Table 4.
Median (25th, 75th percentiles) model-predicted values of the area under the concentration-time curve over a dosing interval for each drug in blood plasma and the estimated unbound drug area under the plasma concentration-time curve in blood plasma cervicovaginal fluid, at both first dose and multiple doses
BP AUCτ (μg•h/L) | BP fAUCτ (μg•h/L) | CVF AUCτ (μg•h/L) | CVF AUCτ:BP AUCτ ratio | CVF AUCτ:BP fAUCτ ratio | |
---|---|---|---|---|---|
Efavirenz | |||||
First dose | 24.5 (16.1, 30.3) | 0.245 (0.161, 0.303) | 0.0127 (0.0746, 0.193) | 0.00527 (0.00298, 0.0128) | 0.527 (0.298, 1.28) |
Multiple dose | 46.7 (33.9, 106) | 0.470 (0.339, 1.06) | 0.262 (0.110, 0.579) | 0.00655 (0.0125, 0.000744) | 0.655 (0.0744, 1.25) |
Atazanavir | |||||
First dose | 25.3 (6.19, 43.9) | 3.55 (0.867, 6.15) | 5.66 (8.36, 2.12) | 0.299 (0.0846, 1.55) | 2.14 (0.604, 11.1) |
Multiple dose | 54.6 (11.5, 68.1) | 7.64 (1.61, 9.54) | 5.53 (3.18, 11.4) | 0.173 (0.0719, 0.596) | 1.24 (0.514, 1.24) |
Lamivudine 150 mg twice daily | |||||
First dose | 3.86 (3.58, 4.20) | 2.31 (2.15, 2.52) | 10.0 (6.07, 48.9) | 2.77 (1.35, 1.62) | 4.62 (2.24, 27.0) |
Multiple dose | 3.17 (2.71, 5.47) | 1.90 (1.62, 3.28) | 27.7 (14.5, 59.2) | 5.92 (4.29, 19.5) | 9.86 (7.15, 32.5) |
Lamivudine 300 mg once daily | |||||
First dose | 10.1 (9.49, 13.6) | 6.06 (5.70, 8.15) | 62.2 (10.4, 287) | 5.40 (0.976, 30.6) | 8.98 (1.63, 51.0) |
Multiple dose | 12.9 (4.35, 17.9) | 7.73 (2.61, 10.7) | 36.1 (0.526, 99.2) | 2.81 (0.53, 9.97) | 4.67 (0.878, 16.6) |
Tenofovir | |||||
First dose | 2.56 (1.71, 4.68) | 2.38 (1.59, 4.35) | 4.18 (7.30, 18.1) | 1.57 (0.132, 13.7) | 1.68 (0.141, 14.7) |
Multiple dose | 2.32 (1.21, 4.08) | 2.16 (1.13, 3.79) | 4.56 (1.78, 10.6) | 1.52 (0.722, 7.40) | 1.64 (0.776, 7.95) |
Ratios for CVF AUCτ:BP AUCτ and CVF AUCτ:BP fAUCτ are provided as median (25th, 75th percentiles) for each drug at each sampling visit
AUCτ area under the plasma concentration-time curve during the dosing interval, BP blood plasma, CVF cervicovaginal fluid, fAUCτ unbound drug area under the plasma concentration-time curve in BP