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
MOA of integrase strand transfer inhibitors (INSTI)
binds to HIV integrase and inhibits DNA strand transfer
Raltegravir
- class
- therapeutic indication
- INSTI
2. initial tx HIV
Elvitegravir
- class?
- therapeutic indications?
- creatine clearance?
- INSTI
- initial HIV tx
- <70 ml/min
Dolutegravir
- class?
- therapeutic indications?
- INSTI
2. initial HIV tx
MOA of protease inhibtiors
target = HIV protease
mimic peptide targets for the protease
block the maturation of virion particles after budding
Ritonavir
- class?
- therapeutic indications?
- protease inhibitor
2. booster - increase T1/2 of coadministered ARV drug due to CYP3A4 effect
what are NNRTIs not active against
HIV-2
NNRTIs MOA
Target = reverse transcriptase
bind to a site on enzyme distinct from the active site
do not require phospohrylation for activation
what class is efavirenz and rilpivirine
NNRTI
what classes of drugs are reserved for tx experienced HIV patients
CCR5 receptor antagonists
Fusion inhibitor
what drug must you screen for tropism before use?
Maraviroc
what are the CCR5 coreceptor antagonists
Maraviroc
theraputic indication for maraviroc
tx expereinced pts with CCR5 tropic virus
what drug is a fusion inhibitor
enfuvirtide
therapeutic indication for enfuvirtide
tx experience pt with evidence of HIV replication even with ARV tx
pre-exposre prohphylaxis
Tenofovir disproxil fumerate and emtricitibine
what drug is not advised for post exposure prophylaxis
Abacavir - b/c need screening for HLA-B5701