TABLE 1

Pharmacokinetics of the statins

AtorvastatinCerivastatinFluvastatinLovastatinPitavastatinPravastatinRosuvastatinSimvastatin
Dose, mg40a0.3a20–40a40a2a40a20–40–80a40–60a
Dose formOpen acida,bOpen acida,bOpen acida,bLactonea,bOpen acida,cOpen acida,bOpen acidaLactonea,b
Optimal time of dosingAny time of daydEveningdBedtimedWith meals morning and eveningdAny time of daycBedtimedAny time of daydEveningd
Absorption, %30b,c98b,c98b,c31b,c80c37b,c50c65–85b,c
tmax, h2–4a,b,c2.5–3a,b,c0.5–1.5a,b,c2–4a,b,c1–1.8 a,c0.9–1.6a,b,c3–4a,c1.3–2.4a,b,c
Bioavaibility, % a,b,c,d12a,b,c,d60a,b,c,d10–35a,b,c,d<5a,b,c,d>60a,c,d18a,b,c,d20a,c,d<5a,b,c,d
SolubilityLipophilicdLipophilicdLipophilicdLipophilicdLipophilicdHydrophilicdHydrophilicdLipophilicd
Effect of food on bioavailability↓13b,c,d,eNob,d↓15–25b,c,d,e↑50b,c,d,eNOd,e↓30b,c,d,eNOc,d,eNOb,c,d,e
↑23c
Protein binding>98c,d,e>99.5b,c,d>98b,c,d,e96–98.5b,c,d,e96c,d,e43–54c,d,e88c,d,e>95b,c,d,e
logP (N-octanol/water partition coefficient)1.11a,c1.69a,c1.27a,c1.70a,c1.49a,c−0.84a,c−0.33a,c1.60a,c
Primary metabolic pathwayCYP3A4a,b,c,d,eCYP3A4
CYP2C8a,b,c,d,e		CYP2C9a,b,c,d,eCYP3A4a,b,c,d,eCYP2C9
Minimallya,c,d,e		CYP3A4
Minimallya,b,c,d,e		CYP2C9
Minimallya,c,d,e		CYP3A4a,b,c,d,e
Lipid-lowering metabolitesActivec,eActivec,eMainly inactivec,eActivec,eNoc,eMainly inactivec,eNoc,eActivec,e
IC50, nM15.2c,e13.1c,e17.9c,e2.7–11.1c,e6.8c,e55.1c,e12c,e18.1c,e
Hepatic excretion, %>70b,c,eNA>68b,c,e>70b,c,eNA46–66b,c,e90c,e78–97b,c,e
Renal excretion, %2c,d,e<30c,d,e6c,d,e30c,d,e<2c,d,e60c,d,e10c,d,e13c,d,e
Clearance, l · h−1 · kg−10.25b0.20b0.97b0.26–1.1b0.81b0.45b
t1/2, h11–30b,c,e2–3b,c,e0.5–2.3b,c,e2.5–3b,c,e11b,c,e0.8–3b,c,e20b,c,e1.9–3b,c,e

  • ↵a Shitara and Sugiyama (2006).

  • ↵b Corsini et al. (1999).

  • ↵c Mukhtar et al. (2005).

  • ↵d Schachter (2005).

  • ↵e Saito (2009).