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22 Cards in this Set
- Front
- Back
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Points of action for various antiviral drugs
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Penetration
Uncoating Early protein synthesis Nucleic acid synthesis late protein synthesis packaging |
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Penetration drug
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T20 (HIV)
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Uncoating drugs
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Amantadine
Rimantidine (influenza A) |
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Early protein synthesis blockers
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fomivirsen (CMV)
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blockers of nucleic acid synthesis
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Inhibitors of RNA/DNA polymerases; purine, pyrimidine analogs, acyclovir (HSV)/ganciclovir (CMV)
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Late protein synthesis inhibitors
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Protease inhibitors, e.g., Ritonavir, Indinivir (HIV)
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Packaging and assembly blockers
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neuraminidase inhibitors (zanamavir--for influenza)
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Acyclovir
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* Guanosine Analog
* Must be phosphorylated to triphosphate for activity * viral thymidine kinase does initial phosphorylation * greater affinity for viral DNA polymerase; binds irreversibly * chain terminator and inhibitor of DNA polymerase |
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Acyclovir is used in these infections
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HSV and VZV
minimal toxicity |
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Valacyclovir
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prodrug of acyclovir
(converted to acyclovir and valine) same moa as acyclovir |
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valacyclovir uses:
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acute zoster (VSV), genital herpes (HSV)
minimal toxicity |
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Famciclovir
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Prodrug of penciclovir
guanosine analog converted to penciclovir in gut and liver different rate of phosphorylation, intracellular half life, DNA polymerase Does NOT cause chain termination |
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Famciclovir uses
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acute zoster (VSV)
genital herpes mucocutaneous HSV (in HIV+) topical cream for herpes labialis minimal toxicity |
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Ganciclovir (DHPG)
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guanosine analog
mechanism same as acyclovir in HSV, but effective against CMV |
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Ganciclovir uses
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life-threatening CMV (retinitis, pneumonitis)
especially in immunocompromised SIGNIFICANT TOXICTY: HEMATOLOGIC MYELOSUPPRESSION |
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Cidofovir
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nucleotide analog
cellular enzymes phosphorylate it to active form inhibits viral DNA polymerase |
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Cidofovir uses
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Severe CMV (retinitis)
Toxicity: Renal |
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Foscarnet
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Pyrophosphate analog
-activity against viral DNA polymerase, reverse transcriptase, and RNA polymerase in vitro -blocks pyrophosphate binding site of viral DNA polymerase |
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Foscarnet uses
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acyclovir-resistant HSV or VSV
CMV retinitis, other CMV unresponsive to ganciclovir |
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Foscarnet Toxicity
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Renal
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Fomiversen Sodium
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antisense oligonucleotide
complementary to immediate-early region of CMV nucleic acid inhibits viral replication Injected into eye (intravitreally) |
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Fomiversen Toxicity
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Uveitis, Intraocular Pressure
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