Week 2: lipid lowering drugs

Question 1

What is the mechanism of statin drugs?

Answer 1

• inhibit HMG CoA reductase, which catalyzes HMG CoA to mevalonate in the synthesis of cholesterol
• less cholesterol is formed by liver, more LDL receptors left unoccupied and are unregulated, more receptors to take up cholesterol, which reduces amount of circulating cholesterol.

Question 2

What are side effects of statin drugs?

Answer 2

• liver: may cause rise in liver enzymes, indicating liver damage
• muscles: pain and/or weakness of muscles, myositis or rhabdomyolysis.

Question 3

What is the mechanism of niacin-nicotinic acid in lowering lipids?

Answer 3

• inhibits lipase activity, decreasing breakdown of lipids and lowering formation of LDL and VLDL.
• increases HDL, but has no effect in lowering CV risk

Question 4

What are the side effects of niacin?

Answer 4

• slow release niacin: greater potential for hepatotoxicity, must monitor liver enzymes
• instantaneous release niacin: flushing
• both inhibit renal tubular secretion of uric acid–>gout