Brands, Medical Use, Clinical Data
- Hypoglycemic Agents
Brands / Synonyms
Actoplus MET; Actoplus MET XR; Actos; Actost; Duetact; Pioglitazona [Inn-Spanish]; Pioglitazone Hydrochloride; Pioglitazone [Ban:Inn]; Pioglitazonum [Inn-Latin]
Treatment of Type II diabetes mellitus
Pioglitazone, a member of the drug group known as the thiazolidinediones or "insulin sensitizers", is not chemically or functionally related to the alpha-glucosidase inhibitors, the biguanides, or the sulfonylureas. Pioglitazone targets insulin resistance and, hence, is used alone or in combination with insulin, metformin, or asulfonylurea as an antidiabetic agent.
Mechanism of Action
Pioglitazone acts as an agonist at peroxisome proliferator activated receptors (PPAR) in target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR-gamma receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In this way, pioglitazone enhances tissue sensitivity to insulin.
Following oral administration, in the fasting state, pioglitazone is first measurable in serum within 30 minutes, with peak concentrations observed within 2 hours. Food slightly delays the time to peak serum concentration to 3 to 4 hours, but does not alter the extent of absorption.
Hypogycemia; LD50=mg/kg (orally in rat)
Biotrnasformation / Drug Metabolism
ACTOS is contraindicated in patients with known hypersensitivity to this product or any of its
In vivo drug-drug interaction studies have suggested that pioglitazone may be a weak inducer of CYP
450 isoform 3A4 substrate.