Lipid lowering drugs

Question 1

Statins 1

Answer 1

• All generic names that end in “statin” are HMG CoA reductase inhibitors
• Prevent the conversion of HMG CoA to mevalonate (key regulatory step in cholesterol synthesis)
• Inhibiting this nz results in less cholesterol formed in the liver

Question 2

Statins 2

Answer 2

• Less cholesterol synthesis leads to unoccupied LDL receptors, and then up regulation of the LDL receptors
• This in turn increases LDL uptake in the liver and thus reduces circulating LDL
• Statins are also anti-inflammatory and can help prevent rupture of plaque, and might prevent alzheimer’s

Question 3

Side effects of statins

Answer 3

• Elevates liver nzs (serum liver transaminases) indicating liver damage
• Must monitor the liver nzs
• Some pts develop muscle weakness (myositis: inflammation of muscle) or rhabdomyolysis (breakdown of muscle)
• Stop statins if muscle symptoms occur

Question 4

Niacin

Answer 4

• Inhibits lipase activity thereby decreasing lipid breakdown and reducing formation of VLDL, LDL, and triglycerides
• Niacin also increases HDL, but this increase does not lower CV risk
• Niacin may decrease risk of AD

Question 5

Administration of Niacin

Answer 5

• Slow release and instantaneous release
• Both types decrease LDL but instantaneous is much more effective at increasing HDL levels
• Slow release niacin has a greater potential for hepatotoxicity so liver nzs must be monitored
• Instantaneous release niacin creates an uncomfortable, itchy flushing reaction (pts can be treated w/ ASA before to prevent)
• Both forms inhibit renal secretion of uric acid leading to gout