Table 1.
Mean pharmacokinetic parameters on day 1 and day 13 following multiple nalbuphine oral doses
| Parameter | Statistics | Hemodialysis patients | Healthy subjects | ||
|---|---|---|---|---|---|
| 30 mg QD | 180 mg BID | 30 mg QD | 180 mg BID | ||
| Day 1 | Day 13 | Day 1 | Day 13 | ||
| AUC inf (ng•h/mL) | N | 4 | 4 | 7 | 8 |
| Mean | 142.5 | 2635.38 | 49.53 | 588.40 | |
| SD | 33.28 | 2038.01 | 30.04 | 214.08 | |
| CV% | 23.4 | 77.3 | 60.7 | 36.4 | |
| AUC last (ng•h/mL) | N | 15 | 9 | 9 | 8 |
| Mean | 73.43 | 1457.74 | 40.55 | 529.85 | |
| SD | 41.81 | 1016.26 | 22.96 | 179.93 | |
| CV% | 56.9 | 69.7 | 56.6 | 34.0 | |
| AUC tau (ng•h/mL) | N | 15 | 9 | 9 | 8 |
| Mean | 43.2 | 760.87 | 31.53 | 351.15 | |
| SD | 24.97 | 538.28 | 16.93 | 118.21 | |
| CV | 57.8 | 70.7 | 53.7 | 33.7 | |
| ARAUC tau ratio | Ratio of Mean | 2.7 | NA | 1.6 | NA |
| C max (ng/mL) | N | 15 | 9 | 9 | 8 |
| Mean | 6.28 | 82.78 | 5.2 | 44.21 | |
| SD | 3.36 | 55.81 | 2.78 | 14.54 | |
| CV | 53.5 | 67.4 | 53.5 | 32.9 | |
| T max (h) | N | 15 | 9 | 9 | 8 |
| Min | 1.0 | 2.0 | 2.0 | 2.0 | |
| Median | 5.0 | 5.0 | 3.0 | 4.0 | |
| Max | 18 | 7.1 | 5.0 | 6.0 | |
| T 1/2 (h) | N | 4 | 4 | 7 | 8 |
| Mean | 10.49 | 14.23 | 6.81 | 8.58 | |
| SD | 2.22 | 3.24 | 2.79 | 2.05 | |
| CV | 21.1 | 22.7 | 41.0 | 23.9 | |
Subjects were titrated every 3–4 days from 30 mg QD on Day 1 to 30 mg BID then 60 mg BID, 120 mg BID and finally 180 mg BID over a 14-day period. Data shown for Day 1 and Day 13 only.
Abbreviations: ARAUC tau accumulation ratio (mean AUCtau Day 4/Mean AUCtau Day 1), AUC inf area under plasma concentration-time curve from time zero extrapolated to infinite time, AUC last area under the plasma concentration-time curve from time zero to the last measureable concentration, AUC tau area under plasma concentration-time curve over dosing interval (0-12 hr), BID twice daily, C max maximum observed plasma concentration, CV coefficient of variation, ER extended release, h hour, Max maximum, Min minimum, n number of subjects, NA not applicable, QD once daily, T max time of maximum observed plasma concentration, T 1/2 plasma half life.