-
Statins
- - First-line therapy for lowering LDL
- - HMG-CoA reductase inhibitors
- - Reduce production of VLDL/IDL/LDL
- - Increase expression of LDL-R
- - Contraindicated in liver disease, pregnancy/nursing
- - Muscle-toxicity (esp. high doses, interacting meds)
-
Lovastatin
- - Low potency
- - CYP3A4 metabolism
-
Simvastatin
- - Low potency
- - CYP3A4 metabolism
-
Pravastatin
- - Low potency
- - Not metabolized by CYP450 enzymes
-
Fluvastatin
- - Low potency
- - CYP2C9 metabolism
-
Atorvastatin
- - High potency
- - CYP3A4 metabolism
-
Rosuvastatin
- - High potency
- - CYP2C9 metabolism
-
Pitavastatin
- - Medium potency
- - CYP2C9, CYP2C8 metabolism
-
Bile Acid Sequestrants (aka Resins)
- - Add-on therapy to statins or Monotherapy for pt's who can't tolerate statins
- - Bind to/promote excretion of bile acids in intestinal lumen
- - Increase bile acid production
- - Increase expression of LDL-R
- - Contraindicated in elevated TG > 400
- - Constipation + drug interactions
-
Cholestyramine
- Bile acid sequestrant
-
Cholestipol
- Bile acid sequestrant
-
Colesevelam
- Bile acid sequestrant
-
Niacin
- - Add-on therapy to statins
- - Decrease TG synthesis in liver
- - Decreases FFA --> liver, decreased TG & VLDL/IDL/LDL
- - Increases HDL
- - Facial flushing
- - IR, SR, ER formulations
-
Fibrates
- - First-line therapy for lowering TG
- - PPARα agonist
- - Upregulate LPL, which breaks down TG's to FFA's
- - Contraindicated in severe liver disease
- - Myopathy (esp. Gemfibrozil + statin)
- - Increase effects of Warfarin
- - Dose-adjusted for renal function
-
Gemfibrozil
- - Fibrate
- - Increased risk of myopathy + statins
-
Fenofibrate
- - Fibrate
- - No increased risk of myopathy + statin
-
Cholesterol Absorption Inhibitor
- - Add-on therapy to statins for lowering LDL (~18%)
- - Impacts NPC1L1 sterol transporter
- - Reduces absorption of cholesterol at small intestine brush border
- - Upregulation of LDL-R
- - Contraindicated in severe liver disease
-
Ezetimibe
- Cholesterol absorption inhibitor (only one)
-
Fish oils (Omega-3 FA's)
- - EPA & DHA
- - Decrease TG's (4g/day)
- - Decrease risk of sudden cardiac death (~1 g/day)
- - Smelling of fish
- - Better absorbed with food
- - Read the label to acheive needed dose
-
Plant Sterols
- - Competitively block cholesterol aborption in small intestines
- - Naturally occurring in plants + margarine/chews
- - TLC diet recommends 2 g/day
- - Difficult to acheive this dose
|
|
