Diabetes pharmacology Flashcards
Which drug is a first generation sulphonylurea?
Tolbutamide
Which drugs are second generation sulphonylureas?
Glibenclamide
Glipizide
How do sulphonylureas stimulate insulin release?
Displaces the binding of ADP-Mg2+ from the SUR1 subunit, closing the KATP channel, allowing the membrane depolarisation to occur that stimulates insulin release
What is the difference between first and second generation sulphonylureas?
Second are more potent and longer acting
What is the disadvantageous side effect of sulphonylureas?
Weight gain
In which patients is the risk of hypoglycaemia caused by sulphonylureas increased?
Elderly
Impaired hepatic/renal function
Which drugs are examples of glinides?
Repaglinide
Nateglinide
How do glinides work?
Binds to SUR1 subunit at a benzamino site, closing the KATP channel and triggering insulin release
Are sulphonylureas or glinides more likely to cause hypoglycaemia?
Sulphonylureas
When are glinides taken and why?
Before meals
Combats post-prandial rise in glucose
What do glucagon-like peptide 1 (GLP1) and glucose dependant insulinotropic peptide (GIP) do and when are they released?
Released in response to ingestion of food
GLP-1 and GIP stimulate insulin secretion from pancreatic beta cells and delay gastric emptying
GLP-1 decreases glucagon release from pancreatic alpha cells
Which drugs mimic the action of GLP-1?
Incretin analogues
Which drug is an incretin analogue?
Extenatide
What are the effects of incretin analogues?
Increases insulin secretion
Suppresses glucagon secretion
Slows gastric emptying
Decreases appetite
What are some of the advantages of using incretin analogues?
Cause modest weight loss
Reduce hepatic fat accumulation
How is extenatide administered?
Subcutaneously twice daily