She's on sibutramine. Why is sibutramine dangerous? Is there habit

Content

Weight loss drugs are prescribed in combination with diet and physical activity. In many cases, such therapy does not give positive results, then they resort to the help of potent substances. One of them is Sibutramine. The drug is used for obesity to reduce weight that threatens the health of the patient.

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 the feeling of hunger, the activation of the feeling of fullness. 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 food absorption refers to stimulators of signal transmission between brain neurons. There is a release of serotonin and norepinephrine into the intercellular space (synapse). Sibutramine blocks the reverse signal, due to which the concentration of neurotransmitters in the synapse increases. The postsynaptic cells receive a signal about saturation more actively, and the body does not require additional nutrition.

Molecules of the active substance stimulate thermogenesis - the production of thermal energy. As a result, metabolism is accelerated, 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 with the use of capsules is complemented by an increase in the level of high-density lipoprotein. At the same time, there is a decrease in the amount of triglycerides, cholesterol, 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 in 1-2 hours. Sibutramine is excreted through the kidneys, the half-life is 16 hours.

Indications for use

Medicines with sibutramine are potent drugs. It must be understood that self-medication is strictly prohibited. It is important to take Sibutramine only after consulting a specialist. The course of treatment should be under the supervision of a physician. 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 the appointment is the ineffectiveness of other methods of treatment.
• Insulin-dependent diabetes (type 2) with a body mass index of 27 kg / m² or more.
• Dyslipoproteinemia is a metabolic pathology characterized by a violation of the quantitative and qualitative indicators of lipoproteins in plasma.

Contraindications

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

• secondary obesity for organic reasons (diseases of the endocrine system, central nervous system);
• eating disorders (anorexia, bulimia);
• toxic goiter;
• violation of blood flow in the parts of the brain, peripheral vessels;
• generalized tic (Tourette cider);
• heart disease (ischemia, arrhythmia, stroke, congenital heart disease);
• severe pathologies of the kidneys, liver;
• allergy to the active substance;
• pathology of the psyche;
• arterial hypertension (increased pressure);
• hormonally active tumor of the adrenal glands or other localization (pheochromocytoma);
• prostate adenoma;
• a decrease or complete absence of the lactase enzyme (hypolactasia);
• angle-closure glaucoma;
• pregnancy and breastfeeding period;
• alcohol, drug, pharmaceutical addiction.

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

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

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, convulsions;
• anorexia;
• constipation, hemorrhoids;
• overflow of vessels with blood (hyperemia);
• increased bleeding due to a decrease in the number of platelets (thrombocytopenia);
• increased blood pressure;
• increased heart rate, tachycardia;
• loss of appetite;
• jade, purpura;
• increased activity of liver enzymes.

Mode of application

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

The appearance of side effects, poor tolerance of the components of the drug does not mean the immediate cancellation of Sibutramine. Its dosage is reduced to a minimum level of 5 mg. The deterioration of the patient's health indicates the need to end therapy. Course treatment can last up to 12 months. This is the maximum duration of the drug.

special instructions

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

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

drug interaction

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.

Preparations with sibutramine

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

Name	Description	Peculiarities
Reduxin	Used for alimentary obesity	Many side effects
Goldline	Indian remedy for the treatment of overweight	Causes addiction with long-term use
	Accelerates lipid metabolism	Gets rid of food addiction
	It is prescribed in cases where excess weight threatens the life of the patient	Requires a long time
Sibutrex	Suppresses the feeling of hunger	Large list of contraindications
	Overweight treatment	The appearance of constant thirst
Reductil	Enhances the feeling of satiety	Sold online only
Lindax	Anoretic remedy for dietary obesity	Not used as a dietary supplement, only as a medicine

The price of Sibutramine

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

The cost of Sibutramine is overestimated due to its inaccessibility. Foreign analogues of the road due to transportation costs. Basically, the medicine is purchased through an online pharmacy or a supplement store. Price range in Moscow:

Name of place of purchase	Cost, rubles For 30/60/90 capsules
Reduksin Pharmacy
Jiggy-Jig online pharmacy for adults
Euro Pharma
Online Steroid Pharmacy
FitPharma
ZdravCity
Avicenna Pharma

Video

As you know, sticking to a diet is very difficult. Often, many of those who cannot boast of remarkable willpower, after several days of dieting, give up all attempts to overcome obesity, due to the fact that they cannot moderate their own appetite. Yes, this situation is not uncommon.

Over the years, the number of unsuccessful attempts to use food restrictions increases, which entails a strong decrease in self-esteem, and this is already a triggering factor for the development of deep psychological complexes and severe depression.

