Diabetic Drugs Flashcards

1
Q

What is Metformin?

A

A hydrophilic biguanide - the first line treatment for T2DM

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are the main clinical factors of Metformin?

A
  1. It is a potent glucose lowering drug
  2. Weight neutral / losing
  3. Very cheap
  4. Typically given as 500mg 2x daily
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is the 3 physiological mechanisms of Metformin?

A
  1. Lowers hepatic glucose production
  2. Increases intestinal GLP-1 secretion
  3. Decreases lipogenesis + fat production in the liver
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are the 2 main side effects of Metformin?

A
  1. Gastrointestinal intolerance - diarrhoea, bloating, pain etc.
  2. Metformin associated lactic acidosis - in acute kidney injury
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is the pharmacological effects of SGLT2 inhibitors?

A

Sugar secreted in urine - roughly 2500kcal lost a week due to this

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is the main physiological effect of SGLT2 inhibitors?

A

Increases renal glucose loss

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is inhibited by SGLT2 inhibitors?

A

Renal sodium glucose transporter 2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What are dapagliflozin, canagliflozin and empagliflozin examples of?

A

SGLT2 inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are the 5 main side effects of SGLT2 inhibitors?

A
  1. Genital mycotic infection
  2. Diabetic Ketoacidosis
  3. Hypovolaemia
  4. Hypotension
  5. Fournier gangrene - rare but severe
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What 2 diabetic medications should be omitted in acutely unwell patients?

A

Metformin and SGLT2 inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What are Thiazolidinediones? What are their pharmacological effect?

A

They are PPAR gamma ligands that bind to and activate PPAR gamma, forming a complex with co-activator

This results in transactivation of many target genes, some beneficial and some adverse

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What do thiazolidinediones ultimately lead to?

A

Increased insulin sensitivity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What are the main effects of thiazolidinediones on adipocytes?

A

They increase differentiation from pre-adipocytes to adipocytes, increases subcutaneous fat mass storage

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is ‘lipid steal’ and what class of drug is it a result of?

A

‘Lipid steal’ is when FFA uptake removes fat from liver and muscle, reducing lipotoxicity.
It results from the use of thiazolidinediones in T2DM.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What can thiazolidinediones be known as?

A

They are referred to as ‘dirty’ insulin sensitisers - are the only true insulin sensitiser used in the treatment of T2DM

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

At what point in the treatment of T2DM would you use thiazolidinediones?

A

As a follow up to metformin when cost is an issue
OR
Used when there is a need to minimise hypoglycaemia in a patient

17
Q

What are the 3 main side effects of thiazolidinediones?

A
  1. Weight gain - fat mass increased
  2. Fluid retention
  3. Fracture risk - can be doubled
18
Q

How do Sulphonylureas work to treat T2DM?

A

They act on pancreatic beta cells to increase insulin secretion

19
Q

How can Sulphonylureas cause hypoglycaemia?

A

They are glucose independent drugs and can secrete insulin when it is not needed - leading to a high insulin concentration and ultimately hypoglycaemia

20
Q

What is the molecular mechanism of Sulphonylureas?

A
  1. Bind to SUR1
  2. Closure of ATP sensitive K+ channel
  3. Rise in membrane potential trigger voltage sensitive Ca+ channel
  4. Calcium influx leads to insulin secretion
21
Q

What class of drug does gliclazide belong to?

A

Sulphonylureas

22
Q

What are the 2 main side effects of sulphonylureas?

A
  1. Hypoglycaemia
  2. Weight gain - due to increased appetite and metabolic effects of the drug
23
Q

What do Incretin drugs do in the treatment of T2DM?

A

They act via an amplifying pathway to increase intestinal secretion of insulin when blood glucose levels are high

24
Q

What are some effects of GLP-1 in the body? (muscle, fat, liver, stomach, heart, brain)

A
  1. Increased glucose uptake and storage in muscle and fat
    Decreased glucose production from the liver
  2. Increased insulin production and decreased glucagon secretion
  3. Decreases gastric emptying
  4. Increases HR and cardiac function
  5. Decrease appetite
25
Q

What class of drugs do DPP4 inhibitors belong to?

A

Incretin drugs

26
Q

What are DPP4 inhibitors? What do they do?

A

DPP4 inhibitors are insulin secretagogues that inhibit the breakdown of GLP-1 and GIP

27
Q

Why will DPP4 inhibitors not cause hypoglycaemia?

A

Their action is glucose dependent

28
Q

What are the side effects of DPP4 inhibitors?

A

Very little - generally well tolerated
May cause an increased risk of pancreatitis

29
Q

What class of drugs do GLP-1 Receptor Agonists belong to?

A

Incretin drugs

30
Q

What do GLP-1 receptor agonists work to do?

A

Promote insulin secretion in a glucose dependent mechanism and lower glucagon

31
Q

What class of drugs are liraglutide and semaglutide examples of?

A

GLP-1 receptor agonists (incretin drugs)

32
Q

What are the 3 main side effects of GLP-1 receptor agonists?

A
  1. Nausea and vomiting
  2. Gallstones
  3. Slight chance of pancreatitis
33
Q

What diabetic drug have been approved for use in obese patients without diabetes?

A

GLP-1 receptor agonists

34
Q

What drug classification does Metformin belong to?

A

Anti-diabetics

35
Q

What is the mechanism of action of Gliclazide?

When would you prescribe it?

A

Gliclazide stimulates production and secretion of insulin through the beta cell sulphonylurea receptor. This increases the amount of insulin made by the pancreas, decreasing blood sugar levels.

Gliclazide is prescribed to patients with type 2 diabetes mellitus, alongside lifestyle changes such as exercise and implementing a healthy diet.

36
Q

What is the mechanism of action of Insulin?

When would you prescribe it?

A

Insulin facilitates the passage of glucose across cellular membranes in order to promote glucose uptake in cells.

It is prescribed to patients with type 1 (and sometimes 2) diabetes mellitus.

37
Q

What is the mechanism of action of Metformin?

When would you prescribe it?

A

Metformin inhibits gluconeogenesis (the synthesis of new glucose) and increasing insulin sensitivity in order to lower blood sugar levels.

Metformin is commonly prescribed to patients that have type 2 diabetes mellitus.