pharmachologic effect
Oral hypoglycemic drug of the thiazolidinedione series. The action of pioglitazone depends on the presence of insulin. It is a highly selective peroxisome proliferator-activated receptor agonist (PPARγ). PPARγ receptors are found in adipose, muscle, and liver. Activation of nuclear PPARγ receptors modulates the transcription of a number of insulin-responsive genes involved in glucose control and lipid metabolism. Aktos® reduces insulin resistance in peripheral tissues and in the liver, as a result of which there is an increase in the consumption of insulin-dependent glucose and a decrease in the release of glucose from the liver. Unlike sulfonylurea drugs, pioglitazone does not stimulate insulin secretion from pancreatic β-cells.
In type 2 diabetes mellitus, a decrease in insulin resistance under the action of Actos® causes a decrease in blood glucose concentration, a decrease in plasma insulin levels and a decrease in HbA1c (glycated hemoglobin). In combination with sulfonylurea drugs, metformin or insulin, the drug improves glycemic control.
In type 2 diabetes mellitus with impaired lipid metabolism during treatment with the drug, a decrease in triglyceride levels and an increase in HDL levels are noted. At the same time, the level of LDL and total cholesterol in such patients does not change.Dosing regimen
The dose is set individually.
Aktos® is administered orally 1 time / day, regardless of food intake.
In monotherapy, for patients in whom diabetes mellitus compensation is not achieved with the help of diet therapy and exercise, Aktos® is prescribed at a dose of 15 mg or 30 mg 1 time / day. If necessary, the dose can be gradually increased to 45 mg / day.
With monotherapy, the maximum dose of Actos® is 45 mg 1 time / day.
If monotherapy fails, combination therapy should be considered.
In combination therapy with sulfonylurea derivatives, Aktos® is prescribed at a dose of 15 mg or 30 mg 1 time / day. At the beginning of treatment with Aktos®, the dose of the sulfonylurea derivative can be left unchanged, with the development of hypoglycemia, the dose of the latter must be reduced.
In combination with metformin, Actos® is prescribed at a dose of 15 mg or 30 mg 1 time / day. At the beginning of treatment with Aktos®, the dose of metformin can be left unchanged. The risk of developing hypoglycemia with this combination is negligible, so the need for dose adjustment of metformin is unlikely.
In combination with insulin Actos® is prescribed at a dose of 15 mg or 30 mg 1 time / day. At the beginning of treatment with Actos®, the dose of insulin can be left unchanged. With the development of hypoglycemia and a decrease in plasma glucose concentration to a level of less than 100 mg / dL, the dose of insulin can be reduced by 10-25%. Further adjustment of the dose of insulin should be carried out individually, taking into account the level of glycemia.
In combination therapy, the maximum dose of Actos® is 30 mg / day.
In patients with renal insufficiency, dose adjustment of Aktos® is not required.
There are no data on the use of Aktos® in combination with other thiazolidinedione preparations.
Side effect
From the endocrine system: hypoglycemia (2% – in combination with a sulfonylurea drug, 8-15% – in combination with insulin).
On the part of the hematopoietic system: 1-1.6% – anemia (with monotherapy and combination therapy); a decrease in hemoglobin (2-4%) and hematocrit, which are observed mainly 4-12 weeks after the start of treatment and remain relatively constant (not associated with any clinically significant hematological effects and most often due to an increase in plasma volume).
From the side of metabolism: edema (4.8% – with monotherapy, 15.3% – with combination with insulin); 5% – increase in body weight; rarely – increased activity of CPK.
On the part of the digestive system: about 0.25% – an increase in ALT activity > 3 times from VGN; rarely – hepatitis.
On the part of the organ of vision: very rarely – the development or progression of diabetic macular edema, accompanied by a decrease in visual acuity. A direct relationship between the development of macular edema and the intake of pioglitazone has not been established. Physicians should consider the possibility of developing macular edema if patients complain of decreased visual acuity.
From the side of the cardiovascular system: in US placebo-controlled studies, the incidence of serious cardiovascular side effects associated with an increase in BCC did not differ in patients who received Actos® and Actos® alone in combination with a sulfonylurea, metformin or placebo. In a clinical study, concomitant use of Actos® and insulin in a small number of patients with a history of heart disease has shown cases of congestive heart failure. Patients with heart failure III and IV functional classes according to the NYHA classification did not participate in clinical trials on the use of the drug, therefore Aktos® is contraindicated for this group of patients.
According to post-marketing data, cases of congestive heart failure have been reported in patients with the use of Actos®, regardless of the indication of pre-existing heart disease.
Contraindications for use
diabetes mellitus type 1;
diabetic ketoacidosis;
severe heart failure III-IV functional class according to the NYHA classification;
pregnancy;
lactation (breastfeeding);
age up to 18 years;
hypersensitivity to the components of the drug.
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