In order to somehow level out the shortcomings of dietary nutrition, as well as give themselves a little strength, many losing weight resort to the help of medications. Most often, these drugs are based on a chemical called sibutramine.

What is it - an unconditional good, promising the eradication of a serious misfortune, or a time bomb that can finally undermine health? First, a few words about the mechanism of action of sibutramine.

The effect of Sibutramine on the human body

I note that we are talking about a potent drug, and not about something harmless. This should be clearly understood. And it should be taken very seriously. That is why it cannot be bought in a pharmacy without a doctor's prescription, but, of course, you and I know that this has not stopped anyone yet. Perhaps this is where the “root of evil” lies, but more on that later.

Sibutramine is a substance that blocks the reuptake of neurotransmitters at certain synapses. As a result, the number of nerve impulse transmission stimulators increases significantly.

As a result, the occurrence of excitation in some centers of the brain, which are responsible for the appearance of a feeling of satiety, is accelerated. These structures are located in the hypothalamic region.

In this situation, even a small amount of food can cause satiety. Given the small amount of food consumed, a negative energy balance is created in the body, which activates the processes of lipolysis. The ill-fated body fat slowly begins to disappear. As a matter of fact, this is the ultimate goal of every losing weight.

But the action of sibutramine does not end there. As a result of stimulation of adrenergic receptors, there is a slight hyperthermia. It is known that even with a slight increase in body temperature, metabolic processes, including lipolysis, are greatly accelerated. It is quite predictable that the hated kilograms "melt like the last snow under the rays of the April sun."

But on the other hand"

It would seem, what more could you want? From now on, the problems of many people suffering from excessive obesity will be solved once and for all, and we will forget about obesity, like a nightmare. But not everything is so rosy, and for everything in life, sooner or later, you have to pay, and not always with money. And because sibutramine for weight loss has not very positive reviews.

The bitter truth is revealed precisely when it comes to the side effects of sibutramine. Unfortunately, the frequency of their occurrence tends to 20 percent, and sometimes even exceeds this figure.

Among the frequently encountered side effects the following states should be distinguished:

Feeling unwell, constant headaches, sleep and wake disturbances;
Multiple allergic reactions;
Gross violations of the heart rhythm;
Migraine;
Significant increase in blood pressure;
Gastrointestinal disorders: diarrhea, constipation, nausea, vomiting, abdominal pain;
Anorexia;
Intestinal disorders: gastritis, enteritis;
Multiple lesions of the joints by the type of arthritis;
Violations or cessation of the menstrual cycle;
Damage to the upper respiratory tract.

The deplorable picture is aggravated even more, given the efforts of some businessmen to popularize sibutramine and drugs based on it. By the way, the names of the latter are well known to everyone: Meridia, Lindaksa, Reduksin, Xenical. Isn't it familiar names?

On the Internet, you can find a lot of thematic resources that provide dizzying weight loss stories. According to the owners, people who got rid of obesity communicate there, just by taking the medications mentioned above.

After a little study of rave reviews, we can conclude that this medicine is harmless, like ascorbic acid or aspirin, and that its use does not bode well. But they assure you it is not.

The ultimate goal of such resources is to create a false sense of security for sibutramine and its analogues. These are ordinary entrepreneurs who want to earn as much money as possible, they are not interested in your problems.

Diet pills Sibutramine is a drug, and, therefore, its use should be dictated by the presence of indications. The only situation in which the manufacturer recommends the appointment of these pills is obesity in a severe stage, in the absence of the effect of other measures aimed at reducing excess weight.

Before you start taking such funds, you must obtain the approval of an experienced specialist. During the entire course of the drug, and this is a very long period, from six months to a year, it is necessary to periodically visit the clinic to assess your own condition.

Conclusion

In any case, you need to understand that sibutramine and its derivatives are, as they say, the last line of defense, and therefore they should be used only in extreme cases.

Gross formula

C 17 H 26 ClN

Pharmacological group of the substance Sibutramine

Nosological classification (ICD-10)

CAS code

106650-56-0

Characteristics of the substance Sibutramine

Sibutramine hydrochloride monohydrate is a white to off-white crystalline powder. Solubility in water: 2.9 mg/ml at pH 5.2. Partition coefficient (octanol/water): 30.9 (pH 5.0). Molecular weight 334.33.

Pharmacology

pharmachologic effect- anorexigenic.

