Class: Thiazolidinedione Antidiabetic
Dosage Forms. Tablet: 2 mg, 4 mg, 8 mg
Common FDA Label Indication, Dosing, and Titration.
1. Diabetes mellitus: 4 mg po daily or 2 mg po bid; may titrate to max of 8 mg daily as monotherapy or in combination with a sulfonylurea, metformin, or insulin
1. Polycystic ovary syndrome: 8 mg po daily
MOA. Rosiglitazone is a thiazolidinedione antihyperglycemic and a potent peroxisome proliferator-activated receptor-gamma (PPAR [γ]) agonist used to improve insulin sensitivity in patients with Type II diabetes. Insulin-dependent glucose disposal in skeletal muscle is improved and hepatic glucose production is decreased; both actions contribute to rosiglitazone’s glucose-lowering effects.
Drug Characteristics: Rosiglitazone
Medication Safety Issues: Rosiglitazone
Drug Interactions: Rosiglitazone
Adverse Reactions: Rosiglitazone
Efficacy Monitoring Parameters. Preprandial blood glucose between 70 and 130 mg/dL, HbA1c <7%.
Toxicity Monitoring Parameters. Weight for assessment of edema, Hgb, LFTs; symptoms of hypoglycemia include nausea, sweating, and loss of consciousness; seek care for bone pain, yellowing of skin or eyes, eye pain, or shortness of breath. Eye exam.
Key Patient Counseling Points. Monitor blood glucose in frequent intervals (2-4 times per day). May take without regard to food. May require several weeks for max effect.
Clinical Pearls. Causes edema, which may exacerbate underlying CHF, use with caution. Premenopausal anovalatory individuals may resume ovulation. Not for use in children. Thiazolidinediones are as effective as metformin, but have greater risk of adverse effects, so used as second line (both as monotherapy and in combination). Rosiglitazone has more CV effects than pioglitazone, so pioglitazone is preferred in this class. Patient and prescriber must be enrolled in REMS.