Exam 1 - Thiazolidinediones (TZDs)

Question 1

What do all drugs in the Thiazolidinediones (TZDs) class end in?

Answer 1

glitazone

Question 2

What are the characteristics of Thiazolidinediones (TZDs) ?

Answer 2

● Not hypoglycemic agent
● MOA : increase tissue insulin sensitivity → enhance the uptake of fatty acids and glucose from plasma to fat/muscle
● Dependent on presence of insulin (does not cause insulin release)
● Activate PPAR­γ which increases transcription of LPL, GLUT­4, others
● Reduce expression of leptin (may increase appetite)

Question 3

Which are the Thiazolidinediones (TZDs) drugs?

Answer 3

Rosiglitazone ( Avandia )

Pioglitazone ( Actos )

Question 4

What are the characteristics of Rosiglitazone ( Avandia ) and Pioglitazone ( Actos )?

Answer 4

● Increases effectiveness of insulin and reduces amount of exogenous l insulin req. by 30%
● Liver Function Test baseline, and at 2 months and every 6­-12 months thereafter
● Slow onset ~ 2 months for max effect
● S.E. = weight gain (2­-10 lbs)
● Fluid retention ( ↑ plasma volume, ↑ extravasular fluid (Bad if CHF pt))
● Increase subcutaneous fat but not visceral fat
● Increased incidence of CHF
● 83% increased risk of bladder cancer w/ pioglitazone
● ↑HDL ↓TG with pioglitazone
● ↑ total cholesterol, ↑HDL ↑LDL with rosaglitazone
● GI disturbances, fatique, headache, contradicted in
pregnancy and breast­feeding
● ↑ bone fractures in women: decreases bone mineral density
● Macular edema