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Atorvastatin (Lipitor®)
| Drug Overview | |
|---|---|
| Drug Class | Statins |
| Mechanism | HMG-CoA Reductase Inhibitor |
| Primary Uses | ASCVD Prevention; Hyperlipidemia |
| Route | Oral |
| Dose Range | 10–80 mg daily |
| Intensity | Moderate–High |
| LDL Reduction | 35–60% |
| Metabolism | CYP3A4 |
| Half-life | ~14 hours (active metabolites longer) |
| Elimination | Hepatic |
| Renal Adjustment | No |
| Black Box Warning | No |
| FDA Approval | 1996 |
Overview
Atorvastatin is a high-potency statin used for LDL reduction and prevention of atherosclerotic cardiovascular disease.
It is one of the most commonly prescribed statins and has strong outcome data in both primary and secondary prevention.
It is considered a cornerstone therapy in cardiovascular risk reduction.
Mechanism of Action
Primary Target:
- HMG-CoA reductase (rate-limiting enzyme in hepatic cholesterol synthesis)
Physiologic Effects:
- ↓ Hepatic cholesterol production
- ↑ LDL receptor expression
- ↑ LDL clearance from circulation
Net Effect:
- Significant LDL reduction
- Plaque stabilization
- Reduced cardiovascular events
LDL reduction is dose-dependent.
Indications
- Secondary prevention after:
Dosing
Moderate-Intensity:
- 10–20 mg daily
High-Intensity:
- 40–80 mg daily
No renal adjustment required.
Dose selection is based on ASCVD risk category.
Adverse Effects
Muscle:
- Myalgias
- Myositis
- Rare rhabdomyolysis
Hepatic:
- Mild ALT elevation
Metabolic:
- Slight increase in diabetes risk
Risk increases with:
- High dose
- CYP3A4 inhibitors
- Combination with Gemfibrozil
Drug Interactions
Metabolized by CYP3A4.
Interaction risk with:
- Macrolide antibiotics
- Azole antifungals
- Protease inhibitors
- Grapefruit juice
Higher myopathy risk when combined with:
Monitoring
- Lipid panel (4–12 weeks after initiation)
- Liver enzymes (baseline; repeat if clinically indicated)
- Monitor for muscle symptoms
Routine CK monitoring is not required unless symptomatic.
Comparison Within Class
Compared to Rosuvastatin:
- Slightly less potent per mg
- Higher CYP interaction burden
- More lipophilic
Compared to Pravastatin:
- More potent
- Greater LDL reduction
- More drug interactions
Clinical Role:
- Excellent first-line high-intensity option
High-Yield Pearls
- Strong outcome data in secondary prevention
- High-intensity therapy reduces events significantly
- No renal dosing adjustment
- CYP3A4 interactions are clinically important
- Discontinuation increases ASCVD risk