Learning Objective:

By the end of this section, learners should be able to describe the mechanism of action, classify statins by intensity, identify their effects on lipid profiles, recognize common adverse effects, and understand important drug interactions.

Drugs & Intensity Classification

• Common Statins:
  • Atorvastatin,
  • Rosuvastatin,
  • Simvastatin,
  • Pravastatin,
  • and other “statins.”
• High-intensity statins: Atorvastatin and rosuvastatin at their highest therapeutic doses → lower LDL-C by≥50%.
• Moderate/low-intensity statins: Lower doses produce smaller reductions in LDL-C.

Mechanism of Action

• HMG-CoA reductase inhibition in hepatocytes →
  • ↓ hepatic cholesterol synthesis
  • ↑ LDL receptor expression on hepatocytes
  • ↓ plasma LDL cholesterol
• Additional effect: Decreased VLDL synthesis → ↓ triglycerides

Clinical Effects

• Reduction of LDL-C, total cholesterol, and triglycerides
• Stabilization or regression of atherosclerotic plaques
• Primary prevention and secondary prevention of cardiovascular events

Side Effects

• Musculoskeletal: Myalgia, myopathy (monitor creatine kinase)
• Severe: Rhabdomyolysis (rare but life-threatening)
• Hepatic: Hepatotoxicity (monitor liver function tests)

Drug Interactions

• Gemfibrozil: ↑ risk of rhabdomyolysis
• Cytochrome P450 inhibitors (e.g., certain antifungals, macrolides): ↑ statin toxicity

Activity