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| | HIV Protease inhibitors |
 | | Rifamycins acceleratethe metabolism of protease inhibitors (through induction of hepatic P450cytochromeoxidases), resulting in subtherapeutic levels of the proteaseinhibitors.In addition, protease inhibitors retard the metabolism of rifamycins,resultingin increased serum levels of rifamycins and the likelihood ofincreased drugtoxicity. |
 | | All of the HIV protease inhibitors that have been approved and most that are in development, are non-hydrolysable transition state peptidomimetics in which the cleavage site peptide linkage is replaced is replaced by transition state isosteres, such as statine, norstatine, hydroxyethylene, a reducedamide,hydroxyethyl, or dihydroxyethylene. |
 | | Nelfinavir is a relatively small protease inhibitor with goodoral bioavailability (52% in rats at 50 mg/kg; 9-42% in monkeys at 25mg/kg).Although, the half life after 25 mg/kg i.v. |
| www.arches.uga.edu /~ketona/bcmb8010/inhibitors.html (2446 words) |
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