Table 1.
List of statins as a single-ingredient product licensed by the Food & Drug Administration and European Medicines Agency
Statin | Solubility | Type | Synthetic state | Pharmacokinetic parameters | |||||||||
Cytochrome P450 subclass | Half-life (hours) | Clearance (L/hour) | Hepatic extraction | Excretion | |||||||||
Systemic | Oral | Hepatic | Renal | Urine | Faecal | ||||||||
Atorvastatin | Lipophilic | Fully synthetic | Active drug | CYP3A4 | Mean* | 17.8 | 157 | >70% | 1.20% | 70% | |||
Range† | 13.8–20.7 | ||||||||||||
Lipitor‡ | Dose§: 20, 40, 80 mg | REF: 58 | REF: 59 | REF: 58 | REF: 60 | ||||||||
REF: 61 62 | |||||||||||||
Cerivastatin | Lipophilic | Fully synthetic | Active drug | CYP2C8 and CYP3A4 | Mean* | 2.96 | 13 | 24%–30% | 70% | ||||
Range† | 2.2–4.0 | ||||||||||||
Lipobay‡¶ | Dose§: 0.2 to 0.3 mg | ||||||||||||
REF: 63–65 | REF: 63 | REF: 66 67 | REF: 66 67 | ||||||||||
Fluvastatin | Lipophilic | Natural statin | Active drug | CYP2C9 some CYP2C8 | Mean* | 1.9 | 68 | 120–180 | 69 | 73% | 6% | 93% | |
Range† | 1.5–2.4 | ||||||||||||
Lescol‡ | Dose§: 40 to 80 mg | REF: 68 | REF: 69 70 | REF: 71 | REF: 72 | REF: 68 | REF: 68 | ||||||
REF: 73–76 | |||||||||||||
Lovastatin | Lipophilic | Natural statin | Prodrug | CYP3A4 | Mean* | 2.7 | 18–75 | 175–351 | 69% | 9.60% | 83.20% | ||
Range† | 2.6–2.8 | ||||||||||||
Mevacor‡** | Dose§: 20 to 40 mg | REF: 71 | REF: 69 77 78 78 | REF: 79 | REF: 71 | REF: 71 | |||||||
REF: 76 78 80 | |||||||||||||
Pitavastatin | Lipophilic | Fully synthetic | Active drug | Partially: CYP2C8 and CYP2C9 | Mean* | 10.7 | 16–26 | 15% | 79% | ||||
Range† | 6.9–13.1 | ||||||||||||
Livalo‡ | Dose§: 1, 2, 4 mg | REF: 81–84 | REF: 85 | REF: 85 | |||||||||
REF: 81–84 86 87 | |||||||||||||
Rosuvastatin | Hydrophilic | Fully synthetic | Active drug | Partially: CYP2CP and CYPC19 | Mean* | 14.2 | 49 | 273–281 | 82 | 12 | 63% | 5%–10% | 90% |
Range† | 10.1–24.4 | ||||||||||||
Crestor‡ | Dose§: 5, 10, 20, 40 mg | ||||||||||||
REF: 88–93 | REF: 94 | REF: 88 | REF: 95 | REF: 94 | REF: 94 | REF: 94 96 | REF: 96 | ||||||
Pravastatin | Hydrophilic | Semisynthetic | Active drug | None | Mean* | 2.17 | 57 | 24–27 | 46%–66% | 20% | 71% | ||
Range† | 1.6–2.6 | ||||||||||||
Pravachol‡ | Dose§: 10, 20, 40 mg | REF: 97 | REF: 97–99 | REF: 59 | REF: 97 | REF: 97 | |||||||
REF: 80 97 100–103 | |||||||||||||
Simvastatin | Lipophilic | Semisynthetic | Prodrug | CYP3A4 | Mean* | 4.6 | 32 | 2000–3100 | >79% | 13% | 58% | ||
Range† | 1.6–7.9 | ||||||||||||
Zocor‡ | Dose§: 20, 40, 60 mg | REF: 104 | REF:105–107 | REF:79 | REF: 104 108 | REF:104 108 | |||||||
REF: 92 105 106 109–115 |
Cerivastatin is withdrawn from the market and lovastatin is not licensed in Great Briatin and Switzerland
*Mean calculated as the average of the means of the cited references.
†Range of the means from the cited references.
‡Common brand name.
§Half-life reported from indicated doses from the cited references.
¶Withdrawn from the market due to rhabdomyolysis in 2001.
**Not commonly prescribed anymore and not licensed in Great Britain and Switzerland.