Inhibits the reuptake of neurotransmitters - serotonin and norepinephrine from the synaptic cleft, potentiates the synergistic interactions of the central norepinephrine and serotonergic systems. Reduces appetite and the amount of food consumed (increases the feeling of fullness), increases thermogenesis (due to mediated activation of beta 3-adrenergic receptors), has an effect on brown adipose tissue. Forms active metabolites in the body (primary and secondary amines), significantly superior to sibutramine in its ability to inhibit the reuptake of serotonin and norepinephrine. In research in vitro active metabolites also block the reuptake of dopamine, but 3 times weaker than 5-HT and norepinephrine. Neither sibutramine nor its active metabolites affect the release of monoamines and MAO activity, do not interact with neurotransmitter receptors, including serotonergic, adrenergic, dopaminergic, benzodiazepine and glutamate (NMDA), do not have anticholinergic and antihistamine effects. Inhibits uptake of 5-HT by platelets and may alter platelet function.

Weight loss is accompanied by an increase in serum HDL concentration and a decrease in triglycerides, total cholesterol, LDL and uric acid.

During treatment, there is a slight rise in blood pressure at rest (by 1-3 mm Hg) and a moderate increase in heart rate (by 3-7 beats / min), but in isolated cases more pronounced changes are possible. With 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 2-year studies in rats and mice, at doses that resulted in an observed total area under the concentration-time curves (AUCs) for the two active metabolites 0.5-21 times higher than that of MRDH, increased the incidence of benign tumors testicular interstitial tissue predominantly in male rats. No carcinogenic effect was found in mice and female rats. Does not have a mutagenic effect, does not affect fertility. When doses were administered 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. However, in studies conducted on Dutch Belted rabbits under conditions where the AUCs of active metabolites of sibutramine were 5 times higher than when using MRDH, anomalies in physical development were found in offspring (changes in the shape or size of the muzzle, auricle, tail, bone thickness ).

After oral administration, it is rapidly absorbed from the gastrointestinal tract by at least 77%. During the "first pass" through the liver, it undergoes biotransformation under the influence of the CYP3A4 isoenzyme of cytochrome P450 with the formation of two active metabolites (mono- and didesmethylsibutramine). After taking a single dose of 15 mg C max monodesmethylsibutramine is 4 ng / ml (3.2-4.8 ng / ml), didesmethylsibutramine - 6.4 ng / ml (5.6-7.2 ng / ml). Cmax is achieved after 1.2 hours (sibutramine), 3-4 hours (active metabolites). Simultaneous food intake lowers Cmax of metabolites by 30% and increases the time to reach it by 3 hours without changing AUC. It is quickly distributed on fabrics. Protein binding is 97% (sibutramine) and 94% (mono- and didesmethylsibutramine). The equilibrium concentration of active metabolites in the blood is reached within 4 days after the start of treatment and is approximately 2 times higher than the plasma level after taking a single dose. T 1/2 sibutramine - 1.1 h, monodesmethylsibutramine - 14 h, didesmethylsibutramine - 16 h. Active metabolites undergo hydroxylation and conjugation to form inactive metabolites, which are excreted mainly by the kidneys.

The use of the substance Sibutramine

Complex maintenance therapy of overweight patients with alimentary obesity with a body mass index of 30 kg / m 2 or more or with a body mass index of 27 kg / m 2 or more, but in the presence of other risk factors due to overweight (sugar type 2 diabetes, dyslipoproteinemia).

Contraindications

Hypersensitivity, the presence of organic causes of obesity, anorexia nervosa or bulimia nervosa, mental illness, Gilles de la Tourette syndrome, coronary heart disease, decompensated heart failure, congenital heart disease, peripheral arterial occlusive disease, tachycardia, arrhythmia, cerebrovascular disease (stroke, transient disorders cerebral circulation), arterial hypertension (BP> 145/90 mm Hg), hyperthyroidism, severe liver or kidney dysfunction, benign prostatic hyperplasia, accompanied by the presence of residual urine, pheochromocytoma, glaucoma, established pharmacological, drug and alcohol dependence, simultaneous reception or a period of less than 2 weeks after the abolition of MAO inhibitors or other drugs acting on the central nervous system (including antidepressants, antipsychotics, tryptophan), as well as other drugs to reduce body weight.

Application restrictions

Epilepsy, motor-verbal tic (involuntary muscle contractions, impaired articulation), children and the elderly (safety and efficacy in children under 18 years of age and in people over 65 years of age have not been determined).

Use during pregnancy and lactation

It is not known whether sibutramine and its metabolites pass into breast milk. During breastfeeding, use is not recommended.

