Version May 2024
| Variable | Atorvastatin | Fluvastatin | Lovastatin | Pitavastatin | Pravastatin | Rosuvastatin | Simvastatin |
| LDL cholesterol reductions (dose range, mg) | 38 to 54% (10 to 80) | 17 to 33% (20 to 80) | 29 to 48% (20 to 80) | 31 to 41% (1 to 4) | 19 to 40% (10 to 40) | 52 to 63% (10 to 40) | 28 to 41% (10 to 40) |
| Elimination half-life (hours) | 15 to 30 | 0.5 to 2.3 | 2.9 | 12 | 1.3 to 2.8 | 19 | 2 to 3 |
| Bioavailability (%) | 12 | 19 to 29 | 5 | 51 | 18 | 20 | 5 |
| Protein binding (%) | 80 to 90 | >99 | >95 | 99 | 43 to 55 | 88 | 94 to 98 |
| Solubility | Lipophilic | Lipophilic | Lipophilic | Lipophilic | Hydrophilic | Hydrophilic | Lipophilic |
| Cytochrome P450 metabolism* | 3A4 | 2C9 | 3A4 | Limited | Limited | Limited | 3A4 |
| Active metabolites | Yes | No | Yes | Yes | No | No | Yes |
| Transmembrane transporters¶ | OATP1B1/1B3 BCRP | OATP1B1/1B3 | OATP1B1 | OATP1B1/1B3 | OATP1B1/1B3 | OATP1B1/1B3 BCRP | OATP1B1/1B3 |
| Effect of food on absorption of drug | None | Negligible | Increased absorption | Decreases | Decreased absorption | None | None |
| Optimal time of administration | Anytime | IR: evening (or morning and evening if taken twice daily) XR: anytime | IR: with evening meal (or with morning and evening meal if taken twice daily) XR: evening | Anytime | Evening | Anytime | Evening |
| Renal excretion of absorbed dose (%) | 2 | <6 | 10 | 15 | 20 | 10 | 13 |
LDL: low-density lipoprotein; OATP: organic anion transporting polypeptide; BCRP: breast cancer resistance protein; IR: immediate release; XR: extended release; CYP: cytochrome P450.
* Listed CYP isoenzymes are those that each statin is primarily dependent on for clearance; those with a minor role are not listed. For full information, refer to the Lexicomp drug monograph section on metabolism/transport effects.
¶ Coadministration of drugs that inhibit these transporters can substantially increase statin exposure and potential toxicity. Statins may be minor substrates of other transporters; these are not listed. Refer to the topic review of statin properties for additional detail.آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟
