Term
Acyclovir
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- guanine analogue
- chain termination via thymidine kinase phosphorylation; rest of phosphorylations done by cellular enzymes to make active agent
Virus:
- HSV 1&2
- VZV
Notes:
- selective for virally infected cells due to first phosphorylation by thymidine kinase of the virus |
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Term
Valacyclovir
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- L-valine ester of acyclovir gets converted to acyclovir in blood
- guanosine analogue, chain terminator via thymidine kinase activation
Viruses:
- HSV 1 & 2
- VZV
Notes:
- better oral absorption than acyclovir |
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Term
Famciclovir
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- chain termination via same mechanism as acyclovir
Viruses:
- HSV 1 & 2
- VZV
Notes:
- oral pro-drug of penciclovir
- longer intracellular 1/2 life than acyclovir |
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Term
Ganciclovir
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- inhibits CMV DNA polymerase
- activated by viral and cellular kinases
Viruses:
- CMV
Toxicity:
- bone marrow and kidney |
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Term
Valganciclovir
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- inhibits CMV DNA polymerase
- activated by viral and cellular kinases
- L-valine of ganciclovir
Viruses:
- CMV
Toxicity/activity:
- bone marrow, nephrotoxicity
- better oral absportion than ganciclovir |
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Term
Cidofovir
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- acyclic cytosine analogue
- chain termination and inhibition of viral DNA polymerase
Viruses:
- broad spectrum
- good for acyclovir resistance in Herpes
- Adenoviruses
- Papillovirues
- pox viruses
Toxicity:
- nephrotoxicity
- has phosphonate group allowing phosphorylation of human cells |
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Term
Foscarnet
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- pyrophosphate anologue
- chain termination by complexing with DNA polymerase to prevent removal of pyrophosphate from nucleoside triphosphates during chain elongation
Viruses:
- Herpes viruses including acyclovir-resistant strains
~ HSV, CMV
Toxicity:
- nephrotoxic |
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Term
Ribavirin
- mechanism
- viruses covered
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Definition
Mechanism:
- guanosine analogue
Viruses:
- many DNA and RNA viruses
- RSV
- Hepatitis C
- Lassa fever virus |
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Term
Amantidine
Rimantidine
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- binds M2 protein on Influenza A and interferes with its ion channel activity thus preventing uncoating of the virus
Virus:
- Influenza A only
Notes:
- side effects include: insomnia, dizziness, difficulty concentrating -- less with amantidine |
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Term
Oseltamivir (oral)
Zanamivir (inhaled)
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- neuramindase inhibitor thus preventing viral release from cell
Virus:
- Influenza A & B
Notes:
- can be given as prophylaxis in an outbreak |
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Term
Interferons
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- glycoproteins that activate cellular ribonucleases which digest viral DNA
- inactivate initiation factor required for initiation of translation of mRNA
- enhance APCs
- modulate cell proliferation
Viruses:
- Hep B and C
- certain malignancies |
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Term
Nucleoside Reverse transcriptase inhibitors (NRTIs)
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- nucleoside analogues → chain termination
Viruses:
- HIV
Notes:
- should not be used alone due to resistance |
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Term
Non-nucleoside reverse transcriptase inhibitors
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- bind near active site of RTase inducing a conformational change that inhibits the synthesis of viral DNA
Viruses:
- HIV
Notes:
- resistance occurs rapidly if used as solo treatment |
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Term
Protease inhibitors
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- inhibits maturation of virus by preventing cleavage of polyproteins
Virus:
- HIV
Notes:
- lopinavir, ataznavir, and darunavir are most popular
- [PI] boosted when used with ritonavir |
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Term
Fusion inhibitors
(T-20- enfurvirtide)
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- blocks conformational change in gp-41 that is necessary for fusion
Virus:
- HIV
Toxicity and Notes:
- IM injection
- Toxic effects = injection site reactions, GI intolerance, hypotension, pruritus, myalgia |
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Term
Raltegravir
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- integrase inhibitor
- inhibits insertion of viral cDNA into host genome
Virus:
- HIV
Toxicity:
- diarrhea, nausea |
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Term
Miraviroc
- mechanism
- viruses covered
- toxicity, activity, or notes |
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Definition
Mechanism:
- CCR5 inhibitor
- prevents co-stimulation necessary for fusion
Virus:
- HIV
Toxicity:
- hepatotoxic
- S/E: cough, fever, upper respiratory infection, rash, musculoskeletal pain, abd. pain, dizziness |
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