Metformin + [Sibutramine + Microcrystalline Cellulose] (Metformin + [Sibutramine + Microcrystalline cellulose])

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Hypoglycemic synthetic and other agents

Appetite regulators

Included in the formulation
  • Reduxin® Met
    capsulespills inwards 
    Promomed Rus, Open Company     Russia
    • АТХ:

    A.08.A   Preparations for the treatment of obesity (excluding dietary products)

    Pharmacodynamics:

    Combined anti-glycemic agent.

    Metformin

    Reduces the absorption of glucose from the intestine and enhances its peripheral utilization, increasing the sensitivity of tissues to insulin, inhibits gluconeogenesis in the liver. Reduces the level of low density lipoproteins and triglycerides in blood plasma. Does not cause hypoglycemic reactions, does not affect the secretion of insulin β-cells of the pancreas. By suppressing the inhibitor of the tissue plasminogen activator, it has a fibrinolytic effect. Stabilizes or reduces body weight.

    Sibutramine

    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, but increases the number of high-density lipoproteins in blood plasma.

    Microcrystalline cellulose

    Enterosorbent, has a nonspecific detoxification effect. Binds and removes from the body exo and endotoxins, allergens, microorganisms and products of their vital activity, xenobiotics.

    Pharmacokinetics:Metformin
    After oral administration, up to 50-60% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 2.5 hours. Does not bind to plasma proteins. It accumulates in muscle tissue, salivary glands, kidneys and liver. The half-life is 6 hours. Elimination by the kidneys is unchanged.

    Sibutramine

    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- anddidezmethylsibutramine, the concentration of which in the blood reaches 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 of sibutramine is 1.1 hours; monodesmethylsibutramine - 14 hours; Didesmethylsibutramine - 16 h. Elimination by the kidneys.

    Microcrystalline cellulose

    Does not have a systemic effect.

    Indications:

    Diabetes mellitus type 2 - insulin-independent, alimentary obesity.

    ICD-10

    IV.E65-E68.E66   Obesity

    IV.E70-E90.E78   Disorders of lipoprotein metabolism and other lipidemia

    IV.E10-E14.E11   Non-insulin-dependent diabetes mellitus

    Contraindications:

    Organic causes of obesity, anorexia nervosa, decompensated cardiovascular insufficiency, thyrotoxicosis, severe violations of the liver and kidneys, elderly age over 65 years, individual intolerance of the drug components.

    Carefully:

    Arrhythmia, cholelithiasis, neurologic disorders (convulsions).

    Pregnancy and lactation:

    Recommendations for FDA - Category B. Penetrates into breast milk, apply with caution.

    Dosing and Administration:

    Inside since morning during meal or on an empty stomach 1 time / sut. 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.

    The cardiovascular system: tachycardia.

    Digestive system: loss of appetite, constipation, sometimes - exacerbation of hemorrhoids.

    Muscular system: symptoms of lactic acidosis - cramps of the calf muscles.

    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 P 450: ketonazole, ciclosporin, erythromycin.

    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.

    The use of alcohol (especially on an empty stomach) during treatment increases the concentration of lactic acid inplasma and increased risk of hypoglycemia.

    Special instructions:

    If there is no effect for 3 months - a decrease in body weight by 5%, the drug should be finished.

    Instructions
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