TABLE 2

Overview of PK of atorvastatin, pitavastatin, and rosuvastatin and the effect of rifampicin on the hepatic uptake and biliary clearance of these statins

Values are means ± S.D. (n = 3 for atorvastatin, n = 3 for pitavastatin, and n = 4 for rosuvastatin).

Statin PKPlasmaBile
Substrate Alone+ RifampicinFold ChangeSubstrate Alone+ RifampicinFold Change
AtorvastatinCmax (ng/ml)1.79 ± 0.845.16 ± 1.032.88216.88 ± 114.98161.73 ± 86.170.75
AUC0–120 min/120-240 min (ng/ml)18.09 ± 10.73112.79 ± 46.067.2413517.33 ± 5809.527780.25 ± 3676.670.58
Percent biliary excretion13.00 ± 5.597.48 ± 3.540.58
Biliary clearance (L/h)87.78 ± 78.426.31 ± 6.380.07
Hepatic extraction ratio0.82 ± 0.080.51 ± 0.090.62
PitavastatinCmax (ng/ml)1.47 ± 0.432.43 ± 0.703.0365.07 ± 7.2772.12 ± 20.351.11
AUC0–120 min/120-240 min (ng/ml)19.51 ± 11.8932.64 ± 17.622.631448.33 ± 129.391288.33 ± 281.690.89
Percent biliary excretion1.03 ± 0.090.91 ± 0.200.89
Biliary clearance (L/h)5.33 ± 2.731.16 ± 0.860.22
Hepatic extraction ratio0.84 ± 0.010.72 ± 0.080.87
RosuvastatinCmax (ng/ml)18.43 ± 3.1548.28 ± 10.252.628927 ± 13026384.25 ± 207.580.72
AUC0–120 min/120-240 min (ng/ml)186.57 ± 44.90578.73 ± 152.913.10140123 ± 34948118572.00 ± 28916.470.85
Percent biliary excretion10.01 ± 2.508.47 ± 2.070.85
Biliary clearance (L/h)46.66 ± 13.2713.18 ± 5.390.28
Hepatic extraction ratio0.82 ± 0.030.71 ± 0.070.87