Which medications in the drug class Antiretroviral Agent, Protease Inhibitor are used in the treatment of HIV Infection and AIDS?

Updated: Dec 02, 2019
  • Author: Nicholas John Bennett, MBBCh, PhD, MA(Cantab), FAAP; Chief Editor: Michael Stuart Bronze, MD  more...
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Answer

Antiretroviral Agent, Protease Inhibitor

PIs inhibit protein precursors necessary for HIV infection of uninfected cells.

Atazanavir (Reyataz)

An azapeptide HIV-1 PI, atazanavir prevents virion maturation by selectively inhibiting Gag and Gag-Pol polyproteins in HIV-1–infected cells.

Darunavir (Prezista)

This HIV-1 PI selectively inhibits HIV-encoded Gag-Pol polyprotein cleavage in infected cells, thereby preventing mature virus particle formation. It is indicated for HIV disease that has not responded to treatment with other antiretroviral agents. Coadminister with low-dose ritonavir (ritonavir-boosted therapy decreases elimination and increases darunavir serum concentration).

Darunavir is typically coadministered with other anti-HIV agents (eg, NRTIs). Food increases maximum plasma concentration (Cmax) and area under the curve (AUC). This agent is indicated for HIV infection in antiretroviral treatment–experienced adults (eg, those with HIV-1 strains resistant to more than one PI).

Fosamprenavir (Lexiva)

Fosamprenavir is a prodrug that is converted to amprenavir by cellular phosphatases in vivo.

Lopinavir and ritonavir (Kaletra)

Lopinavir inhibits HIV protease and renders the enzyme incapable of processing polyprotein precursor, leading to production of noninfectious immature HIV particles. Ritonavir inhibits CYP3A metabolism of lopinavir, increasing plasma levels of lopinavir.

Nelfinavir (Viracept)

Nelfinavir inhibits HIV-1 protease, resulting in the production of an immature and noninfectious virus.

Indinavir (Crixivan)

Indinavir prevents formation of protein precursors necessary for HIV infection of uninfected cells and viral replication.

Ritonavir (Norvir)

This HIV PI is used as a part of double or triple therapy with nucleosides and other protease inhibitors.

Saquinavir (Invirase)

Saquinavir inhibits HIV protease and renders the enzyme incapable of processing polyprotein precursor, leading to production of noninfectious immature HIV particles.

Tipranavir (Aptivus)

A nonpeptidic PI that inhibits HIV replication. Indicated for combination antiretroviral treatment in adults with HIV-1 infection who have evidence of viral replication and who are highly experienced with treatment or who have HIV-1 strains that are resistant to multiple PIs.

Tipranavir must be coadministered with ritonavir (200 mg) to attain therapeutic levels (ie, tipranavir/ritonavir). Administration alone, without ritonavir-boosted levels, is not effective. Genotypic or phenotypic testing and/or treatment history should guide use.


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