Included in the formulation
АТХ:A.10.B.D Combination of biguanides and sulfonylurea derivatives
A.10.B.D.03 Metformin and rosiglitazone
Pharmacodynamics: 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.
Rosiglitazone
A drug from the group of thiazolidinediones enhances the sensitivity of target tissues to insulin. Slows the development of systolic arterial hypertension and renal dysfunction, reduces the concentration of free fatty acids. Prevents the development of hyperglycemia.
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.
Rosiglitazone
After oral administration, fasted to 99% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 1 hour. The connection with plasma proteins is 99.8%.
The therapeutic effect develops after the onset of admission. Metabolism in the liver.
The elimination half-life is 3-4 hours. Elimination by the kidneys is the form of metabolites, about 25% is excreted through the intestine.
Indications:It is used for the treatment of non-insulin dependent diabetes mellitus II type.
IV.E10-E14.E11 Non-insulin-dependent diabetes mellitus
Contraindications:Diabetes I type - insulin-dependent, coma, ketoacidosis, individual intolerance.
Carefully:Concomitant diseases of the endocrine system affecting carbohydrate metabolism: adenohypophysis and adrenocortical insufficiency, dysfunction of the thyroid gland.
Pregnancy and lactation:Recommendations for FDA - Category B. Penetrates into breast milk, apply with caution.
Dosing and Administration:Inside, regardless of the time of meal.The initial dose of metformin / rosiglitazone is 1000/4 mg, increases gradually, with a step of 500/4 mg / day to a maximum of 2000/8 mg.
The highest daily dose: metformin / rosiglitazone: 2000/8 mg.
The highest single dose: metformin / rosiglitazone: 2000/8 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:Development of hypoglycemia.
Treatment: sugar inside, with loss of consciousness - intravenous injection of 40% dextrose solution.
Interaction:Increase the concentration of the drug in the blood plasma inhibitors of the isoenzyme 3A4 cytochrome P450: 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 in the blood plasma and increases the risk of hypoglycemia.
Special instructions:During pregnancy and lactation, the drug is canceled, the treatment of diabetes continues with injections of insulin