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25 Cards in this Set
- Front
- Back
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What antiviral drugs inhibit viral replication at "penetration and uncoating"?
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Please take my COAT off D-E-A-R!
Docosanol- HSV1 Enfuvirtide- HIV (gp41) Amantadine- blocks M2 proton pump (prophy FluA not FluB) Rimantidine- similar to amant. |
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What antiviral drugs inhibit viral replication at "assembly and release"?
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Dorothy ASSEMBLED munchkins in OZ
Zanamavir & Oseltamivir tx of Flu A & B. works at end/viral budding step by inhibiting viral NEURAMINIDASE. reduces severity and duration os sxs, not curative. |
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What is special about Oseltamivir?
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It is effective against H5N1 strain of flu. Oral prodrug
(zanamivir is inhaled) |
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What antiviral drug is a Humanized monoclonal antibody?
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Palivizumab
directed against the F prot of RSV and is used in prophy tx of RSV in high risk infants |
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What antiviral drugs inhibit viral replication at "Nucleic Acid Synthesis"?
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V-GRAFT is the new target for NA synthesis
Vidarabine Ganciclovir Ribavarin Acyclovir Foscarnet Trifluridine |
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Whats great about Acyclovir?
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The most perfect drug ever: guanosine analog w acyclic side chain.
HSV 1 & 2, VZV DOC for herpes encephalitis, chickenpox in adolescents and adults Extremely potent inhibitor of VIRAL DNA POL |
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What other drugs do we think of with Acyclovir?
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Valacyclovir- a prodrug for higher theraputic levels 3-5X greater serum conc HSV2
Penciclovir- acyclovir analogue HSV1. well tolerated Famciclovir- prodrug form of Penciclovir |
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What do we use Vidarabine for?
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It is an adenosine analogue
Used for tx of OCULAR herpes simplex infections. |
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What do we use Ganciclovir for?
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CMV retinitis
another acyclic guanine analog closely related to acyclovir bc it can be phosphorylated to a limited extent by cellular kinase its use is limited to severe CMV infections in immunocomprimised pts |
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What do we use Ribavarin for?
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For RSV in kids
In comb w IFN-alpha for Hep C!!! |
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What is trifluridine?
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Athymidine analogue, 3 H's in 5-methyl group of thymidines have been replaced by flourines.
MOA: Inhibits thyidylate synthetase and feedback inhibits other steps in pyrimidine biosynthesis. |
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What is trifluridine used for?
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DOC for herpetic conjunctival keratitis (about the same effect as vidarabine)
BC this drug is rapidly metabolized by nucleotidases, it is only useful in metabolically inactive sites (ie: the eye) |
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What is unique about foscarnet?
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It is a inhibitor of viral DNA synthesis but in tow ways.
1) it inhibits HSV and CMV-encoded DNA POL 2) in inhibits HIV-encoded reverse transcriptase |
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What are the uses for foscarnet?
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Effective against ganciclovir-resistant CMV retinitis in AIDS pts
DOC for acyclovir-resistant HSV in AIDS pts |
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What are the dose limiting toxicities of foscarnet?
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Nephrotoxicity and symptomatic hypocalcemia
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What is the prototypic NUCLEOSIDE Reverse Transcriptase inhibitor?
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Zidovudine (AZT)
sunthetic thymidine analogue HIV RT is 100 times more likely to use AZT instead of thymidine. |
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What is a big prob with the NRTIs?
NUCLEOSIDE |
All NRTIs have the potential to induce LACTIC ACIDOSIS as a result of their MITOCHONDRIAL toxicity
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What are the other NRTIs?
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ddI- Didanosine (peripheral neuropathy, fatal pancreatitis)
3TC- lamivudine (in comb w IFN-alpha--->tx HepB) d4T- Stavudine & ddC-Zalcitabine (peripheral neuropathy) abacavir (severe hypersensitivity and hepatomegaly) |
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When do we use a nucleoTIDE reverse transcriptase inhibitor?
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Antiviral activity in RESTING cells
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What are the nucleoTIDE RTIs?
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tenofovir disoproxil (in comb w ddI inc risk of pancreatitis)
cidofovir (ganc and fosc resistant CMV retinitis) adefovir (hepB, nephrotox) |
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What are the non-NRTIs?
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Efavirenz- 1x daily dose, fewest side effects. SUPERIOR
Delaviridine (rash, fatigue, nausea) Nevirapine (hepatotoxicity, Stevens Johnson syndrome, toxic epidermal necrolysis) |
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What are the protease inhibitors?
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all the -AVIRs
MOA: bind to the catalytic site of the HIV encoded protease, blocking the cleavage of the multiprotein gag-pol precursor into mature proteins Should ONLY be used in comb therapy w 1 or more nucleoside ANALOG |
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What can significantly decrease serum conc of PIs?
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Inducers of CYP34A (RIFAMPIN)
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If we want to tx Hep C??
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Ribavarin and IFN alfa-2B
IFN alfa2B alone ---> Hep B |
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What are the more serious side effects of PIs?
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Lipodystrophies
Hyperglycemias Hypertriglyceridemias atazanavir has the lowest incidence of lipodystrophies |
