Antiviral Agents: HIV Infections Flashcards
Nucleoside reverse transcriptase inhibitors (NRTIs)
MOA: decrease viral DNA synthesis Activation required -P Renal elimination Well tolerated AE: N/V/D, headache, neuropathy, pancreatitis, anemia
Mechanisms of action
1) ⬇️ entry into host cell
2) ⬇️ conversion of viral RNA to DNA
3) ⬇️ integration of viral DNA into host DNA
4) ⬇️ processing of viral polyprotiens
1) enfluvirtide, maraviroc
2) reverse transcriptase inhibitors, NRTIs, NNRTIs
3) integrase inhibitors, ratelgravir, elvitegravir
4) protease inhibitors
Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
HIV
MOA: direct inhibitor of reverse transcriptase, enzyme inhibitor
-admin in active form
* no activation required
-not as well tolerated as NRTIs
AE: sensitive to gastric pH (food/no food)
Rash, hepatotoxicty
⬆️ drug inx riskenzyme inducers
Protease inhibitors
HIV
MOA: inhibit final step in HIV maturation
*⬆️ drug inx: inhibit metabolism/transport of other drugs
-“ritonavir boosting”- on purpose drug rxn to ⬆️ resistance ability
*class wide: drugs sensitive to gastric pH
AE: hyperglycemia, DM, dislipidemia, fat maldistribution, ⬇️ bone density, hepatotoxicty, n/v/d, weakness
Cobicistat (tyboost)
-“boosting agent”
Strong inhibitor of CYP mediated drug metabolism, on purpose to cause drug inx
- to increase the concentration of other antiviral drugs
- take w/food
- no actual antiviral activity
- ⬇️ resistance ability
Integrase inhibitors
HIV
MOA: inhibits viral DNA replication
* metabolized by step 2- glucoronidation
* available always in combo product (stribild)
AE: d/n, HA, fatigue, itching, possible myalgia/Rhabdomyalgia
HIV fusion inhibitor
-enfluvirtide (fuzeon)
MOA: inhibits entry of HIV into CD4 cells
*SQ injection-rxns:rotate sites
-⬇️ drug inx risk
AE: bacterial pneumonia, hypersensitivity rxn
CCR5 antagonist
-Maraviric (selzentry)
MOA: inhibits viral entry into CD4 cells
-doesn’t work on every strain
* requires test to determine if it will work
-PO
AE: cough, dizzy, fever, rash, abdominal pain, musculoskeletal symptoms, hepatotoxicty
Zidovudine *Abacavir: hypersensitivity rxn, genetic test needed Didanosine Tenofovir Stavudine Entecavir Lamivudine Emtricitabine
NRTI’s
HIV
*Efavirenz: inx w/ bc pills Etravirine Rilpivirine Nevirapine Delavirdine *all enzyme Inducers
NNRTI’s
HIV
Lopinavir Atazanavir *ritonavir Fosamprenavir Saquinavir Tipranavir Indinavir Darunavir
Protease inhibitors
HIV
Raltegravir
Elvitegravir
Dolutegravir
Integrase inhibitors
HIV
Enfluvirtide (fuzeon)
HIV infusion Inhibitor
-entry inhibitor
Maraviroc (selzentry)
CCR5 antagonist
-entry inhibitor
