Pharmacology: Thiazolidinediones(TZDs) Flashcards Preview

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Flashcards in Pharmacology: Thiazolidinediones(TZDs) Deck (16)
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1

describe the molecular mechanism of TZDs

they are PPARgamma ligands, they bind to the PPARgamma gene and results in formation of complex with a co-activator

2

what effect do TZDs have on the target PPARgamma genes

increase transcriptional activation

3

how many target genes are there for TZDs

100s, some beneficial some adverse

4

what type of cells do TZDs mainly effect

adipocytes

5

what is the net result of TZDs activity

increased insulin sensitivity

6

describe the effect of TZDs on adipocytes

increase differentiation from pre-adipocytes to adipocytes, increases subcutaneous fat mass, increases adiponectin

7

describe the action of adiponectin

acts on liver to increase insulin sensitivity

8

describe what the action of 'lipid steal' is as part of TZDs actions

when free fatty acid uptake removes fat from liver and muscle, reducing lipotoxicity

9

what are TZDs also known as

glitazones

10

how potent are TZDs

quite potent 15-20mmol/mol HbAC1 reduction, esp in obese women

11

what effect to TZDs have on weight and why

weight gain(2-3kg), due to increase fat mass and fluid retention

12

what effect to TZDs have on BP

lower it, SBP by around 4.7 and DBP by around 3.8

13

what is the only available TZD, and what dose is used

pioglitazone, 15-30mg od

14

what side effects may be seen with TZD use

weight gain, fluid retention(eg peripheral oedema), fracture risk

15

why is there an increased fracture risk with TZD use

increased fat accumulation in bone marrow and decreased bone density

16

describe where TZDs are used in T2DM treatment pathway

second line(after first line metformin)
used when compelling need to reduce hypoglycaemia or when cost is major issue(very cheap)