TABLE 2.
Pharmacokinetic parameters for cidofovir formed in vivo following intravenous administration of cyclic HPMPC to HIV-infected patientsa
| Cyclic HPMPC dose (mg/kg) | Tmax (h) | Cmax (μg/ml) | β (h−1) | t1/2β (h) | AUC0–tlast (μg · h/ml) | AUC0–∞ (μg · h/ml) | AUMC0–∞ (μg · h2/ml) | MRT (h) | % Dose excreted in 24 h | % of total AUC | % of i.v. CDV AUCb |
|---|---|---|---|---|---|---|---|---|---|---|---|
| 1.5 | 1.58 (0.20) | 0.253 (0.045) | 0.234 (0.069) | 3.21 (1.02) | 1.11 (0.19) | 1.30 (0.15) | 6.75 (1.74) | 5.16 (1.13) | 8.43 (1.84) | 16.0 (3.81) | 12.2 (1.44) |
| 3.0 | 1.75 (0.27) | 0.617 (0.170) | 0.205 (0.049) | 3.66 (1.40) | 3.23 (1.07) | 3.50 (1.10) | 20.4 (10.8) | 5.64 (0.99) | 10.6 (3.45) | 17.3 (3.10) | 16.4 (5.14) |
| 5.0 | 1.58 (0.204) | 1.41 (0.821) | 0.174 (0.063) | 4.37 (1.29) | 5.54 (1.19) | 5.80 (1.19) | 32.7 (8.85) | 5.63 (0.982) | 10.0 (1.59) | 17.6 (3.59) | 16.3 (3.33) |
| 7.5 | 1.63 (0.250) | 1.40 (0.231) | 0.137 (0.005) | 5.06 (0.200) | 7.49 (1.68) | 7.81 (1.74) | 51.8 (12.4) | 6.62 (0.25) | 8.19 (1.06) | 16.7 (2.34) | 14.6 (3.26) |
| Mean | 1.64 (0.228) | 3.98 (1.26) | 5.68 (1.01) | 9.40 (2.33) | 16.9 (3.17) | 14.9 (3.77) |
a
β, elimination rate constant; t1/2β, elimination half-life; AUMC0–∞, area under the first moment of the concentration-time curve from time zero to infinity; MRT, mean residence time; the other abbreviations are defined in the text. Values are means (SDs).
b
Based on historical data for intravenous (i.v.) cidofovir (CDV) without probenecid (7).