Antiretrovirals Flashcards
which antivirals alter cytochrome p450 and are often used to increase concentrations of ARV drugs that are metabolized through those pathways
Ritonavir - CYP3A4 and 2D6cytochrome; results in large increases in plasma concentrations of drugs
Atazanavir - CYP3A4 and CYP2C9
what are the nucleoside reverse transcriptase inhibitors (NRTI)
- Abacavir
- Lamivudine
- Tenofovir disoproxil fumarate
- Tenofovir alafenamide
- Emtricitabine
what are the protease inhibtiors
“-navir”
what are the non-nucleoside reverse trasncriptase inhibitors (NNRTI)
Efavirenz
Rilpivirine
what are the integrade strand transfer inhibtiros?
“-gravir”
fusion inhibitor
enfuvirtide
co-receptor antagonists
maraviroc
MOA of NRTIs
target = reverse transcriptase
mimic nucleotides to inhibit nucleotide binding to the catalytic site and cause chain termination when incorporated into DNA
require cellular kinases to convert to triphosphate form
Lamivudine:
- class?
- administration?
- therapeutic indications
- NRTI
- oral
- initial tx for HIV, chronic HBV (w/ interferon)
Emtricitabine
- class?
- administration?
- how does it differ from lamivudine
- therapeutic indications?
- NRTI
- oral
- longer T1/2; doesn’t treat HBV
- initial tx of HIV
All antiretrovirals are administered orally besides what drug? how is it administered?
Enfuvirtide
- 2x daily - subQ injection
what drug should be geneitcally screened for HLA-B5701 due to hypersensitivity reactions (fever, rash, fatigue, GI; re-challenge = fatal)
Abacavir
Abacavir:
- class?
- therapeutic indication
- NRTI
2. initial tx of HIV
Tenofovir disoproxil fumarate:
- class?
- therapeutic indications?
- NRTI
2. inital tx HIV, chronic HBV (w/ interferon)
who is tenofovir disoproxil fumarate contraindicated for
pts with renal impairment