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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 pioglitazone
A10BD05
Forms & Strengths
- Metformin HCl/Pioglitazone 500 mg/15 mg tablet
- Metformin HCl/Pioglitazone 850 mg/15 mg tablet
- Metformin HCl/Pioglitazone 1000 mg/15 mg tablet
Adult Dosing
- Initial: 1 tablet (500/15 mg or 850/15 mg) once or twice daily with meals
- Titration: Gradually increase dose based on efficacy and tolerability, up to a maximum daily dose of 2000 mg metformin / 45 mg pioglitazone
Pediatric Dosing
- Safety and efficacy not established in pediatric patients under 18 years of age
Indications
- Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus when treatment with both metformin and pioglitazone 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
- Pioglitazone is a thiazolidinedione that acts as an agonist for peroxisome proliferator-activated receptor gamma (PPAR-gamma), improving target cell response to insulin without increasing insulin secretion
Contraindications
- Established New York Heart Association (NYHA) Class III or IV heart failure
- Renal disease or renal dysfunction (e.g., eGFR < 30 mL/min/1.73m2)
- Acute or chronic metabolic acidosis, including diabetic ketoacidosis
- Known hypersensitivity to metformin, pioglitazone, or any component of the formulation
- Active bladder cancer or history of bladder cancer
Adverse Reactions
- Upper respiratory tract infection
- Edema and weight gain
- Hypoglycemia (when used with insulin or insulin secretagogues)
- Diarrhea, nausea, and abdominal discomfort
- Bone fracture
- Lactic acidosis (rare associated with metformin)
Drug Interactions
- Strong CYP2C8 inhibitors (e.g., gemfibrozil) significantly increase pioglitazone exposure
- CYP2C8 inducers (e.g., rifampin) may decrease pioglitazone efficacy
- Cationic drugs eliminated by renal tubular secretion (e.g., cimetidine) may increase metformin concentration
- Carbonic anhydrase inhibitors increase risk of lactic acidosis
- Insulin or insulin secretagogues increase risk of hypoglycemia
Curated Content: Needs Vetting Before Put to Clinical Use