Fibric acid derivaties and Niacin Flashcards
Drugs
Clofibrate
Gemifibrozil
Fenofibrate
M.O.A
Activates PPAR-a -> Regulates gene transcription -> decrease TG & LDL-C - increase HDL-C
Effects
- Mediate expression of lipoprotein lipase
- Catalyze hydrolysis & removal of TG from VLDL
- Decrease expression of apolipoprotein C
- Decrease Expression enzyme oxidizing fatty acids
- Mediate expression of A-1 & A2
- Increase expression of cholesterol transport proteins
Indications
- Prevent Pancreatitis (very high TG levels)
- Reduce risk CHD
- Lipidemia - not improved by life changes and drugs
Adverse Effects
G.I - Most common
Blood cell deficiencies
Hypersensitivity
Myopathy & Rhabdomyolysis - Avoid w/statins
Niacin (Vitamin B3) - M.O.A
Inhibits formation & secretion hepatic VLDL
G protein - coupled receptor binding
-> - Decreased LDL-C,
- Lipoprotein (a) (consistet decrease, only niacin)
- Decrease TG
- Increased HDL-C & HDL2
Niacin - Indications
Primary hyperlipidemia
Mixed dyslipidemia
Reduce risk pancreatitis(very high TG)
Reduce risk M.I - Men w/H.cholesterolemia & atherosclerosis
Niacin - Adverse
High doses:
Flushed skin
Pruritus
(Pretreatment w/aspirin or adm sustained release prep)
Hepatitis
Hyperuricemia & Gout
Gi distress - aggravate PUD
Increased blood glucose - Aggravate DM