The two-year time period can be reduced by using an elimination procedure. It's used as monotherapy, in patients uncontrolled by diet and exercise, to reduce insulin resistance and lower elevated blood glucose. It's also indicated for use in combination with metformin in patients who are not adequately controlled with diet, exercise, and rosiglitazone or metformin. Insulin resistance is a primary feature of type 2 diabetes. Rosiglitazone works primarily by increasing sensitivity to insulin in muscle and adipose tissue, and by inhibiting hepatic gluconeogenesis.
Glycemic control is improved, while circulating insulin levels are reduced.
Rosiglitazone is well absorbed, with peak plasma concentrations occurring about one hour following oral administration. The drug is extensively metabolized, primarily by the CYP2C8 isoenzyme, to metabolites which have insignificant therapeutic activity. Rosiglitazone may be taken with or without food. Dosage adjustments are not required in the elderly or in patients with renal impairment. Anemia has also been reported, particularly when rosiglitazone is combined with metformin.