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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 sulfonylureas
A10BD02
Forms & Strengths
- Metformin HCl / Glipizide: 250 mg / 2.5 mg tablet
- Metformin HCl / Glipizide: 500 mg / 2.5 mg tablet
- Metformin HCl / Glipizide: 500 mg / 5 mg tablet
- Metformin HCl / Glyburide: 250 mg / 1.25 mg tablet
- Metformin HCl / Glyburide: 500 mg / 2.5 mg tablet
- Metformin HCl / Glyburide: 500 mg / 5 mg tablet
Adult Dosing
- Initial dose: 1 tablet daily or twice daily with meals, adjusted based on effectiveness and tolerance
- Metformin/Glipizide max dose: 2,000 mg / 20 mg per day
- Metformin/Glyburide max dose: 2,000 mg / 20 mg per day
- Titrate slowly (e.g., every 2 weeks) to minimize gastrointestinal side effects and hypoglycemia risk
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
- Not recommended for use in children under 18 years of age
Indications
- Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus
- Second-line therapy when diet, exercise, and single-agent therapy (metformin or sulfonylurea) are inadequate
Mechanism of Action
- Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization
- Sulfonylureas stimulate insulin secretion from the pancreatic beta cells by closing ATP-sensitive potassium channels
- Combined action addresses both insulin resistance and impaired insulin secretion
Contraindications
- Hypersensitivity to metformin or sulfonylureas
- Renal disease or renal dysfunction (e.g., eGFR < 30 mL/min/1.73m2)
- Acute or chronic metabolic acidosis, including diabetic ketoacidosis, with or without coma
- Type 1 diabetes mellitus
- Concomitant intravascular administration of iodinated radiocontrast materials (metformin component)
Adverse Reactions
- Hypoglycemia (due to sulfonylurea component)
- Gastrointestinal disturbances (diarrhea, nausea, vomiting, abdominal pain, flatulence)
- Lactic acidosis (rare, severe, linked to metformin accumulation)
- Vitamin B12 deficiency with chronic use
- Weight gain
- Dizziness, headache, skin rash
Drug Interactions
- Alcohol: increases the risk of lactic acidosis and hypoglycemia
- Cationic drugs eliminated by renal tubular secretion (e.g., cimetidine, digoxin, morphin): may increase metformin plasma concentrations
- Drugs that produce hyperglycemia (e.g., thiazides, corticosteroids, sympathomimetics): may lead to loss of glycemic control
- CYP2C9 inhibitors or inducers: can alter the metabolism of sulfonylureas
- Beta-blockers: can mask symptoms of hypoglycemia and alter glycemic response
Curated Content: Needs Vetting Before Put to Clinical Use