latter, when it remains in the bloodstream longer, can lead to an increase in the appetite for sweets, and therefore weight gain. This claim is again proven by an 8-week intervention program focused on better stress management, after which the participants had the desired reduction in BMI.

Sleep

Diet programs

There are undoubtedly many benefits to losing weight without a specific diet plan, the biggest being the financial side. Complete diet programs, including food packages, are often not the cheapest thing. On the other hand, if you are just starting to get interested in a healthy lifestyle, you will definitely not regret this investment. You will not have to learn how to count calories, spend several hours compiling a menu or in the store choosing suitable foods. Undoubtedly, the most famous diets include low-carbohydrate, protein and box diets. However, intermittent fasting is also important, which will help in cases where you have been losing weight for a long time and the weight loss stops or slows down significantly. You can choose from several different models according to the duration of the fasting period, the so-called fasting.

Before you decide on any of the weight loss drugs, first try the methods mentioned above, which do not cost you anything. Currently, you can choose from a large number of diets for vegans, vegetarians, but also meat lovers. If you still decide to reach for one of the medicines, give preference to those whose distribution has been approved by ŠÚKL – the State Institute for Drug Control. Avoid medicines containing sibutramine as well as other prohibited weight loss medicines and consult your doctor about the others.