Side effects of Sibutramine

In placebo-controlled studies, 9% of patients treated with sibutramine (n=2068) and 7% of patients treated with placebo (n=884) discontinued treatment due to side effects.

In placebo-controlled studies, the most common side effects were dry mouth, anorexia, insomnia, constipation, and headache.

The following are side effects that were observed in patients taking sibutramine, with a frequency of ≥1% and more often than in the placebo group. Next to the name is the frequency of occurrence of this side effect in the group taking sibutramine, in brackets - similar data in the placebo group.

Body as a whole: headache 30.3% (18.6%), back pain 8.2% (5.5%), flu-like syndrome 8.2% (5.8%), accidental injury 5.9% (4.1%), asthenia - 5.9% (5.3%), abdominal pain - 4.5% (3.6%), chest pain - 1.8% (1.2%), pain in the neck - 1.6% (1.1%), allergic reactions - 1.5% (0.8%).

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): tachycardia - 2.6% (0.6%), vasodilation (skin hyperemia with a feeling of warmth) - 2.4% (0.9%), migraine - 2.4% (2.0%), hypertension / increased blood pressure - 2.1% (0.9%), heart rate - 2.0% (0.8%).

From the digestive tract: anorexia - 13.0% (3.5%), constipation - 11.5% (6.0%), increased appetite - 8.7% (2.7%), nausea - 5.9% (2.8%) %), dyspepsia — 5.0% (2.6%), gastritis — 1.7% (1.2%), thirst — 1.7% (0.9%), vomiting — 1.5% (1 .4%), exacerbation of hemorrhoids - 1.2% (0.5%).

From the musculoskeletal system: arthralgia — 5.9% (5.0%), myalgia — 1.9% (1.1%), tenosynovitis — 1.2% (0.5%), joint diseases — 1.1% (0.6 %).

From the nervous system and sensory organs: dry mouth - 17.2% (4.2%), insomnia - 10.7% (4.5%), dizziness - 7.0% (3.4%), nervousness - 5.2% (2, 9%), anxiety - 4.5% (3.4%), depression - 4.3% (2.5%), paresthesia - 2.0% (0.5%), drowsiness - 1.7% ( 0.9%), arousal - 1.5% (0.5%), emotional lability - 1.3% (0.6%), taste changes - 2.2% (0.8%), ear diseases - 1.7% (0.9%), ear pain - 1.1% (0.7%).

From the respiratory system: rhinitis - 10.2% (7.1%), pharyngitis - 10.0% (8.4%), sinusitis - 5.0% (2.6%), increased cough - 3.8% (3.3 %), laryngitis — 1.3% (0.9%).

From the side of the skin: rash - 3.8% (2.5%), sweating - 2.5% (0.9%), herpes simplex- 1.3% (1.0%), acne - 1.0% (0.8%).

From the genitourinary system: dysmenorrhea - 3.5% (1.4%), urinary tract infections - 2.3% (2.0%), vaginal candidiasis - 1.2% (0.5%), metrorrhagia - 1.0% (0 ,eight%).

Others: generalized edema - 1.2% (0.8%).

Interaction

Inhibitors of microsomal oxidation, incl. inhibitors of CYP3A4 cytochrome P450 (ketoconazole, erythromycin, cyclosporine, etc.) reduce the clearance of sibutramine. Means with serotonergic activity increase the risk of developing serotonin syndrome (agitation, sweating, diarrhea, fever, arrhythmia, convulsions, etc.).

Overdose

Symptoms: increased severity of side effects, most often - tachycardia, increased blood pressure, headache and dizziness.

Treatment: intake of activated charcoal, symptomatic therapy, monitoring of vital functions, with an increase in blood pressure and tachycardia - the appointment of beta-blockers.

Routes of administration

inside.

Sibutramine Substance Precautions

It is necessary to control the level of blood pressure and pulse rate every 2 weeks during the first 2 months of treatment and then once a month. In patients with arterial hypertension at blood pressure >145/90 mm Hg. control should be carried out more carefully and more often, and in the case of a double-registered rise in blood pressure> 145/90 mm Hg. treatment should be discontinued. The appearance during therapy of chest pain, progressive dyspnea (breathing disorder) and edema of the lower extremities may indicate the development of pulmonary hypertension (in this case, it is necessary to consult a doctor).

It is not recommended to simultaneously take drugs that increase the QT interval (astemizole, terfenadine, antiarrhythmic and other drugs), drugs containing ephedrine, phenylpropanolamine, pseudoephedrine, etc. (danger of increasing blood pressure and increasing heart rate), as well as other anorexigenic drugs with a central mechanism of action. Caution should be prescribed against the background of hypokalemia and hypomagnesemia, in case of impaired liver and kidney function of mild to moderate severity.

