sulphonylureas
Table of Contents
sulphonylurea oral hypoglycaemics
see also:
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