Key pharmacokinetic parameters for nucleoside analogues obtained in various mammalian species
| Parameter | Species8-b | Nucleoside Analogue8-a | ||||
|---|---|---|---|---|---|---|
| D4T | ZDV | DDC | 3TC | DDI | ||
| CL(ml/min/kg) | Mouse | 28.7 | 22.7 | 25.0 | ND | 75.0 |
| Rat | 24.0 | 47.0 | 25.2 | 20.0 | 66.0 | |
| Monkey | 14.5 | 26.2 | 7.60 | 12.7 | 12.3 | |
| Dog | ND8-c | 13.9 | ND | 6.06 | 22.7 | |
| Human | 8.17 | 26.7 | 6.33 | 5.41 | 13.5 | |
| Vss (l/kg) | Mouse | 0.76 | 0.73 | 0.59 | ND | 0.90 |
| Rat | 0.70 | 1.61 | 1.54 | 2.70 | 0.99 | |
| Monkey | 0.92 | 1.08 | 0.87 | 1.16 | 0.92 | |
| Dog | ND | 1.00 | ND | 0.87 | 0.95 | |
| Human | 0.53 | 1.40 | 0.54 | 1.30 | 0.81 | |
| T1/2 (h) | Mouse | 0.3 | 1.1 | 1.5 | ND | 0.1 |
| Rat | 0.4 | 1.0 | 1.0 | 1.68-d | 0.6 | |
| Monkey | 0.7 | 0.5 | 1.8 | 1.4 | 1.2 | |
| Dog | ND | 1.0 | ND | 1.78-d | 1.1 | |
| Human | 1.1 | 1.1 | 1.2 | 2.5 | 1.2 | |
| UR(%) | Mouse | ND | 70 | 64 | ND | ND |
| Rat | 79 | 72 | 49 | ND | 28 | |
| Monkey | 44 | 40 | 68 | 46 | 19 | |
| Dog | ND | 65 | ND | ND | 46 | |
| Human | 43 | 19 | 75 | 71 | 50 | |
↵8-a D4T, stavudine; ZDV, zidovudine; DDC, zalcitabine; 3TC, lamivudine; DDI, didanosine.
↵8-b Data from references Hussey et al., 1994; Ibrahim and Boudinot, 1989; Kaul et al., 1991; Knupp et al., 1991; 1992; Patel et al., 1990; Qian et al., 1991; Russell et al., 1990; Russell and Klunk, 1989; van Leeuwen et al., 1992; Wientjes and Au, 1992.
↵8-c ND, not determined.
↵8-d Estimated from clearance and volume terms.