Increases insulin sensitivity in liver, muscle, and adipose tissue.
Initiation in patients with established New York Heart Association (NYHA) class III or IV heart failure.
Use Cautiously in:
CV: angina, chest pain .
Endo: hypoglycemia , hyperglycemia.
CYP2C8 inducers (eg, rifampin)
May decrease rosiglitazone AUC; changes in diabetes treatment may be needed when the CYP2C8 inducer is started or stopped. Clinical and laboratory monitoring is warranted. Adjust the rosiglitazone dose as needed.
CYP2C8 inhibitors (eg, azole antifungal agents [eg, ketoconazole], fluvoxamine, gemfibrozil, trimethoprim)
May elevate rosiglitazone plasma levels, increasing the pharmacologic effects and adverse reactions. Clinical and laboratory monitoring is warranted. Adjust the rosiglitazone dose as needed.
Risk of edema may be increased, even after several months of therapy. Increased risk of CHF and MI. Coadministration is not recommended.
Repeat doses of rosiglitazone may decrease glyburide AUC and Cmax . Clinical and laboratory monitoring is warranted. Adjust the glyburide dose as needed.
Rosiglitazone may reduce nevirapine plasma concentrations. Clinical and laboratory monitoring is warranted. Adjust the nevirapine dose as needed.
Therapeutic Classification: antidiabetics
Pharmacologic Classification: meglitinides
Absorption: Well absorbed (56%) following oral administration.
Protein Binding: >98%.
Metabolism/Excretion: Mostly metabolized by the liver; metabolites are excreted primarily in feces.
Half-life: 1 hr.
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