Included in the formulation
АТХ:A.08.A.A Preparations for the treatment of centralized obesity
A.08.A.A.10 Sibutramine
Pharmacodynamics:Prodrug, pharmacological action due to metabolites that inhibit the reuptake of monoamines (noradrenaline and serotonin). By increasing the content of neurotransmitters in the synapses, it activates central serotonin 5-HT receptors and adrenoreceptors. It suppresses the appetite, which leads to a decrease in food intake. Increases thermogenesis. Due to activation of β3β-adrenoreceptors, metabolism in the brown adipose tissue is accelerated. Metabolites of sibutramine do not inhibit monoamine oxidase, do not affect the release of monoamines. Helps reduce total cholesterol, low-density lipoprotein, triglycerides and uric acid, and also increases the number of high-density lipoproteins in blood plasma.
Pharmacokinetics:After oral administration, up to 77% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 1.2 hours. It is subjected to primary passage through the liver with the formation of two active metabolites: mono- and didesmethylsibutramine, whose concentrations in the blood reach a maximum 3-4 hours after taking the drug.
The connection with plasma proteins is 97%, metabolites - 94%.
Metabolism in the liver: by the hydroxylation and conjugation, inactive metabolites are formed.
The half-life is 1.1 hours; monodesmethylsibutramine - 14 hours; Didesmethylsibutramine - 16 h. Elimination by the kidneys.
Indications:It is used to treat obesity.
IV.E65-E68.E66.0 Obesity caused by excessive intake of energy resources
Contraindications:Organic causes of obesity, anorexia nervosa, decompensated cardiovascular insufficiency, thyrotoxicosis, severe violations of liver and kidney function, elderly age over 65 years, individual intolerance.
Carefully:Arrhythmia, anorexia nervosa, uncontrolled arterial hypertension, cholelithiasis, neurologic disorders (convulsions).
Pregnancy and lactation:Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.
Dosing and Administration:Inside the morning with food or on an empty stomach 1 time / day. The initial dose is 10 mg. With poor tolerance, 5 mg.
The highest daily dose: 15 mg.
The highest single dose: 15 mg.
Side effects:Central and peripheral nervous system: insomnia, paresthesia, emotional lability.
Cardiovascular system: tachycardia.
Digestive system: loss of appetite, constipation, sometimes - exacerbation of hemorrhoids.
Allergic reactions.
Overdose:Increased side effects.
Treatment is symptomatic.
Interaction:Increase the concentration of the drug in the blood plasma inhibitors of the isoenzyme 3A4 cytochrome P450: ketonazole, ciclosporin, erythromycin.
The drugs with serotonergic activity increase the risk of developing serotonin syndrome.
Reduced glycemic control while applying the drug to the thiazide diuretics, calcium channel blockers slow, lithium preparations, glucocorticoids, isoniazid, sympathomimetics, nicotinic acid, phenytoin, phenothiazines, thyroid hormones.
With simultaneous application with furosemide, a dose reduction is necessary.
Special instructions:If there is no effect for 3 months - a decrease in body weight by 5% - the drug should be finished.