Statin Medications: Cholesterol Drug Review for the PTCE

What Are Statins?

Statins, also called HMG-CoA reductase inhibitors, are the most widely prescribed class of cholesterol-lowering medications. They work by blocking the enzyme HMG-CoA reductase in the liver, which reduces cholesterol production and increases LDL receptor expression. This leads to lower LDL ("bad") cholesterol and modestly higher HDL ("good") cholesterol.

Common Statins (Generic / Brand)

• Atorvastatin (Lipitor) - Most prescribed statin, high potency
• Rosuvastatin (Crestor) - Highest potency statin
• Simvastatin (Zocor) - Moderate potency, important drug interactions
• Pravastatin (Pravachol) - Fewer drug interactions (not CYP3A4 metabolized)
• Lovastatin (Mevacor) - Take with evening meal for best absorption
• Fluvastatin (Lescol) - Lower potency
• Pitavastatin (Livalo) - Minimal CYP metabolism

Key Side Effects

• Myopathy and rhabdomyolysis - Muscle pain, weakness, and in rare cases, breakdown of muscle tissue. Patients should report unexplained muscle pain immediately.
• Hepatotoxicity - Liver function tests should be monitored. Statins are contraindicated in active liver disease.
• Increased blood glucose - Statins may modestly increase blood sugar levels, particularly at higher doses.

Important Drug Interactions

Simvastatin and lovastatin are metabolized by CYP3A4, making them susceptible to interactions with CYP3A4 inhibitors like grapefruit juice, clarithromycin, itraconazole, and certain HIV protease inhibitors. These combinations increase the risk of myopathy. Pravastatin and rosuvastatin have fewer CYP-mediated interactions.

Counseling Points

Most statins should be taken in the evening because cholesterol synthesis peaks at night. However, atorvastatin and rosuvastatin have long half-lives and can be taken at any time. Avoid grapefruit with simvastatin and lovastatin. Report any muscle pain or dark urine promptly.

Statin questions are high-yield on the PTCE. Know the brand-generic pairs and key interactions.