Antivirals Flashcards
acyclovir
- alpha (HSV 1,2) herpes antivirals (nucleoside analog)
- PRO-DRUG activated by viral thymidine kinase and incorporated into elongating DNA chain leading to termination
- elevate some HIV NRTIs (tenofovir). resistance with long term use in immunosuppressed (all nucleoside analogs)
- HSV 1 and 2, VZV in immunocompromised pts, prophylaxis in BMT, HSV encephalitis
cidofovir
- Alpha, Beta, Gamma herpes (nucleoside analog)
- cytosine derivative->converted to active ANP-diphosphates by cellular kinases (does not need virus thymidine kinase) and act as competitive inhibitors of viral DNA polymerase. may act as chain terminators as well.
- resistance after long term treatment in immunosuppressed pts
- thymidine kinase negative or thymidine kinase altered HSV strains, CMV
famciclovir
- alpha herpes antivirals (nucleoside analog)
- diacetyl ester prodrug of peniclovir (acyclic guanine derivative w/ 3’ OH group) causes chain termination
- resistance after long term treatment in immunosuppressed
- HSV 1 and 2
valacyclovir
- alpha (HSV 1,2) herpes antivirals
- PRO-DRUG activated by viral thymidine kinase and incorporated into elongating DNA chain leading to termination (nucleoside analog)
- elevate some HIV NRTIs (tenofovir)
- HSV 1 and 2, VZV in immunocompromised pts, prophylaxis in BMT, HSV encephalitis
foscarnet
-Alpha, Beta and Gamma herpes antivirals (non-nucleoside analogs)
-phosphonoformate analog of pyrophosphate (non-competitive inhibitor of HSV DNA polymerase)
-
-HSV 1 and 2, CMV
docosanol
- alpha herpes antivirals (non-nucleoside analogs)
- saturated fatty alcohol
- mixed evidence of efficacy
- topical cream for HSV 1 and 2
gangciclovir
- Beta and Gamma herpes antivirals (nucleoside analog)
- hydroxymethylated derivative of acyclovir phosphorylated by a virally encoded protein kinase
- granulocytopenia, thrombocytopenia
- life threatening CMV, retinitis in immunocompromised patients
fomivirsen
-Beta and Gamma herpes antivirals (antisense RNA)
-“antisense RNA against CMV” is all that is mentioned in notes
-
-CMV retinitis in immunocompromised patients (only used in the eye)
amantadine
- Influenza antivirals (viral uncoating inhibitor)
- block acidification of virion by binding M2 protein
- administration must occur within 48 hours of symptoms
- influenza A only (also anti-parkinsonian drug)
oseltamivir
-Influenza antivirals (neuraminidase inhibitor)
-ORAL-blocks release of virions from the surface of infected cells
-
-influenza A and B
zanamivir
-influenza antivirals (neuraminidase inhibitor)
-aerosol- blocks the release of virions from the surface of infected cells
-
-influenza A and B
lamivudine
- Hepatitis B antivirals (NRT inhibitor)
- nucleoside analog reverse transcriptase inhibitor
- well tolerated but virus acquires resistance
- HBV
simeprevir
- Hep C antivirals (2nd generation protease inhibitor)
- Oral- inhibits NS3/4 (serine protease)
- interacts with many HIV drugs, rapid resistance if used alone
- genotype I only of Hepatitis C, use with ribavirin and IFN alpha 2a
sofosbuvir
-Hep C antivirals (nucleoside inhibitor)
-Oral-nucleoside inhibitor targets NS5B
-
-Hep C (close to 100% clearance of chronic infection when used with protease inhibitors)
enfuvirtide
- HIV antiviral- entry inhibitor
- C peptide mimi- binds gp41–> stops fusion
- expensive and local inflammation!
- HIV