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.
- Diabetic ketoacidosis.
- 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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Pregnancy and lactation:
The category of action on the fetus by the FDA is 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 is prescribed at 15-30 mg; if necessary, the dose is incrementally increased to 45 mg per day.
Blood: decreased sugar levels – hypoglycemia, anemia (in 1-1.6% of cases), changes in bilirubin, aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase and gamma glutamyltransferase.
headache, sinusitis, myalgia, dental integrity disorder, pharyngitis, edema (4.8% of cases with monotherapy and 15.3% with combination with insulin.
Treatment is symptomatic.
ketoconazole inhibits the metabolism of pioglitazone.
With the simultaneous use of Actos pioglitazone and oral contraceptives, a reduction in the effectiveness of contraception is possible.
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.
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It is necessary to stop treatment if jaundice occurs.
In patients with an ovulatory cycle in the premenopausal period, the reception can cause ovulation and increase the risk of pregnancy – contraception is necessary.