Hiv Flashcards
What are the strongest indications for initiating antiretroviral therapy (ART)?
- AIDS-defining illness
- Low CD4+ cell count (< 500 cells/mm3)
- High viral load
What is the typical regimen for antiretroviral therapy (ART)?
- 3 drugs to prevent resistance:
- 2 NRTIs (Nucleoside Reverse Transcriptase Inhibitors)
- Preferably an integrase inhibitor
- Most ARTs active against HIV-1 and HIV-2
What drugs are used in pre-exposure prophylaxis (PrEP)?
Tenofovir + Emtricitabine
Name some NRTIs used in HIV treatment.
- Abacavir (ABC)
- Emtricitabine (FTC)
- Lamivudine (3TC)
- Tenofovir (TDF)
- Zidovudine (ZDV; formerly AZT)
What is the mechanism of action for NRTIs?
- Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain
- Tenofovir is a nucleotide; others are nucleosides requiring phosphorylation to be active
What mnemonic can help remember NRTIs?
Have you dined (vudine) with my nuclear (nucleosides) family?
What are some adverse effects of NRTIs?
- Myelosuppression
- Nephrotoxicity
- Abacavir: Contraindicated in patients with HLA-B*5701 mutation
Name some NNRTIs used in HIV treatment.
- Doravirine
- Efavirenz
- Rilpivirine
What is the mechanism of action for NNRTIs?
- Bind to reverse transcriptase at a site different from NRTIs
- Do not require phosphorylation to be active or compete with nucleotides
What are common adverse effects of NNRTIs?
- Rash
- Hepatotoxicity
- Efavirenz: Vivid dreams, CNS symptoms
Name some drugs classified as Integrase Strand Transfer Inhibitors.
- Bictegravir
- Dolutegravir
What is the mechanism of action for Integrase Strand Transfer Inhibitors?
Inhibit HIV genome integration into the host cell chromosome by reversibly inhibiting HIV integrase
Name some Protease Inhibitors used in HIV treatment.
- Atazanavir
- Darunavir
- Lopinavir
- Ritonavir
What is the mechanism of action for Protease Inhibitors?
- Prevent maturation of new virions by inhibiting HIV-1 protease
- Protease cleaves polypeptide products of HIV mRNA into functional parts
What are the boosting agents for Protease Inhibitors?
- Ritonavir
- Cobicistat