Sibutramine. Instructions for use. Price, analogues, reviews

According to statistics, people who have a large overweight to reduce it more often resort to pharmacology. In the top of the most popular drugs for weight loss include sibutramine. According to the manufacturer's instructions, on the impact of spectrum it is anorectic, its use reduces appetite and food cravings.

Shape and composition of the drug release

Sibutramine initial development took place in the field of psychology. Its intended use as an antidepressant. However, during testing of the drug was found excellent anorectic effect. Later it began to prescribe for the treatment of obesity varying degrees.

The medicine is available in capsule form for oral consumption. They comprise a light crystalline powder, hue of which may vary from white to cream color.

Active ingredient - sibutramine hydrochloride monohydrate. That it was the name of the drug. In contact with water the active component is dissolved, but the process takes place optimally at pH 5.2.

pharmacological properties

On a spectrum of pharmacological effects on the body Sibutramine refers to anorexigenic prodrug - a group of appetite regulators. To start the process of reuptake of neurotransmitters (serotonin and noradrenaline) it must disintegrate into active metabolites (amines first and second order).

As a result of the synergy of the noradrenergic and serotonergic systems raises the following pharmacological effects:

• thermogenesis growth (increased heat generation body is due to activation of beta-3-adrenoceptors);
• strengthening the feeling of satiety, thereby reducing the amount of food consumed;
• It affects the brown adipose tissue, the most difficult amenable to splitting.

Slimming result occurs due to the simultaneous effects of these three factors. loss of appetite does not lead to the fact that the body begins to defer reserves as fat, as happens in ordinary cases.

This algorithm reactions arises from the fact that a person needs to maintain a constant temperature, and to break down fats are the main source of heating.

Due to the fact that sibutramine increases the production of heat by the body, the need to replenish body fat receptors are not seeing. Thus, there is a gradual adaptation to the new fat options. The achieved result remains stable after withdrawal of the drug subject to DTX mode.

Studies of the drug showed its ability to block the reuptake of dopamine - the pleasure hormone, as well as change of platelet function. However, this effect is 3 times less than the effects on norepinephrine and serotonin.

The instructions on the use of Sibutramine stated that it:

• It does not influence the release monaminov;
• It does not affect the activity of the MAO inhibitors;
• It has an antihistamine effect;
• It does not cause a decrease in cholinergic activity;
• It does not interact with neurotransmitter receptors.

In view of the absence of contraindications to, and compliance with the dosage recommendations of the expert in the Russian Federation Sibutramine is approved for use.

Pharmacodynamics and Pharmacokinetics

In the process of using the drug in the patient's blood, a change of quality of the blood.

In particular there is:

• increasing the concentration of high density lipoproteins and decrease low density lipoprotein;
• decrease in the proportion of triglycerides;
• reducing the amount of total cholesterol and uric acid.

Studies have found that during treatment occurs insignificant increase in blood pressure (3 mm Hg) and heart rate (up to 7 beats per minute). What is the main reason for the ban of the drug for patients with heart problems.

Passing through the liver, a drug disintegrates into 2 components (mono- and didesmetilsibutramin) .Preparat characterized by relatively high bioavailability. Absorption of active ingredients is 77%, protein binding 97%.

The maximum concentration of sibutramine in the blood observed after 1-2 hours, and its decay products - 3-4 hours. However, the simultaneous use of food extend this period by an average of 30%.

It is metabolized in the liver cells. The half-life of sibutramine is about 1 hour. Its breakdown products - metabolites begin excreted within 14-16 hours. Moreover excretion of inactive metabolites occurs via the kidneys products as sibutramine and active substances through the bile.

Indications

Sibutramine, instructions for use which has a lot of contraindications, appointed by no means all patients to get rid of excess weight.

Indications for the application can be:

• alimentarnroe-structural obesity 2.3 and 4 degrees;

  

• overweight, complicated insulin dependent diabetes mellitus;
• the presence of large-scale body fat associated with impaired lipid metabolism (dyslipoproteinaemia).

All lighter cases, experts advise not to use sibutramine given the large number of contraindications and side effects.

Contraindications

Sibutramine, instructions for use which indicates the seriousness of its effects on the human body, it is dangerous to use the majority of patients.

