Antiretrovirals Flashcards
Maraviroc
CCR5 inhibitor
Enfuvirtide
Fusion (gp41) inhibitor
Injection site irritation
Raltegravir
Integrase Strand Inhibitor
Metabolized by Glucuronidation
Very few side effects, well-tolerated
NRTI’s
Nucleoside Analogs - Chain Terminators
All metabolized by kidney except Abacavir
M184V mutation - will be selected for if you use this as mono therapy. Don’t.
Abacavir (ABC)
NRTIs
HLA-B57:01 - Steven’s Johnson Syndrome
Should I re-challenge? NO.
I have no idea why. But NO.
Metabolized by LIVER
Didanosine
NRTIs
Pancreatitis, Peripheral neuropathy
Stavudine
NRTIs - Thymidine Analog
Pancreatitis, Peripheral neuropathy
Lamivudine
NRTIs
No SE listed
Tenofovir
NRTIs
AKI (Fanconi), Bone Density loss
Zidovudine (AZT)
NRTIs - Thymidine Analog
Bone marrow suppression, Mitochondrial Toxicity
M184V mutation - will be selected for if you use this as mono therapy. Don’t.
Zalcitabine
NRTIs
Aphthous Ulcerations
Delaviridine
NNRTI - bind to a pocket in RT’s
Liver metabolism
K103N mutation
Efavirenz
NNRTI- bind to a pocket in RT’s
Liver metabolism
K103N mutation
Etravirine
NNRTI- bind to a pocket in RT’s
Liver metabolism
K103N mutation
Elvitegravir
Integrase Strand Inhibitor
Metabolized by Glucuronidation
Very few side effects, well-tolerated
Dolutegravir
Integrase Strand Inhibitor
Metabolized by Glucuronidation
Very few side effects, well-tolerated
Protease Inhibitors
Metabolized by liver, inhibit isoenzyme 3A4
End in -navir
GI side effects
I84V mutation
Atazanavir
Protease inhibitor
I84V mutation
Darunavir
Protease inhibitor
I84V mutation
Indinavir
Protease inhibitor
I84V mutation
Cobicistat
CYP450 inhibitor
Like Ritonavir
Often combined with Elvitegravier
When to start therapy?
NOW. As soon as someone has a diagnosis. NEVER STOP THERAPY.
Post Exposure Prophylaxis
Within 72 hours for 28 days
Reduces risk by 80%
M184V
NRTI mutation
K103N
NNRTI mutation
Ritonavir
Inhibits CYP450, boosting the action of protease inhibitors
Preferred Therapy Regimens
R/PI + 2 NRTI’s
INSTI + 2 NRTI’s