Oral anti-diabetic drugs

Description

• Insulin resistance (IR) is evident in skeletal muscle, liver and adipose tissue, the major target tissues of insulin action. The development of IR in peripheral tissues is exacerbated by chronically elevated free fatty acids (FFA). Initially hyperinsulinemia compensates for IR thus preserving normal glucose tolerance. However, over time, hepatic and beta cell compensation deteriorates, culminating in fasting hyperglycaemia. The elevated FFAs lead to increased triglyceride levels and may thus worsen the CAD status. Pioglitazone, a member of the thiazolidinedione class of antidiabetic agents, improves glycaemic control by improving insulin sensitivity. It is a highly selective and potent agonist for the peroxisome proliferator-activated receptor-gamma (PPAR-γ). Activation of PPAR-γ nuclear receptors regulates the transcription of insulin-responsive genes involved in the control of glucose and lipid metabolism. Pioglitazone stimulates the production of GLUT-4 and it increases the glucose uptake in adipose and muscle cells. In addition, PPAR-γ responsive genes also participate in the regulation of fatty acid metabolism and thus have shown to confer beneficial effects on cardiovascular functions and lipid parameters.

Indications

• Pioglitazone hydrochloride (POZITIV^®) is indicated as monotherapy in patients not controlled by diet and exercise alone, to decrease blood glucose levels in patients with Type 2 Diabetes. POZITIV^® is indicated for use in combination with a sulfonylurea or metformin who, diet and exercise plus a single anti-diabetic agent does not result in adequate glycaemic control.

Dosage

• Dosage should be individualized on the basis of both effectiveness and tolerability while not exceeding the maximum recommended daily dose.
• It should be given once daily with meals and started at a low dose. In case of inadequate response, the dose can be increased to a maximum of 45 mg once daily.