Drugs to Treat Hyperlipidemia

Question 1

statins

Answer 1

• competitively block HMG-CoA Reductase, the rate-limiting enzyme in cholesterol synth pathway
• also stabilize plaques, reduce inflammation, reverse endothelial dysfunction, decrease thrombogenicity
• risk of bilateral muscle pain, diabetes, hepatitis, cognitive effects
• metabolized via CYP450 pathway

Question 2

ezetimibe

Answer 2

• cholesterol absorption inhibitor that impairs dietary and biliary cholesterol absorption at the brush border of the intestine
• inhibit the Niemann-Pick C1 like 1 (NPC1L1) protein
• risk of hepatitis, rhabdomyolysis

Question 3

• Alirocumab (Praluent®)

- Evolocumab (Repatha®)

Answer 3

• PCSK9-inhibitors

- antibodies against PCSK9 interfere with its binding of the LDL-R, this leads to higher LDL-R and less LDL-C levels

Question 4

• colesevalam
• colestipol
• cholestyramine

Answer 4

Bile Acid Sequestrants

• used to reduce LDL by binding bile acids and preventing their reabsorption
• contraindicated in pts with dysbetalipoproteinemia
• risk of GI effects, vitamin ADEK deficiency, PKU

Question 5

Fibrates

Answer 5

• Fibrates activate PPARɑ to increase the expression of genes that encode enzymes that increase the metabolism of triglycerides and enhances the production of HDL
• risk of hepatitis, GI effects, gallstones, myopathy, presence in breast milk
• many drug interxns: bile acid sequestrants, colchicine…
• GEMFIBROZIL is CYP2C8 inhibitor

Question 6

Niacin

vitamin B3

Answer 6

• lowers VLDL and LDL, antioxidant

- risk of flushing, blood glucose elevation, uric acid elevation, hepatitis, and muscle toxicity, prolonged PT