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Anti-viral Drugs
anti-virals
20
Pharmacology
Graduate
09/16/2009

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Cards

Term
Antivirals
Definition
  • Class-Antivirals
  • Mechanism-several mechanisms including penetration, uncoating, genome replication, assembly, release 
  • Include: (Enfuvirtide); (Amantadine); (AZT; Lamivudine; Nevirapine; Foscarnet; Acyclovir; Ribavirin); (Ataznavir; Saquinavir; Lopinavir; HAART); (Relenza; Tamiflu)
  • Special-viruses use host cell organelles for replication so very difficult to target and avoid damage to human cells
  • Term
    Enfuvirtide (Fuzeon)
    Definition
  • Class-Anti-attachment drugs
  • Mechanism- blocks HIV entry by blocking the entry of virus into Th (helper T) cells (KNOW)
  • Target-HIV
  • Special-none
  • Term
    Amantadine
    Definition
  • Class-Anti-uncoating/anti-penetration drug
  • Mechanism-inhibits uncoating by targeting viral protein M2 required for uncoating; therefore virus cannot penetrate
  • Target-Influenza A
  • Special-mild CNS toxicity (dizziness, malaise)*; must take AT the time of infection; concern with resistance via alteration of M2
  • Term
    AZT (zidovudine, ZDV)
    Definition
  • Class-NRTI (nucleoside reverse transcriptase inhibitor) aka anti-retrovirals
  • Mechanism-inhibits reverse transcriptase at the ACTIVE site, leading to cDNA chain termination
  • Target-HIV
  • Special-bone marrow toxicity*, headache*, nausea*; drug is not highly selective so dose limited on how much you can give a person w/AIDS before it's toxic; high affinity by HIV reverse transcriptase so difficulty keeping high concentrations of AZT for long-term
  • Term
    Lamivudine
    Definition
  • Class-NRTI (nucleoside reverse transcriptase inhibitor) aka anti-retrovirals
  • Mechanism-inhibits reverse transcriptase, leading to cDNA chain termination at active site
  • Target-HIV
  • Special-newer form NRTI with fewer side effects
  • Term
    Nevirapine
    Definition
  • Class-NNRTI (non-nucleoside reverse transcriptase inhibitor)
  • Mechanism-binds to reverse transcriptase near active site inhibiting proper production of cDNA
  • Target-HIV
  • Special-severe risk of hepatic toxicity
  • Term
    Efavirenz
    Definition
  • Class-NNRTI (non-nucleoside reverse transcriptase inhibitor)
  • Mechanism-binds to reverse transcriptase near active site inhibiting proper production of cDNA
  • Target-HIV
  • Special-has a longer half-life than its counterpart Nevirapine (once a day dosing), BUT CNS side effects (peripheral neuropathy*, pancreatitis*, lactic acidosis*)
  • Term
    Foscarnet
    Definition
  • Class-targets genome replication
  • Mechanism-binds to viral DNA polymerase, inhibiting further activity
  • Target-resistant Herpes simplex virus =HSV (only used for serious viral illnesses)
  • Special-toxic with many s/e (electrolyte d/o) since viruses and humans both have DNA polymerase (although drug has higher affinity for viral polymerase)
  • Term
    Norvir/Rayataz
    Definition
  • Class-protease inhibitor
  • Mechanism-inhibits HIV-1 protease (an enzyme used to cleave proteins needed for final virion assembly)
  • Target-HIV, Hep C
  • Special-multiple drug interactions; GI intolerance
  • Term
    Acyclovir
    Definition
  • Class-nucleoside analog/DNA chain terminator (NRTI?)
  • Mechanism-activated by viral TK to AcyGTP, inhibits viral thymidine kinase (anti-Herpes)*** which then inhibits DNA polymerase
  • Target-Herpes simplex (HSV)**, VZV (varicella-zoster)
  • Special-decreases shedding and recurrence compared to placebo; excellent selectivity because drug has high affinity for viral enzyme and low affinity for human enzyme since we target the step before DNA polymerase; *toxicity includes anorexia, nausea, headache, rash*
  • Dosage*-recurrent infection po 3xday for 1 year; intermittent infection po 5xday for 5 days
  • Term
    Ganciclovir
    Definition
  • Class-nucleoside analog/DNA chain terminator
  • Mechanism-inhibits viral DNA polymerase, resulting in termination of elongation of viral DNA
  • Target-CMV (cytomegalovirus)
  • Special-may cause retinitis; give parenteral
  • Term
    Ribavirin
    Definition
  • Class-nucleoside analog (look like nucleotides and when plugged in they damage or terminate DNA)
  • Mechanism-leads to error-prone formation of DNA
  • Target-viral infections like HCV (HepC virus); also for respiratory syncytial virus in children*
  • Special-due to amt of side effects, given with INF(alpha) that has been pegylated (bound up) with polyethylene glycol which interfers with viral synthesis
  • Term
    Ataznavir
    Definition
  • Class-protease inhibitor
  • Mechanism-interfers with HIV-1 protease that cleaves between Gag and Pol
  • Target-HIV
  • Special-none.
  • Term
    Saquinavir
    Definition
  • Class-protease inhibitor
  • Mechanism-inhibits HIV-1 protease (an enzyme used to cleave proteins needed for final virion assembly)
  • Target-HIV
  • Special-soft-gel capsule to improve low bioavailability; taken with P450 (CYP3A) inhibitor ritonavir to boost their effective levels (Also true for Lopinavir and Ataznavir); drug interactions with anesthetics and anticoagulants*
  • Term
    HAART
    Definition
    • Highly affective antiretroviral therapy
    • A combination of drugs including DNA chain termination and protease inhibitors drugs. This helps to stop virus from replicating and decreases chance of mutation
    Term
    Oseltamivir (Tamiflu)
    Definition
  • Class-neuraminidase inhibitors
  • Mechanism-inhibits viral neuraminidase which prevents release and uptake of new virions
  • Target-Influenza A & B
  • Special-treat early if possible; taken orally; can shorten flu infection
  • Term
    Zanamivir (Relenza)
    Definition
  • Class-neuraminidase inhibitors
  • Mechanism-inhibits viral neuraminidase which prevents release and uptake of new virions
  • Target-Influenza A & B
  • Special-treat early if possible; inhalable; can shorten flu infection (equivalent to oral Tamiflu agent)
  • Term
    Interferon
    Definition
  • Class-endogenous glycoprotein
  • Mechanism-the process of putting recombinant DNA from the virus into a bacterium to make endless supplies of viral proteins which can then be given to a patient to interfer with viral synthesis activities (INF-alpha)
  • Target-chronic viral hepatitis
  • Special-parenteral; very toxic
  • Term
    Iododeoxyuridine
    Definition
    • Class-Antiviral
    • Mechanism-pyrimidine analog
    • Target-Herpes keratitis (antiherpetic activity)
    • Cidal/Static-
    • Special-Competitive antagonist of thymidine; topical medication; also Trifluridine
    Term
    Anti-retrovirals
    Definition

     

  • Class-Anti-retrovirals
  • Mechanism-nucleoside reverse transcriptase inhibitors (NRTI) or non-nucleoside reverse transcriptase inhibitors (NNRTI) or protease inhibitors (PI)
  • Target-HIV
  • Includes: AZT (NRTI); Norvir/Rayatax (PI); Efavirenz (NNRTI)
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