Composition, structure and packing
Tablets from white to almost white, round, biconvex, one side of which is squeezed out "15" on the other - "ACTOS".
1 tab. pioglitazone (as hydrochloride) 15 mg.
Inactive ingredients: lactose monohydrate, hydroxypropylcellulose, carboxymethylcellulose calcium, magnesium stearate.
Tablets from white to almost white, round, biconvex, one side of which is squeezed out "30" on the other - "ACTOS".
1 tab. pioglitazone (as hydrochloride) 30 mg.
Inactive ingredients: lactose monohydrate, hydroxypropylcellulose, carboxymethylcellulose calcium, magnesium stearate.
Tablets from white to almost white, round, biconvex, one side of which is squeezed out "45" on the other - "ACTOS".
1 tab. pioglitazone (as hydrochloride) 45 mg.
Inactive ingredients: lactose monohydrate, hydroxypropylcellulose, carboxymethylcellulose calcium, magnesium stearate.
Pharmacotherapeutic group: oral hypoglycemic agents.
Pharmacological action
Oral hypoglycemic drug, a derivative of thiazolidinedione series. Is a potent and highly selective agonist at gamma-receptors, peroxisome proliferator-activated (PPARγ). PPARγ-receptors are found in fat, muscle and liver. Activation of PPARγ nuclear receptors modulates the transcription of several genes that are sensitive to insulin, involved in controlling glucose and lipid metabolism. Actos reduces insulin resistance in peripheral tissues and the liver, as a result of that, the rate of insulin-glucose and reduced glucose output from the liver. Unlike sulfonylureas, pioglitazone does not stimulate insulin secretion from β-cells of the pancreas.
In diabetes type 2 insulin resistance by reducing the drug Actos causes a decrease in blood glucose levels, lower levels of plasma insulin and hemoglobin A1c (glycosylated hemoglobin, HbA1c). In a monotherapy and in combination with sulfonylurea, metformin or insulin drug improves control of blood sugar levels.
In diabetes type 2 with lipid disorders during treatment with the drug there is a decrease in triglycerides and increase HDL. The level of LDL and total cholesterol in these patients does not change.
Using the drug Actos in patients with type 2 diabetes performed echocardiographic examination revealed a marked increase in the average left ventricular mass index, or a noticeable decrease in the average cardiac index.
Pharmacokinetics
Absorption
After oral administration, pioglitazone is found in fasting plasma after 30 minutes. Cmax in plasma is reached after 2 hours when eating there was a slight increase in the time to Cmax of 3-4 hours, but the extent of absorption is not changed.
Distribution
After a single dose of pioglitazone apparent Vd averaged 0.63 ± 0.41 (mean ± SD-standard deviation) l / kg. Pioglitazone is largely bound to serum proteins in human blood (> 99%), mainly albumin and to a lesser extent - with other serum proteins. The metabolites of pioglitazone M-III and M-IV also significantly associated with serum albumin (> 98%). Both healthy volunteers and in patients with insulin-dependent diabetes (type II) equilibrium concentration of pioglitazone is about 30-50% of peak concentrations of total pioglitazone serum and 20% -25% of the AUC.
Metabolism
Pioglitazone is extensively metabolized in the liver by hydroxylation and oxidation reactions with the formation of metabolites. Metabolites M-II, M-IV (hydroxide derivatives of pioglitazone) and M-III (keto derivative of pioglitazone) exhibit pharmacological activity in models of type 2 diabetes in animals. Pioglitazone metabolism in the liver occurs with the participation of the major cytochrome P450 (CYP2C8 and CYP3A4). In the in vitro study, pioglitazone did not inhibit the activity of P450. In vivo studies were carried out.
Breeding
T1 / 2 of unchanged pioglitazone is 3-7 hours, total pioglitazone (pioglitazone and active metabolites) - 16-24 hours clearance of pioglitazone is 5-7 l / h After oral administration, about 15-30% of the dose of pioglitazone is found in urine.
The kidneys remove the small quantity of pioglitazone, mainly in the form of metabolites and their conjugates. It is believed that when administered most of the dose is excreted in the bile in unchanged form and in the form of metabolites and excreted in the feces. Concentration of pioglitazone and active metabolites in serum remained at a high level at 24 h after a single daily dose.
