Cholesterol Medications: Prescription Statins & Cholesterol Absorption Inhibitors to Lower LDL, Total Cholesterol & Cardiovascular Risk

Elevated cholesterol — particularly high LDL (low-density lipoprotein) cholesterol — is one of the major modifiable risk factors for cardiovascular disease, heart attack, and stroke. Cholesterol-lowering medications work through different mechanisms to reduce LDL, total cholesterol, and triglycerides, and in some cases raise HDL (high-density lipoprotein) cholesterol. The most widely prescribed class is the statins (HMG-CoA reductase inhibitors), which remain the cornerstone of pharmacological cholesterol management. All cholesterol medications featured here require a prescription.

Statins: How They Work

Statins inhibit the enzyme HMG-CoA reductase, the rate-limiting step in hepatic cholesterol synthesis. Reduced intracellular cholesterol stimulates upregulation of LDL receptors on liver cells, which remove more LDL from the bloodstream. Statins reduce LDL cholesterol by typically 30–55% depending on the agent and dose, and have proven cardiovascular event reduction (heart attacks, strokes) in clinical outcome trials. They are taken once daily, usually in the evening (except rosuvastatin and atorvastatin, which can be taken at any time).

Cholesterol Medications at Lucas Clinic

• Crestor (Rosuvastatin) 5–40 mg Tablets — the most potent statin by milligram; not metabolised by CYP3A4; once daily at any time
• Lipitor (Atorvastatin) 10–80 mg Tablets — the world’s best-selling prescription medication; metabolised by CYP3A4; once daily at any time
• Zetia (Ezetimibe) 10 mg Tablets — cholesterol absorption inhibitor (not a statin); blocks NPC1L1 in the small intestine; often combined with a statin for additional LDL lowering
• Zocor (Simvastatin) 5–40 mg Tablets — older, widely-used statin; 80 mg dose restricted due to myopathy risk; taken in the evening

Common Statin Side Effects

Myalgia (muscle aches) is the most common complaint, affecting 5–10% of patients. Serious statin-induced myopathy or rhabdomyolysis is rare. Statins require periodic liver function monitoring. They are contraindicated in pregnancy and in active liver disease. Patients should report unexplained muscle pain, tenderness, or weakness to their prescriber.