Rosiglitazone

Mechanism :

Agonist for peroxisome proliferator-activated- receptor-gamma. Helps decrease blood glucose levels by improving the response to insulin without actual increase in levels of insulin. It enhances tissue sensitivity to insulin instead of simulating secration of insulin.It lowers glucose by improving target cell response to insulin without involving pancreatic cell, activates production of gene products that help in glucose and lipid metabolism.

Indication :

• Not FDA approved for paediatric use but may be used for type 2 DM in addition to metformin, lifestyle changes, diet.

Contraindications :

Type 1 Diabetes Mellitus

NYHA class III / IV failure

Stable ischemic heart disease

Active liver disease or transaminase level more than 2.5 times the upper limit of normal

osteoperosis

Dosing :

Adverse Effect :

Hypoglycaemia – especially in combination with other hypoglycemic drugs

Edema- if dose-related edema occurs use catiously

Cardiovascular – Heart failure ( higher incidence in patients taking insulin), High blood pressure, Coronary artery disease

Hepatic failure, increased liver enzymes, hepatitis

Diarrhoea, Anaemia, blurred vision, macular edema

Increased risk of fractures in females

Can exacerbate heart failure

Interaction :

Hypoglycemic agents- May worsen the hypoglycemia

Beta- Blockers- Enhance the hypoglycemic effect of the drug

Cholestyramine- Decreases the concentration of rosiglitazone, Need to administer rosiglitazone 2 hours prior to cholestyramine

Hepatic Dose :

Don’t initiate if active liver disease or transaminase level more than 2.5 times the upper limit of normal

Pregnanacy :

Not indicated during pregnancy