Pharmacology of Diabetes

Question 1

What are 4 drugs used in the treatment of diabets?

Answer 1

1. Metformin
2. DPP-4 inhibitors
3. Sulphonylureas
4. SGLT-2 inhibitors

Question 2

What is the principle drug target for Metformin?

Answer 2

AMP activated protein kinase

Question 3

What is the principle drug target for DPP-4 inhibitors?

Answer 3

Dipeptidyl peptidase-4 (DPP-4)

Question 4

What is the principle drug target for Sulphonylureas?

Answer 4

ATP-sensitive K+ channels

Question 5

What is the principle drug target for SGLT-2 inhibitors?

Answer 5

Sodium-glucose co-transporter-2

Question 6

What is the drug target type for Metformin?

Answer 6

Enzyme

Question 7

What is the drug target type for DPP-4 inhibitors?

Answer 7

Enzyme

Question 8

What is the drug target type for Sulphonylureas?

Answer 8

Ion channels

Question 9

What is the drug target type for SGLT-2 inhibitors?

Answer 9

Transport protein

Question 10

What is the location for the actions of Metformin?

Answer 10

Hepatocyte mitochondria

Question 11

What is the location for the actions of DPP-4 inhibitors?

Answer 11

Vascular endothelium

Question 12

What is the location for the actions of Sulphonylureas?

Answer 12

Pancreatic beta cells

Question 13

What is the location for the actions of SGLT-2 inhibitors?

Answer 13

Proximal convoluted tubule

Question 14

What is the action of Metformin?

Answer 14

Decreased gluconeogenesis

Question 15

What is the action of DPP-4 inhibitors?

Answer 15

Increased plasma incretin levels

Question 16

What is the action of Sulphonylureas?

Answer 16

Insulin secretion

Question 17

What is the action of SGLT-2 inhibitors?

Answer 17

Decreased glucose reabsorption

Question 18

What are the 3 key steps to pharmacology?

Answer 18

1. Identify the patient’s problem
2. Specify the therapeutic objective
3. Select a drug on the basis of comparative efficacy, safety, cost and sustainability

Question 19

What does it mean if a drug is ionized?

Answer 19

Ionized = less lipid soluble

Less absorption, into blood
Good distribution, once in blood

Question 20

What are the main side effects of Metformin?

Answer 20

GI effects

Question 21

When is Metformin most effective?

Answer 21

In the presence of endogenous insulin, so with some residual functioning pancreatic islet cells.

Question 22

What are the main side effects of DPP-4 inhibitors?

Answer 22

Upper respiratory tract infections

Question 23

When are DPP-4 inhibitors only effective?

Answer 23

When some residual pancreatic beta-cell activity is present

Question 24

What are the main side effects of Sulphonylurea?

Answer 24

1. Weight gain

2. Hypoglycaemia

Question 25

When is Sulphonylurea only effective?

Answer 25

When some residual pancreatic beta-cell activity is present

Question 26

How can weight gain associated with sulphonylurea be mitigated?

Answer 26

The concurrent administration with Metformin

Question 27

What is an example of a Sulphonylurea?

Answer 27

Gliclazide

Question 28

What is an example of a DPP-4 inhibitor?

Answer 28

Sitagliptin

Question 29

What is an example of a SGLT-2 inhibitor?

Answer 29

Dapaglifozin

Question 30

What is gliclazide an example of?

Answer 30

Sulphonylurea

Question 31

What is sitagliptin an example of?

Answer 31

DPP-4 inhibitor

Question 32

What is dapaglifozin an example of?

Answer 32

SGLT-2 inhibitor

Question 33

What are the main side effects of SGLT2 inhibitors?

Answer 33

1. Uro-genital infections 2. Slight decrease in bone density 3. Can worsen beta-ketoacidosis (stop immediately)1

Question 34

What can SGLT2 inhibitors cause?

Answer 34

1. Weight loss | 2. Reduction in BP

Question 35

When is SGLT2 less effective?

Answer 35

Patients with renal impairment