Table 2.
Pharmacokinetic parameters of nevirapine and its metabolites after a single dose (group A) and at steady state (group B)
| Drug | Pharmacokinetic parameters fora: |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Group A after single dose |
Group B at steady state |
|||||||||
| Cmax (μM) | Tmax (h) | t1/2 (h) | AUC12 (μM · h) | AUCt (μM · h) | AUCinf (μM · h) | Ctrough (μM) | Cmax (μM) | Tmax (h) | AUC12 (μM · h) | |
| Nevirapine | 5.7 (3.8–12.1) | 2 (0.5–8) | 99 (53–217) | 59.2 (38.0–66.9) | 513.0 (380.0–592.0) | 560 (430–684) | 21.8 (13.5–36.5) | 26.7 (19.1–50.2) | 2 (0–4) | 291.8* (161.9–459.8) |
| 2-Hydroxynevirapine | 0.02 (0.01–0.08) | 1 (0.5–24) | 99 (48–882) | 0.10 (0.05–0.32) | 0.97 (0.59–3.59) | 1.55 (0.85–4.36) | 0.01 (0.00–0.01) | 0.01 (0.01–0.02) | 2 (1–8) | 0.11* (0.06–0.17) |
| 8-Hydroxynevirapine | Not detected | Not detected | Not detected | Not detected | Not detected | Not detected | 0.04 (0.03–0.08) | 0.07 (0.05–0.14) | 2 (1–14) | 0.76 (0.46–1.29) |
| 3-Hydroxynevirapine | 0.01 (0.01–0.03) | 24 (6–72) | 59 (35–217) | 0.09 (0.04–0.12) | 1.14 (0.47–2.12) | 1.37 (0.73–2.40) | 0.11 (0.05–0.23) | 0.18 (0.08–0.49) | 1 (0–8) | 1.76 (0.77–4.17) |
| 12-hydroxy nevirapine | 0.32 (0.14–0.72) | 12 (2–24) | 61 (43–1,221) | 3.12 (1.10–5.16) | 27.11 (12.47–54.92) | 34.92 (14.17–78.17) | 0.51 (0.18–2.67) | 1.00 (0.50–3.81) | 3 (1–12) | 9.53** (4.18–34.42) |
| 4-Carboxynevirapine | 0.03 (0.02–0.12) | 12 (2–24) | 48 (25–81) | 0.23 (0.12–0.46) | 2.37 (0.82–6.88) | 2.77 (0.90–7.24) | 0.08 (0.03–0.21) | 0.13 (0.09–0.27) | 3 (1–14) | 1.12** (0.75–2.65) |
a
Values are medians (ranges).
*
, P < 0.001 for the AUC12 at steady state compared to the AUCinf after a single dose;
**
, P < 0.01 for the AUC12 at steady state compared to the AUCinf after a single dose.