Oral hypoglycaemic agents Flashcards
(20 cards)
Name a biguanide:
Metformin
How does metformin work?
Insulin sensitizer. Reduces gluconeogenesis in the liver . It also slows intestinal absorption of sugars and improves peripheral glucose uptake and utilisation.
Reduces LDL and VLDL. and increase HDL.
What are the pharmacokinetics of metformin?
Well absorbed orally.
Not bound to serum proteins
Not metabolised
Excreted via urine.
ADR’s metformin?
GI
Lactic acidosis in those with renal failure. Rare
Vit B12 uncommon
Contraindications/DDIs of metformin?
Renal/heaptic disease Diabetic ketoacidosis >80 years old Congestive Heart Failure Alcohol abuse
Give some examples of sulfonylureas:
Glicazide, glipizide, glimepiride
What is the mechanism of action of sulfonylureas?
Stimulation of beta cells to release insulin. Block ATP sensitive K+ channels resulting in depolarisation and Ca2+ influx and causing Insulin release.
Reduction in hepatic glucose production
increase peripheral insulin sensitivity.
Describe the PK’s of sulfonylureas:
Bind to serum proteins
Metabolised by the liver
Excreted by liver or kidney
Duration ranges fro 12 to 24 hrs
ADR’s of sulfonylureas:
Weight gain
Hyperinsulinaemia
Hypoglycaemia
Contraindications/DDI’s with sulfonylureas:
Renal impairment
Hepatic impairment
Name some examples of DDP-4 Inhibitors:
Sitagliptin, Vildagliptin, Saxagliptin, Linagliptin
What is the mechanism of action of DDP-4 Inhibitors?
Inhibit the DDP-4 enzyme which breaks down GLP-1. GLP-1 is responsible for increasing Insulin secretion and increasing sensitivity to Insulin.
What are some of the side effects of DDP-4 Inhibitors?
Nasopharyngitis
Headache
Pancreatitis
Name some examples of Sodium Glucose Co-transporter 2 Inhibitors:
Dapagliflozin
Canagliflozin
Empagloifozin
What is the mechanism of action of Sodium Glucose Co-transporter 2 Inhibitors:
Inhibit SGLT2 in the tubular lumen of the kidney. Less glucose is reabsorbed. Lowers blood glucose.
What are the adverse effects of SGLT2 inhibitors?
Female genital mycotic infections (e.g. vulvovaginal candidiasis)
UTI’s
Urinary frequency
Hypotension
Name some examples of GLP -1 Receptor Agonists:
Exenatide
Lirlutide
What is the mechanism of action of GLP-1 receptor agonists?
Act on GLP-1 receptors and increase native insulin release.
Enhance satiety Slow gastric emptying time
What are the PK’s of GLP-1 Receptor agonists?
Polypeptides - must be administered subcut.
What are the adverse effect of GLP-1 agonists?
Nausea Vomiting Diarrhoea Constipation Pancreatitis
