Antidiabetics - GLP-1 agonists Flashcards

1
Q

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

A

3 - GLUT-2

  • once inside the beta cell glucose is metabolised into ATP
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2
Q

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-

A

3 - K+
- intracellular K+ will then begin to rise
- cellular depolarisation occurs

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3
Q

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+

A

4 - Ca2+
- increases intracellular Ca2+
- increased Ca2+ causes insulin filled vesicles to fuse with the beta cell and release insulin

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4
Q

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

A

1 - pancreas
4 - ileum/colon

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5
Q

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

A

2 - glucagon like peptide-1 (GLP-1)

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6
Q

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)

A

4 - Glucose-dependent insulinotropic peptide (GIP)

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7
Q

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?

A
  • 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
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8
Q

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

A

3 - slows gut motility

  • this increases mechanoreceptor firing, increasing fullness feeling
  • slows the digestion and absorption of glucose, so slower glucose spike
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9
Q

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

A

3 - inhibits alpha cells
- reduces glucagon release
- less glucagon means less gluconeogenesis in the liver

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10
Q

Does glucagon like peptide-1 (GLP-1) increase or decrease insulin release?

A
  • increases insulin secretion form beta cells
  • binds GPCR Gas
  • increases cAMP causes insulin secretion
  • glucose dependent release
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11
Q

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

A

3 - Dulaglutide
4 - Exenatide

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12
Q

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

A

4 - all of the above

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13
Q

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

A

5 - all of the above

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14
Q

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

A

4 - all of the above

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15
Q

What can combining insulin with a GLP-1 agonists (Dulaglutide and Exenatide) lead to?

1 - DKA
2 - Hyperosmolar Hyperglycaemic State
3 - Hyperglycaemia
4 - Hypoglycaemia

A

4 - Hypoglycaemia

  • patients should always carry a glucose source
  • has also been linked with thyroid cancer
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16
Q

When prescribing a GLP-1 agonists (Dulaglutide and Exenatide) we should use caution with all of the following EXCEPT which one?

1 - renal impairment
2 - gastroparesis
3 - parathyroid disease
4 - hepatic impairment
5 - acute pancreatitis
6 - thyroid disease

A

2 - parathyroid disease

17
Q

How are GLP-1 agonists (Dulaglutide and Exenatide) typically administered?

1 - IV
2 - oral
3 - SC
4 - IM

A

3 - SC

18
Q

When should GLP-1 agonists (Dulaglutide and Exenatide) typically be administered via SC?

1 - once a week on same day and time
2 - with all meals
3 - in the morning
4 - in the evenings

A

1 - once a week on same day and time

19
Q

GLP-1 agonists (Dulaglutide and Exenatide) are an anti-diabetic medications. Are Dulaglutide and Exenatide 1st line treatment for hyperglycaemia in T2DM?

A
  • no
20
Q

GLP-1 agonists (Dulaglutide and Exenatide) are an anti-diabetic medications. When are Dulaglutide and Exenatide indicated in their use?

1 - if metformin is not tolerated
2 - part of dual therapy
3 - part of triple therapy
4 - all of the above

A

3 - part of triple therapy

  • typically a GLP-1 with metformin and glicazide