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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 |
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Antivirals for Herpesviruses:
1-7 |
Acyclovir; Valacyclovir; Famciclovir; Ganciclovir; Cidofovir; Foscarnet; Fomivirsen sodium
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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 |
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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 |
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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 |
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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 |
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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 |
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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 |
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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 |
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Antiviral Drugs for Respiratory Viruses
1-3 |
Ribavirin; Amantadine; Zanamavir
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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 |
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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 |
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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 |
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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 |
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Zanamavir
1. MOA 2. Properties 3. Use |
1. neuraminidase inhibitors (neu. cleaves terminal sialic acid from glycoconjugates)
2. intranasally; orally 3. Influenza A/B |
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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 |
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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 |
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Lamivudine - NRTI
1. Toxicity |
1. less than many other anti-retrovirals; pancreatitis
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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 |
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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 |
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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 |
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Highly Aggressive Anti-Retroviral Therapy
1. 2. 3. |
1. 1 NNRTI & 2 NRTI
2. 1 PI & 2 NRTI 3. NRTI |
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NNRTI-Base HAART:
PI-Base HAART: |
Efavirenz; 2-5 pills/day
Lopinavir; 8-10 pills/day |
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Early antiviral therapy is better because:
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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 |
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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 |
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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 |