Protease Inhibitors

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Protease Inhibitors

  • cause most rapid reduction of HIV-1 in vitro / in vivo

  • resistance becoming a problem

  • induces own metabolism (so increasing dose)

Drugs in Class

  • Ritonavir

  • Indinavir

  • Nelfinavir

  • Saquinavir

Mechanism of Action

  • prevent HIV protease from cleaving gag and gag-pol

  • competitive inhibitors

Adverse Effects

  • nausea

  • vomiting

  • abdominal pain

  • circumoral paraesthesia

  • glucose intolerance

  • fatigue

  • hypertriglyceridaemia

  • fat redistribution

  • multiple drug interaction

Pharmacokinetics

  • well absorbed orally 65-70%

  • food increases absorption so taken with meals

  • ritonavir not as well tolerated due to GI effects

 

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