The drug is contraindicated in the categories of people who are diagnosed:

• presence of individual intolerance medicament component;
• severe hepatic or renal dysfunction;
• ischemia;
• genetic heart defects;
• decompensated violation of myocardial function;
• systemic atherosclerosis;
• Tourette's syndrome;
• nature of mental illness (including uncontrolled absorption attacks or complete rejection of food);
• syndrome increased systolic or diastolic blood pressure;
• any form of pharmacological dependencies;
• obesity organic origin;
• violation of heart rhythm, including tachycardia;
• circulatory disorders of the brain;
• stroke;
• closure glaucoma;
• hyperthyroidism;
• chromaffinoma;
• benign prostatic hyperplasia;
• During pregnancy and breastfeeding;
• motor and verbal involuntary muscle contractions;
• convulsions and seizures.

In addition, there are strict restrictions on compatibility with other drugs acting on the central nervous system. Concurrent use is prohibited not only monoamine oxidase inhibitors, antipsychotics, sedatives, other pharmacological agents to reduce the weight and L-tryptophan.

Their reception is possible only 2 weeks after discontinuation of therapy with the use of sibutramine.

At what age can use the drug

Sibutramine, instructions for which the application has strict age limits, allowed to receive only people over 18 years (only in the absence of contraindications). The lower threshold is 65 years of age, when it is reached the use of the drug would cause serious harm to health.

Instructions for use, the dosage of the drug sibutramine

The current medical practice is that this drug is given only in the most extreme cases, when other methods of getting rid of excess fat does not give the desired effect. It has the right to appoint a person with medical training and experience weight correction.

After starting Sibutramine is necessary to maintain strict control of blood pressure and heart rate.

The minimum frequency of checks is at least 2 weeks during the first two months. Then, their number can be reduced to 1 times in 30 days. When fixing significant increases in pressure or arrhythmia detection frequency of inspections is increased. If performance data values ​​reach the limit boundaries (140/90 mm Hg), sibutramine stopped.

The medicine is taken once a day. The optimal time for this - the morning. Allowed the use of both fasting and after breakfast. The drug should enter the stomach in the whole shell, so it is prohibited to open or chew.

To facilitate swallowing the capsule washed down with water. The standard dose is 10 mg. In the case of weakly pronounced side effects, it is reduced by half.

In the absence of the desired effect within 1 month, the dosage is increased to 15 mg. Common to the majority of cases the duration of treatment is 1 year. However, in case of receiving high-dose, duration of use Sibutramine adjusted. Use of the drug in no way excludes the presence of physical activity.

Side effects

According to statistics from each of 9 100 patients faces the reverse side of the drug to reduce appetite. Possible adverse reactions occur with the cardiovascular, nervous, digestive and urinary system, and the musculoskeletal system, ENT-organs and skin.

The list of possible side effects:

• sleep disturbance;
• dizziness;
• pain in the neck, back or chest;
• migraine;
• pain in the abdomen or pelvis;
• prostration;
• fever (in the absence of infection);
• allergic reactions including rash, acne;
• generalized edema;
• thrush;
• palpitations and tachycardia;
• burning sensation on the skin;
• Blood pressure jump;
• appearance feelings phobia, depressive state;
• dry mouth and constant thirst;
• inflammation of the mucous membrane of the stomach;
• disruption of the normal process of defecation;
• nausea (often accompanied by vomiting);
• difficulty digestion with pains in the stomach;
• uncontrolled growth of food needs;
• thrombosis hemorrhoidal veins;
• a complete lack of appetite;
• increased sweating;
• change the perception of flavors;
• muscle pain;
• inflammation of the articular tissues;
• joint pain, having a volatile character;
• inflammation of the synovial linings of tendons;
• nervous excitement;
• constant craving for sleep;
• paresthesia;
• instability of emotional states;
• pain in the ear;
• cough;
• allergic rhinitis;
• inflammation of the sinuses;
• pharyngeal mucosa pathology, larynx and ligaments;
• urinary tract infections;
• painful menstruation;
• of bleeding, not associated with menstruation.

