Diabetes - Core Drugs Flashcards
List core drugs for diabetes.
metformin
sitagliptin
gliclazide
dapaglifozin
What drug class is sitagliptin in?
Dipeptidyl-peptidase 4 (DPP-4) inhibitors
What drug class is gliclazide in?
sulphonylurea
What drug class in dapaglifozin?
Sodium-glucose co-transporter (SGLT2) inhibitors
What is the primary mechanism of action of metformin?
activates AMPK in hepatocyte mitochondria > inhibits ATP production > blocks gluconeogenesis > blocks glucose output > blocks adenylate cyclase > promotes fat oxidation
Both help restore insulin sensitivity
What is the drug target for metformin?
5′-AMP-activated protein kinase (AMPK)
What are the main side effects of metformin?
GI: abdominal pain, decreased appetite, diarrhoea, vomiting
What does metformin need to access tissues?
organic cation transporter-1 (OCT-1)
What is the mechanism of action of sitagliptin?
inhibits the action of DPP-4 in vascular endothelium and metabolise incretins in plasma
What are the main side effects of sitagliptin?
Upper respiratory tract infections, flu-like symptoms
Serious allergic reactions/ avoid in patients with pancreatitis
What is the mechanism of action of gliclazide?
Inhibit the ATP-sensitive potassium channel on pancreatic beta cell > stimulates Ca2+ influx > insulin vesicle exocytosis
What are side effects of gliclazide?
weight gain
hypoglycaemia
What is the mechanism of action of dapaglifozin?
Reversibly inhibits SGLT2 in PCT > reduce glucose reabsorption > ^ urinary glucose excretion
What are the side effects of dapaglifozin?
Uro-genital infections due to ^glucose load
Slight decrease in bone formation
Can worsen diabetic ketoacidosis (stop immediately
DPP-4 I’s and sulphonylureas are only effective when?
only when some residual pancreatic beta-cell activity is present
Weight gain when taking glicazide is mitigated by what?
concurrent administration with metformin
The risk of what associated with sulphonylureas should be discussed with the patient?
hypoglycaemia
SGLT 2 inhibitors are less effective in what patients?
those with renal impairment
