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FIU - PPAR drugs
PPAR drugs
7
Pharmacology
Graduate
12/16/2011

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Cards

Term
PPAR-alpha, ligands
Definition
fatty acids or fibrates
Term
PPAR-alpha mechanism of action
Definition
dimerizes w/ RXR -> migration to nucleus -> bind to PP-response element on DNA -> transcription of gene for lipoprotein lipase (FA catabolism)
Term
PPAR-gamma ligands
Definition
prostaglandins, leukotrienes and "-glitazones"
Term
PPAR-gamma mechanism of action
Definition
dimerizes w/ RXR -> migration to nucleus -> binding with PP-response element -> transcription of genes involved in storage of FAs and others -> increased insulin sensitivity
Term
-fibrates, effect? SEs?
Definition
fibric acid derivatives
all end in -fibrate EXCEPT gemfibrizol
activate PPAR-alpha
main effect - Decrease TGs
SEs - when combined w/ statins -> rhabdomyolysis -> renal failure
Term
-glitazones, effect? SEs? benefits?
Definition

thiazolidinediones

activate PPAR-gamma

Tx of Type II DM - improved sensitivity to insulin

some affinity for PPAR alpha, so also decrease TGs

SEs - edema and heart failure

*do not cause hypoglycemia (like SUs and repaglinide), but slow onset

Term
HbA1C, target value?
Definition
glycated hemoglobin
provide estimate of blood sugar over past 3-4 months
HbA1C < 7 (= average blood sugar of 150mg/dl)
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