Table 2.
Pharmacokinetic parameters of rivaroxaban after the administration of a single 10 mg dose of oral rivaroxaban to healthy controls and subjects with mild, moderate and severe renal impairment
| Renally impaired groups | ||||
|---|---|---|---|---|
| Healthy controls (n=8) | Mild impairment (n=8) | Moderate impairment (n=8) | Severe impairment (n=8) | |
| AUC (µg l−1 h) | 1247 (49.3) | 1 863 (30.9) | 2 068 (33.1) | 2 228 (37.0) |
| AUCnorm (g l−1 h) | 9439 (49.6) | 14 780 (31.6) | 15 440 (28.1) | 15 940 (48.5) |
| Cmax (µg l−1) | 172.3 (30.7) | 217.5 (37.9) | 206.2 (26.0) | 232.2 (33.1) |
| Cmax,norm (g l−1) | 1304 (25.9) | 1 725 (37.4) | 1 540 (23.9) | 1 662 (34.6) |
| t1/2 (h) | 8.3 (38.4) | 8.7 (50.1) | 9.0 (38.6) | 9.5 (31.8) |
| CL/F (l h−1) | 8.0 (49.3) | 5.4 (30.8) | 4.8 (33.1) | 4.5 (37.0) |
| fu (%) | 7.3 (19.3) | 5.4 (30.7) | 8.2 (32.4) | 7.6 (23.2) |
| tmax (h)* | 2.0 (0.5–4.0) | 2.0 (1.0–6.0) | 3.0 (1.0–4.0) | 3.0 (2.0–4.0) |
| CLR (l h−1) | 2.4 (46.5)† | 1.2 (29.2) | 0.7 (33.1) | 0.5 (40.4) |
| Aeur (%) | 29.2 (25.8)† | 20.2 (28.0) | 13.1 (53.1) | 10.4 (35.8) |
| AUC ratio (90% CI) vs. healthy controls‡ | – | 1.44 (1.08, 1.91) | 1.52 (1.15, 2.01) | 1.64 (1.24, 2.17) |
| Cmax ratio (90% CI) vs. healthy controls‡ | – | 1.28 (1.07, 1.55) | 1.12 (0.93, 1.34) | 1.26 (1.05, 1.51) |
Data are given as geometric mean (% coefficient of variation) unless indicated otherwise.
*
Median (range).
†
n= 7.
‡
Calculated by analysis of variance.
Aeur, amount of drug excreted via urine; AUC, area under the plasma concentration–time curve; AUCnorm, bodyweight and dose-normalized AUC; CI, confidence interval; CL/F total body clearance; CLR, renal clearance of drug; Cmax, maximum plasma concentration; Cmax,norm, bodyweight and dose-normalized Cmax; fu, fraction of unbound drug in plasma; t1/2, terminal elimination half-life; tmax, time to reach Cmax.