TABLE 2.
Plasma lopinavir pharmacokinetic parametersb
| Parameter | Value for group |
||||||
|---|---|---|---|---|---|---|---|
| Efavirenz (n = 20) + lopinavir-ritonavir dose of: |
Nevirapine (n = 18) + lopinavir-ritonavir dose of: |
No NNRTIs (n = 20) + 2 tablets of lopinavir-ritonavir (400/100 mg) BD | |||||
| 3 tablets (600/150 mg) BD | 4 capsules (533/133 mg) BD | 2 tablets (400/100 mg) BD | 3 tablets (600/150 mg) BD | 4 capsules (533/133 mg) BD | 2 tablets (400/100 mg) BD | ||
| Geometric mean AUC0-12 (μg·h/ml) (%CV) [range] | 91.8 (58) [23.1-263.6] | 65.7 (39) [27.1-150.6] | 54.0 (65) [11.9-166.5] | 112.9 (30) [66.9-165.8] | 68.1 (53) [30.6-166.5] | 61.5 (52) [26.9-157.9] | 110.1 (34) [65.3-226.1] |
| No. of patients (%) with AUC0-12 (μg·h/ml) ofa: | |||||||
| <67.5 | 4 (20) | 11 (55) | 13 (65) | 1 (6) | 10 (56) | 12 (67) | 1 (5) |
| 67.5-90 | 5 (25) | 6 (30) | 2 (10) | 4 (22) | 2 (11) | 2 (11) | 5 (25) |
| 90-121.5 | 5 (25) | 2 (10) | 4 (20) | 4 (22) | 4 (22) | 2 (11) | 7 (35) |
| >121.5 | 6 (30) | 1 (5) | 1 (5) | 9 (50) | 2 (11) | 2 (11) | 7 (35) |
| Geometric mean Cmax (μg/ml) (%CV) [range] | 11.1 (46) [4.5-27.0] | 8.3 (37) [4.1-16.6] | 7.5 (43) [2.2-13.6] | 12.2 (23) [8.1-17.5] | 8.4 (43) [4.5-15.5] | 7.7 (39) [3.5-14.3] | 12.2 (30) [7.8-25.7] |
| No. of patients (%) with Tmax (h) of: | |||||||
| 0 | 4 (20) | 2 (11) | 6 (33) | 1 (6) | |||
| 2 | 10 (50) | 9 (45) | 11 (55) | 5 (28) | 6 (33) | 7 (39) | 7 (35) |
| 4 | 5 (25) | 2 (10) | 5 (25) | 8 (44) | 3 (17) | 7 (39) | 10 (50) |
| 6 | 5 (25) | 4 (20) | 4 (20) | 2 (11) | 3 (17) | 3 (17) | 3 (15) |
| 8 | 1 (5) | 1 (6) | |||||
| Geometric mean C12 (μg/ml) (%CV) [range] | 2.9 (189) [0.1-13.8] | 1.9 (116) [0.1-11.5] | 1.2 (256) [0.1-9.6] | 5.4 (64) [1.4-10.2] | 2.3 (159) [0.3-13.0] | 1.8 (119) [0.3-10.8] | 5.6 (52) [2.0-17.6] |
| No. of patients (%) with C12 (μg/ml) of: | |||||||
| <1 | 3 (15) | 3 (15) | 8 (40) | 4 (22) | 5 (28) | ||
| 1-<5 | 9 (45) | 16 (80) | 9 (45) | 8 (44) | 9 (50) | 10 (56) | 8 (40) |
| 5-<10 | 5 (25) | 3 (15) | 8 (44) | 3 (17) | 2 (11) | 11 (55) | |
| 10+ | 3 (15) | 1 (5) | 2 (11) | 2 (11) | 1 (6) | 1 (5) | |
| Geometric mean t1/2 (h) (%CV) [range] | 4.6 (81) [1.5-24.6] | 3.8 (55) [1.3-9.4] | 3.5 (78) [1.4-12.0] | 7.1 (63) [2.5-18.2] | 6.4 (133) [2.0-65.2] | 4.0 (54) [1.7-14.5] | 7.7 (60) [3.1-29.1] |
a
Categories prespecified as 75%, 100%, and 135% of the target AUC0-12, 90 μg·h/ml.
b
Note that the limit of assay detection was 0.102 μg/ml. Also note that the coefficient of variation (%CV) was calculated using the formula 100 × [sqrt(exp{[SD of ln(var)2} − 1)].