Protease Inhibitors

Protease inhibitors constitute a new class of agent for HIV infection. In its process of replication, HIV produces protein and also a protease which cleaves the protein into component parts that are subsequently reassembled into virus particles; protease inhibitors disrupt this essential process.

Protease inhibitors have been shown to reduce viral RNA concentration ('viral load'), increase the CD4 count and improve survival when used in combination with other agents and compared against placebo. They are extensively metabolised by isoenzymes of the cytochrome P450 system, notably by CYP 3A4 which is involved in the metabolism of many drugs. Plasma t1/, for each of these is in the range 2-i h. The drugs have broadly similar therapeutic effects and include:

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