Paper II
2019 February (2010 Scheme)

Question

Protease inhibitors

Q53 marksShort Notes

Answer

Protease inhibitors are antiretroviral drugs used in HIV infection.

Examples

  • Ritonavir, Lopinavir, Atazanavir, Indinavir

Mechanism of action

  • Inhibit HIV protease, blocking cleavage of the gag-pol polyprotein into functional structural/enzymatic proteins, resulting in immature, non-infectious virions

Uses

  • Combination antiretroviral therapy (ART), typically boosted with low-dose ritonavir (CYP3A4 inhibition increases plasma levels of the co-administered PI)

Adverse effects

  • GI upset
  • Lipodystrophy
  • Dyslipidaemia, insulin resistance
  • Hepatotoxicity
  • Multiple drug interactions (CYP450 inhibition)

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