Table 6; online.
Atorvastatin and O-hydroxyatorvastatin pharmacokinetic parameters by dose level
| Atorvastatin | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Dose (mg/kg) |
Cmax (ng/mL) |
C24 (ng/mL) | Trough 2 weeks (ng/mL) |
Trough 6 weeks (ng/mL) |
Tmax (hours) |
Half Life (hours) |
AUC0-∞ (ng*hr/mL) |
CL/F (L/hr/kg) |
Vd/F (L/kg) |
| 0.125 (n=6) | 5.80 (2.32-8.53) | BQL (BQL-0.38) | BQL (BQL-0.91) | BQL (BQL-0.26) | 1.5 (1-2) | 5.5 (4.4-7.9) | 41.9 (31.5-42.9) | 29.8 (16.6-39.8) | 222 (190-287) |
| 0.25 (n=5) | 9.49 (4.02-22.5) | BQL (BQL-1.54) | BQL (BQL-1.11) | BQL (BQL-2.19) | 1 (1-6) | 6.0 (5.6-6.2) | 122.8 (38.4-171.7) | 20.2 (14.6-60.00) | 163 (130-519) |
| 0.5 (n=3) | 21.70, 82.6 | BQL, 1.33 | 4.30 (BQL-12.8) | BQL, 6.0 | 1, 2 | 5.3 (4.2-6.3) | 330.9 (188.1-473.6) | 18.7 (10.6-26.80) | 153 (65-242) |
| 0.75 (n=6) | 41.4 (29.3-469) | BQL (BQL-2.89) | BQL (BQL-10.7) | BQL (BQL-5.56) | 1 (1-2) | 4.3 (3.1-5.1) | 356.5 (210.6-2890.9) | 21.7 (14.7-34.20) | 158 (65-212) |
| O-hydroxyatorvastatin metabolite | |||||||||
| Dose (mg/kg) |
Cmax (ng/mL) |
C24 (ng/mL) | Trough 2 weeks (ng/mL) | Trough 6 weeks (ng/mL) | Tmax (hours) |
Half Life (hours) | AUC0-∞ (ng*hr/mL) |
CL/F (L/hr/kg) |
Vd/F (L/kg) |
| 0.125 (n=6) | 1.87 (0.92-3.42) | BQL (BQL-0.67) | BQL (BQL-1.97) | BQL (BQL-0.87) | 6 (2-6) | 6.2 (4.1-9.1) | 40.2 (18.1-42.7) | N/A | N/A |
| 0.25 (n=5) | 4.91 (3.86-5.35) | BQL (BQL-1.07) | BQL (BQL-1.55) | BQL (BQL-2.59) | 2 (1-6) | 5.6 (2.7-8.5) | 64.6 (45.6-81.0) | N/A | N/A |
| 0.5 (n=3) | 11.10, 18.10 | BQL, 2.13 | 7.01 (BQL-17.7) | BQL, 12.4 | 1 , 2 | 6.8 (6.3-7.3) | 178.6 (145.5-211.8) | N/A | N/A |
| 0.75 (n=6) | 24.6 (9.27-49.9) | BQL (BQL-5.64) | BQL (BQL-9.57) | BQL (BQL-13.1) | 2 (1-6) | 5.3 (4.3-6.9) | 238.4 (154.9-1062.1) | N/A | N/A |
BQL: Below quantitative level (<0.25 or <2.5 ng/mL)
Values are reported as medians with a range. If only two values are available, both are reported.