TABLE 2.
Pharmacokinetic parameters and historical references for indinavir, nelfinavir, and saquinavira
| Inhibitor(s) and type of valve | AUCss (μg · h/ml) | AUC0→∞ (μg · h/ml) | Cmax,ss (μg/ml) | Cmax (μg/ml) | Cmin,ss (μg/ml) | Tmax,ss (h) | CL/F (ml/min) |
|---|---|---|---|---|---|---|---|
| SQV + APV | 2.58 (0.15–5.01) | 1.15 (0.12–2.18) | 0.071 (0.01–0.14) | 1.0 (0.56–2.18) | 12,854 (871–22,837) | ||
| Reference value (16) | 3.21 | 0.95 | 0.14 | 2 | 4,237 | ||
| Ratio | 0.81 | 1.21 | 0.52 | 0.68 | 3.03 | ||
| IDV + APV | 13.63 (10.79–16.47) | 7.01 (6.22–7.81) | 0.13 (0.09–0.17) | 0.75 (0.70–0.98) | 1,052 (805–1,298) | ||
| Reference valueb | 21.85 | 8.98 | 0.18 | 0.80 | 610 | ||
| Ratio | 0.62 | 0.78 | 0.73 | 1.05 | 1.72 | ||
| NFV + APV | 20.03 (10.83–29.23) | 3.58 (2.10–5.05) | 1.70 (0.47–2.93) | 3.63 | 722 (409–1,034) | ||
| Reference valuec | 17.4 | 3.18 | 1.49 | —d | 718 | ||
| Ratio | 1.15 | 1.12 | 1.14 | 1.00 | |||
| IDV + APV (single dose) | 11.18 (7.63–14.73) | 5.50 (3.77–7.24) | |||||
| Reference value (24) | 17.11 | 7.17 | |||||
| Ratio | 0.65 | 0.77 |
a
Values for pharmacokinetic parameters are means (95% CI), except for Tmax, for which values are medians (nonparametric; 95% CI). SQV, saquinavir; IDV, indinavir; NFV, nelfinavir; APV, amprenavir.
b
Merck & Co., complete prescribing information for indinavir.
c
B. Kerr, personal communication.
d
—, reference value unavailable.