Drug Treatments T2D

Question 1

Sulfonylureas

• properties
• examples
• side effects

Answer 1

-all bound to plasma proteins so longer half life
-all orally active
E.g. glipizide, gliclazide

Major Side Effect:
-Hypoglycaemia

Question 2

Sulfonylureas
-MOA
primary + secondary

Answer 2

stimulates endogenous insulin release
-binds to ATP sensitive K channel to promote insulin secretion

secondary

• Sensitize ß-cells to glucose
• Decrease lipolysis
• Decrease clearance of insulin by the liver

Question 3

Biguanide drugs

-MOA

Answer 3

1) Increase glucose uptake in muscle
- increased GLUT4 translocation through AMPK
increases insulin sensitivity

2) Decrease glucose production by liver through AMPK and gene expression

Question 4

Thiazolidinediones

Example
MOA

side effects:

Answer 4

E.G Pioglitazone

can reduce the effectiveness of OCP

This is the only one that is approved

Activate peroxisome proliferator-activated receptor-g (PPARg)

increases insulin sensitivity

adverse effects: weight gain, fluid retention, subject to interactions due to liver metabolism

Question 5

Glucagon-like peptide-1 analogs

Give Example

Answer 5

sc injection
facilitates glucose control
promotes satiety
augments pancreas response

E.g. Exenatide

Question 6

DPP IV inhibitors

• vildagliptin (reversible)
• sitagliptin (reversible)
• saxagliptin (covalently bound)

Answer 6

e. g.
- vildagliptin (reversible)
- sitagliptin (reversible)
- saxagliptin (covalently bound)

oral hypoglycaemic agents

increased levels of incretins GLP-1 and GIP

cancer risk

Question 7

SGLT 2

Answer 7

High capacity
Low affinity

inhibit glucose transporter in small intestine and proximal straight tubule(90% glucose absorption occurs here)

Dapagliflozin
Canagliflozin

Question 8

SGLT 1

Answer 8

Low capacity
High affinity

found in proximal convulated tubule

Question 9

Effects of SGLT2 Inhibitors

Answer 9

• Increased insulin sensitivity in muscle
• increased insulin sensitivity in liver
• improved beta cell function
• decreased gluconeogenesis

side effects- weight loss, dehydration, can worsen UTI and thrush

Question 10

Insulin

-Hepatic effects

Answer 10

Increases glycogenesis

Inhibits

• gluconeogenesis
• glycogenolysis
• ketogenesis

Question 11

Insulin

-Skeletal muscle effects

Answer 11

increases GLUT 4 translocation=more glucose uptake
increases glucose oxidation, glycogenesis, amino acid uptake, protein synthesis

Decreases:
Glycogenolysis
amino acid release

Question 12

Therapeutic uses

of sulfonylureas

Answer 12

best patient is
over 40 yrs. old
DM duration less than 10 yrs.
daily insulin (if taking) less than 40 units

Question 13

Properties of metformin

Answer 13

• orally active
• does not bind to plasma protein
• excreted unchanged in urine
• also used for PCOS

Question 14

Glitazones (thiazolidinediones)

Answer 14

Activate peroxisome proliferator-activated receptor-g (PPARg)
PPARs involved in transcription of insulin-responsive genes and in regulation of adipocyte lipid metabolism

orally active

Question 15

4 causes of hyperglycaemia

Answer 15

Insulin resistance

B cell dysfunction

Loss of B cell mass

SGLT2 Inhibitors

Question 16

Properties of metformin

Answer 16

orally active
does not bind plasma proteins
excreted unchanged in urine
can be combined

Question 17

What class does exenatide belong to?

Answer 17

GLP 1 analog

Glucagon-like peptide-1 analogs

Question 18

DDP 4 inhibitors

given an example

Answer 18

orally active
cancer risk
few side effects
so GI side effects

increased levels of Incretins GLP-1 and GIP

-sitagliptin