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Questions and Answers
What is the mechanism of action of statins?
What is the mechanism of action of statins?
What is the result of inhibiting HMG-CoA reductase by statins?
What is the result of inhibiting HMG-CoA reductase by statins?
How should statins be administered when used in combination with bile acid sequestrants?
How should statins be administered when used in combination with bile acid sequestrants?
What is the compensatory mechanism resulting from inhibition of HMG-CoA reductase by statins?
What is the compensatory mechanism resulting from inhibition of HMG-CoA reductase by statins?
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What is the role of statins when used in combination with niacin or ezetimibe?
What is the role of statins when used in combination with niacin or ezetimibe?
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Study Notes
Mechanism of Action of Statins
- Statins inhibit HMG-CoA reductase, a rate-limiting enzyme in the mevalonate pathway, thereby reducing hepatic cholesterol synthesis
- This leads to increased clearance of low-density lipoprotein (LDL) cholesterol from the bloodstream, resulting in decreased serum LDL levels
Inhibiting HMG-CoA Reductase
- Inhibiting HMG-CoA reductase reduces the production of mevalonate, a precursor to cholesterol
- This reduction in mevalonate leads to increased expression of LDL receptors, enhancing LDL uptake in the liver
Administering Statins with Bile Acid Sequestrants
- When used in combination with bile acid sequestrants, statins should be administered at least 2 hours before or 4-6 hours after taking the sequestrant
- This timing helps minimize the potential for reduced statin absorption due to bile acid sequestration
Compensatory Mechanism
- Inhibition of HMG-CoA reductase by statins induces an increase in HMG-CoA reductase expression, a compensatory response to maintain cholesterol synthesis
- This compensatory mechanism can lead to drug resistance and decreased statin efficacy over time
Combination Therapy with Niacin or Ezetimibe
- Statins can be used in combination with niacin to enhance LDL reduction and improve high-density lipoprotein (HDL) levels
- Combination therapy with ezetimibe, an intestinal cholesterol absorption inhibitor, can further reduce LDL levels and improve cardiovascular outcomes
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Description
Test your knowledge of the mechanism of action of antihyperlipidemic agents, particularly statins and HMG-CoA reductase inhibitors. Understand how these medications inhibit cholesterol biosynthesis in the liver.
