Hyperlipidemia Drugs

Question 1

Statin

• Levostatin
• Simvastatin

Answer 1

• most effective and best tolerted
  
  • can use with other drugs
• use:
  
  • inhibit HMG-CoA = dec cholesterol
  • inc affinity LDL receptors in liver
    
    • inc LDL clearance and dec plasma LDLs
• Toxicities:
  
  • possible increase in liver ezymes
  • teratogenic
  • interact with CYP450s

Question 2

Niacin

Answer 2

• act as vit B3 when converted to NAD
• VLDL secretion inhibitor
• use:
  
  • converted nicacin = inhibit VLDL production, secretion
  • inc lipoprotein lipase activity = increase clearance of VLDL
  • raise HDLs
• Toxicities:
  
  • cutaneous flushing and itching
  • elevated liver enzyme
  • Gi distress and ulcers

Question 3

Cholestryamine

Colestipol

Answer 3

• bile acid sequestriants
• oldest and safest drug
• use:
  
  • large pos. charge -> bind bile acid in GI tract lumen = inhibition to reuptake in ileum/jejunum
  • dec bile = inc of bile production in liver = inc LDL uptake and clearance from plasma
  • use if statins don’t ineffective
• Toxicities:
  
  • constipation/bloating
  • interaction with drug b/c charged

Question 4

Gemfimbrozil

Answer 4

• Fibrates (PPAR activator)
• mechanism:
  
  • unclear
  • act on PPAR-a in liver
  • activate -> inc lipoprotein lipase -> dec VLDLs -> inc HDLs
• Toxicities:
  
  • avoid with patients with liver disease
  • high cholesterol gallstones

Question 5

Ezetimibe

Answer 5

• sterol absorption inhibitor
• excreted in bile -> absored -> metabolized
• mechanism
  
  • inhibits intestinal absorption of phytosterols and cholestrol -> dec LDL
    
    • inhibit transport protein NPC1L1 in jejunal enterocytes for uptake cholesterol
    • liver LDL receptors inc -> removal of LDl from plasma
    • bile acid sequestriants will inhibit ezetimibe absorption
    • can use with statins