Dyslipidemia Medications

Question 1

Atorvastatin (Lipitor)

Answer 1

Statins
Decreasing the rate of cholesterol synthesis also increases LDL receptors on the liver, thus clearing more LDL from plasma.
Know that statins also have some anti-inflammatory/plaque stabilizing properties. Know they are the most effective medications for lowering LDL and Total Cholesterol.
• Indication: Hypercholesterolemia, primary and secondary CHD prevention in at-risk patients, hypertriglyceridemia in patients who already have hypercholesterolemia
• Mechanism: HMG-CoA reductase inhibitor (see Summary Slide)
• Elimination: hepatic metabolism via the CYP3A4 pathway, excreted in bile and urine.
• Metabolized via CYP3A4
• Adverse effects: myalgias, myopathy, rhabdamyopathy
• Interaction: Clarithromycin
• Pregnancy Category X
• Co-administration with fibrates increases risk of muscle injury
• Teaching points: Avoid drinking grapefruit juice, especially in large amounts, increase serum levels of atorvastatin

Question 2

Gemfibrozil (Lopid)

Answer 2

Fibrate
o Indication: elevated TGs
o Mechanism: mechanism of action is as PPARα (peroxisome proliferator-activated alpha) agonists and that they are primarily used to reduce triglyceride levels.
o Elimination: liver metabolism, excretion in urine and feces
o Adverse Effects: rash, GI upset, gallstones, hepatotoxicity (monitor LFTs), myopathy. Contraindicated in severe kidney disease.
o Interactions: statins (increased risk of myopathy), warfarin (increased anticoagulation effects)

Question 3

Niacin

Answer 3

o Indication: elevated TGs, mixed hyperlipidemia
o Mechanism: Reduces LDL and TGs and increases HDL via multiple MOAs (see Summary slide). MULTIPLE
o Metabolism: Hepatic metabolism, excreted mainly in urine
o Adverse Effects: facial flushing, nausea/vomiting, liver toxicity (monitor LFTs), hyperglycemia, gouty arthritis
o Flushing is minimized in extended-release forms, but still present. It tends to decrease over the first month of therapy. It can be diminished by taking 325 mg. of aspirin 30 min. before therapy – but this carries risks for GI bleed.

Question 4

Omega-3-acid ethyl esters (fish oil) (Lovaza)

Answer 4

o Indication – elevated TGs (> 500). Can reduce TGs 20% to 50%. Adjunct to diet.
o Side/adverse effects: burping, GI upset, change in sense of taste. Caution if fish or shellfish allergy. Elevation of ALT, can raise LDL in some patients.
o Cautions: Lovaza (and any fish oil supplements) have anti-platelet properties and can prolong bleeding time. It should be discontinued prior to surgery!
o Interactions: Any anti-platelet or anti-coagulant medication – can increase bleeding risks