Half-Life of Rosuvastatin (Crestor)
Rosuvastatin has a half-life of approximately 19 hours, which is among the longest half-lives of all statin medications. 1
Pharmacokinetic Properties of Rosuvastatin
Rosuvastatin has several key pharmacokinetic characteristics that distinguish it from other statins:
- Elimination half-life: 19 hours 1
- Absorption: Peak plasma concentrations reached 3-5 hours after oral dosing 1
- Bioavailability: Approximately 20% 1
- Distribution: Mean volume of distribution at steady-state is approximately 134 liters 1
- Protein binding: 88% bound to plasma proteins, mostly albumin 1
- Metabolism: Not extensively metabolized; only about 10% of a dose is recovered as metabolite 1
- Excretion: Primarily excreted in feces (90%) 1
Comparison to Other Statins
Rosuvastatin's long half-life provides several clinical advantages:
| Statin | Half-life (hours) |
|---|---|
| Rosuvastatin | 19 |
| Atorvastatin | 14 |
| Pitavastatin | 12 |
| Fluvastatin | 3 |
| Simvastatin | 2-3 |
| Pravastatin | 1.8 |
Clinical Implications of Rosuvastatin's Long Half-Life
The extended half-life of rosuvastatin offers several clinical benefits:
- Sustained lipid-lowering effect: The long half-life contributes to rosuvastatin's potent and sustained lipid-lowering effects 3
- Once-daily dosing: The pharmacokinetic profile supports convenient once-daily administration 1
- Alternative dosing regimens: The long half-life makes rosuvastatin suitable for alternate-day dosing in patients who experience statin-related side effects with daily administration 4
- Minimal drug interactions: Rosuvastatin undergoes minimal metabolism via the cytochrome P450 system, reducing the potential for drug interactions 3
Special Population Considerations
- Renal impairment: Plasma concentrations increase approximately 3-fold in patients with severe renal impairment (CLcr < 30 mL/min/1.73 m²) 1
- Asian patients: Asian subjects show approximately 2-fold elevation in median exposure (AUC and Cmax) compared to White subjects, requiring dosage adjustment 1
- Elderly patients: No significant differences in plasma concentrations between elderly (≥65 years) and non-elderly populations 1
Clinical Relevance
The long half-life of rosuvastatin contributes to its high potency and efficacy in reducing LDL cholesterol (52-63% reduction with 10-40 mg doses) 3. This pharmacokinetic property allows for consistent lipid-lowering effects throughout the 24-hour dosing interval, potentially improving patient adherence and clinical outcomes.