Table 2.
Pharmacokinetic parameters of bupropion and its metabolites in 17 healthy subjects (control) and patients with renal impairment after a single oral 150 mg dose
| Parameter | Control | Impaired kidney function | % Difference and P value vs. control |
|---|---|---|---|
| Bupropion | |||
| AUC (µg ml−1 h) | 0.49 ± 0.29 | 1.1 ± 0.37 | +126% (<0.0001) |
| Cmax (ng ml−1) | 66.1 ± 33.7 | 123 ± 41.8 | +86% (0.001) |
| tmax (h) | 4 (2–5) | 3 (2–5) | – (0.39) |
| t1/2 (h) | 8.1 ± 7.2 | 19.4 ± 4.4 | +140% (0.001) |
| CL/F (l h−1) | 414 ± 264 | 155 ± 46.8 | −63% (0.001) |
| Hydroxybupropion | |||
| AUC (µg ml−1 h) | 13.9 ± 7.2 | 12.5 ± 6.3 | −10% (0.57) |
| Cmax (ng ml−1) | 404 ± 175 | 372 ± 151 | −8% (0.50) |
| tmax (h) | 8 (4–12) | 5.5 (4–12) | – (0.39) |
| t1/2 (h) | 23.5 ± 10.2 | 27.5 ± 11.5 | +17% (0.36) |
| Hydrobupropion | |||
| AUC (µg ml−1 h) | 6.6 ± 1.2 | 8.2 ± 5.3 | +24% (0.82) |
| Cmax (ng ml−1) | 208 ± 49.9 | 245 ± 157 | +18% (0.75) |
| tmax (h) | 6 (4–12) | 5 (4–6) | – (0.07) |
| t1/2 (h) | 34.7 ± 14.0 | 49.7 ± 12.5 | +43% (0.005) |
| AUC ratios | |||
| OH-BUP : BUP | 35.8 ± 25.4 | 12.2 ± 6.3 | −66% (<0.0001) |
| H2-BUP : BUP | 23.8 ± 27.8 | 7.5 ± 3.4 | −69% (0.001) |
| OH-BUP : H2-BUP | 2.1 ± 1.1 | 1.7 ± 0.9 | −18% (0.29) |
The results are presented mean ± SD (median with range for t max). The percentage difference was calculated from the means, and the P values are given for the absolute changes. AUC area under plasma concentration-time curve; Cmax maximum plasma concentration; max time to maximum plasma oncentration; t 1/2 half-life; CL/F apparent oral clearance; bupropion, BUP; hydroxybupropion, OH-BUP; hydrobupropion, H2-BUP.