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26 Cards in this Set

  • Front
  • Back
1. Virucides

2. Antivirals

3. Immunomodulators
1. inactivate intact viruses

2. inhibit viral replication @ cellular level

3. augment/modify host response to infection
Antivirals for Herpesviruses:
1-7
Acyclovir; Valacyclovir; Famciclovir; Ganciclovir; Cidofovir; Foscarnet; Fomivirsen sodium
Acyclovir
1. MOA
2. Properties
3. Use
4. Toxicity
1. guanosine analogue; valine group allows better intestinal absorption; chain terminator and inhibitor of viral DNA pol
2. IV, oral, topical; 2.5hr h.l.; adjust dosage for renal impairment
3. HSV, VZV
4. minimal; does not affect host enzymes; GI symptoms
Valacyclovir
1. MOA
2. Properties
3. Use
4. Toxicity
1. prodrug of acyclovir; same as acyclovir
2. almost 100% conversion to acyclovir
3. VZV, HSV
4. minimal
Famciclovir
1. MOA
2. Properties
3. Use
4. Toxicity
1. guanosine analogue; converted to penciclovir in GI/liver; does NOT cause chain termination
2. penciclovir - poor absorption; fam - 75% bioavailability
3. VZV, HSV
4. minimal
Ganciclovir
1. MOA
2. Properties
3. Use
4. Toxicity
1. guanosine analogue; similar to acyclovir
2. IV, oral, ocular insert; 3hr HL; CSF; oral prodrug
3. life-threatening CMV
4. SIGNIFICANT - hematologic myelosuppression (additive with zidovudine), thrombocytopenia, anemia
Cidofovir
1. MOA
2. Properties
3. Use
4. Toxicity
1. nucleotide analogue; inhibits viral DNA pol
2. 3hr HL; long intracellular HL - long dosing intervals
3. significant CMV disease - IV only
4. renal toxicity - need IV saline/probenecid
Foscarnet
1. MOA
2. Properties
3. Use
4. Toxicity
1. pyrophosphate analogue; against viral DNA/RNA pol, rev txcriptase; blocks pyrophosphate binding site of viral DNA pol - chain terminator
2. IV; renal excretion
3. acyclovir-resistant HSV or VZV; ganciclovir-resistant CMV
4. renal; anemia
Fomivirsen sodium
1. MOA
2. Properties
3. Use
4. Toxicity
1. inhibits viral replication
2. injection into eye
3. CMV in AIDS
4. inflammation; increased intraocular pressure
Antiviral Drugs for Respiratory Viruses
1-3
Ribavirin; Amantadine; Zanamavir
Influenza viruses have two protuberances: ____ (15) and ____ (9)

_____ binds to sialic acid residues on cells to allow virus to bind

_____ cleaves remaining sialic acids after adsorption, to avoid re-penetrating the same cell
H and N

hemagglutinin

neuraminidase
1. 1918 pandemic
2. 1957 pandemic
3. 1968 pandemic
4. current
1. H1N1
2. H2N2 (most likely for next)
3. H3N2
4. H5N1 avian virus - not yet jumped to humans
Ribavirin
1. MOA
2. Properties
3. Use
4. Toxicity
1. guanosine analogue; competitive inhibitor of DNA/RNA synthesis
2. given by aerosol
3. pneumonitis due to RSV
4. minimal if aerosolized
Amantadine
1. MOA
2. Properties
3. Use
4. Toxicity
1. cyclic amine - targets ion channel; prevents uncoating of virus; interferes with release of viral RNA genome
2. oral; good absorption; 12hr HL
3. Influenza A; Parkinson's; resistance develops quickly
4. GI intolerance; CNS effects - insomnia/anxiety/psychosis; potentiated by antihistamines
Zanamavir
1. MOA
2. Properties
3. Use
1. neuraminidase inhibitors (neu. cleaves terminal sialic acid from glycoconjugates)
2. intranasally; orally
3. Influenza A/B
Antiviral Drugs for HIV
1. NRTI's - 3
2. NNRTI's - 3
3. Protease Inhibitors - 6
1. Zidovudine; Lamivudine; Tenofovir
2. Nevirapine; Delavirdine; Efavirenz
3. Saquinavir; Ritonavir; Indinavir; Nelfinavir; Amprenavir; Lopinivir
Zidovudine - NRTI
1. MOA
2. Used
3. Toxicity
1. Competitive inhibition of reverse transcriptase and chain termination
2. combination therapy only
3. hematologic; lactic acidosis; hepatomegaly
Lamivudine - NRTI
1. Toxicity
1. less than many other anti-retrovirals; pancreatitis
Tenofovir - NRTI
1. MOA
2. Used
3. Toxicity
1. less dependent on phosphorylation
2. 1st-line agent
3. GI complaints, rare renal failure; avoid combo with didanosine
NNRTI's
1. MOA
2. Use
3. Toxicity
1. direct binding to rev txcriptase at different site than NRTI
2. combo therapy only
3. rash, hepatoxicity; contraindicated with pregnancy
Protease Inhibitors
1. MOA
2. Properties
3. Use
4. Toxicity
1. inhibit HIV aspartic protease -> production of non-infectious virus
2. oral; poor CNS penetration; cytochrom p450
3. combo therapy only
4. GI; diabetes; inhibitor of cytochrome p450
Highly Aggressive Anti-Retroviral Therapy
1.
2.
3.
1. 1 NNRTI & 2 NRTI
2. 1 PI & 2 NRTI
3. NRTI
NNRTI-Base HAART:

PI-Base HAART:
Efavirenz; 2-5 pills/day

Lopinavir; 8-10 pills/day
Early antiviral therapy is better because:
1. HIV mutations increase with time
2. HIV immunity wanes with progression
3. may prevent spread to other organs
4. immunodeficiency may be only partial
1. Immunomodulators

2. Interferons
1. compounds that alter IR via direct/indirect interaction with T/B cells and APC (IL's, interferons)
2. produced by cells in response to viral infection - antiviral, antiproliferative, immunomodulatory
Interferon Alpha drug
1. MOA
2. Properties
3. Use
4. Toxicity
1. blocks viral transcription/translation
2. inactivated in GI tract
3. hep B/C; papillomavirus; HIV
4. flu-like symptoms; CNS disorders