Women of childbearing age during the period of treatment should use adequate contraceptive measures.

It should be borne in mind that sibutramine can reduce salivation and contribute to the development of caries, periodontal disease, candidiasis and oral discomfort. During treatment it is recommended to limit the use of alcohol.

Rapid weight loss without any effort sounds very tempting to many who are tired of extra pounds. Therefore, "magic" drugs for weight loss are, and, apparently, always will be in demand among the predominantly female population, dissatisfied with their weight.

Sibutramine hydrochloride monohydrate, discovered by the international corporation Abbott Laboratories on the threshold of the last decade of the last century and did not justify its first purpose as an antidepressant, turned out to be a pronounced anorectic. The action of this substance in terms of suppressing the feeling of hunger turned out to be unexpectedly effective, and the loss of excess kilograms was so significant that it began to be used as a cure for obesity since 1997, prescribing overweight patients caused by uncontrolled food intake.

Why is sibutramine banned?

The fame of Sibutramine as an effective fat burner, which also eliminates the desire to snack, quickly spread across countries and continents, since the problem of excess weight is quite acute not only in the United States, but also in most economically developed countries of Europe. The World Health Organization considers this problem as an epidemic and, naturally, the emergence of a new drug that eliminates hunger and stimulates metabolic processes in the body was received more than favorably. Sibutramine and medicines containing it began to be prescribed to overweight patients right and left.

However, reports of mental disorders in patients taking drugs with this active ingredient began to appear quite quickly. Among them, cases of suicides, acute cardiovascular pathologies with a fatal outcome, especially among the elderly, have become more frequent. In addition, preparations with Sibutramine can, according to some reports, cause drug-like dependence. All these facts and the long list of side effects that came to light during more thorough research into the properties of this drug explains why Sibutramine is banned. Since 2010, the sale of drugs with this active ingredient has been temporarily discontinued in the European Union, in Australia, the USA, Canada and Ukraine, in Russia they can only be bought with a doctor's prescription.

Indications for the use of this remedy are primary nutritional obesity of the II-III degree, when the body mass index goes off scale for 30-35 kg / m² with the ineffectiveness of other methods of treatment. Both immediately after the appearance, and at the present time, this medicine for extra pounds was not recommended for everyone, but in especially severe cases of obesity. The Sibutramine treatment regimen assumes a low-calorie diet and exercise. It is also prescribed to people suffering from non-insulin dependent diabetes, hyper- or hypoproteinemia. In this case, the recommended body mass index of the patient is 27kg/m² and above.

Complex therapy, including drugs with Sibutramine, is carried out under the supervision of a specialist with practical experience in the treatment of overweight. An important part of it is the formation of the patient's psychological readiness to change their habits in terms of diet and diet, as well as changes in lifestyle, and maintain them after drug treatment is discontinued.

ATX code

A08AA10 Sibutramine

Active ingredients

Sibutramine

Pharmacological group

For weight loss

appetite regulators

pharmachologic effect

Anorexigenic drugs

Pharmacodynamics

The mechanism of action of this substance is that it contributes to the rapid satisfaction of hunger, activating the feeling of satiety and, thereby, reducing the amount of food consumed without effort on the part of the patient.

The beginning of the transmission of chemical signals (for example, about satiety during a meal) between brain neurons is the release of neurotransmitters, serotonin and norepinephrine, into the intercellular space (synapse), where the signal is received. Sibutramine molecules block the return of neurotransmitters back to the presynaptic cell. Due to this, the concentration of serotonin and norepinephrine increases in the synapse, potentiating the stimulation of the neuron receiving the impulse. The saturation signal enters the postsynaptic cells more intensively, the body does not require a large amount of food. In addition, the drug increases the production of heat by the body, boosting metabolic processes and forming monodemethyl- and didemethylsibutramine - active metabolites that can themselves inhibit the reuptake of released neurotransmitters (serotonin and norepinephrine), as well as the pleasure hormone dopamine, but to a much lesser extent. By acting in this way, Sibutramine contributes to the rapid emergence of a feeling of satiety, moreover, it becomes permanent. The desire to snack disappears by itself, food intake is significantly reduced, which leads to rapid weight loss.

The active substance and its active metabolites are indifferent to the release of the monoamine oxidase enzyme and its activation, do not interact with neurotransmitters, including catecholamines, serotonin, histamine, acetylcholine, glutamic acid and benzodiazepines. They inhibit the uptake of membrane serotonin receptors by platelets and may alter their function.

