Table 2.

Pharmacokinetic properties of currently available statins (23)

DrugBioavailabilityExcretiont½ (hours)Major MetabolitesProtein BindingEffects of Renal/Hepatic Impairment
Atorvastatin (Lipitor®)Extensively absorbed ∼14% absolute bioavailability after first pass metabolism via CYP3A4Metabolized <2% urine14Ortho and para-hydroxylated derivatives (active)>98%Plasma levels not affected by renal disease; increased plasma levels with severe liver disease
Fluvastatin (Lescol®)98% absorbed ∼24% absolute bioavailability after first pass via CYP2C9Metabolized <6% urine, ∼90% fecal<1Hydroxylated metabolites (active, do not circulate systemically)>89%Increased plasma levels with severe liver disease
Lovastatin (Mevacor®)35% absorbed <5% absolute bioavailability after first pass via CYP3A4Metabolized 10% urine, 83% fecal3 to 4b-Hydroxyacid; 6-hydroxy derivative and other metabolites>95%Increased plasma levels with severe liver disease
Pravastatin (Pravacol®)34% absorbed ∼17% absolute bioavailability after first pass metabolismMetabolism/renal 20% urine, 70% fecal1.83α-Hydroxy isomeric metabolite>50%Increased plasma levels with severe renal and liver disease
Rosuvastatin (Crestor®)20% absorbed ∼8% absolute bioavailability after first pass metabolismMetabolism/renal 10% urine, 90% fecal20.8>88%Increased plasma levels with severe renal and liver disease
Simvastatin (Zocor®)60 to 80% absorbed <5% absolute bioavailability after first pass via CYP3A4Metabolism/renal 13% urine, 60% fecal3β-Hydroxy acid; 6-hydroxy-methyl derivatives>95%Increased plasma levels with severe renal and liver disease