Diet pills with sibutramine: instructions and treatment

Currently, the sale of medicines with this active ingredient is temporarily discontinued in the territory of the European Union, in Australia, the USA, Canada and Ukraine, in Russia they can only be bought on prescription. However, no prohibitions can not deal with consumer demand, purchase medicines with Sibutramine without a medical prescription does not pose a problem. True, there is no guarantee that you will not receive a counterfeit medicine.

[1], [2], [3], [4], [5], [6], [7], [8], [9]

Indications of the tablets with sibutramine for weight loss

These funds are prescribed in the therapeutic complex schemes for weight reduction in the following cases:

• primary alimentary obesity II-III degree, when the body mass index rises from 30-35 kg / m ²  with ineffectiveness of other methods of treatment;
• the body mass index of the patient is 27 kg / m ²  and higher if he has insulin-independent diabetes, hyper- or hypoproteinemia.

[10], [11], [12]

Release form

Capsules, dosed at 0,005, 0,01, 0,015 g of the active ingredient.

Names of diet pills containing sibutramine

• original medications Meridia and Reductil (Abbevie Deutschland GMBH and Co. For Abbott Laboratories, Germany)
• generics - Lindax (Zentiva, Czech Republic), Reduxin (Promed, Russia), Gold Line, Slimia, Obustat, Redus, Sibutril, Slimex (India), Obustafit, Sibutrex and Sibutrim (India-United Kingdom).

[13], [14], [15], [16]

Pharmacodynamics

The active ingredient of these drugs used to reduce body weight is the central action anorectic Sibutramine. It works as follows: By influencing appetite centers in the human brain, it contributes to the rapid satisfaction of hunger, activates a feeling of satiety and, thereby, reduces the amount of food consumed without effort on the part of the patient.

The beginning of the transmission of chemical signals (for example, about saturation during food intake) between the neurons of the brain is the release of neurotransmitters, serotonin and norepinephrine, into the intercellular space (synapse), where the signal is obtained. Sibutramine molecules block the return of the neurotransmitters back to the presynaptic cell. Due to this, the synapse increases the concentration of serotonin and norepinephrine, potentiating the stimulation of the neuron receiving the impulse. The saturation signal enters the postsynaptic cells more intensively, the body does not require the intake of a large amount of food. In addition, the drug increases the production of heat by the body, boosting the metabolic processes, which contributes to fat burning. Forms monodemetyl- and didmetylsibutramine-active metabolites, capable in themselves to inhibit the re-acquisition of released neurotransmitters (serotonin and norepinephrine), and also - the pleasure hormone of dopamine, but to a much lesser extent. Working in this way, Sibutramine promotes the rapid development of a feeling of satiety, and, it becomes permanent. Significantly reduced food intake, 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 receptors of serotonin by platelets and can change their functions.

Reducing fat deposits with these medications is accompanied by an increase in the level of high-density lipoproteins ("good" cholesterol) in the blood serum on the background of a quantitative decrease in triacylglycerides, total cholesterol due to "bad" and uric acid.

Most drugs with Sibutramine are mono drugs. However, Reductil and Reduxin preparations are complex, containing in addition to the main active ingredient, microcrystalline cellulose is a natural and non-food-producing non-food product. He has the property of staying in the stomach, swelling under the influence of liquid, thus providing a feeling of satiety. In combination with Sibutramine complements its action. Microcrystalline cellulose is able to absorb not only water, but also putrefactive bacteria, cleans the intestines and prevents food poisoning.

[17], [18], [19], [20]

Pharmacokinetics

At oral reception there is a fast absorption of an active component from a gastrointestinal tract (about 80%). Getting into the liver, Sibutramine is metabolized to monodemethyl- and didbutylsibutramine. At the end of 72 minutes after using the drug, dosed at 0.015 g, the greatest concentration of the active ingredient is observed, and from three to four hours its metabolites are observed. Taking the capsule along with the food, the patient reduces the largest concentration of active metabolites by one 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 with good speed in the tissues of the body. The concentration of active substances in the serum achieves a state of equilibrium four days after the start of therapy and twice exceeds their serum concentration, determined after the first intake.

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

[21], [22]

Dosing and administration

The drug is taken once in the morning regardless of food intake. Treatment begins with a single capsule of 0.01 g, which is swallowed whole and washed down with water in sufficient quantity. If you lose less than two kilograms of weight 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 canceled as ineffective in this case, since higher dosages are not recommended.

Treatment stops in the following cases:

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

Treatment with this drug is probably no more than two years.

[31], [32], [33]

Use of the tablets with sibutramine for weight loss during pregnancy

The results of tests of Sibutramine in laboratory animals indicate that this active substance has no effect on fertility, however, the teratogenic effect of sibutramine on the fetus was observed in descendants of experimental rabbits. They have been found to have physical anomalies concerning the appearance, as well as the structure of the skeleton.

Medications containing Sibutramine are not allowed for pregnant and lactating women. Throughout the treatment course and one and a half months after the end of treatment with these drugs, female fertile age patients should use reliable contraceptives.

