HIV protease inhibitors

Viral protease cleaves precursor proteins into proteins required for viral replication. The inhibitors of this protease (saquinavir, ritonavir, indinavir, and nelfinavir) represent abnormal proteins that possess high antiviral efficacy and are generally well tolerated in the short term. However, prolonged administration is associated with occasionally severe disturbances of lipid and carbohydrate metabolism. Biotransformation of these drugs involves cyto-chrome P450 (CYP 3A4) and is therefore subject to interaction with various other drugs inactivated via this route.

For the dual purpose of increasing the effectiveness of antiviral therapy and preventing the development of a therapy-limiting viral resistance, inhibitors of reverse transcriptase are combined with each other and/or with protease inhibitors.

Combination regimens are designed in accordance with substance-specific development of resistance and pharmacokinetic parameters (CNS penetrability, "neuroprotection," dosing frequency).

Envelope

Matrix protein

Reverse transcriptase

Integrase

Mature virus

Envelope

Matrix protein

Reverse transcriptase

Integrase

Mature virus

Inhibitors of reverse transcriptase

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