Included in the formulation
АТХ:A.10.B.G.03 Pioglitazone
Pharmacodynamics:Selective binding to peroxisome proliferator-activated receptor γ (PPAR-γ) receptor, 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.
Pharmacokinetics:Absorption is fast. 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).
Indications: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 by one of the above means.
IV.E10-E14.E11 Non-insulin-dependent diabetes mellitus
Contraindications:Diabetes mellitus type 1.Diabetic ketoacidosis.
Severe heart failure.
Liver disease in the acute stage.
Level alanine aminotransferase, exceeding the norm by 2.5 times.
Pregnancy and breastfeeding.
Carefully:Edema syndrome.Anemia.
Age under 18 years (safety and efficacy in this age group are not defined).
Pregnancy and lactation:The action category for the fetus is FDA - C. The drug is contraindicated in pregnancy and during breastfeeding.
Dosing and Administration:The drug is prescribed 1 time per day inside (regardless of food intake). With monotherapy pioglitazone appoint 15-30 mg each; if necessary, the dose is incrementally increased to 45 mg per day.
Side effects:Blood: decrease in sugar levels - hypoglycemia, anemia (in 1-1.6% of cases), changes in bilirubin level, aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase and gamma-glutamyltransferase. Others: headache, sinusitis, myalgia, dental integrity disorder, pharyngitis, edema (in 4.8% of cases with monotherapy and in 15.3% with combination with insulin.
Overdose:Treatment is symptomatic.
Interaction:Ketoconazole inhibits the metabolism of pioglitazone. With the simultaneous use of pioglitazone and oral contraceptives, a reduction in the effectiveness of contraception is possible.
Special instructions:The development of hypoglycemia in combination therapy necessitates a reduction in the dose of concomitant sulfonamides or insulin. Against the background of renal failure, dose adjustment is not required. It is necessary to stop treatment if jaundice occurs.
Patients with anovulatory cycle in the pre-menopausal period may cause ovulation and increase the riskpregnancy - contraception is necessary.