HIV Protease Inhibitor Pharmacokinetics
From Proteopedia
| HIV Protease Inhibitor Pharmacokinetics | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Parameter | Ritonavir | Tipranavir | Indinavir | Saquinavir | Amprenavir | Fosamprenavir | Lopinavir | Darunavir | Atazanavir | Nelfinavir | |
| Tmax (hr) | 4.4 | ~3 | 1.5 | 3.7 | .98 | 1.5-4 | 2 | .5 | 2-4 | 3.1 | |
| Cmax (ng/ml) | 13120 | 14600 | 8100 | 2297 | 4901 | 4820 | 11.9 | 2730 | ~4393 | 4701 | |
| Bioavailability (%) | -- | -- | 65 | 4 | -- | -- | -- | -- | 68 | 20-80 | |
| Protein Binding (%) | 99 | >99 | 61 | 98 | 90 | 90 | 99 | 95 | 86 | 98 | |
| T1/2 (hr) | 4.8 | 4.2 | 1.2 | 4.5 | 5.5 | 7.7 | 6.1 | 29.4 | 5.3 | 3.3 | |
| AUC (ng/ml/hr) | 128100 | 46500 | 20900 | 13467 | 11999 | 35000 | 117600 | 4746 | ~26045 | 31906 | |
| Clearance (L/h) | ~8.4 | 32.4 | 49.5 | 36.7 | 56.8 | 84.4 | 1.7 | 32.8 | 13.6 | 37.3 | |
| Dosage (mg) | 600 | 600 | 800 | 1000 | 600 | 1400 | 280 | 400 | 400 | 1250 | |
| Metabolism | Hepatic (CYP3A4 & CYP2C19) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4 & CYP3A5) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | Hepatic (CYP3A4) | |
For Pharmacokinetic Data References, See: References
