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ALIMENTARY TRACT AND METABOLISM › DRUGS USED IN DIABETES › BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS › Combinations of oral blood glucose lowering drugs
metformin and rosiglitazone
A10BD03
Forms & Strengths
- Tablet: 500 mg metformin hydrochloride / 2 mg rosiglitazone
- Tablet: 500 mg metformin hydrochloride / 4 mg rosiglitazone
- Tablet: 1000 mg metformin hydrochloride / 2 mg rosiglitazone
- Tablet: 1000 mg metformin hydrochloride / 4 mg rosiglitazone
Adult Dosing
- Initial dose based on current regimen, typically 500 mg/2 mg or 500 mg/4 mg once or twice daily with meals.
- Titrate gradually based on efficacy and tolerability, up to a maximum daily dose of 2000 mg metformin / 8 mg rosiglitazone.
Pediatric Dosing
- Safety and efficacy have not been established in pediatric patients (< 18 years).
Indications
- Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both metformin and rosiglitazone is appropriate.
Mechanism of Action
- Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization.
- Rosiglitazone is a thiazolidinedione (TZD) that acts as a selective agonist for peroxisome proliferator-activated receptor gamma (PPAR-gamma), improving target cell response to insulin without increasing insulin secretion.
Contraindications
- Hypersensitivity to metformin, rosiglitazone, or any component.
- Renal disease or renal dysfunction (e.g., serum creatinine >= 1.5 mg/dL for males, >= 1.4 mg/dL for females, or abnormal creatinine clearance).
- Acute or chronic metabolic acidosis, including diabetic ketoacidosis.
- New York Heart Association (NYHA) Class III or IV heart failure.
- Active bladder cancer or history of bladder cancer.
Adverse Reactions
- Hypoglycemia (when used with insulin or secretagogues)
- Weight gain
- Edema and fluid retention
- Heart failure exacerbation
- Upper respiratory tract infection
- Headache
- Back pain
- Diarrhea, nausea, and abdominal discomfort (metformin-associated)
Drug Interactions
- Strong inhibitors of CYP2C8 (e.g., gemfibrozil) may significantly increase rosiglitazone exposure.
- Strong inducers of CYP2C8 (e.g., rifampin) may decrease rosiglitazone exposure.
- Carbonic anhydrase inhibitors (e.g., topiramate, zonisamide) increase the risk of lactic acidosis.
- Cationic drugs eliminated by renal tubular secretion (e.g., digoxin, amiloride, morphine, procainamide, quinidine, quinine, ranitidine, triamterene, trimethoprim, vancomycin) may compete with metformin elimination.
- Alcohol potentiates the effect of metformin on lactate metabolism.
Curated Content: Needs Vetting Before Put to Clinical Use