Antiretrovirals Flashcards
What are the antiretroviral drug classes?
Fusion inhibitors
Reverse transcriptase inhibitors
Integrase inhibitors
Protease inhibitors
What is the only antiretroviral used that is not po?
Enfuvirtide- fusion inhibitor; binds gp41
What is HAART therapy?
Highly active antiretroviral therapy
2 NRTIs + 1 of the following: NNRTI, protease inhibitor, integrase inhibitor
How do NRTIs work?
Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain- lack 3’OH group
What NRTI is a nucleotide?
Tenofovir
What NRTI is used during pregnancy to reduce the risk of fetal transmission?
Zidovudine
How are nucleoside reverse transcriptase inhibitors activated?
Phosphorylated
NRTIs can cause bone marrow suppression, how can this be reversed?
G-CSF (Filgrastim)
EPO
What is the mechanism of action of NNRTIs?
Bind to reverse transcriptase at site different from NRTIs
Do NNRTIs require phosphorylation to be active?
No
What side effects are common to all NNRTIs?
Rash
Hepatotoxicity
How do protease inhibitors work?
Assembly of virions depends on HIV-1 protease- protease inhibitors inhibit formation of functional viral proteins
What effect does ritonavir have on the CYP450 sytem?
Inhibitor
What is the ending of all protease inhibitors?
-navir
What drug used to treat TB is contraindicated with protease inhibitors? Why?
Rifampin
CYP450 inducer which decreases effect drug levels
