Diabetes Drugs

Question 1

Biguanides mechanism of action

Answer 1

Not fully understood, increases peripheral insulin sensitivity by increasing glucose uptake, decreasing hepatic gluconeogenesis and reducing glucose absorption in the gut

Question 2

Example of biguanides

Answer 2

Metformin

Question 3

Side effects of biguanides

Answer 3

Weight loss, reduced microvascular complications, GI upset, lactic acidosis

Question 4

Contraindications of biguanides

Answer 4

Avoid in liver and renal dysfunction

Question 5

Administration of biguanides

Answer 5

Start low go slow 500mg-1g BD

Question 6

Mechanism of action of SUs

Answer 6

Displace ADP-Mg2+ at the SUR1subunit closing KATP channels preventing K+ efflux resulting in depolarisation of the B cells in the pancreas which stimulates voltage gated calcium channels resulting in insulin release

Question 7

Examples of SUs

Answer 7

Short acting: Gliclazide, tolbutamide

Long acting: Glibenclamide, glipizide

Question 8

Side effects of SUs

Answer 8

Hypoglycaemia, weight gain

Question 9

Should SUs be taken with or without food

Answer 9

WITH

Question 10

Glinides mechanism of action

Answer 10

Binds to benzamide site of the SUR1 subunit, closes the KATP channel preventing K+ efflux resulting in depolarisation and stimulating insulin release

Question 11

Examples of glinides

Answer 11

Repaglinide, nateglinide

Question 12

Side effects of glinides

Answer 12

Less likely to cause hypoglycaemia, safer in CKD, weight gain

Question 13

When should glinides not be used

Answer 13

Severe hepatic impairment, breastfeeding

Question 14

DDP4 inhibitors mechanism of action

Answer 14

Competitive inhibition of DDP-4 to increase insulin release, decrease glucagon release, delay gastric emptying

Question 15

Examples of DDP4 inhibitors

Answer 15

Sitagliptin

Question 16

Side effects of DD4 inhibitors

Answer 16

Nausea, watch in renal impairment

Question 17

Incretin analogues mechanism of action

Answer 17

GLP-1 receptor analogues stimulating insulin release, decrease glucagon release, delay gastric emptying, resistant to DDP4 breakdown

Question 18

Examples of incretin analogues

Answer 18

Liraglutide, exenatide

Question 19

Incretin analogues side effects

Answer 19

Weight loss + cardiac benefits, nausea

Question 20

Alpha-glucosidase inhibitors mechanism of action

Answer 20

A-glucosidase is a brush border enzyme that breakdown dietary carbs, starch + dissacharides to absorbable glucose, inhibition prevents glucose absorption reducing a large spike in blood glucose after eating

Question 21

Examples of alpha-glucosidase inhibitor

Answer 21

Acarbose, miglitol

Question 22

Side effects of alpha-glucosidase inhibitor

Answer 22

Flatulence, loose stools, diarrhoea, abode pain, bloating due to colonic bacteria reacting with undigested carbs

Question 23

Thiazolidinediones mechanism of actions

Answer 23

PPARgamma agonist that binds to RXR receptor in adipocytes to act as a transcription factor to increase expression of genes that increase insulin release and affect lipid metabolism (decrease fatty acid release from adipose tissue + promotes storage, tissues have to find alternative energy sources so enhances peripheral glucose uptake)

Question 24

Examples of TZDs

Answer 24

Pioglitazone

Question 25

Side effects of TZDs

Answer 25

Weight gain, fluid retentions (CHF), hepatotoxicity (except for pioglitazone), fractures, risk of DKA, risk of bladder cancer

Question 26

SGLT2 inhibitors mechanism of action

Answer 26

Inhibits glucose reabsorption by blocking SLGt2 channel in PCT promoting excretion

Question 27

Examples of SGLT2 inhibitors

Answer 27

empagliflozin, canagliflozin, dapaglifloxin

Question 28

Side effects of SGLT2 inhibitors

Answer 28

UTIs/thrush, hypotension (water follows glucose), risk of bladder cancer, risk of euglycaemic acidosis, weight loss, cardiac benefits,