HIV anti-retroviral Flashcards
What three drugs make up ART
Two reverse transcriptase inhibitors and an integrase inhibitor
Why is ART so important
18 million lives saved between 2000 and 2021
Why is a combination therapy used for ART
Reduces likelihood that drug resistance will occur
How are ART drugs metabolised
Bictegravir: CYP3A4 and UGT1A
Tenofovir Alafenamide: Carboxylesterase 1 in the liver
Emtricitabine:excreted in urine unmetabolised
How does HIV infect cells
- Enters CD4 cells
- Reverse transcriptase converts HIV RNA into Viral DNA
- Integrase enzymes insert viral DNA into cell genome
- Cell machinery replicates HIV proteins
How does HIV cause disease
Kills CD4 T cells causing immune deficiency
Which ART drugs are reverse transcriptase inhibitors
Tenofovir Alafenamide and Emtricitabine
How do reverse transcriptase inhibitors treat HIV
- Integrates into HIV RNA causing termination of viral DNA production
- Stops reverse transcriptase copying HIV RNA into viral DNA preventing integration into cell genome
Which ART drug is a prodrug
Tenofovir Alafenamide- metabolised by carboxylesterase 1
How does Bictegravir ART work
Binds to active site of HIV integrase blocking the integration of viral DNA into host cell genome preventing replication
What class of drug are the ART drugs
Small molecules