Diabetes drug MOA's

Question 1

What is a very common side effect of diabetes treatment?

Answer 1

Weight gain

Question 2

Which diabetes treatment does not cause weight gain?

Answer 2

Metformin

Question 3

What is orlistat and why is it sometimes used in T2DM?

Answer 3

Pancreatic Lipase Inhibitor
Reduces break down of fats in the intestines thus reducing absorption of fats
More is excreted

Question 4

State 7 classes of drugs that are used to treat T2DM and state how they work.

Answer 4

Insulin: reduces HGO
Metformin: insulin sensitiser
Sulphonylureas: makes existing pancreas produce more insulin
Alpha-glucosidase inhibitors: prolongs absorption of glucose from the intestine
Thiazolidinediones: act on insulin resistance (central + peripheral)
GLP-1 agonists + DPP4 inhibitors: increase insulin secretion + have anti-glucagon effect
SGLT2 inhibitors: act on PCT to increase glycosuria

Question 5

When should you NOT use metformin?

Answer 5

Severe liver failure
Severe cardiac failure
Mild renal failure

Question 6

Name one sulphonylurea.

Answer 6

Glibenclamide

Given to lean patients with T2DM (as causes weight gain)

Question 7

Explain how sulphonylureas work.

Answer 7

Bind to receptors + block the ATP-sensitive K+ channel

Leads to Ca2+ influx, which causes insulin release

Question 8

Name one alpha-glucosidase inhibitor. Explain how it works and state 1 side effect.

Answer 8

Acarbose
Prolongs absorption of oligosaccharides + allows the body to cope with the loss of 1st phase insulin
Side effect: flatus

Question 9

Name a thiazolidinedione. What are its effects?

Answer 9

Pioglitazone
=PPAR agonist
Insulin sensitises mainly in peripheral tissues (leads to peripheral weight gain)

Question 10

What does GLP-1 do?

Answer 10

Responsible for the incretin effect (where oral glucose stimulates more insulin than IV glucose)
Stimulates insulin + suppresses glucagon

Question 11

What breaks down GLP-1?

Answer 11

Dipeptidyl peptidase-4 (DPP4)

Question 12

How do gliptins work?

Answer 12

Inhibit DPP4 (increase half life of GLP1)
Increases [GLP1]
Decreases [glucagon]
Decreases [glucose]
Neutral on weight

Question 13

Name a GLP1 agonist. Describe the action of GLP1 agonists

Answer 13

Exenatide.
Injectable, long acting
Decrease [glucagon]
Decrease [glucose]
Reduces gastric emptying + increases satiety thus cause weight loss

Question 14

Name an SGLT2 inhibitor and describe its mechanism of action

Answer 14

Empaglifozin
Inhibits Na-Glu transporter
Increases glycosuria

Question 15

What weight loss treatment may cause T2DM to go into remission?

Answer 15

Gastric bypass surgery

Question 16

By what mechanisms does metformin reduce insulin resistance?

Answer 16

Reduced HGO

Increases peripheral glucose disposal

Question 17

What is the problem with injectable insulin? What has been created as an alternative to this?

Answer 17

Forms hexamer under skin, thus needs 30 mins before effective
Insulin analogues are rapid acting