Question
Protease inhibitors in HIV infection.
Q7 3 marks Short 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)
1 Antiviral Drugs
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