Tablets from white to almost white, round, biconvex, one side of which is squeezed out "15" on the other - "ACTOS".
1 tab. pioglitazone (as hydrochloride) 15 mg.
Inactive ingredients: lactose monohydrate, hydroxypropylcellulose, carboxymethylcellulose calcium, magnesium stearate.
Tablets from white to almost white, round, biconvex, one side of which is squeezed out "30" on the other - "ACTOS".
1 tab. pioglitazone (as hydrochloride) 30 mg.
Inactive ingredients: lactose monohydrate, hydroxypropylcellulose, carboxymethylcellulose calcium, magnesium stearate.
Tablets from white to almost white, round, biconvex, one side of which is squeezed out "45" on the other - "ACTOS".
1 tab. pioglitazone (as hydrochloride) 45 mg.
Inactive ingredients: lactose monohydrate, hydroxypropylcellulose, carboxymethylcellulose calcium, magnesium stearate.
Pharmacotherapeutic group: oral hypoglycemic agents.
Pharmacological action
Oral hypoglycemic drug, a derivative of thiazolidinedione series. Is a potent and highly selective agonist at gamma-receptors, peroxisome proliferator-activated (PPARγ). PPARγ-receptors are found in fat, muscle and liver. Activation of PPARγ nuclear receptors modulates the transcription of several genes that are sensitive to insulin, involved in controlling glucose and lipid metabolism. Actos reduces insulin resistance in peripheral tissues and the liver, as a result of that, the rate of insulin-glucose and reduced glucose output from the liver. Unlike sulfonylureas, pioglitazone does not stimulate insulin secretion from β-cells of the pancreas.
In diabetes type 2 insulin resistance by reducing the drug Actos causes a decrease in blood glucose levels, lower levels of plasma insulin and hemoglobin A1c (glycosylated hemoglobin, HbA1c). In a monotherapy and in combination with sulfonylurea, metformin or insulin drug improves control of blood sugar levels.
In diabetes type 2 with lipid disorders during treatment with the drug there is a decrease in triglycerides and increase HDL. The level of LDL and total cholesterol in these patients does not change.
Using the drug Actos in patients with type 2 diabetes performed echocardiographic examination revealed a marked increase in the average left ventricular mass index, or a noticeable decrease in the average cardiac index.
Pharmacokinetics
Absorption
After oral administration, pioglitazone is found in fasting plasma after 30 minutes. Cmax in plasma is reached after 2 hours when eating there was a slight increase in the time to Cmax of 3-4 hours, but the extent of absorption is not changed.
Distribution
After a single dose of pioglitazone apparent Vd averaged 0.63 ± 0.41 (mean ± SD-standard deviation) l / kg. Pioglitazone is largely bound to serum proteins in human blood (> 99%), mainly albumin and to a lesser extent - with other serum proteins. The metabolites of pioglitazone M-III and M-IV also significantly associated with serum albumin (> 98%). Both healthy volunteers and in patients with insulin-dependent diabetes (type II) equilibrium concentration of pioglitazone is about 30-50% of peak concentrations of total pioglitazone serum and 20% -25% of the AUC.
Metabolism
Pioglitazone is extensively metabolized in the liver by hydroxylation and oxidation reactions with the formation of metabolites. Metabolites M-II, M-IV (hydroxide derivatives of pioglitazone) and M-III (keto derivative of pioglitazone) exhibit pharmacological activity in models of type 2 diabetes in animals. Pioglitazone metabolism in the liver occurs with the participation of the major cytochrome P450 (CYP2C8 and CYP3A4). In the in vitro study, pioglitazone did not inhibit the activity of P450. In vivo studies were carried out.
Breeding
T1 / 2 of unchanged pioglitazone is 3-7 hours, total pioglitazone (pioglitazone and active metabolites) - 16-24 hours clearance of pioglitazone is 5-7 l / h After oral administration, about 15-30% of the dose of pioglitazone is found in urine.
The kidneys remove the small quantity of pioglitazone, mainly in the form of metabolites and their conjugates. It is believed that when administered most of the dose is excreted in the bile in unchanged form and in the form of metabolites and excreted in the feces. Concentration of pioglitazone and active metabolites in serum remained at a high level at 24 h after a single daily dose.
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