Antiretroviral Drugs Flashcards
What are the different types/targets of HIV Drugs?
Copreceptor antagonists
Fusion Inhibitors, Integrase inhibitors, Protease inhibitors, Nucleoside and non-nucleoside reverse transcritase inhibitors
Which Drugs are NRTIS?
Zidovudine Lamivudine Abacavir Tenofovir Emtricitibine
What is the MOA of NRTIs
Targets reverse transcriptase. prevents nucleotide binding to the catalytic site ==> Chain termination. Fits in the active site of Reverse Trasncriptase.
What are the adverse effects of NRTIs?
Lactic Acidosis, fatty liver disease, and lipodystrophy
Adverse effects of Abacavir?
Allergic reactions. increased risk of cardiac events, lower effectiveness of methadone.
What is a benefit of Lamivudine?
One of the least toxic antiretroviral drugs .
What is the benefit of using Emtricitabine?
Half life is longer (>24hrs) than others in its class.
Unique adverse effects of Tenofovir?
Renal and bone toxicity. Drug crosses placenta and decreases bone density in fetus.
unique adverse effects of Zidovudine?
Myelosupression, fatuige, malaise, nausea, headache, etc…
MOA of NNRTIs.
Bind to a site other than the active site on Reverse Transcriptase.
Common Adverse effects of NNRTIs?
Rash, Steven Johnson Syndrome, hepatotox, effects Cyt p450 enzymes.
How does resistance develop to Efavirenz?
A sigle base change in gene for rev. Transcriptase.
Adverse effects of Nevirapine?
Rash, Hepatitis(cqn be fulminant!
How to Protease inhibitor drugs work?
Mimic Peptide targets of protease, blcock maturation of virion particles.
Common Adverse effects of Protease inhibitors?
Cyt P450 Enzymes ==> Drug interactions, Hyperlipidemia, lipodystrophy, hapatotox.
Unique Pharmkinetics of Atazanavir?
Food increases bioavailability. Acid Needed. PPIs contraindicated
Adverse effects of Ritonavir?
POTENT inhbitor of CYP3A4 Cyt P450 enzyme. Increased half life of combined drugs.
What drug is combined with Darunavir?
Ritonavir because it increases half life
Adverse effects of Maraviroc?
Cough, URT infections, postural hypotension, arthralgia, myalgia.
Indications for Maraviroc?
Good for CCR5 tropic virus. but not others. Screen for tropisms first!
How do fusion inhibitors work on virally infected cell?
Prevent viruses from bringing membranes together in order to bud off from cell.
What is unique about the administration of Enfuvirtide?
Only parenterally delivered antiretroviral agent.
Adverse effects of Enfuvirtide?
Painful erythematous nodule at sote of injection, increased risk of bacterial pnumonia.
How do integrase inhibiting drugs work?
Prevent virus from integrating its DNA into the host DNA! Only infefected til cells die!
Adverse effects of Raltegravir?
Myopathy, rhabdomyolysis, creatine kinase elevation
Pharmicokinetics of Elvitegravir?
Requires co-admin with cobicistat which inhibits CYP3A4
Benefits of using Dolutegravir?
Can work on viruses that have developed resistance to other Integrase inhibitors.
When is it reccomended to start antiretroviral treatment?
Good to start at any level of immunosupression! Reccomendations get stronger as CD4 counts go lower.
Why is ARV treatment reccomended?
Prevents transmission of virus to others!
What is the standard of care of ARV therapy?
3 drugs from 2 different classes. 1PI and 2 NRTIs or 1II and 2 NRTIs.
