PMCOL 344 – Antivirals Exam Study Guide.
Amantadine - answer✔Prophylaxis and treatment of influenza A. Inhibits pH depending
uncoating of virus by blocking M2. CNS effects at higher doses and not safe in pregnancy.
Rimantadine - answer✔Prophylaxis and treatment of influenza A. Inhibits pH depending
uncoating of virus by blocking M2. CNS effects at higher doses (less than amantadine) and not
safe in pregnancy.
Tamiflu (oseltamivir) - answer✔Selective viral neuroaminidase inhibitor to treat both influenza
A and B. Transition-state analog so binds with high affinity and prevents new viral particles from
being released from infected cells. Co-administered with probenecid to maintain peak plasma
conc. Nausea and vomiting!
Zanamivir (Relenza) - answer✔Selective viral neuroaminidase inhibitor to treat both influenza
A and B. Competitive inhibitor, prevents new viral particles from being released from infected
cells. Slightly diff molecular binding site than Tamiflu so retains activity even if resistant to
Tamilu. Nausea, diarrhea, sinusitis.
Acyclovir - answer✔Acyclic nucleoside analog. Inhibits replication of HSV and VZV. Must be
converted to acyclovir triphosphate (partly by virus machinery) to inhibit viral DNA pol and be
incorporated into DNA as a chain terminator.
Ganciclovir - answer✔Acyclic nucleoside analog. Inhibits replication of HSV and CMV. Must
be converted to ganciclovir triphosphate (partly by virus machinery) to inhibit viral DNA pol and
be incorporated into DNA as a chain terminator. Dose limiting bone marrow toxicity.
Phosphonoformic acid (Foscarnet) - answer✔Pyrophospate analog that blocks the PPi binding
site of viral DNA pol. Active against CMV and HSV/VZV acyclovir-resistant infections. Dose
limiting renal toxicity.
Ribavirin - answer✔Purine (Guanine) nucleoside analogue. Inhibits IMP dehydrogenase and
depletes GTP + dGTP. Treats broad number of DNA and RNA viruses (but also affects
uninfected cells). Only treatment known for RSV.
zidovudine (AZT) - answer✔Nucleoside reverse transcriptase inhibitor - must be metabolized
by cellular enzymes to the triphosphate version. Competitively inhibits RT and are DNA chain
terminators. Bone marrow suppression dose limiting toxicity. for HIV.