Table 1.
Buprenorphine and norbuprenorphine pharmacokinetic parameters after administration of 2, 4, 8, 12 or 16 mg intravenous buprenorphine to five non-dependent intravenous heroin users.
| Buprenorphine | ||||||
|---|---|---|---|---|---|---|
| Buprenorphine dose (mg) | 2 | 4 | 8 | 12 | 16 | Mean Intravenous |
| Cmax (μg/L) | 21.6 | 56.3 | 110.8 | 164.5 | 174.8 | --- |
| AUCINF (predicted)* (h.μg/L) | 41.4 ±3.0 | 75.9 ± 3.6 | 153.3 ±4.6 | 245.1 ± 27.7 | 269.1 ± 12.9 | --- |
| Cl** (L/h) | 49.8 ± 4.1 | 53.2 ± 2.4 | 52.4 ± 1.6 | 54.7 ± 3.5 | 60.0 ± 2.7 | 54.0 ± 1.7 |
| t1/2 Lambda z*** (h) | 21.8 ± 3.7 | 27.5 ± 4.9 | 28.0 ± 3.0 | 22.3 ± 2.6 | 25.6 ± 1.1 | 25.0 ± 1.3 |
| Vz (predicted)/F**** (L/h) | 743.0 ± 73.5 | 887.5 ± 115.0 | 804.5 ± 69.1 | 702.6 ± 102.0 | 894.5 ± 113.2 | 806.4 ± 38.2 |
| Norbuprenorphine | ||||||
|---|---|---|---|---|---|---|
| Buprenorphine dose (mg) | 2 | 4 | 8 | 12 | 16 | Mean Intravenous |
| Cmax (μg/L) | 1.6 | 1.2 | 2.8 | 6.8 | 5.6 | --- |
| AUClast***** (h.μg/L) | 8.0 ± 3.8 | 11.0 ± 3.4 | 27.6 ± 6.9 | 41.5 ± 9.4 | 61.1 ± 14.6 | --- |
All values are mean ± standard error of the mean.
Abbreviations:
*
AUCINF (predicted): Extrapolation of the area under the plasma concentration-time curve to infinity.
**
Cl: Plasma clearance.
***
t1/2 Lambda z: Elimination half-life.
****
Vz (predicted)/F: Volume of distribution/bioavailability.
*****
AUClast (predicted): Extrapolation of the area under the plasma concentration-time curve to last.