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15 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Acyclovir (MOA):
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Inhibits viral DNA synthesis by competing with dGTP for the viral DNA polymerase AND by chain termination following incorporation into the viral DNA
Activation requires a 3-step phosphorylation Requires HSV-specific thymidine kinase (initial phosphorylation) and host cell enzymes |
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Acyclovir (Kinetics):
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Oral bioavailability is unaffected by food
IV and topical formulations available Diffuse rapidly into most tissues & body fluids Cleared mainly via kidney |
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Acyclovir (Indications):
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Oral
First episode genital herpes Recurrent genital herpes Genital herpes suppression Varicella (chicken pox) Zoster (shingles) |
IV
Severe HSV infection Herpes encephalitis Neonatal HSV infection Topical Herpes labialis |
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Acyclovir (Resistance):
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Alteration of viral thymidine kinase
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Acyclovir (Adverse Reactions):
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Nausea
Diarrhea Headache Renal dysfunction or neurologic toxicity (IV) |
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Valacyclovir:
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L-valyl ester prodrug of acyclovir
Rapidly converted to acyclovir after oral administration Kinetics: Oral Indications: Treatment of first or recurrent genital herpes; More effective in treating VZV than acyclovir |
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Famciclovir:
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Converted to penciclovir after oral administration
MOA: Competitive inhibition of viral DNA polymerase |
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Docosanol:
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MOA: Inhibits fusion between plasma membrane and the HSV envelope
Kinetics: topical A saturated 22-carbon aliphatic alcohol |
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Trifluridine:
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MOA: competes with TTP for incorporation by viral DNA polymerase
Activation requires phosphorylations by host cell enzymes Indications: Treatment of herpes keratitis and acyclovir-resistant HSV infections Not for systemic use |
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Ganciclovir (MOA):
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Competitively inhibits viral DNA polymerase and cause termination of DNA elongation
Phosphorylation-dependent drug activation Initial phosphorylation is mediated by the CMV-specific protein kinase phosphotransferase UL9 |
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Ganciclovir (Resistance):
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ovir (Resistance):
Mutation in UL97 |
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Ganciclovir (Indication):
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CMV (Cytomegaloviruses) prophylaxis or CMV retinitis treatment
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Ganciclovir (Adverse Reactions):
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Myelosuppression (esp. IV)
Nausea, diarrhea, fever, rash, headache, insomnia, peripheral neuropathy, and retinal detachment CNS toxicity, hepatotoxicity Carcinogenic and embryotoxic at high doses in animals |
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Foscarnet:
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MOA: Inhibits viral DNA/RNA polymerase & HIV reverse transcriptase
Kinetics: IV only; Renal clearance Indications: Effective for CMV(Cytomegaloviruses) retinitis treatment Adverse reactions: Renal impairment; Electrolyte disturbance; CNS toxicity (seizure) |
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Cidofovir:
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MOA: Inhibits viral DNA polymerase; Phosphorylation-dependent activation
Kinetics: IV must be administered with probenecid to reduce nephrotoxicity; hydration! Indications: Treatment of CMV retinitis Adverse reactions: Dose-dependent nephrotoxicity (reduced by saline prehydration) |
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