Antihyperlipidemics Flashcards
What is involved in the non-drug approach?
Diet, weight loss, exercise, no smoking or excess alcohol (to much > increased VLDL/TGs); lots of omega-3s
What are the bile acid-binding resins?
Cholestyramine, Colestipol, Colesevelam
What is the MOA of Cholestyramine?
Prevents GI bile acid reabsorption into liver > increased bile production and LDL receptor expression
When would you use Cholestyramine?
To decrease LDL 10-25%, increase HDL 3-5%; second line drugs used in combo with others
What are the side effects of Cholestyramine?
Nausea, bloating, impairs absorption of vitamins ADEK; may increase VLDL < 5% in patients with high TGs
What is the MOA of Colestipol?
Prevents GI bile acid reabsorption into liver > increased bile production and LDL receptor expression
When would you use Colestipol?
To decrease LDL 10-25%, increase HDL 3-5%; second line drug used with others
What are the side effects of Colestipol?
Nausea, bloating, impairs absorption of vitamins ADEK; may increase VLDL < 5% in patients with high TGs
What is the MOA of Colesevelam?
Prevents GI bile acid reabsorption into liver > increased bile production and LDL receptor expression
When would you use Colesevelam?
To decrease LDL 10-25%, increase HDL 3-5%; second line drug used with others
What are the side effects of Colesevelam?
Nausea, bloating; may increase VLDL < 5% in patients with high TGs
What are the statins?
Rosuvastatin, Atorvastatin, Simvastatin, Lovastatin, Pravastatin, Fluvastatin
What is the MOA of Rosuvastatin?
Competitive inhibition of HMG-CoA Reductase > reduced liver cholesterol synthesis. Liver pulls from plasma cholesterol to maintain its levels
When would you use Rosuvastatin?
To decrease LDL 20-60%, increase HDL 5-15%, decrease TGs 10-30%; has the highest potency at 20hr HL
What are the side effects of Rosuvastatin?
Increased ALT/AST and CPK > myopathy; skin rxns; possible carcinogenicity and teratogenicity > NO pregnancy
What is the MOA of Atorvastatin?
Competitive inhibition of HMG-CoA Reductase > reduced liver cholesterol synthesis. Liver pulls from plasma cholesterol to maintain its levels
When would you use Atorvastatin?
To decrease LDL 20-60%, increase HDL 5-15%, decrease TGs 10-30%; 14 hr HL, decreases TG
What are the side effects of Atorvastatin?
Increased ALT/AST and CPK > myopathy; skin rxns; possible carcinogenicity and teratogenicity > NO pregnancy
What is the MOA of Simvastatin?
Competitive inhibition of HMG-CoA Reductase > reduced liver cholesterol synthesis. Liver pulls from plasma cholesterol to maintain its levels
When would you use Simvastatin?
To decrease LDL 20-60%, increase HDL 5-15%, decrease TGs 10-30%; prodrug
What are the side effects of Simvastatin?
Increased ALT/AST and CPK > myopathy; skin rxns; possible carcinogenicity and teratogenicity > NO pregnancy
What is the MOA of Lovastatin?
Competitive inhibition of HMG-CoA Reductase > reduced liver cholesterol synthesis. Liver pulls from plasma cholesterol to maintain its levels
When would you use Lovastatin?
To decrease LDL 20-60%, increase HDL 5-15%, decrease TGs 10-30%; prodrug
What are the side effects of Lovastatin?
Increased ALT/AST and CPK > myopathy; skin rxns; possible carcinogenicity and teratogenicity > NO pregnancy
What is the MOA of Pravastatin?
Competitive inhibition of HMG-CoA Reductase > reduced liver cholesterol synthesis. Liver pulls from plasma cholesterol to maintain its levels
When would you use Pravastatin?
To decrease LDL 20-60%, increase HDL 5-15%, decrease TGs 10-30%; no increased absorption with food
What are the side effects of Pravastatin?
Increased ALT/AST and CPK > myopathy; skin rxns; possible carcinogenicity and teratogenicity > NO pregnancy
What is the MOA of Fluvastatin?
Competitive inhibition of HMG-CoA Reductase > reduced liver cholesterol synthesis. Liver pulls from plasma cholesterol to maintain its levels
When would you use Fluvastatin?
To decrease LDL 20-60%, increase HDL 5-15%, decrease TGs 10-30%; lowest potency
What are the side effects of Fluvastatin?
Increased ALT/AST and CPK > myopathy; skin rxns; possible carcinogenicity and teratogenicity > NO pregnancy
What is the MOA of Ezetimibe?
Inhibits jejunal uptake of cholesterol
When would you use Ezetimibe?
To decrease LDL additional 12-18%; no effect on TGs or HDL; given with simvastati; 2hr before/4hr after bile resins
What are the side effects of Ezetimibe?
GI, headache, muscle/joint pain
What are the Vitamin B3 derivatives?
Nicotinic acid and Niacin
What is the MOA of Nicotinic Acid?
Inhibits adipose lipolysis by blocking lipase > decreased FA supply to liver > decreased VLDL > decreased LDL > increased HDL
When would you use Nicotinic Acid?
To decrease VLDL/TG <50%; decrease LDL 15-30%; increase HDL 15-30%
What are the side effects of Nicotinic Acid?
Peptic ulceration; severe vasomotor flushing, increase insulin resistance, hyperuricemia, gout; increases endothelial/tPA function, decreases fibrinogen
What is the MOA of Niacin?
Inhibits adipose lipolysis by blocking lipase > decreased FA supply to liver > decreased VLDL > decreased LDL > increased HDL
When would you use Niacin?
To decrease VLDL/TG <50%; decrease LDL 15-30%; increase HDL 15-30%; also lowers Lp(a); contraindicated with diabetes, peptic ulcers, liver disease, pregnancy, gout
What are the side effects of Niacin?
Peptic ulceration; severe vasomotor flushing, increase insulin resistance, hyperuricemia, gout
What are the fibric acid derivatives?
Gemfibrozil, fenofibrate
What is the MOA of Gemfibrozil?
Increase liver FA oxidation via LPL > decreased VLDL and TGs; decreased LDLs and increased HDL due to increased apoAI/II
When would you use Gemfibrozil?
To decrease VLDL/TG <30%, decrease LDL 5-20%, increase HDL 10-20%
What are the side effects of Gemfibrozil?
GI, gallstones, increased liver enzymes when used with statins (except rosuvastatin)
What is the MOA of Fenofibrate?
Increase liver FA oxidation via LPL > decreased VLDL and TGs; decreased LDLs and increased HDL due to increased apoAI/II
What are the side effects of Fenofibrate?
Same as gemfibrozil with less GI effects
When would you use Fenofibrate?
To decrease LDL (better than Gemfibrozil)
