Rosuvastatin Half-Life
Rosuvastatin has an elimination half-life of approximately 19 hours, making it one of the longest-acting statins available. 1, 2
Pharmacokinetic Profile
- The elimination half-life ranges from 13 to 21 hours in humans, with most sources citing approximately 19 hours as the standard value 1, 2, 3, 4
- Peak plasma concentrations (Tmax) are reached 3 to 5 hours after oral administration under fasting conditions 1, 2, 5
- The absolute oral bioavailability is approximately 20% 2, 5
Clinical Implications of the Long Half-Life
- The extended half-life of 19 hours allows for once-daily dosing and provides sustained HMG-CoA reductase inhibition throughout the 24-hour period 3, 6
- Rosuvastatin's long half-life makes it suitable for alternate-day dosing regimens (e.g., Monday-Wednesday-Friday) in patients who cannot tolerate daily statin therapy, particularly those experiencing myalgias 7
- When discontinuing rosuvastatin before surgery or procedures, the 19-hour half-life should be considered to ensure adequate drug clearance, similar to recommendations for other long-acting medications 1
Comparison to Other Statins
- Rosuvastatin has the longest half-life among commonly used statins: atorvastatin (14 hours), pitavastatin (12 hours), fluvastatin (3 hours), pravastatin (1.8 hours), lovastatin (2-3 hours), and simvastatin (2 hours) 1
- The prolonged half-life, combined with high potency, distinguishes rosuvastatin from shorter-acting statins like simvastatin and lovastatin (half-lives of 2-3 hours) 1, 3
Metabolism and Excretion Characteristics
- Rosuvastatin is not extensively metabolized; approximately 10% undergoes metabolism, primarily via CYP2C9 (not CYP3A4) 1, 2
- Following oral administration, rosuvastatin and its metabolites are primarily excreted in feces (90%), with approximately 10% renal excretion 1, 2
- The drug demonstrates minimal accumulation with repeated dosing despite its long half-life 5