13-14 Antivirals Flashcards
Cyclophosphamine
Alkylating, Mustard nitrogen
Prodrug, activated by P450, toxic metabolite= acrolein -> hemorrhagic cystitis
Mechlorethamine (Mustargen)
Alkylating, Nitrogen mustard
Most effective G1-M phase
Part of MOPP regimen Hodgkin disease
Tox: vesicant, hematologic, hyperuricemia, renal damage, N/V, sterility, teratogenic
Acyclovir
Valacyclovir
anti-HSV, guanosine analogue, P by viral thymidine kinase ->inhibits viral DNA polymerase. Accumulates in infected cells.
DOC HSV 1&2 (oral, top, iv), genital herpes (red shedding, inc healing, de pain), herpes keratitis (topical), neon/encephalitis (IV), hairy leukoplakia (AIDS).
Prophy: pregnancy (safe), organ transplant, immunocompromised
Non toxic to nl cells, lethargy + zidovudine, nephrotoxic IV high dose
Valacyclovir: prodrug, better bioavail, longer acting
Famciclovir
Penciclovir
anti-HSV, P by viral thymidine kinase (similar to acyclovir)
kidney excretion
Famciclovir: prodrug
Trifluridine
Topical for resistant HSV
Visual haze SE
Docosanol
Inhibits viral fusion: HSV can’t enter cell
Topical/OTC cold sores
Tox: skin irritation, HA
Valganciclovir
Ganciclovir
P by thymidine kinase (HSV) and viral protein kinase phosphotransferase (CMV)
Gancyclovir: IV-life/sight-threatening CMV, immunocomp supp. risk of neutropenia/thrombocytopenia, N/F, rash, abnl LFTs
Valgancyclovir: prodrug, oral, prophy, transplants, ocular implants.
Cidofovir
Cytosine analogue -> inhibits viral DNA polymerase (no intracellular P/activation)
CMV retinitis and resistant HSV
Nephrotoxic (+hydration+probenecib)
Foscarnet
Directly inhibits viral DNA, RNA polymerase & reverse transcriptase
Use: CMV retinitis, resistant HSV (can combo +ganciclovir)
Nephrotoxic
Fomivirsen
Antisense compound complimentary to mRNA (CMV)
Inhibits protein synth +replication of CMV
For ophtalm use (intravitral inject) CMV retinitis (AIDS)
tox: ocular infl, visual impairement
