Catapult Pharmacology

Catapult Pharmacology

Fibrates

Fibrates are used in the treatment of hypertriglyceridemia.  Fibrates activate PPARs, which are transcription factors.  PPARs increase production of HDL and decrease levels of triglycerides.  These medications can stimulate gallstone formation and myositis. Gemfibrozil should not be used with statins due to increased risk of rhabdomyolysis.

Class Drugs

  • Fenofibrate

  • Gemfibrozil

Class Mechanism of Action

Activates transcription factors called PPARs (peroxisome proliferator-activated receptors)

  • The activated PPARs increase HDL by induction of transcription of apolipoproteins (apoA-I and apoA-II) that increase production of HDL

  • The activated PPARs decrease triglycerides by induction of transcription of genes for lipoprotein lipase and decreasing transcription of apoC-III. Fibrates stimulate uptake of fatty acids.

  • LDL production is decreased due to decreased levels of triglycerides

Class Applications

Hypertriglyceridemia

  • Generally used as a second agent in severe hypercholesterolemia or in familial hyperlipidemia

Class Adverse Effects

  • GI disturbance

  • Gallstone formation

  • Myositis

  • Avoid concomitant therapy of gemfibrozil with statins due to possibility of development of rhabdomyolysis

Drug Table

Drug Name Application Comments Image
Fenofibrate "Fence" "Fiber Bars"
Gemfibrozil "Gems" "Fiber Bars"