Slimming pills with sibutramine: instructions and course of treatment

Currently, the sale of drugs with this active ingredient has been temporarily suspended in the European Union, Australia, the USA, Canada and Ukraine, in Russia they can only be purchased with a doctor's prescription. However, no bans can combat consumer demand; purchasing medications with Sibutramine without a doctor's prescription is not a problem. However, there is no guarantee that you will not receive a counterfeit drug.

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Indications sibutramine pills for weight loss

These drugs are prescribed in therapeutic complex schemes for weight loss in the following cases:

• primary alimentary obesity of II-III degree, when the body mass index exceeds 30-35 kg/m2 ^and other treatment methods are ineffective;
• the patient's body mass index is 27 kg/m2 ^or higher if he has non-insulin-dependent diabetes, hyper- or hypoproteinemia.

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Release form

Capsules dosed at 0.005, 0.01, 0.015 g of active ingredient.

Names of diet pills containing sibutramine

• original medicines Meridia and Reductil (Abbvie Deutschland GmbH & Co. for Abbott Laboratories, Germany)
• generics – Lindaxa (Zentiva, Czech Republic), Reduksin (Promomed, Russia), Gold Line, Slimia, Obestat, Redyus, Sibutril, Slimex (India), Obestafite, Sibutrex and Sibutrim (India-UK).

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Pharmacodynamics

The active ingredient in these weight loss medications is the centrally acting anorectic Sibutramine. It works by influencing the appetite centers in the human brain, helping to quickly satisfy hunger, activating the feeling of satiety and thus reducing the amount of food consumed without any effort on the part of the patient.

The beginning of the transmission of chemical signals (for example, about satiety during food intake) between neurons of the brain 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 in the synapse increases, potentiating the stimulation of the neuron receiving the impulse. The signal of satiety enters the postsynaptic cells more intensively, the body does not require the intake of large amounts of food. In addition, the drug increases the production of heat by the body, forcing metabolic processes, which promotes fat burning. It forms 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 working in this way, Sibutramine promotes a rapid and permanent feeling of satiety. 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 enzyme monoamine oxidase and its activation, do not interact with neurotransmitters, including catecholamines, serotonin, histamine, acetylcholine, glutamic acid and benzodiazepines. They suppress the capture of membrane serotonin receptors by platelets and can change their functions.

The reduction of fat deposits with the help of these medications is accompanied by an increase in the level of high-density lipoproteins (“good” cholesterol) in the blood serum against the background of a quantitative reduction in triacylglycerides, total cholesterol at the expense of “bad” cholesterol and uric acid.

Most medications with Sibutramine are monodrugs. However, Reductil and Reduksin are complex drugs that contain, in addition to the main active ingredient, microcrystalline cellulose, a natural non-food product that has no side effects. It has the property of swell under the influence of liquid when retained in the stomach, thus providing a feeling of satiety. In combination with Sibutramine, it complements its action. Microcrystalline cellulose 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 component is rapidly absorbed from the gastrointestinal tract (about 80%). When entering the liver, Sibutramine is metabolized into monodemethyl- and didemethylsibutramine. The highest concentration of the active ingredient is observed 72 minutes after taking the drug, dosed at 0.015 g, and its metabolites are observed from three to four hours. Taking the capsule with food, the patient reduces the highest concentration of active metabolites by a third, and the time of its determination increases by three hours, without changing the total concentration and distribution. Sibutramine (almost completely) and its metabolites (>90%) bind to serum albumins and spread quickly in body tissues. The concentration of active substances in the blood serum reaches equilibrium four days after the start of therapy and is twice their serum concentration determined after the first dose.

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

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Dosing and administration

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

Treatment is stopped in the following cases:

• when the patient loses less than 5% of their initial weight over three months;
• when weight loss has stabilized at less than 5% of the initial weight;
• when, after already achieving weight loss, the patient again gains three kilograms or more.

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

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Use sibutramine pills for weight loss during pregnancy

The results of Sibutramine tests 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 laboratory rabbits. They were found to have physical anomalies related to appearance, as well as skeletal structure.

Medicines containing Sibutramine are prohibited for use by pregnant and lactating women. Throughout the entire course of treatment and for one and a half months after the end of treatment with these drugs, female patients of fertile age must use reliable contraception.

Contraindications

• age restrictions: not prescribed to minors and persons over 65 years of age;
• secondary obesity caused by diseases of the endocrine and central nervous systems, and other organic causes;
• eating disorders – bulimia, anorexia (present or in history);
• mental pathologies;
• generalized tic;
• circulatory disorders in parts of the brain (present or in history);
• toxic goiter;
• myocardial ischemia (present or in history), tachyarrhythmia, chronic decompensated dysfunction of the heart muscle;
• circulatory disorders in peripheral vessels;
• uncontrolled hypertension (blood pressure above 145 mm Hg);
• severe degrees of liver and/or kidney dysfunction;
• 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 ingredients of the drug.

