Antivirals (lecture) Flashcards
What is the first line Rx for Herpes and its MoA?
Acyclovir: DNA chain termination because it is a guanosine analog
How does Acyclovir specifically target HSV?
It is a prodrug that is metabolized by viral thymidine kinase?
Azifothymidine is a part of what class of drugs? What is the MoA of that class?
Nucleoside Reverse Transcriptase Inhibitor: They work as chain terminators of reverse transcriptase
What is the underlying reason for AZT toxicities?
It is a prodrug that is not only broken down by viral enzymes, but is ALSO broken down by the HOST’s healthy cells.
What are the three big side effects of NRTIs?
Macrocytic anemia, neutropenia, lactic acidosis (the big one)
Zidovudine, Emtricitabine, Abacavir, and Lamivudine are all examples of ______ (class of drug).
NRTIs hit RT with ZEAL
What two NRTIs are used with co infection of HIV and HVB?
Emtricitabine and Lamivudine
Abacavir will cause hepatomegaly in what specific population?
People with HLA-B*5701 genotype
Tenovir is a _______ (class of drug) and differs from NRTIs in its activity how?
NucleoTIDE analog RT inhibitor, so it is active in resting cells
Nevirapine, Rilpivirine, Etravirine, delavirdine, and Efacvirenz are all examples of what class of Rx?
Non-nucleoside reverse transcriptase inhibitors
What NNRTI is used prophylactically for vertical transmission?
Nevirapine
What NNRTI is contraindicated in pregnancy?
Efavirenz
What is the last line NNRTI?
Etravirine
Which NNRTI is known to cause Stevens Johnson Syndrome?
Nevirapine
What is the MoA of Lamivudine and tenofovir? How are they used in the context of HIV infection?
DNA polymerase inhibitors first used for HBV, but are also effective in HIV treatment (co-infection).
What is the MoA of Maraviroc?
Inhibition of gp 120 (HIV receptor) and CCR5 (T cell receptor) binding. This inhibits binding of HIV with T cells. WILL NOT WORK IF SWITCH TO CXCR5 (of the T cell).
What is the MoA of Enfuvirtide?
Lock gp 41 (HIV co receptor) in its extended conformation, inhibiting cell fusion.
What is the MoA of Raltegravir?
HIV integrase inhibitor.
‘-teg’ –> inTEGrate
Protease inhibitors all end in ______.
-navir
What is the first line protease inhibitor in pregnant patients?
Ritonavir - this also increases the activity of other protease inhibitors
As a general rule, is there cross resistance of drugs within a class?
NO. If one drug in a class doesn’t work, trying another of the same class is commonplace.
Ribavirin is used in what two viral infections?
HCV and RSV (aerosolized)
HCV protease inhibitors have the suffix ______.
-previr
What is the MoA and use of Sofosbuvir?
HCV RNA synthase inhibitor.