Pharmacology Flashcards
Give an example and the effects of a biguanide
Metformin
- decrease hepatic glucose production
- Increase insulin sensitivity
What is a contraindication of metformin?
Renal impairment
90% of metformin is excreted by the kidneys. If GFR is low due to renal impairment, metformin will not be excreted efficiently.
Give an example of a sulphonylurea
Gliclazide
What is the MoA of gliclazide?
Acts on beta cells.
agonises the SUR1 K+ transporter
which stimulates the complimentary influx of Ca2+
and therefore the exocytosis of insulin
agonises SUR1 transporters on beta cells which increases the secretion of insulin
What are the 2 classes of incretin drugs?
GLP1 receptor agonists
DPP4 inhibitors
Give an example of a GLP1 receptor agonist
Byetta (Exenatide)
What is the MoA of GLP1 receptor agonists?
Same as the function of GLP1 -
acts on pancreas to increase the amount of insulin secreted, and decrease the amount of glucagon secreted.
…………tide
What is the MoA of DPP4 inhibitors?
Prevents the degredation of endogenous GLP1, therefore levels of GLP1 are highr, which acts to increase the amount of insulin, and decrease the amount of glucagon secreted by the pancreas.
Gove an example of a DPP4 inhibitor
sitagliptin
Give an example of an SGLT2 inhibitor
Canagliflozin
…………..gliflozin
What is the MoA of SLGT2 inhibitors?
blood glucose reabsorbed in the proximal tubule in the kidney by SGLT2 (and 1) transporters.
In T2DM, SLGTs get more efficient, ie they reabsorb more glucose before they are overwhelmed and any is excreted.
SLGT2 inhibitors reduce the efficiency of SLGT2 transporters and therefore more glucose is excreted into the urine, thereby lowering the blood glucose.
Other than reducing blood glucose, what positive effects do SGLT2 inhibitors have?
When glucuse is excreted, water follows, therefore water retention is decreased, this lead to:
- weight loss
- reducing blood pressure
Also, excreting glucose reuduces the calories in:out ratio.
What do SLGT2 inhibitors increase the risk of?
UTIs
due to glucose in urine.
GLP1 receptor agonists common part of name
……………..tide
SGLP2 inhibitor common part of name
….gliflozin