Pharmacokinetic parameters (mean ± S.D.) of EFV in rats (n = 3–5) and monkeys (n = 3–8)
| Parameter | Rat | Monkey | ||||
|---|---|---|---|---|---|---|
| Intravenous dose (mg/kg) | 2 | 5 | 151-a | 1 | 5 | 151-a |
| CLp (ml/min/kg) | 68.2 ± 10.1 | 65.7 ± 8.7 | 42.9 ± 6.6 | 11.6 ± 1.5 | 11.4 ± 4.3 | 4.6 ± 0.5 |
| Vdss(liter/kg) | 4.4 ± 1.9 | 5.5 ± 0.7 | 1.5 ± 0.5 | 2.4 ± 0.2 | 3.8 ± 0.7 | 2.4 ± 0.2 |
| T1/2 (h) | 0.8 ± 0.2 | 1.3 ± 0.3 | 1.3 ± 0.2 | 2.6 ± 0.3 | 4.2 ± 0.7 | 7.2 ± 1.1 |
| AUC0–∞ (μM · min) | 95 ± 15 | 245 ± 32 | 1,900 ± 290 | 275 ± 36 | 1,500 ± 484 | 10,400 ± 1,100 |
| Oral dose (mg/kg) | 10 | 2 | ||||
| Cmax(μM) | 0.82 ± 0.35 | 0.50 ± 0.18 | ||||
| Tmax(h) | 0.6 ± 0.2 | 2.9 ± 1.5 | ||||
| F (%) | 16 ± 5 | 42 ± 15 | ||||
↵1-a Infused over 5 min.