Table 11. Lipid-controlling efficacy and pharmacological features of currently used statins.
Lovastatin | Pravastatin | Simvasattin | Fluvastatin | Atorvastatin | Rosuvastatin | Pitavastatin | ||
---|---|---|---|---|---|---|---|---|
Daily dose, mg | 20–40 | 10–40* | 20–40 | 20–80 | 10–80 | 5–20† | 1–4 | |
LDL-C reduction, % | ||||||||
24–28 | 20 | 20 | 40 | 1 | ||||
30–36 | 40 | 40 | 20 | 80 | 10 | 2 | ||
39–45 | 80 | 40 | 20 | 5–10 | 4 | |||
46–52 | 40–80 | 20 | ||||||
Metabolism | CYP3A4 | sulfonation | CYP3A4 | CYP2C9 | CYP3A4 | CYP2C9 | Glucuronidation (partial CYP2C9) | |
Protin binding, % | >95 | 43–67 | 95–98 | 98 | 98 | 88 | >99 | |
Half-life, hr | 2–4 | 2–3 | 1–3 | 0.5–3 | 13–30 | 19 | 12 | |
Hydrophilicity | − | + | − | − | − | + | − | |
Elimination | Hepatobiliary | Hepatobiliary | Hepatobiliary | Hepatobiliary | Hepatobiliary | Hepatobiliary | Hepatobiliary | |
Renal elimination fraction, % | 10 | 20 | 13 | <6 | <2 | 28 | 15 |
LDL-C, low density lipoprotein cholesterol; CYP, cytochrome P450.
*40–80 mg in Caucasian countries.
†5–40 mg in Caucasian countries.