The reduction of body fat with the help of these medications is accompanied by an increase in the level of high-density lipoprotein ("good" cholesterol) in the blood plasma against the background of a quantitative decrease in triacylglycerides, total cholesterol due to "bad" and uric acid.

During treatment with these medications, cases of a slight increase in blood pressure and heart rate were mainly recorded, but there were also more serious changes in these parameters. Most medications with sibutramine are monopreparations, however, in addition to the main active ingredient, Reduxin also contains microcrystalline cellulose, a natural and non-food product without side effects. It has the property, lingering in the stomach, to swell under the influence of liquid, thus providing a feeling of satiety. In combination with sibutramine, it complements its action. It is able to absorb not only water, but also putrefactive bacteria, cleanses the intestines well and prevents food poisoning.

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Pharmacokinetics

When taken orally, the active ingredient is rapidly absorbed from the gastrointestinal tract (about 80%). Once in the liver, Sibutramine is metabolized into monodemethyl- and didemethylsibutramine. After 72 minutes after taking the drug, dosed at 0.015 g, the highest concentration of the active ingredient is observed, and from three to four hours - its metabolites. Taking the capsule with food, the patient reduces the maximum concentration of metabolites by a third, and the time to reach it increases by three hours, without changing the total concentration and distribution. Sibutramine (almost completely) and its metabolites (>90%) bind to serum albumin and are distributed at a good rate in body tissues. The concentration of active substances in the blood serum reaches a state of equilibrium after four days from the start of therapy and is twice as high as their serum concentration determined after the first dose.

Excretion from the body of inactive demethylated metabolites occurs mainly in the urine, less than 1% is excreted in the feces. The half-life of sibutramine is 66 minutes, its metabolites (monodesmethyl- and didesmethylsibutramine) are 14 and 16 hours, respectively.

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Sibutramine use during pregnancy

The results of tests of Sibutramine on laboratory animals indicate that this active substance does not affect the ability to fertilize, however, the teratogenic effect of sibutramine on the fetus was observed in the offspring of experimental rabbits. They were identified physical anomalies regarding the appearance, as well as the structure of the skeleton.

Medicines containing Sibutramine should not be used by pregnant and lactating women. Throughout the course of treatment and one and a half months after the end of treatment with these drugs, female patients of childbearing age should use reliable contraception.

Contraindications

• age restrictions: not assigned to minors and persons over 65 years of age;
• secondary obesity caused by diseases of the endocrine and central nervous system, other organic causes;
• eating disorders - bulimia, anorexia (available or in history);
• mental pathologies;
• generalized tick;
• circulatory disorders in the brain (in the presence or in history);
• toxic goiter;
• ischemic heart disease (in the presence or in history), rhythm and heart rate disturbances, chronic decompensated dysfunction of the heart muscle;
• circulatory disorders in peripheral vessels;
• uncontrolled increase in blood pressure above 145 mmHg;
• severe degrees of impaired liver and / or kidney function;
• prostate adenoma with urinary retention;
• pheochromocytoma
• substance abuse and/or alcoholism;
• angle-closure glaucoma;
• hypolactasia, glucose-galactose malabsorption syndrome;
• known sensitization to sibutramine and/or other drug ingredients.

With special care, it is prescribed to patients with a history of: hypertension, circulatory disorders, muscle spasms, coronary insufficiency, epilepsy, hepatic and / or renal dysfunction, cholelithiasis, glaucoma, hemorrhages, tics, as well as taking medications that disrupt blood clotting.

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Side effects of Sibutramine

This substance is a very effective anorectic, and, naturally, for those who want to lose weight and read rave reviews, of which there are many, the question arises: Why is Sibutramine dangerous?

Of course, like any substance, it can cause allergies. In most cases, this is not anaphylactic shock, but a more harmless reaction of the body, for example, a rash from Sibutramine. Unpleasant, but not dangerous. If you stop taking it, it will itch and pass.

A more serious consequence is addiction. This drug is not recommended for more than one year, but people who start taking it often cannot stop, they develop a real drug addiction, which, in fact, is a subspecies of drug addiction. Not everyone. However, who can guarantee that his body will be resistant to this property of this drug?

