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. 2019 Aug 1;8(9):664–675. doi: 10.1002/psp4.12447

Table 2.

Observed and predicted pharmacokinetic parameters and effect of perpetrators on all major atorvastatin‐related species following oral administration of atorvastatin 40 mg

40 mg atorvastatin 40 mg + itraconazole 40 mg + rifampicin 40 mg + dulaglutide
Obs Pred Pred/Obs Obs ratio Pred ratio Pred/Obs Obs ratio Pred ratio Pred/Obs Obs ratio Pred ratio Pred/Obs
Atorvastatin
AUC (ng/mL • hour) 54.2–99 78.6 (48) 0.79–1.45 3.3 2.56 (2.47–2.67) 0.78 7.3 7.66 (7.20, 8.15) 1.05 0.786 (0.752, 0.821) 0.758 (0.736–0.780) 0.96
Cmax (ng/mL) 12.7–19.5 18.2 (49) 0.93–1.43 1.2 1.33 (1.30–1.35) 1.1 10.5 9.42 (9.03–9.84) 0.90 0.296 (0.246, 0.355) 0.22 (0.21–0.23) 0.74
Tmax (hour) 0.5–1 0.72 (0.36–1.08) 0.72–1.44 2.5 1.08 0.43
O‐hydroxyatorvastatin
AUC (ng/mL • hour) 77.5–102 93.5 (52) 0.92–1.21 0.83 0.85 (0.81–0.89) 1.02 0.937 (0.887, 0.990) 0.941 (0.916–0.965) 1
Cmax (ng/mL) 7.7–14.4 11.9 (48) 0.83–1.55 0.17 0.22 (0.21–0.23) 1.3 0.393 (0.330, 0.467) 0.361 (0.336–0.388) 0.92
Tmax (hour) 1–3 1.26 (1.08–2.16) 0.42–1.26 5 1.8 0.36
Atorvastatin lactone
AUC (ng/mL • hour) 50.7–78.2 64.4 (47) 0.82–1.27 4.0 3.44 (3.26–3.63) 0.68
Cmax (ng/mL) 3.8–8 3.75 (60) 0.47–0.99 2.3 2.78 (2.64–2.92) 1.2
Tmax (hour) 2–3 1.93 (1.03–3.86) 0.64–0.97
O‐hydroxy atorvastatin lactone
AUC (ng/mL • hour) 128–187 162 (39) 0.87–1.27 0.71 1.18 (1.14–1.21) 1.7
Cmax (ng/mL) 10.5–14.5 7.3 (50) 0.50–0.70 0.29 0.61 (0.58–0.64) 2.1
Tmax (hour) 3–4 2.25 (1.2–9.33) 0.56–0.75

Data for atorvastatin alone are from five studies reporting all four major atorvastatin‐related species.1, 2, 3, 5 Observed mean values are the means from all studies, predicted values for AUC and Cmax are the reported as geometric mean (CV%), and the predicted Tmax is reported as median (range). Data for atorvastatin with itraconazole, rifampicin, and dulaglutide are from single studies with each inhibitor.1, 3, 14 Observed ratio values are reported means or geometric means (90% confidence interval) in the case of dulaglutide, predicted values for AUC and Cmax  ratios are geometric means (90% confidence interval), predicted Tmax ratio is reported as median difference (presence ‐absence of dulaglutide). AUC, area under the plasma concentration‐time curve; Cmax, maximum plasma concentration; Obs, observed; Pred, predicted; Tmax, time to maximum plasma concentration.