Contraindications

• age restrictions: is not assigned to minors or persons over 65;
• secondary obesity caused by diseases of the endocrine and central nervous system, other organic causes;
• eating disorders - bulimia, anorexia (in the presence or in the anamnesis);
• mental pathologies;
• generalized tick;
• circulatory disorders in the brain (in the presence or in the anamnesis);
• toxic goiter;
• myocardial ischemia (in the presence or in anamnesis), tachyarrhythmia, chronic decompensated cardiac muscle dysfunction;
• circulatory disturbance in peripheral vessels;
• uncontrolled hypertension (blood pressure above 145mm Hg);
• severe degrees of hepatic and / or renal dysfunction;
• adenoma of the prostate with delayed urination;
• 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.

With special care is assigned to patients who have a history of: hypertension, circulatory disorders, muscle spasms, coronary artery failure, epilepsy, hepatic and / or renal dysfunction, cholelithiasis, glaucoma, hemorrhages, tics, and - taking medications that disrupt blood clotting.

[23], [24], [25]

Side effects of the tablets with sibutramine for weight loss

Undesirable effects usually appeared in the first month of treatment, and if it continued, the frequency and intensity of these effects decreased with time. Negative actions, in the main, were reversible and passed with the withdrawal of the drug.

According to the results of post-marketing clinical testing, more often than in 10% of cases the following undesirable consequences of taking medicines with Sibutramine were observed: constipation, insomnia, dry mouth. More often than in 1% of cases, but less often than in 10% there were: tachyarrhythmia, hypertension, atrial fibrillation, vasodilation, nausea, exacerbation of hemorrhoids, headache, fainting, numbness of limbs, anxiety, excessive sweating, taste distortion.

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

• the risk of non-fatal heart attack, stroke, heart attack in patients taking Sibutramine increases by 16% compared with those who took placebo;
• reactions of sensitization from rashes to anaphylaxis;
• decrease in the number of platelets and violation of their functions, autoimmune damage to the walls of blood vessels;
• psychosis, mania, suicidal intentions and thoughts about it, depression;
• convulsions, short-term dips in memory, amnesia;
• when used simultaneously with drugs releasing serotonin, the serotonin syndrome developed;
• loss of vision clarity;
• upset stomach, vomiting, gastrointestinal bleeding;
• hair loss, rash, including hemorrhagic;
• acute interstitial nephritis, mesangiocapillary glomerulonephritis, difficulty urinating;
• disorders of ejaculation and menstrual cycle, anorgasmia, impotence, uterine bleeding.

In laboratory analyzes, hepatic enzymes were elevated.

With the withdrawal of the drug occasionally there was a headache and increased appetite.

[26], [27], [28], [29], [30]

Overdose

Taking doses of Sibutramine exceeding the recommended ones increases the likelihood of developing undesirable effects and increasing their severity. The consequences of an overdose have not been sufficiently studied and there is
No specific antidote.

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

It is necessary to monitor the patient's condition within 24 hours after receiving an overestimated amount of the drug. When the symptoms of side effects develop, appropriate treatment measures are carried out. The most characteristic consequences of an overdose, increased blood pressure and rapid heart rate, stop with ß-adrenoblockers.
The use of the "artificial kidney" apparatus in case of exceeding the dosage is inadvisable, as studies show that the metabolic products of Sibutramine are practically not eliminated by hemodialysis.

[34], [35]

Interactions with other drugs

Not applicable in combination:

• with other medicines that stop mental pathologies or are addressed to patients with alimentary obesity, which have a central effect;
• with drugs that inhibit the enzymatic activity of monoamine oxidase (between the medications containing sibutramine and monoamine oxidase inhibitors, there should be a time interval of at least two weeks);
• with drugs that stimulate the production of serotonin, and suppressing its reverse capture;
• with drugs inactivating microsomal enzymes of the liver;
• with drugs that can cause heart palpitations and increase blood pressure, as well as to excite the sympathetic nervous system.

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

It should also be noted that sibutramine and alcohol are not compatible.

[36], [37], [38], [39]

Storage conditions

The storage conditions of preparations based on Sibutramine do not differ from those for most drugs. Storage temperature should not exceed 25 ° C. The preparation does not need to be removed from the original packaging and left in places accessible to young children.

[40], [41]

Shelf life

Shelf life - up to three years

[42], [43], [44]

Reviews

Reviews of the drugs for losing weight with Sibutramine are often negative, quite a lot of complaints about side effects from the nervous system and the psyche that encourage many to stop treatment. And not everyone can get rid of the undesirable consequences of the reception. Judging by the reviews, these effects are not always reversible. Quite a lot of reviews say that people are very sorry for their decision to resort to this drug.

However, a lot of reviews are frankly positive, emphasizing the high effectiveness of this substance, and, in addition to dry mouth, no other side effects are called.

Doctors speak about the drug rather restrained, emphasizing the high efficiency of Sibutramine and the need to comply with the rules of its use, as well as the danger of self-treatment, since the drug causes serious side effects.