There will be no true narcotic high from Sibutramine, but upon cancellation, which is recommended to be carried out gradually, sensations similar to “withdrawal” may appear. This happens even with a short, three months, taking the drug. These are dizziness and migraines, sleep disturbances and anxiety, irritability or apathy and thoughts of suicide. Sibutramine has a direct effect on the brain and the central unequal system. This is how he fights overeating and overweight. But it is not always possible to influence the psyche and nervous system without undesirable consequences. The first appointments of Sibutramine were accompanied by severe neuropsychiatric disorders, suicides, deaths from acute cardiac and brain pathologies, patients became addicted to the drug and its long-term use turned into sad consequences. Modern dosages of Sibutramine are much lower than those recommended at the beginning, the drug is better purified, but undesirable effects, albeit less pronounced, still remain. During the period of therapy with this medicine, you can not perform work at heights, drive vehicles, work with mechanisms that require increased concentration of attention. This drug is contraindicated in people who have or have a history of alcohol or drug addiction as the effects will be cumulative.

The instructions for the drug indicate that side effects most often occurred in the first month of treatment, and if it continued, then over time the frequency and intensity of these effects decreased. The adverse effects were mostly reversible and resolved with discontinuation of the drug.

The most common were: palpitations, hypertension, flushing of the skin with sensations of warmth, constipation, complete lack of appetite, exacerbation of hemorrhoids, nausea, a feeling of dryness in the mouth, insomnia, fainting, numbness of body parts, panic attacks, increased sweating, taste perversion.

In the post-registration study SCOUT, initiated by the relevant body of the European Union after many cases of severe adverse events, in which many patients with obesity and a high probability of cardiovascular diseases took part, the following data were obtained: the risk of non-fatal (!) heart attack, stroke, heart attack in patients taking Sibutramine increased by 16% compared with those patients who took placebo. However, what is very comforting, with the help of resuscitation measures, 1.4% more patients were saved who took the real drug. But deaths, both from vascular pathologies and from all causes, in both groups of patients occurred with the same frequency.

Undesirable effects have been observed in the form of allergies ranging from minor rashes to anaphylactic shock. The number of platelets in the blood decreased, that is, the blood did not clot well, there were cases of autoimmune damage to the walls of blood vessels (hemorrhagic purpura), mental disorders, which have already been mentioned above. In these cases, treatment was recommended to stop.

The nervous system reacted to the drug with convulsions, short-term memory lapses, and amnesia.

Pain syndromes in the head, back, ears, visual and hearing disorders, digestion, ENT diseases, herpes. The list of side effects is endless. It is completed by the message that occasionally the withdrawal syndrome is accompanied by a headache and an increase in appetite (!).

For women planning to have children after a course of Sibutramine, it makes sense to seriously think about it. The drug is teratogenic, its ability to cause mutations has not yet been confirmed, but this remedy is used for a very short time and, most importantly, often not officially. Therefore, additions to the list are still possible.

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Dosage and administration

The drug is taken once in the morning, regardless of the meal. Treatment begins with one capsule of 0.01 g, which is swallowed whole and washed down with water in sufficient quantities. With a loss of less than two kilograms of weight during the first four weeks of therapy and good tolerance, a higher daily dosage of 0.015 g is prescribed. If in the next four weeks the weight is reduced by less than two kilograms, the drug is canceled as ineffective in this case, since higher dosages are not recommended.

Treatment is stopped in the following cases:

• when for three months the patient loses less than 5% of the initial weight;
• when weight loss has stabilized at less than 5% of initial weight;
• when, after already achieved weight loss, the patient regains three kilograms or more.

Treatment with this drug is possible for no more than two years.

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Instructions for use:

Sibutramine is a synthetic drug used in the treatment of alimentary obesity.

pharmachologic effect

Sibutramine with the active ingredient of the same name refers to drugs that accelerate the onset of satiety. This leads to a decrease in food intake without psychological stress, and, as a result, to weight loss.

Medicines containing sibutramine do not release monoamines and are not MAO inhibitors. Also, the drug has no affinity for adrenergic, serotonergic, muscarinic, dopaminergic, benzodiazepine, histamine and NMDA receptors.

Sibutramine's analogs

The analogues of Sibutramine for the active substance are the drugs Goldline, Meridia, Lindax and Slimia.

If necessary, the doctor can replace the medication with one of the Sibutramine analogues with a similar therapeutic effect. These include Reduxin, which contains sibutramine and microcrystalline cellulose as active ingredients, and Fepranone with the active substance amfepramone.

Indications for the use of Sibutramine

According to the instructions, Sibutramine is prescribed as part of a complex maintenance therapy for overweight:

• With alimentary obesity (body mass index - from 30 kg / m2 or more);
• With alimentary obesity (body mass index - from 27 kg / m2 or more), if there are other risk factors associated with overweight, including hyperlipidemia and type 2 diabetes.

