thiazolidinedones Flashcards
what are TZDs?
PPAR gamma agonists
what is PPAR gamma?
a transcription factor
what does TZD binding to PPAR gamma cause?
the formation of a complex with a co activator, leading to transcriptional activation of PPAR gamma target genes (there are 100s of these)
what is the main effect of TZD?
on adipocytes, ultimately leading to insulin sensitivity on the liver
what is the other name of TZDs?
glitazones
where is fat mass increased as a result of TZD?
in subcutaneous depots and to “suck out” fat from viscera (liver and pancreas) and muscle
does TZD lead to increased or reduced inflammatory cytokines?
reduced
is adiponectin reduced as a result of TZD?
No
in who are TZDs particularly effective?
obese women
do TZDs lead to an increase in weight?
yes due to fat mass and fluid retention
what does TZD lead to a reduction in?
blood pressure
what is the only available TZD?
pioglitizone
what is the normal dose of pioglitazone?
15-30mg od
what are the main side effects of TZDs?
weight gain
fluid retention (results in peripheral oedema and doubles risk of hospitalisation of HF)
fracture risk due to fat accumulation in bone marrow (up to double the risk)
are TZDs used in Over 65s?
no, only very rarely with proper cardiac and fracture risk assessment