Table 8.
Predicted, observed and predicted/observed ratios for AUC, Cmax and Ctrough: Comparison of changes in LPV exposure with CYP inhibitors or inducers
| CYP modulator | CYP modulator regimen [mg] |
LPV/RTV regimen [mg] |
Pred AUC ratio |
Obs AUC ratio |
Ratio pred/obs, AUC† |
Pred Cmax ratio |
Obs Cmax ratio |
Ratio pred/obs, Cmax |
Pred Ctrough ratio |
Obs Ctrough ratio |
Ratio pred/obs, Ctrough† |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Omeprazole | 40 QD | 400/100 BID | 1.04 | 1.07 | 0.98 | 1.03 | 1.08 | 0.96 | 1.06 | 1.03 | 1.03 |
|
| |||||||||||
| Ketoconazole | 200 SD | 400/100 BID | 1.52 | 0.87 | 1.74 | 1.52 | 0.89 | 1.70 | 1.45 | 0.75 | 1.94 |
|
| |||||||||||
| 400/100 BID | 0.66 | 0.25 | 2.65 | 0.64 | 0.45 | 1.42 | 0.59 | 0.01 | 59.0 | ||
| Rifampin | 600 QD | 400/400 BID | 1.02 | 0.98 | 1.04 | 1.01 | 0.93 | 1.09 | 1.02 | 1.03 | 0.99 |
| 800/200 BID | 0.91 | 0.84 | 1.08 | 0.90 | 1.02 | 0.88 | 0.92 | 0.43 | 2.14 | ||
|
| |||||||||||
| RTV | 100 BID | 400/100 BID | 1.47 | 1.46 | 1.01 | 1.39 | 1.28 | 1.09 | 1.59 | 2.16 | 0.74 |
Abbreviations: AUC= area under the plasma concentration-time curve, BID= twice daily, Cmax= maximum plasma concentration, Ctrough= trough plasma concentration, CYP= cytochrome P450, LPV= lopinavir, obs=observed, mg=milligram, pred=predicted, QD=once daily, SD=single dose, RTV=ritonavir
†
Predicted ratios were derived from arithmetic means; the type of means for the observed ratios is not specified in the lopinavir/ritonavir U.S. prescribing information.