Paper II
2017 February (2010 Scheme) · 40 marks · 120 min

Question

Protease inhibitors in HIV infection.

Q73 marksShort Notes

Answer

Protease inhibitors are a class of antiretroviral drugs used in HIV infection.

Examples

  • Ritonavir, Lopinavir, Atazanavir, Indinavir

Mechanism of action

  • Inhibit HIV protease, the enzyme responsible for cleaving the viral gag-pol polyprotein into functional structural and enzymatic proteins needed for the assembly of mature, infectious viral particles
  • Blocking this step produces immature, non-infectious virions

Uses

  • Combination antiretroviral therapy (ART) for HIV infection, typically boosted with low-dose ritonavir (which inhibits CYP3A4, increasing plasma levels of the co-administered protease inhibitor)

Adverse effects

  • GI upset (nausea, diarrhoea)
  • Lipodystrophy (fat redistribution)
  • Dyslipidaemia, insulin resistance/hyperglycaemia
  • Hepatotoxicity
  • Multiple drug interactions (CYP450 inhibition)

Other Years Asked


Revise MBBS
Preview