Table 2.
Predicted effect of residual induction on raltegravir pharmacokinetics at days 1, 7, 14, and 28 post-rifampicin, efavirenz, and rifabutin dosing
| Absence inducer | After stopping inducer | DDI ratio (residual induction) | |
|---|---|---|---|
| Raltegravir—day 1 after stopping rifampicin | |||
| Ctrough [ng/mL] | 107 (69) | 84 (51) | 0.78 |
| AUC0-τ [ng×h/mL] | 7312 (38) | 6192 (30) | 0.85 |
| Raltegravir—day 7 after stopping rifampicin | |||
| Ctrough [ng/mL] | 128 (76) | 128 (76) | 1.00 |
| AUC0-τ [ng×h/mL] | 7740 (41) | 7739 (41) | 1.00 |
| Raltegravir—day 14 after stopping rifampicin | |||
| Ctrough [ng/mL] | 128 (76) | 128 (76) | 1.00 |
| AUC0-τ [ng×h/mL] | 7740 (41) | 7740 (41) | 1.00 |
| Raltegravir—day 28 after stopping rifampicin | |||
| Ctrough [ng/mL] | 128 (76) | 128 (76) | 1.00 |
| AUC0-τ [ng×h/mL] | 7740 (41) | 7740 (41) | 1.00 |
| Raltegravir—day 1 after stopping efavirenz | |||
| Ctrough [ng/mL] | 108 (83) | 82 (49) | 0.76 |
| AUC0-τ [ng×h/mL] | 7357 (40) | 6191 (28) | 0.84 |
| Raltegravir—day 7 after stopping efavirenz | |||
| Ctrough [ng/mL] | 129 (82) | 115 (71) | 0.89 |
| AUC0-τ [ng×h/mL] | 7777 (42) | 7243 (38) | 0.93 |
| Raltegravir—day 14 after stopping efavirenz | |||
| Ctrough [ng/mL] | 129 (82) | 123 (79) | 0.95 |
| AUC0-τ [ng×h/mL] | 7778 (42) | 7547 (41) | 0.97 |
| Raltegravir—day 28 after stopping efavirenz | |||
| Ctrough [ng/mL] | 129 (82) | 127 (83) | 0.99 |
| AUC0-τ [ng×h/mL] | 7778 (42) | 7716 (42) | 0.99 |
| Raltegravir—day 1 after stopping rifabutin | |||
| Ctrough [ng/mL] | 107 (82) | 102 (79) | 0.95 |
| AUC0-τ [ng×h/mL] | 7336 (40) | 7098 (38) | 0.97 |
| Raltegravir—day 7 after stopping rifabutin | |||
| Ctrough [ng/mL] | 128 (82) | 128 (82) | 1.00 |
| AUC0-τ [ng×h/mL] | 7553 (42) | 7744 (42) | 1.00 |
| Raltegravir—day 14 after stopping rifabutin | |||
| Ctrough [ng/mL] | 128 (82) | 128 (82) | 1.00 |
| AUC0-τ [ng×h/mL] | 7554 (42) | 7753 (42) | 1.00 |
| Raltegravir—day 28 after stopping rifabutin | |||
| Ctrough [ng/mL] | 128 (82) | 128 (82) | 1.00 |
| AUC0-τ [ng×h/mL] | 7554 (42) | 7754 (42) | 1.00 |
The results are represented as geometric mean (CV)
AUC0-τ area under the concentration–time curve to tau; Ctrough trough concentration; DDI drug-drug interaction