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ALIMENTARY TRACT AND METABOLISM › DRUGS USED IN DIABETES › BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS › Biguanides
buformin
A10BA03
Forms & Strengths
- Oral tablets: 50 mg
- Oral tablets (sustained-release): 150 mg
Adult Dosing
- Type 2 diabetes mellitus: 50 mg to 150 mg daily, divided into 1 to 3 doses with meals
- Maximum recommended daily dose: 150 mg/day
Pediatric Dosing
- Safety and efficacy in pediatric patients under 18 years have not been established
- Not recommended for use in children
Indications
- Management of type 2 diabetes mellitus as monotherapy or in combination with other oral antidiabetic agents when diet and exercise alone are insufficient
Mechanism of Action
- Biguanide antihyperglycemic agent
- Decreases hepatic glucose production (gluconeogenesis and glycogenolysis)
- Decreases intestinal absorption of glucose
- Improves insulin sensitivity by increasing peripheral glucose uptake and utilization
Contraindications
- Hypersensitivity to buformin or other biguanides
- Diabetic ketoacidosis, diabetic pre-coma
- Renal impairment (e.g., serum creatinine > 1.5 mg/dL or eGFR < 60 mL/min/1.73m²)
- Acute conditions with the potential to alter renal function (e.g., dehydration, severe infection, shock)
- Acute or chronic metabolic acidosis
- Conditions associated with tissue hypoxia (e.g., decompensated heart failure, respiratory failure, recent myocardial infarction)
- Severe hepatic impairment
- Excessive alcohol intake, acute or chronic
Adverse Reactions
- Lactic acidosis (rare but potentially fatal)
- Gastrointestinal disturbances (nausea, vomiting, diarrhea, abdominal pain, metallic taste, anorexia)
- Decreased vitamin B12 absorption and deficiency with long-term use
- Skin reactions (rash, pruritus, urticaria)
Drug Interactions
- Intravascular iodinated contrast materials: Increase risk of acute renal failure and lactic acidosis
- Cationic drugs eliminated by renal tubular secretion (e.g., cimetidine, digoxin, morphine, procainamide, quinidine, quinine, trimethoprim, vancomycin): May increase buformin concentration
- Alcohol: Increases risk of lactic acidosis and hypoglycemia
- Diuretics, NSAIDs, and antihypertensive drugs (ACE inhibitors, ARBs): May impair renal function and increase lactic acidosis risk
- Glucocorticoids, beta-2 agonists, and thiazides: Tend to increase blood glucose, potentially antagonizing buformin effect
Curated Content: Needs Vetting Before Put to Clinical Use