Actos is an oral antihyperglycemic medication the main component of which is pioglitazone. Additive substances are:
- lactose monohydrate;
- hydroxypropyl cellulose;
- carbossimetilcellulose calcium;
- calcium stearate.
Pharmacology
It is an oral hypoglycemic drug of thiazolidinediones raw. Pioglitazone action depends on insulin presence. It is a highly selective agonist of peroxisome proliferator-activated receptor (PPARγ). PPARγ-receptors are found in fat, muscle and liver tissues.
Activation of PPARγ nuclear receptors modulates several genes transcription that is sensitive to insulin involved in the control of glucose and lipid metabolism. Actos from Canadian Pharmacy reduces insulin resistance in peripheral and liver tissues, resulting in an increase of insulin-dependent glucose consumption and reduced glucose output from the liver. Unlike sulfonylureas, pioglitazone did not stimulate insulin secretion of pancreatic β-cells.
At diabetes 2 type reduction of insulin resistance under drug’s influence Actos causes a decrease in blood glucose concentration, reduces plasma insulin levels and index of HbA1c (glycated hemoglobin). In combination with a sulfonylurea, metformin or insulin drug improves glycemic control.
In diabetes 2 type with lipid disorders on treatment background, there is a decrease in triglyceride levels and increasing high-density lipoprotein levels. In such a case level of low-density lipoprotein and total cholesterol levels in these patients are not changed.
Therapeutic Indications
Diabetes mellitus 2 type:
- For monotherapy or in combined therapy with sulfonylurea, metformin, or insulin;
- As an adjunct to diet therapy and physical exercise.
Contraindications
- type 1 diabetes;
- diabetic ketoacidosis;
- severe heart failure;
- pregnancy;
- during lactation period;
- If you are under 18;
- Hypersensitivity to drug components.
The drug should be used attentively by patients with edema syndrome, anemia, liver failure (increased activity of liver enzymes in the 1-2.4 times of ULN (upper limit of normal)), with mild to moderate heart failure.
Interactions
- Actos in combination with oral contraceptives may decrease the effectiveness of birth control pills.
- There are no changes in pharmacokinetics and pharmacodynamics while using Actos with glipizide, digoxin, indirect anticoagulants, metformin.
- In vitro ketoconazole inhibits pioglitazone metabolism.
- Data on the pharmacokinetic interaction when Actos is taken with erythromycin, astemizole, calcium channel blockers, cisapride, corticosteroids, cyclosporine, lipid-lowering drugs (statins), tacrolimus, triazolam, trimetrexate, and itraconazole is absent.