Gemfibrozil

To what drug class does gemfibrozil belong?
- "Fibrates" -
- Fibric acid antilipemics
- PPAR-alpha antagonists
What is PPAR-alpha?

A nuclear transcription factor.
True or false?

The active site of gemfibrozil's chemical structure resembles a fatty acid.

True
What are the indications associated with gemfibrozil?

Types IV and V hyperlipidemia
True or false?

Gemfibrozil is more effective than statins, and the statins tend to be add-ons or alternative therapies to the fibrates.

False.

Fibrates are typically alternatives or add-ons to the statins.
What is gemfibrozil's target MOA?
- Activates (agonist) PPAR-alpha and PPREs
- Mimics free fatty acids
Where is PPAR-alpha expressed in the body?
- Hepatocytes
- Skeletal muscle
- Macrophages
- Heart
How does gemfibrozil's MOA lead to decreased triglycerides in the body?
- Increased muscle cell expression of LPL
- Increased uptake of triglyceride rich lipoproteins
- Decreased hepatic expression of ApoC-III (inhibitor of LPL)
- Increased transcription of apoA-I and II (HDL apolipoproteins)
Type IV hyperlipidemia is characterized by?
Type V?
- IV: hypertriglyceridemia
- V: high VLDL and chylomicrons
What are some adverse effects associated with gemfibrozil?
- GI discomfort (most common)
- Gallstone formation (with older drugs from class)
- Myopathy
- Arrhythmia
The three overall outcomes from activation of PPAR-alpha by gemfibrozil are...
- 1.) Increased plasma HDL
- 2.) Decreased plasma triglycerides
- 3.) Decreased triglyceride synthesis

Author

jdonaldson

73757

Card Set

Gemfibrozil

Description

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Updated

2011-03-19T00:22:21Z

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