It should be prescribed with special caution to patients with a history of hypertension, circulatory disorders, muscle spasms, coronary artery insufficiency, epilepsy, liver and/or kidney dysfunction, gallstone disease, glaucoma, hemorrhages, tics, and those taking medications that impair blood clotting.

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Side effects sibutramine pills for weight loss

Adverse effects usually appeared within the first month of treatment, and if treatment was continued, the frequency and intensity of these effects decreased over time. Negative effects were generally reversible and disappeared with drug withdrawal.

According to the results of post-marketing clinical testing, the following adverse effects of taking medications with Sibutramine were observed more often than in 10% of cases: constipation, insomnia, dry mouth. More often than in 1% of cases, but less often than in 10% of cases, the following were observed: tachyarrhythmia, hypertension, atrial fibrillation, vasodilation, nausea, exacerbation of hemorrhoids, headache, fainting, numbness of the extremities, anxiety, increased sweating, taste perversion.

Clinically significant side effects that were recorded during testing of this substance:

• the risk of non-fatal heart attack, stroke, or cardiac arrest in patients taking Sibutramine increases by 16% compared to those patients taking placebo;
• sensitization reactions from rashes to anaphylaxis;
• decreased platelet count and impaired platelet function, autoimmune damage to the walls of blood vessels;
• psychosis, mania, suicidal intentions and thoughts about it, depression;
• convulsions, short-term memory lapses, amnesia;
• when used simultaneously with drugs that release serotonin, serotonin syndrome developed;
• loss of visual acuity;
• upset stomach, vomiting, gastrointestinal bleeding;
• hair loss, rash, including hemorrhagic;
• acute interstitial nephritis, mesangiocapillary glomerulonephritis, difficulty urinating;
• ejaculation and menstrual cycle disorders, anorgasmia, impotence, uterine bleeding.

Laboratory tests showed elevated liver enzymes.

Headache and increased appetite were occasionally observed upon drug withdrawal.

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Overdose

Taking Sibutramine doses higher than recommended increases the likelihood of adverse effects and their severity. The effects of overdose have not yet been sufficiently studied and
there is no specific antidote.

As part of first aid in case of overdose, gastric lavage and enterosorbents are prescribed for an hour from the moment of taking a dose exceeding the recommended one.

It is necessary to monitor the patient's condition for 24 hours after taking an excessive amount of the drug. If symptoms of side effects develop, appropriate treatment measures are taken. The most typical consequences of an overdose, increased blood pressure and increased heart rate, are relieved with ß-blockers.
The use of an "artificial kidney" device in case of an overdose is inappropriate, since, as studies show, the metabolic products of Sibutramine are practically not eliminated by hemodialysis.

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Interactions with other drugs

Not used in combination with:

• with other drugs that relieve mental pathologies or are intended for patients with alimentary obesity, which have a central effect;
• with drugs that inhibit the enzymatic activity of monoamine oxidase (there should be a time interval of at least two weeks between taking medications containing sibutramine and monoamine oxidase inhibitors);
• with drugs that stimulate the production of serotonin and suppress its reuptake;
• with drugs that inactivate liver microsomal enzymes;
• with drugs that can cause increased heart rate and increase blood pressure, as well as stimulate the sympathetic nervous system.

Preparations containing Sibutramine do not affect the pharmacodynamics of oral contraceptives.

It should also be taken into account that sibutramine and alcohol are not compatible.

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Storage conditions

The storage conditions for Sibutramine-based drugs are no different from those for most medications. The storage temperature should not exceed 25°C. The drug should not be removed from its original packaging and left in places accessible to small children.

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Shelf life

Shelf life: up to three years

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Reviews

Reviews of weight loss products with Sibutramine are often negative, there are quite a lot of complaints about side effects from the nervous system and psyche, which prompt many to stop treatment. Moreover, not everyone manages to get rid of the unwanted consequences of taking it. Judging by the reviews, these effects are not always reversible. Quite a few reviews say that people regret their decision to resort to this drug.

However, there are many reviews that are frankly positive, emphasizing the high effectiveness of this substance, and, apart from dry mouth, no other side effects are mentioned.

Doctors speak about the drug rather reservedly, emphasizing the high effectiveness of Sibutramine and the need to follow the rules for its use, as well as the danger of self-medication, since the drug causes serious side effects.