Antiretrovial Therapy
● Combined tx, managing infection on HIV
● Multiple antiretroviral drugs
○ Attacks on multiple stage of HIV life cycle
● Suppress viral replication
○ Improvement of immune function
○ Prevention on progression of AIDS
● Suppression of HIV viral load
○ Under detectable levels
● Restoration and preservation of immune function
○ Increase in CD4+T cell count
● Reduce HIV related morbidity + mortality
● HIV transmission prevention
● Life expectancy improvement
Mechanism
● ART on blocking different stage of HIV life cycle
○ Viral entry on host cell
○ Reverse transcription of viral RNA ⇒ DNA
○ Integration of viral DNA ⇒ Host gene
○ Maturation assembly
■ Viral particles build up
● Multiple drug (drug cocktail)
○ Prevention of viral resistance
○ Improves treatment effectiveness Major classes
● Nucleoside and Nucleotide Reverse Transcriptase Inhibitor
○ Blocking reverse transcriptase enzyme
○ Prevention of conversion of viral RNA to DNA
■ ex)
● Zidovudine
● Lamivudine
● Tenofovir
● Abacavir
● Non-Nucleoside Reverse Transcriptase Inhibitors
○ Binds directly to reverse transcriptase
○ Inhibits its activity
■ ex)
● Efavirenz
● Nevirapine
● Etravirine
● Protease Inhibitors
○ Inhibition of HIV protease enzyme
○ Prevention of maturation of viral particles
■ ex)
● Lopinavir
● Atazanavir
● Darunavir
● Integrase Strand Transfer Inhibitors
○ Blocking integration of viral DNA entering host genome
■ ex)
● Taltegravir ● Dolutegravir
● Bictegravir
● Entry or Fusion Inhibitors
○ Prevention of HIV from entering CD4 cells in first place
■ ex)
● Maraviroc
○ CCR5 antagonist
● Eufuvirtide
○ Fusion inhibition