Characteristic | Lovastatin | Pravastatin | Simvastatin | Atorvastatin | Fluvastatin | Cerivastatin |
Maximal dose (mg/day) | 80 | 40 | 80 | 80 | 40 | 0.4 |
Maximal serum LDL cholesterol reduction (%) | 40 | 34 | 47 | 60 | 24 | 28 |
Serum LDL cholesterol reduction (%)1-150 | 34 | 34 | 41 | 50 | 24 | 28 |
Serum triglyceride reduction (%)1-150 | 16 | 24 | 18 | 29 | 10 | 13 |
Serum HDL cholesterol increase (%)1-150 | 8.6 | 12 | 12 | 6 | 8 | 10 |
Plasma half life (hours) | 2 | 1–2 | 1–2 | 14 | 1.2 | 2–3 |
Effect of food on drug absorption | Increased absorption | Decreased absorption | None | None | Negligible | None |
Optimal time of administration | With meals (morning and evening) | Bedtime | Evening | Evening | Bedtime | Evening |
Penetration of central nervous system | Yes | No | Yes | No | No | Yes |
Renal excretion of absorbed dose (%) | 10 | 20 | 13 | 2 | < 6 | 33 |
Mechanism of hepatic metabolism | Cytochrome P450 3A4 | Sulfation | Cytochrome P450 3A4 | Cytochrome P450 3A4 | Cytochrome P450 2C9 | Cytochrome P450, 3A4. 2C8 |
↵1-150 This effect was elicited by a daily dose of 40 mg of lovastatin, pravastatin, simvastatin, atorvastatin, and fluvastatin, and by a daily dose of 0.3 mg of cerivastatin in patients with hypercholesterolaemia.
Reproduced from Knopp, N Engl J Med1999;341:498-511, with permission of the publisher.