Podcast
Questions and Answers
Which of the following statements about statins is true?
Which of the following statements about statins is true?
What are common adverse effects associated with the use of Ezetimibe?
What are common adverse effects associated with the use of Ezetimibe?
Which drugs may influence the effectiveness of statin therapy?
Which drugs may influence the effectiveness of statin therapy?
What is a primary action of fibrates in lipid management?
What is a primary action of fibrates in lipid management?
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How should the effectiveness of lipid therapy be monitored?
How should the effectiveness of lipid therapy be monitored?
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What is the primary mechanism by which statins reduce plasma LDL levels?
What is the primary mechanism by which statins reduce plasma LDL levels?
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Which of the following statements about contraindications for statins is accurate?
Which of the following statements about contraindications for statins is accurate?
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Which of the following adverse effects is most closely associated with statin therapy?
Which of the following adverse effects is most closely associated with statin therapy?
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Why are lovastatin and simvastatin classified as pro-drugs?
Why are lovastatin and simvastatin classified as pro-drugs?
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What monitoring should be conducted if a patient on statins demonstrates elevated liver enzymes?
What monitoring should be conducted if a patient on statins demonstrates elevated liver enzymes?
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Which medication is least likely to cause rhabdomyolysis when used as an initial statin therapy?
Which medication is least likely to cause rhabdomyolysis when used as an initial statin therapy?
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What effect do statins have on triglyceride and HDL levels?
What effect do statins have on triglyceride and HDL levels?
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Which statin is primarily excreted renally and may pose less risk in patients with renal impairment?
Which statin is primarily excreted renally and may pose less risk in patients with renal impairment?
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What is a notable adverse effect of Niacin therapy that can be reduced by taking ASA prior to its administration?
What is a notable adverse effect of Niacin therapy that can be reduced by taking ASA prior to its administration?
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Why is Niacin no longer recommended as an add-on therapy to statin therapy?
Why is Niacin no longer recommended as an add-on therapy to statin therapy?
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Which of the following conditions is a contraindication for the use of Niacin?
Which of the following conditions is a contraindication for the use of Niacin?
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What is a potential drug interaction of grapefruit juice in relation to lipid medication?
What is a potential drug interaction of grapefruit juice in relation to lipid medication?
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What should be regularly monitored in patients taking fibrates such as Gemfibrozil or Fenofibrate?
What should be regularly monitored in patients taking fibrates such as Gemfibrozil or Fenofibrate?
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Study Notes
Statins
- Most effective agents for lowering LDL cholesterol
- Decrease inflammation and oxidative stress
- Given post-MI even in the presence of normal lipids, and to reduce stroke risk
- Lovastatin and simvastatin are pro-drugs
- All have a high first-pass extraction rate.
- Cause partial inhibition of HMG CoA reductase
- Cause the liver to upregulate LDL receptors, reducing plasma LDL levels
- Not very effective in patients lacking functional LDL receptors (type IIa)
- Also decrease triglycerides and increase HDL
- Effective as monotherapy, but often combined with bile acid resins
- Absolutely contraindicated in pregnancy or breastfeeding women, and liver disease (pravastatin is excreted renally and may be less of a problem)
- Lovastatin (Mevacor), Atorvastatin (Lipitor), Fluvastatin (Lescol), Pravastatin (Pravachol), and Simvastatin (Zocor), Rosuvastatin (Crestor)
- Fluvastatin, pravastatin, and Rosuvastatin are less lipophilic and may have fewer side effects
- Extended dosing intervals may be helpful (e.g., every other day)
- Adverse Effects:
- Elevation of Liver Enzymes
- Often intermittent
- Does not usually require discontinuation
- Exception: Patients with liver disease or Hx of alcohol abuse
- Monitoring of enzyme levels periodically
- If enzymes elevated > 3X normal, this suggests severe hepatotoxicity, discontinue
- Muscle pain and weakness
- Can indicate rhabdomyolysis (serious condition that can cause kidney failure)
- Can occur with monotherapy
- Risk increases with other drugs
- Creatine kinase activity monitored in this case
- Patients should report muscle pain or weakness immediately
- Simvastatin 80mg not as initial therapy due to a high incidence of rhabdomyolysis
- Elevation of Liver Enzymes
- Administered orally
Cholesterol Absorption Inhibitors
- Ezetimibe (Zetia)
- Inhibits absorption of ingested cholesterol and recycling of bile acids
- Weak as monotherapy, often combined with other agents (statins)
- Hypersensitivity
- Adverse Effects: less hepatotoxicity than other drugs, less incidence of myositis
- Infection and respiratory disorders, coughing, sinusitis
- Administered orally as a pro-drug
- Fibrates can increase levels, bile acid resins will decrease
- Can potentiate statin myositis and liver enzyme elevations from statins
PCSK9 Inhibitors
- Decrease degradation of LDL Receptors in hepatocytes
- Results in an increase in recycled receptors inserted into the cell surface
- Increases LDL uptake from blood
- Injectable
- Large reductions in LDL
- Approved for familial hypercholesterolemia (heterozygous and homozygous forms)
- Evolocumab (Repatha) approved for CV disease (heart attack or stroke) if additional cholesterol lowering is required
- Alirocumab (Praluent) approved for CV disease if additional cholesterol reductions are needed
- Very costly (over 10,000/year)
Niacin (Nicotinic Acid)
- Decreases LDL and VLDL, large increases in HDL
- Inhibits VLDL secretion which decreases LDL production
- Increases in VLDL clearance decreases triglycerides
- Stimulates lipoprotein lipase increasing hydrolysis of VLDL
- Often used in combination with other agents
- Large doses required for efficacy
- Uses: lower triglycerides and hyperlipoproteinemia
- Adverse Effects:
- Flushing and warmth due to cutaneous vasodilation
- ASA 30 min prior will reduce
- Diminishes with time but alcohol ingestion worsens
- Nausea, abdominal pain
- Elevations in blood glucose
- Avoid in PUD
- Liver enzyme elevations
- Toxicity rare, but warrants discontinuation
- Rhabdomyolysis in combination with statins
- Hyperuricemia, arrhythmias
- Severe hyperglycemia in diabetics
- Potentiates the action of antihypertensives
- Contraindicated in gout, rhabdomyolysis, PUD, bleeding, liver disease
- Flushing and warmth due to cutaneous vasodilation
Fibrates
- Gemfibrazole (Lopid), fenofibrate (Tricor)
- Peroxisome Proliferator-Activated Receptor (PPAR) ligands
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