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Pharmacology · single question

What is the mechanism of action of rosuvastatin (Crestor)?

  1. Inhibits ACE to reduce angiotensin II
  2. Inhibits HMG-CoA reductase, reducing hepatic cholesterol synthesis and upregulating LDL receptors
  3. Blocks intestinal cholesterol absorption
  4. Activates lipoprotein lipase to break down triglycerides
Show answer and explanation

Correct answer: B. Inhibits HMG-CoA reductase, reducing hepatic cholesterol synthesis and upregulating LDL receptors

  • A. Incorrect. ACE inhibition is the MOA of ACE inhibitors (lisinopril). Not rosuvastatin.
  • B. Correct. Rosuvastatin inhibits HMG-CoA reductase — the rate-limiting enzyme in hepatic cholesterol biosynthesis. This reduces intracellular cholesterol, upregulates LDL receptors on hepatocytes, and increases LDL clearance from blood.
  • C. Incorrect. Cholesterol absorption inhibition is the MOA of ezetimibe. Rosuvastatin acts in the liver on biosynthesis.
  • D. Incorrect. Lipoprotein lipase activation is the MOA of fibrates (gemfibrozil). Not statins.

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