Antidiabetics - GLP-1 agonists Flashcards
Beta cells of the pancreas are sensitive to blood glucose. What transporter transports glucose into beta cells?
1 - GLUT-4
2 - GLUT-3
3 - GLUT-2
4 - GLUT-1
3 - GLUT-2
- once inside the beta cell glucose is metabolised into ATP
Once glucose enters the cell through GLUT-2 it is metabolised to ATP. Which channel on the beta cell is sensitive to ATP levels and closes in the presence of high ATP?
1 - Na+/K+ ATPase
2 - Na+
3 - K+
4 - Cl-
3 - K+
- intracellular K+ will then begin to rise
- cellular depolarisation occurs
Once glucose enters the cell through GLUT-2 it is metabolised to ATP, causing ATP sensitive K+ channels to close and cause depolarisation. Depolarisation then leads to a voltage gated channel to open. Which channel is this?
1 - Na+/K+ ATPase
2 - Na+
3 - K+
4 - Ca2+
4 - Ca2+
- increases intracellular Ca2+
- increased Ca2+ causes insulin filled vesicles to fuse with the beta cell and release insulin
Incretins are a group of hormones responsible for reducing blood glucose, such as glucagon like peptide-1 (GLP-1). Enteroendocrine cells are specialised cells that are able to release incretins. Which 2 of the following are the locations where enteroendocrine cells can be located?
1 - pancreas
2 - stomach
3 - liver
4 - ileum/colon
1 - pancreas
4 - ileum/colon
During fullness L cells in the ileum and colon secrete peptide YY. In addition, glucose in the blood can also stimulate L cells to secrete incretins. What is the name of this second peptide hormone secreted from L cells?
1 - leptin
2 - glucagon like peptide-1 (GLP-1)
3 - secretin
4 - cholecystokinin
2 - glucagon like peptide-1 (GLP-1)
There is a second incretin that is released into the GIT in response to eating, what is this called?
1 - peptide YY
2 - secretin
3 - cholecystokinin
4 - Glucose-dependent insulinotropic peptide (GIP)
4 - Glucose-dependent insulinotropic peptide (GIP)
Glucose-dependent insulinotropic peptide (GIP) and glucagon like peptide-1 (GLP-1) are both incretins. Does the incretin effect increase or decrease insulin release from the pancreas?
- increase insulin release
- more insulin release when glucose is taken in orally vs when given via IV
- indicates incretins (GLP-1 and GIP) in GIT have a big effect on insulin release
Glucagon like peptide-1 (GLP-1) has a variety of effects that be beneficial in diabetes. What effect does it have on the GIT?
1 - increases gut motility
2 - inhibits glucose absorption
3 - slows gut motility
4 - inhibits enzymes that digest carbohydrates
3 - slows gut motility
- this increases mechanoreceptor firing, increasing fullness feeling
- slows the digestion and absorption of glucose, so slower glucose spike
Glucagon like peptide-1 (GLP-1) has a variety of effects that be beneficial in diabetes. What effect does GLP-1 have on the pancreas?
1 - inhibits beta cells
2 - inhibits delta cells
3 - inhibits alpha cells
4 - inhibits acinar cells
3 - inhibits alpha cells
- reduces glucagon release
- less glucagon means less gluconeogenesis in the liver
Does glucagon like peptide-1 (GLP-1) increase or decrease insulin release?
- increases insulin secretion form beta cells
- binds GPCR Gas
- increases cAMP causes insulin secretion
- glucose dependent release
Which of the 2 are the key core GLP-1 agonists that we need to be aware of?
1 - Gliclazide
2 - Metformin
3 - Dulaglutide
4 - Exenatide
3 - Dulaglutide
4 - Exenatide
In addition to increasing insulin release in a glucose dependent manner, which of the following can GLP-1 agonists (Dulaglutide and Exenatide) do?
1 - reduce stress on beta cells, therefore enhancing beta cells replication
2 - prevents beta-cells apoptosis
3 - inhibition of glucagon secretion
4 - all of the above
4 - all of the above
Which of the following are the most common adverse events associated with GLP-1?
1 - headaches/dizziness
2 - weakness
3 - nausea/vomiting
4 - diarrhoea
5 - all of the above
5 - all of the above
The most common adverse events associated with GLP-1 are
- headaches/dizziness
- weakness
- nausea/vomiting
- diarrhoea
- all of the above
Which of the following are adverse events, BUT are rare?
1 - pruritis (injection site specific)
2 - acute pancreatitis
3 - renal impairment
4 - all of the above
4 - all of the above
What can combining insulin with a GLP-1 agonists (Dulaglutide and Exenatide) lead to?
1 - DKA
2 - Hyperosmolar Hyperglycaemic State
3 - Hyperglycaemia
4 - Hypoglycaemia
4 - Hypoglycaemia
- patients should always carry a glucose source
- has also been linked with thyroid cancer