The presence of at least one of the above features is good reason to adjust the treatment of obesity. The doctor, based on the general condition of the patient, can reduce the dosage of Sibutramine or completely cancel it.

Overdose

Sibutramine, instructions for use which comprises a clear description regimen refers to the number medicines overdose of them can lead to very serious consequences, up to a lethal outcome.

Results in a disproportionate amplification of side effects. If for any reason the correct dose has been exceeded, you must go to the nearest medical facility for rehabilitation therapy.

She, along with reception of sorbents includes:

• symptomatically;
• administration of beta-blockers (for pressure increase and arrhythmias);
• monitor the functioning of the vital organs.

Self rehabilitation at home in case of an overdose of sibutramine is not allowed.

special instructions

Use of the drug is possible only under the supervision of a physician and must be supplemented by complex measures to reduce weight.

The number of required parallel action includes the transition to a proper diet, lifestyle changes, avoiding harmful habits, Light aerobic exercise classes. In some cases, the treatment of obesity requires a diet.

drug interactions

Concurrent use of Sibutramine with other drugs is possible only after the permission of the attending physician.

Among the features of drug interactions should be noted:

• antioxidants such as erythromycin, ketoconazole and tacrolimus Sibutramine slow excretion from the blood, thereby increasing its concentration;
• drugs, characterized by serotonergic effect (Luvox, Paroxetine, Efektin, Citalopram) may cause convulsions, diarrhea, fever and serotonin intoxication capable lead to death;
• ephedrine and pseudoephedrine agent in combination with sibutramine increases the pressure indicators and increase the heart rate;
• means macrolide antibiotic accelerate absorption Sibutramine.

Simultaneous use of alcohol drug does not cause changes in drug effects on the body. However, this practice is not conducive to weight loss.

analogs

In spite of the many side effects, sibutramine is one of the top drugs for weight loss. In trade there are a number of drugs with the same active substance.

Examples of analogues:

• Slim;
• Reduxine (manufactured in standard shapes 3, Me and Light);
• Lindaksa;
• Goldline (classic format and the "Plus");
• Meridia.

Sliema Lindaksa and Meridia are the products of foreign pharmaceutical firms. In view of the policy pursued abroad in relation to Sibutramine, they have ceased to be issued.

For reference sibutramine hydrochloride monohydrate is banned in the United States, European Union, China, Australia, Canada, Mexico, India, New Zealand and Hong Kong. In Russia, it is still in the number of permits, but is realized only by prescription.

Terms, conditions of sale and storage

Due to the nature of the drug effects on man, his purchase in pharmacies is possible only with a prescription. It should be printed on a special form and have all the necessary stamps and signatures.

Sibutramine shelf life is 2 years from date of manufacture. It is always indicated on the outer packaging and blister. Storage Recommendations similar to any medicines - a dark, cool place where children can not reach. Ideal conditions for the placement of the drug - the top shelf of the refrigerator.

Price in drugstores of Moscow, St. Petersburg, regions

The cost of the drug depends on the package volume. In dosage 20 mg of sibutramine it is produced by 50 or 64 pills in a single carton. A 15 milligram version sold at 30 or 100 pieces. in a plastic container or in a mini format of 10 capsules. The greater the dosage and package size, the more expensive the cost acquisition.

The average value of 50 capsules of 20 mg of medicament in the capital is 2 990 rubles. In St. Petersburg, even in the online pharmacies find it quite difficult. Acquisition of Sibutramine (the same 50 capsules of 20 mg) in St. Petersburg cost about twice as much as 4820 rubles.

The average price range for the drug is presented below:

The cheapest you can buy the drug in Moscow. Residents of the Far East, it will cost half as expensive, which is understandable transport costs.

Despite the fact that the internet is among sellers of the drug, there is considerable variation in prices, do you need to buy only in trusted locations. This will minimize the probability of being a fake.

Despite the apparent effectiveness of Sibutramine in the fight against obesity, it is the use of the instructions for use without a doctor's prescription may lead to serious health problems. It is not in vain in the leading countries of the drug was banned back in the 2000s, when they began to enter the patient complained of pain in the heart, pressure surges and nervous disorders.

Registration of the article: Mila Friedan

Video of sibutramine

Review of sibutramine: