2. Hyperlipidemia Treatment

Question 1

HMG-CoA Reductase Inhibitors - Available Drugs

Answer 1

The “statins”

• Lovostatin
• Pravastatin
• Simvastatin
• Atorvastatin
• Rosuvastatin

Question 2

HMG CoA Reductase Inhibitors - MOA

Answer 2

Inhibit cholesterol precursor, mevalonate

• Very large decrease in LDL
• Increase in HDL
• Decrease in TGs

[statins]

Question 3

HMG CoA Reductase Inhibitors - Clinical Use

Answer 3

• Hyperlipidemia

[statins]

Question 4

HMG CoA Reductase Inhibitors - Toxicities

Answer 4

• Hepatotoxicity (Increased liver function tests)
• Rhabdomyolysis (muscle breakdown –> renal failure) especially when used with Fibrates

[statins]

Question 5

Niacin - MOA

Answer 5

Inhibit lipolysis in adipose tissue –> reduces hepatic VLDL secretion into circulation.

• Large decrease in LDL
• Very large increase in HDL
• Decrease in TGs

Question 6

Niacin - Clinical Use

Answer 6

• Hyperlipidemia

Question 7

Niacin - Toxicities

Answer 7

• Red, flushed face (vasodilation) decreased by aspirin or long term use
• —- May interact with antihypertensives
• Hyperglycemia (cause insulin resistance) - acanthosis nigricans
• —- May need to increase diabetes medications in diabetics
• Hyperuricemia - gout exacerbation

Question 8

Bile Acid Resins - Available Drugs

Answer 8

• Cholestyramine
• Colestipol
• Colesevelam

Question 9

Bile Acid Resins - MOA

Answer 9

Prevent intestinal reabsorption of bile acids –> liver uses cholesterol to make more

• Large decrease in LDL
• Slight increase in HDL
• Slight increase in TGs

[Cholestyramine, Colestipol, Colesevelam]

Question 10

Bile Acid Resins - Clinical Use

Answer 10

• Hyperlipidemia

[Cholestyramine, Colestipol, Colesevelam]

Question 11

Bile Acid Resins - Toxicities

Answer 11

• Patients hate it - tastes aweful and causes GI discomfort
• Decreased absorption of fat soluble vitamins
• Cholesterol gallstones especially when used with Fibrates

[Cholestyramine, Colestipol, Colesevelam]

Question 12

Ezetimibe - MOA

Answer 12

Prevent cholesterol reabsorption at the small intestine brush border.

• Large decrease in LDL
• No effect on HDL
• No effect on TGs

Question 13

Ezetimibe - Clinical Use

Answer 13

• Hyperlipidemia

Question 14

Ezetimibe - Toxicities

Answer 14

• Rarely increased Liver function tests.

Question 15

Fibrates - Available Drugs

Answer 15

• Gemfibrozil
• Clofibrate
• Bezafibrate
• Fenofibrate

Question 16

Fibrates - MOA

Answer 16

Upregulate lipoprotein lipase (LPL) –> Incresed TG clearance

• Slight decrease in LDL
• Slight increase in HDL
• Very large decrease in TGs

[Gemfibrozil, Clofibrate, Bezafibrate, Fenofibrate]

Question 17

Fibrates - Clinical Use

Answer 17

• Hyperlipidemia

[Gemfibrozil, Clofibrate, Bezafibrate, Fenofibrate]

Question 18

Fibrates - Toxicities

Answer 18

• Myositis, especially when used with Statins
• Hepatotoxicity - elevated LFTs
• Cholesterol gallstones especially when used with Bile acid binding resins

[Gemfibrozil, Clofibrate, Bezafibrate, Fenofibrate]