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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
glimepiride and rosiglitazone
A10BD04
Forms & Strengths
- Tablet: 1 mg glimepiride / 4 mg rosiglitazone
- Tablet: 2 mg glimepiride / 4 mg rosiglitazone
- Tablet: 4 mg glimepiride / 4 mg rosiglitazone
Adult Dosing
- Initial dose based on previous therapy; commonly start with lowest available strength once daily with breakfast or the first main meal.
- Titrate dose gradually based on glycemic response and tolerability, typically at intervals of 2 weeks or longer.
- Maximum recommended daily dose: 8 mg glimepiride / 8 mg rosiglitazone (administered as separate components or appropriate fixed-dose combinations).
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established.
- Use in patients under 18 years of age is not recommended.
Indications
- As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both glimepiride and rosiglitazone is appropriate.
- Not indicated for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis.
Mechanism of Action
- Glimepiride is a second-generation sulfonylurea that stimulates insulin secretion from pancreatic beta cells and reduces glucose output from the liver.
- Rosiglitazone is a thiazolidinedione that acts as an agonist at peroxisome proliferator-activated receptor gamma (PPAR-gamma), improving target cell response to insulin without increasing insulin secretion.
Contraindications
- Known hypersensitivity to glimepiride, rosiglitazone, or any component of the formulation.
- Type 1 diabetes mellitus or diabetic ketoacidosis.
- Active or history of heart failure (NYHA Class I through IV).
- Active liver disease or baseline serum transaminases exceeding 2.5 times the upper limit of normal.
Adverse Reactions
- Hypoglycemia (associated with the glimepiride component)
- Edema and fluid retention (associated with rosiglitazone)
- Weight gain
- Increased risk of bone fractures
- Upper respiratory tract infection
- Headache
- Anemia
Drug Interactions
- CYP2C9 inhibitors (e.g., fluconazole) may increase glimepiride exposure and risk of hypoglycemia.
- CYP2C9 inducers (e.g., rifampin) may decrease glimepiride efficacy.
- CYP2C8 inhibitors (e.g., gemfibrozil) can significantly increase rosiglitazone exposure.
- CYP2C8 inducers (e.g., rifampin) may decrease rosiglitazone concentrations.
- Beta-blockers, sympatholytics, and MAOIs may mask symptoms of hypoglycemia or potentiate hypoglycemic effects.
- Diuretics and corticosteroids may attenuate glycemic control.
Curated Content: Needs Vetting Before Put to Clinical Use