Lipid Lowering Drugs:

Question 1

Atorvastatin:

Answer 1

HMg-CoA reductase inhibitor

• Prevents the conversion of Acetyl- CoA into cholesterol
• Used for secondary prevention
• Generally well tolerated
• Can cause muscle soreness/ weakness
• RARE but serious: may cause Rnhabdomylosis (breakdown of muscles)
• DDI’s are common (metabolized by P450 CYP enzymes)
• Can cause toxicity
• Statins have effects beyond HMg- CoA reduces inhibitor.

Question 2

Ezetimibe:

Answer 2

Inhibits absorption of cholesterol (Cholesterol- Absorption Inhibitor)

• Usually combined with statins to achieve synergy
• Well tolerated

Question 3

Evolocumab:

Answer 3

• PCSK9 Inhibitor
• Binds PCSK9, preventing PCSK9 from binding LDL-R’s.
• Increases LDL-R density
• Leads to lower LDL circulating in the blood
• Lower’s LDL greater than statins
• Administered by injection (monoclonal antibody)
• 10x the price of a statin
• Precaution: We don’t want to drop the LDL levels TOO low

Question 4

Cholestyramine:

Answer 4

• Bile Acid Sequestrant
• Positively charged drug binds negatively charged bile acids where they are EXCRETED (not reabsorbed)
• Causes bile acids to be transported to the liver (and out of the circulation)
• Interacts non- selectively with negative particles (downside)
• AE’s: GI effects: constipation, bloating and nausea

Question 5

Gemfibrozil:

Answer 5

-Fibrate
-Increases HDL precursors (Apo A1, Apo A2 and ABCA)
-Also lowers TG’s by increasing Acyl- CoA synthase (increasing free fatty acid breakdown and decreasing Apo CIII (which leads to TG synthesis)
AE’s: Nausea, Abdominal Pain and RASH
-Low risk for impaired liver function, impaired renal failure, gallstones and pancreatitis)

Question 6

Niacin (Vitamin B3):

Answer 6

-No prescription needed
-Major impacts on HDL and TG’s, but not on LDL
-Increases HDL by reducing it’s breakdown
-Reduces triglyceride synthesis/ release
AE’s: Flushing due to prostaglandin vasodilation.