Ch 20: Inhibitors of Cholesterol Synthesis
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Questions and Answers

What is the role of statins in cholesterol synthesis?

  • Competitively inhibit HMG-CoA reductase (correct)
  • Activate SREBP2 directly
  • Enhance cholesterol concentration in cells
  • Inhibit LDL receptor gene transcription

What is the consequence of decreased cellular cholesterol concentration?

  • Inhibition of LDL receptor gene expression
  • Inhibition of HMG-CoA reductase
  • Activation of SREBP2 (correct)
  • Activation of cholesterol synthesis

What is the function of SREBP2 in the context of cholesterol regulation?

  • Inhibits HMG-CoA reductase activity
  • Increases cellular cholesterol concentration
  • Down-regulates expression of the gene encoding the LDL receptor
  • Up-regulates expression of the gene encoding the LDL receptor (correct)

What is the consequence of increased LDL receptor expression?

<p>Increased uptake of plasma LDL (D)</p> Signup and view all the answers

What indicates true hepatotoxicity?

<p>Elevations in ALT and AST accompanied by elevations in serum bilirubin concentrations (A)</p> Signup and view all the answers

Which combination results in additive LDL decreases without significant drug interactions?

<p>Statin with a bile acid sequestrant or cholesterol absorption inhibitor (B)</p> Signup and view all the answers

What should be closely monitored when co-administering niacin and a statin?

<p>Development of adverse effects (C)</p> Signup and view all the answers

Which fibrate inhibits both the transport and glucuronidation of statins in the liver?

<p>Gemfibrozil (C)</p> Signup and view all the answers

Which type of statin is preferable in patients taking drugs metabolized by cytochrome P450?

<p>Statin that is not metabolized by P450 enzymes (C)</p> Signup and view all the answers

What may increase the risk of rhabdomyolysis when combined with certain fibrates?

<p>Gemfibrozil (B)</p> Signup and view all the answers

In what type of patients may the combination of niacin and a statin be most useful?

<p>Patients with high levels of LDL cholesterol and low levels of HDL cholesterol (A)</p> Signup and view all the answers

What combination has been reported to be efficacious but may decrease statin clearance?

<p>Fibrates and statins (B)</p> Signup and view all the answers

What is the effect of statins on LDL-cholesterol concentrations?

<p>Reduce by up to about 60% (B)</p> Signup and view all the answers

What is a potential adverse effect of high-potency statins?

<p>Myopathy and/or myositis with rhabdomyolysis (D)</p> Signup and view all the answers

What is the effect of statins on triglyceride concentrations?

<p>Reduce by up to about 40% (D)</p> Signup and view all the answers

What is the mechanism of action of statins?

<p>Reduction of cholesterol synthesis (C)</p> Signup and view all the answers

What is the effect of statins on mortality after a myocardial infarction in primary prevention?

<p>Reduced (B)</p> Signup and view all the answers

What is the primary adverse effect of statins?

<p>Myopathy and/or myositis with rhabdomyolysis (D)</p> Signup and view all the answers

What is the relationship between statin dose and LDL reduction?

<p>Each subsequent doubling of the dose produces an additional 6% LDL reduction (D)</p> Signup and view all the answers

What is the effect of statins on high-risk patients with average or below average LDL-cholesterol levels?

<p>Effective in reducing cardiovascular disease risk (C)</p> Signup and view all the answers

What is the effect of statins on HDL-cholesterol concentrations?

<p>Increase by 10% (B)</p> Signup and view all the answers

What is the evidence for diminished inflammation with statin therapy?

<p>Decreases in acute-phase reactants such as C-reactive protein (C)</p> Signup and view all the answers

What may certain patients with a molecular variant of an organic anion transporter be at higher risk of developing?

<p>Statin-induced myopathy (C)</p> Signup and view all the answers

What is the effect of statins on serum transaminase levels?

<p>High-potency statins can cause increases in serum transaminase levels (D)</p> Signup and view all the answers

Study Notes

Statins and Their Effects

  • Statins have been shown to significantly reduce mortality after a myocardial infarction in both secondary and primary prevention.
  • Statin use is associated with a greater absolute risk reduction in secondary prevention due to higher absolute risk of death in this group.
  • Statins are effective in reducing cardiovascular disease risk for high-risk patients, even with average or below average LDL-cholesterol levels.
  • Statins reduce LDL-cholesterol concentrations by up to about 60%, increase HDL-cholesterol concentrations by 10%, and reduce triglyceride concentrations by up to about 40%.
  • The dose–response relationship of statins is nonlinear, with each subsequent doubling of the dose producing an additional 6% LDL reduction.
  • Statins have pleiotropic effects, including decreased inflammation, reversal of endothelial dysfunction, decreased thrombosis, and improved stability of atherosclerotic plaques.
  • Evidence for diminished inflammation with statin therapy includes decreases in acute-phase reactants such as C-reactive protein.
  • Statins are believed to act by the same mechanism, but differences in potency and pharmacokinetic parameters exist among the seven approved statins.
  • Statins are generally well tolerated, with the main adverse effect being myopathy and/or myositis with rhabdomyolysis, primarily at high doses of the most potent statins.
  • High-potency statins can also cause increases in serum transaminase levels.
  • Plasma creatine kinase levels are not useful for routine monitoring of statin-treated patients.
  • Certain patients with a molecular variant of an organic anion transporter may be at higher risk of developing statin-induced myopathy.

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Test your knowledge of statins and their effects with this quiz. Explore the benefits, dosage relationships, pleiotropic effects, adverse effects, and monitoring considerations of statin therapy.

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