Noncompartmental pharmacokinetic parameters of flurbiprofen before (baseline) and after pretreatment with 200 or 400 mg of fluconazole for 7 days Data are shown as median (range), except for CYP2C9*3/*3 genotype group, in which individual data are presented.
Pharmacokinetic Parameters | Units | CYP2C9*1/*1 (n = 11) | CYP2C9*1/*3 (n = 8) | CYP2C9*3/*3 (n = 2) |
|---|---|---|---|---|
| Baseline | ||||
| CL/F | Liters · hour–1 | 1.6 (1.2–2.2) | 0.9 (0.5–2)* | (0.4, 0.6)*† |
| AUC0–inf | Micrograms · milliliter–1 · hour | 30.8 (23.2–42.7) | 53.7 (24.6–112)* | (85.8, 119)*† |
| T1/2 | Hours | 4.8 (4.2–6.1) | 7.2 (5.5–7.5)* | (9.7, 13.8)*† |
| Cmax | Micrograms · milliliter–1 | 7.6 (4.1–9.5) | 8.9 (4.2–10.7) | (8, 9.4) |
| Tmax | Hours | 1.5 (0.5–2.0) | 2.0 (1.5–6.1) | (2.0, 2.0) |
| V/F | Liters | 10.8 (7.8–13.8) | 9.2 (3.9–22) | (8.2, 8.4) |
| CLf, m | Liters · hour–1 | 0.67 (0.43–0.95) | 0.35 (0.15–0.86)* | (0.05, 0.05)*† |
| 200 mg of fluconazole coadministration | ||||
| CL/F | Liters · hour–1 | 0.8 (0.3–1.1) | 0.5 (0.3–1.1) | (0.3, 0.4)* |
| AUC0–inf | Micrograms · milliliter–1 · hour | 62.3 (46.1–150) | 96.1 (44.1–197) | (136, 152)* |
| T1/2 | Hours | 7.8 (6.1–16.3) | 9.2 (8.0–13.2) | (18.9, 22.6)*† |
| Cmax | Micrograms · milliliter–1 | 5.9 (4–10.2) | 7.7 (5.2–15.5) | (8.6, 8.6) |
| Tmax | Hours | 2.0 (1.0–4.0) | 2.0 (1.8–4.0) | (1, 1.5) |
| V/F | Liters | 8.3 (6.1–13.7) | 7.5 (3.2–14.6) | (10, 10.8) |
| CLf, m | Liters · hour–1 | 0.28 (0.13–0.37) | 0.14 (0.06–0.34)* | (0.02, 0.03)* |
| 400 mg of fluconazole coadministration | ||||
| CL/F | Liters · hour–1 | 0.5 (0.24–0.82) | 0.4 (0.2–0.8) | (0.4, 0.4) |
| AUC0–inf | Micrograms · milliliter–1 · hour | 93.2 (60.7–206) | 133 (65.4–257) | (119, 133) |
| T1/2 | Hours | 9.9 (7.4–12.5) | 13.7 (12.2–17.1)* | (16.1, 16.1)* |
| Cmax | Micrograms · milliliter–1 | 7.5 (4.7–14.4) | 8.4 (3.7–12.2) | (4.3, 8.5) |
| Tmax | Hours | 2.0 (1.0–4.0) | 1.5 (1.0–4.0) | (1.5, 8) |
| V/F | Liters | 7.5 (4.2–11.0) | 7.1 (4.5–16.4) | (8.8, 9.8) |
| CLf, m | Liters · hour–1 | 0.17 (0.07–0.34) | 0.08 (0.04–0.23) | (0.02, 0.02)* |