Actos Pioglitazone (Pioglitazonum)
Selective binding to peroxisome proliferator-activated receptor γ (PPAR-γ), modulation of transcription of insulin-sensitive genes controlling glucose and lipid metabolism. Reduces insulin resistance of peripheral tissues and liver. Effective only in the presence of insulin! Unlike sulfonylureas, it does not release it. Increases insulin-dependent glucose utilization (increases the sensitivity of tissues to insulin) and reduces the production of the last liver.
Absorption is rapid. Eating somewhat slows the attainment of maximum concentration, but does not reduce absorption. The connection with plasma proteins is 99.8% (serum albumin). Biotransformation in the liver to several active metabolites (metabolites II and IV – hydroxy derivatives, metabolite III – keto derivative). Metabolised by CYP2C8 and CYP3A4 in the liver and CYP1A1 in the intestine. The half-life is 3-7 hours. Elimination mainly with feces, kidneys – 15-30% (in the form of metabolites and conjugates).
Diabetes mellitus type 2, as a monotherapy or in combination with derivatives of sulfonamides, metformin or insulin in the absence of the effect of diet therapy, exercise and monotherapy with one of the above.
Contraindications: Type 1 diabetes mellitus.
Severe heart failure.
Liver disease in the acute stage.
The level of alanine aminotransferase, exceeding the norm by 2.5 times.
Pregnancy and breastfeeding.
With caution: Edema syndrome.
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