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  • Tolbutamide-

0.5-1 gm TDS

  • Glibenclamide- 5-20 mg OD or BD
  • Block the Sulfonylurea receptor (SUR1) which constitutes a subunit of the inwardly rectifying ATP-sensitive K+ channel (KATP) in the

membrane of pancreatic β cells.

  • The inward flow of K+ ions is thereby restricted, intracellular K+ concentration falls and the membrane is partially depolarized augmenting Ca2+ channel opening as well as release of Ca2+ from intracellular stores.
  • The Ca2+ ions promote fusion of insulin containing intracellular granules with the

plasma membrane and exocytotic release of insulin.

  • Hypoglycemia
  • Weight gain
  • Hypersensitivity– Rash, photosensitivity, purpura, rarely agranulocytosis
  • Disulfiram like action
  • Dilutional hyponatremia- chlorpropamide due to ADH like action
  • Non- specific side effects– N, V, D, constipation, flatulence, headache, paresthesia
  • DM
  • Diabetes insipidus (Chlorpropamide)
  • Diagnosis of insulinomas and diabetes


  • 500 mg tablet up to 8 tablet per day
  • 850 mg BD
  • Biguanides do not cause insulin release, but presence of insulin is essential for their action.
  • Though the details are not clear, recent studies have recognized activation of AMP dependent protein kinase (AMPK) to play a crucial role in mediating the actions of metformin, the key features of which are:
    1. Suppresses hepatic gluconeogenesis and glucose output from liver. This is the major action responsible for lowering of blood glucose in diabetics.
    2. Enhances insulin-mediated glucose uptake and disposal in skeletal muscle and fat. Insulin resistance exhibited by type-2 diabetics is thus overcome. This translates into— • glycogen storage in skeletal muscle reduced lipogenesis in adipose tissue and enhanced fatty acid oxidation.
    3. Interferes with mitochondrial respiratory chain and promotes peripheral glucose utilization through anaerobic glycolysis
  • GI Side effect- Abdominal pain, anorexia, bloating, nausea, metallic taste, mild diarrhea
  • Tiredness
  • Metformin does not cause hypoglycemia except in overdose.
  • Lactic acidosis
  • Vit. B12 deficiency due to interference with its absorption can occur with high dose of metformin.
  • DOC for all Type II DM except when not tolerated or contraindicated
  • PCOS– improve ovulation and fertility
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