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sulphonylureas

sulphonylurea oral hypoglycaemics

introduction

  • derived from the sulphonamides
  • act by increasing insulin secretion from pancreatic beta cells by binding an ATPase K+ channel ⇒ reduced K efflux ⇒ depolarisation ⇒ opens voltage gated Ca gates ⇒ rise in intracellular calcium ⇒ increased fusion of insulin granulae with the cell membrane ⇒ increased secretion of (pro)insulin.
  • potentially teratogenic and cannot be used in pregnancy or in patients who may become pregnant.
  • can induce weight gain, mainly as a result their effect to increase insulin levels and thus utilization of glucose and other metabolic fuels
  • may cause hypoglycaemia
  • have varying half lives thus some can be taken once a day while others need to be taken bd or tds

1st generation:

  • chlorpropamide
  • tolbutamide (bd or tds dosing)

2nd generation:

  • have increased potency by weight
  • glipizide
  • gliclizide
  • glibenclamide - now the most popular sulfonylurea agent. May cause cholestasis.
  • gliquidone
  • glyclopyramide
  • glimepiride (once daily dosing)
sulphonylureas.txt · Last modified: 2012/01/16 01:08 by 127.0.0.1

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