Drugs and Their Targets in T2DM Flashcards Preview

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Flashcards in Drugs and Their Targets in T2DM Deck (104)
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1

If a drug is insulin dependent, what does this mean?

In order to have an effect, enough insulin must be present

2

Which drugs can be described as insulin independent?

  1. α-glucosidase inhibitors
  2. SGLT2 inhibitors

3

Name two drug classes involved in increasing insulins sensitivity 

  1. Biguanides
  2. Thiazolidinediones (glitazones)

4

As well as impacting insulin sensitivity, what other action do the biguanides and thiazolidinediones share?

Decrease hepatic gluconeogenesis

5

Which drugs will increase insulin secretion?

  1. Sulphonylureas
  2. Incretin mimetics
  3. Glinides
  4. DPP-4 inhibitors

6

Biguanides are insulin ____________

Biguanides are insulin dependent

7

Glinides are insulin ___________

Glinides are insulin dependent

8

α-glucosidase inhibitors are insulin ___________

α-glucosidase inhibitors are insulin independent

9

SGLT2 inhibitors are insulin _____________

SGLT2 inhibitors are insulin independent

10

DPP-4 inhibitors are insulin ______________

DPP-4 inhibitors are insulin dependent

11

GLUT4 is a glucose transport protein associated with which tissues?

Target tissues

(e.g. adipose and skeletal muscle)

12

Describe the process by which insulin is released

  1. Elevated BGL
  2. GLUT2 allows entry of glucose to cell cytoplasm
  3. Glucokinase converts glucose to glucose-6-phosphate
  4. Glucose-6-phosphate is converted to ATP
  5. ATP acts on KATP channel
  6. KATP channel closes and depolarisation of cell occurs
  7. Volages activated Ca2+ channels open
  8. Ca2+ influx triggers exocytosis of insulin storage granules

13

Which drug class works by slowing glucose absorption from the GI tract?

α-glucosidase inhibitors

14

During the insulin secretion mechanism, what exactly causes KATP channel to close?

The ratio of ATP:ADP

15

How many subunits make up the KATP channel?

8

16

Which two types of subunit are involved in the KATP channel?

  1. Kir6.2
  2. SUR1

17

To which subunit will ATP bind to in order to close the KATP channel?

Kir6.2

18

Which substance can bind to the KATP channel in order to keep it open and to which subunit will it bind?

ADP-Mg2+

SUR1

19

To which subunit will the sulphonylurea drug class bind to in the KATP channel and what is the useful effect of this?

SUR1

This induces depolarisation leading to insulin release regardless of whether blood sugars are high or low

20

In order for the sulphonylureas to be of use what is required?

Pancreatic β cells

(this is why this drug class is useless in T1DM)

21

Why may the effect of the sulphonylureas decrease over time in a patient?

β cells decrease over time, even in T2DM

22

Give 4 examples of sulphonylureas

  1. Tolbutamide (1st gen - rarely used)
  2. Glibenclamide
  3. Gliclazide
  4. Glipizide

23

How do the sulphonylureas act?

Displacement of the ADP-Mg2+ from the SUR1 subunit causing closure of the KATP channel and subsequent depolarisation

24

Which risk is associated with sulphonylureas since they act independently to BGLs?

Hypoglycaemia

(BGLs may already be low when administered for example, which would reduce them further)

25

How can the sulphonylureas be administered?

Orally

26

What is the duration of action of the different sulphonylureas?

  1. Short acting - tolbutamide - 4-6 hours
  2. Long acting - glibenclamide, glipizide, gliclazide - 16-48 hours

27

Which type(s) of vascular risks associated with diabetes do the sulphonylureas reduce?

Microvascular complications

28

In which patients is hypoglycaemia a particular risk when taking sulphonylureas?

  1. Elderly (renal function decreases with age)
  2. Reduced hepatic or renal function
  3. Pregnant women

(N.b. Long acting agents pose a higher hypoglycaemic risk)

29

In a treatment algorithm, sulphonylureas will usually be _________ line therapy with __________

In a treatment algorithm, sulphonylureas will usually be second line therapy with metformin

(N.b Not in pregancy; they may also be used 3rd line with TZDs and metformin)

30

Sulphonylureas cause weight ________

Sulphonylureas cause weight gain