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