Contraindications

It is contraindicated to use Sibutramine for weight loss:

• Serious eating disorders, such as bulimia nervosa or anorexia nervosa;
• With an organic cause of obesity;
• Against the background of Tourette's syndrome;
• Against the background of mental illness;
• With occlusive diseases of peripheral arteries;
• Against the background of coronary heart disease, congenital heart defects, chronic heart failure in the stage of decompensation;
• With uncontrolled arterial hypertension;
• Against the background of arrhythmia, tachycardia and various disorders of cerebral circulation, including transient;
• Against the background of severe violations of the liver and kidneys;
• With hyperthyroidism;
• Against the background of pheochromocytoma;
• With benign prostatic hyperplasia with the formation of residual urine;
• During pregnancy and lactation;
• With established pharmacological, drug or alcohol dependence;
• Against the background of glaucoma;
• In case of hypersensitivity to the active substance of the same name or other components that make up the drug.

Sibutramine according to the instructions is contraindicated for use simultaneously with certain medicines, namely:

• With MAO inhibitors;
• With antidepressants, antipsychotics, tryptophan or other drugs that have a depressant effect on the central nervous system;
• With any other medicines, the action of which is aimed at reducing body weight.

Special care requires the appointment of Sibutramine for weight loss:

• Against the background of hypokalemia and hypomagnesemia;
• Simultaneously with medications that increase the QT interval;
• Against the background of impaired liver and kidney function, occurring in mild to moderate severity;
• With epilepsy;
• Along with medicines that can cause an increase in blood pressure and heart rate, including a number of cold, cough and allergy medicines.

Due to the lack of necessary studies, Sibutramine is not prescribed for people over 65 years of age.

How to use Sibutramine

Sibutramine is usually prescribed at an initial dose of 10 mg per day. If weight loss occurs too slowly (less than 2 kg per month), in the absence of severe side effects associated with taking the medication, the daily dosage is increased to 15 mg. If the rate of weight loss does not increase at the indicated dosage, the use of Sibutramine is canceled.

As a rule, the medicine is used for at least a year. If during the first three months of therapy it is not possible to achieve a sufficient level of weight loss (at least 5% of the initial level), the use of Sibutramine is canceled. Also, the medication is canceled if weight gain is observed during therapy.

Sibutramine is prescribed only in cases where any other measures taken do not lead to weight loss (less than 5 kg in three months).

Treatment must be carried out comprehensively. This should include changing the nutritious diet and increasing physical activity. It is a change in the habitual lifestyle that caused obesity is a necessary condition for maintaining the achieved result in weight loss with the use of Sibutramine.

During therapy, blood pressure and changes in heart rate should be monitored. Also during the examination, attention should be paid to chest pain, swelling, progressive dyspnea.

Side effects of Sibutramine for weight loss

Of the disorders of the digestive system, most often when using Sibutramine, according to reviews, there is a loss of appetite, dry mouth, constipation and nausea, and a transient increase in the activity of liver enzymes may develop somewhat less frequently.

Also, while taking Sibutramine, according to reviews, disorders of other systems may occur, which are expressed as:

• Increased sweating, insomnia, headaches, anxiety, dizziness, paresthesias, seizures and taste changes (central and peripheral nervous system);
• Shenlein-Genoch purpura and thrombocytopenia (blood clotting system);
• Palpitations, tachycardia, slight increase in blood pressure, reddening of the skin with a feeling of warmth, exacerbation of hemorrhoids (cardiovascular system).

In some cases, the use of Sibutramine according to reviews can cause acute interstitial nephritis, a more pronounced increase in blood pressure and mesangiocapillary glomerulonephritis.

In most cases, the occurrence of side effects when using Sibutramine for weight loss is observed in the first month of therapy, and their frequency and severity decrease over time.

drug interaction

During treatment, it should be borne in mind that with the simultaneous use of Sibutramine with ketoconazole, erythromycin, troleandomycin, cyclosporine and other drugs that inhibit the activity of the CYP3A4 isoenzyme, the plasma concentration of Sibutramine metabolites may increase, which contributes to a slight increase in the QT interval.

The risk of developing serotonin syndrome increases with the simultaneous use of Sibutramine with:

• 5-HT1 receptor agonists;
• Selective serotonin reuptake inhibitors, such as fluoxetine, citalopram, sertraline and paroxetine;
• Opioid analgesics;
• Ergot alkaloid derivatives;
• Antitussive drugs of central action.

Storage conditions

Sibutramine is a prescription drug with standard storage conditions.