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acyclovir
- U: HSV1 &2
- A: competitive inhibition of HSV DNA polymerase and chain termination by adding onto the primer chain. since it does not have a 3' end, it can not be used for replication
- R: most commonly alter the thymide kinase (that activates the drug and puts the 1st phosphate on) . Can also alter the HSV DNA polymerase. Can have cross resistance to Valcyclovir and Famciclovir.
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Valcyclovir
- same as acyclovir but with L-valyl ester
- rapidly converted to acyclovir and has 3-5x serum concentration than acyclovir
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Famciclovir
- 1st pass metabolism: converted to penciclovir
- penciclovir achieves higher intracellular concentrations
- works the same as acyclovir and for same viruses
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Ganciclovir/Valganciclovir
- U: treat cytomegalovirusz; CMV retinitis in immunocomprise patients
- A: chain termination by acting on CMV polymerase
- R: CMV loses its thymadine kinase that adds on phosphate
- Admin: IV for 2 weeks
- T: very toxic due to incorporation into host DNA.
- AE: granulocytopenia, thrombocytopenia, renal impairment, seizures
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Cidofovir
- U: treat CMV retinitis and broad spectrum anti-viral agent
- A: direct inhibition of viral DNA polymerase and chain terminator
- R: mutation in CMV DNA polymerase (with cross resistence to ganciclovir)
Nucleotide analog = has phosphate on prodrug
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Foscarnet
- U: broad spectrum anti-viral; CMV retinitis, colitis, esophagitis, acyclovir resistent HSV or VSV
- A: Binds pyrophosphate binding site of viral DNA polymerases and inhibits pyrophosphate cleave of nucleotide triphosphates
- T: very toxic
- AE: Anemias, Renal toxicity, HYPOCALCEMIA due to Ca2+ chelation
- Admin: IV
Combine with ganciclovir to lower the toxicity
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Fomivirsen
- U: Treat CMV retinitis
- A: binds IE2 and directs it to be degraded by host RNases
- Admin: direct injection into eye
Antisense DNA Drug
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Interferon alpha
- U: treat chronic hep B and C (also Human hepres virus type 8, AIDS associated Karposi's sarcoma)
- A: works against both DNA and RNA viruses; inhibits transcription, translation, post-translational processing, virus maturation and virus release
- Admin: subQ, no oral bioavailability
pegylated improves bioavailbility by increasing t1/2
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Ribavirin
- U: treat Hep C, respiratory syncytial virus
- A: Guanosine analog and has multiple sites of action due to lowere GTP levels
along with interferon alpha, this is the standard treatment for Hep C
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Adefovir
- U: treat Hep B and HIV
- A: same as the acyclovir (diphosphate = enzyme inhibitor, triphosphate = chain terminator)
- Admin: prodrug
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Lamivudine
- U: Hep B (and HIV but not as well)
- A: HBV enzyme inhibition and chain termination; Nucleoside reverse transcriptase inhibitor for HIV
- R: mutations of HBV polymerase
- Admin: lower doses for HBV, therefore safer than when used for HIV
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Telbivudine
- U: Hep B ONLY
- A: enzyme inhibition & chain termination
- R: mutation of HBV polymerase
Potential cross resistance to other anti-HBV drugs
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Tenofovir
- U: treat Hep B and HIV
- A: prodrug that gtes phosphorylated and does enzyme inhibition and chain termination
- R: mutations of HBV polymerase; Adefovir-resistant HBV has partial resistance to Tenofovir
- Nucleotide drug
- Long t1/2: once a day dosing
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Amantadine & Rimantadine
- U: treat and prophalax influenza A
- A: block the M2 ion channel; prevent fusion of the viral envelope with the phagolysosome membrane; prevent uncoating of virus
- AE: CNS toxicity; alters dopamine metabolism; Rimantadine has higer oral bioavailability and fewer CNS effects
- R: strains are resistant
- anti-infectious: don't give for both treatment and prophylaxis in same household b/o resistance
- Don't give to pregnant/nursing women or patients with psych problems
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Zanamivir
- Neuraminidase inhibitor
- U: both influenza A and B
- A: act to decrease viral release, decrease viral spread, decrease viral entry, increase formation of viral aggregates
- Admin: inhalation or IV (b/o poor oral bioavailibility)
looks like sialic acid, fits into receptor, better because less likely to get resistence
Both can be use to treat and prophylaxis
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Oseltamivir
- Neuraminidase inhibitor
- U: both influenza A and B
- A: act to decrease viral release, decrease viral spread, decrease viral entry, increase formation of viral aggregates
- Admin: oral as prodrug
receptor has to spread out, easier to get resistence, makes pocket rigid
Both can be use to treat and prophylaxis
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Palivizumab (as in Ab)
- U: prophylaxis against respiratory syncytial virus
- A: Ab against RSV F protein
- Admin: IM (has long t1/2)
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