Table 3.
Pharmacokinetic parameters of statins
| Statin | Pitavastatin | Atorvastatin | Fluvastatin | Lovastatin | Pravastatin | Rosuvastatin | Simvastatin |
|---|---|---|---|---|---|---|---|
| Molecular weight | 881 | 1209 | 433.5 | 405 | 446.5 | 1001 | 418.15 |
| Origin | Synthetic | Synthetic | Synthetic | Microbial | Semi-synthetic (microbial origin) | Synthetic | Semi-synthetic (microbial origin) |
| Racemic | No | No | Yes | No | No | No | No |
| Prodrug | No | No | No | Yes | No | No | Yes |
| Log P | 1.49 | 1.11 | 1.27 | 1.70 | −0.84 | −0.33 | 1.60 |
| Absorption (%) | 80 | 30 | 98 | 31 | 37 | 50 | 65–85 |
| Hepatic excretion (%) | NA | >70 | 68 | >70 | 66 | 90 | 78–87 |
| Bioavailability (%) | >60 | 12 | 10–35 | <5 | 17 | 20 | <5 |
| Effect of food on bioavailability (%) | No | Yes (↓13) | Yes (↓15–25) | Yes (↑50) | Yes (↓30) | No | No |
| Protein binding (%) | 96 | >98 | >98 | 96–98.5 | 43–54 | 88 | >95 |
| Tmax | 0.5–0.8 | 2.0–4.0 | 0.5–1.5 | 2.8 | 0.9–1.6 | 3 | 1.3–2.4 |
| T1/2 | 11 | 11–30 | 0.5–2.3 | 2.5–3.0 | 0.8–3.0 | 20 | 1.9–3.0 |
| Renal excretion | <2 | 2 | 6 | 30 | 60 | 10 | 13 |
| 50% inhibitory concentration (nmol/L) | 6.8 | 15.2 | 17.9 | 2.7–11.1 | 55.1 | 12 | 18.1 |
| Lipid-lowering Metabolites | No | Yes, active | Yes, mainly inactive | Yes | Yes, mainly inactive | No | Yes |
| Range of dose (mg) | 1–4 | 10–80 | 20–80 | 10–80 | 5–40 | 5–80 | 5–80 |
| CYP isoforms primarily involving with metabolic pathway | CYP2C9 Minimally | CYP3A4 | CYP2C9 | CYP3A4 | CYP3A4 Minimally | CYP2C9 Minimally | CYP3A4 |
Notes: Log P, logarithm of base 10 of the n-octanol/water partition coefficient of active hydroxy forms of statins.
Abbreviation: CYP, cytochrome P450.
Modified from Fujino et al.37