Sulphonylureas Flashcards
What are examples of sulphonylureas?
- Gliclazide
- Glimpiride
- Glipizide
What are contraindications to sulphonylurea use?
- Acute porphyria (Gliclazide only)
- Presence of Ketoacidosis
- Severe hepatic/renal impairment
- Risk of hypos
When would you use sulphonylureas with caution?
- Renal impairment
- Hepatic impairment
- Pregnancy and breast feeding
- Elderly
- G6PD Deficiency
What is the mechanism of action of sulphonylureas?
Increase insulin secretion from pancreatic islet cells - need residual beta cells. They block ATP-dependent K+ channels in pancreatic β-cell membranes, causing depolarisation of the cell membrane and opening of voltage-gated Ca2+ channels. This increases intracellular Ca2+ concentrations, stimulating insulin secretion
Are sulphonylureas associated with weight gain?
Yes
What are adverse side effects of sulphonylureas?
- Hypoglycaemia
- Weight gain
- Gastro-intestinal upset
- Hepatic impairment
- Hypersensitivity reaction (rash, liver disease)
- Rarely haematological abnormalities
What are people taking sulphonylureas at risk of?
Hypoglycaemia
What are the easiest sulphonylureas to use?
Those which are shorter duration of action and hepatically metabolised e.g. gliclazide
When should sulphonylureas be taken?
With meals
Why may insulin be required in acute illness in hospital inpatientsfor someone on sulphonylureas?
Acute illness can precipitate side effects, and insulin can be more easily controlled in response to acute fluctuations in blood sugar
