10.10 Anti viral – Flashcards
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| What is acyclovir/valacyclovir used for? |
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| HSV, VZV |
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| What is adefovir dipivoxil used for? |
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| HBV |
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| What is cidofovir used for? |
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| CMV, HSV, VZV, EBV, HHV-6 |
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| What is entecavir used for? |
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| HBV |
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| What is famciclovir/penciclovir used for? |
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| HSV, VZV, EBV |
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| What is foscarnet used for? |
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| HSV, VZV, CMV (EBV, HHV-6, HBV, and HIV) |
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| What ganciclovir/valganciclovir used for? |
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| CMV, HSV, VZV, EBV |
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| What is lamivudine used for? |
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| HBV, HIV |
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| What is ribavirin used for? |
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| RSV, HCV, lassa virus |
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| What are NRTIs/NNRTIs used for? |
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| HIV |
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| What is inteferon used for? |
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| HPV, HBV, HCV |
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| What are protease inhibitors used for? |
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| HIV, HCV |
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| What is interferon used for? |
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| RNA tumor viruses |
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| What is oseltamivir/anamivir used for? |
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| Influenza A and B |
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| What is Mab with poison used for? |
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| HIV (in progress) |
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| How do viruses become resistant to DNA/RNA polymerase inhibitors? |
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| change of phosphorylation pathway change of polymerase substrate affinity change in polymerase at NNRTI binding site |
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| What are mechanisms behind the side effects of DNA/RNA polymerase inhibitors? |
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| host DNA/RNA replication inhibition, mitochondrial toxicity, etc. |
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| Name the anti-herpes agents. |
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| acyclovir, valacyclovir, famciclovir, penciclovir, trifluridine, and vidarabine |
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| What durg is an acyclic guanosine derivative? |
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| acyclovir, ganciclovir |
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| In what form is acylcovir given to the pat? |
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| oral, IV, topical |
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| How is acyclovir cleared from the body? |
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| glomerular filtratioln and tubular secretion |
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| What are the side effects of acyclovir (as well as valacyclovir, famciclovir, etc.)? |
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| nausea, diarrhea, headache, tremors, delirum |
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| What is the difference between valacyclovir and acyclovir? |
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| valacyclovir is an L-valyl ester of acyclovir that is converted to acyclovir when ingested |
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| What is famciclovir/how does it work? |
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| prodrug of penciclovir (a guanosine analog); same mechanism as acyclovir except it doesn't cause chain termination |
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| What are the anti-cytomegalovirus agents? |
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| gancylovir, valgancyclovir, cidofovir, foscarnet |
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| How do you get resistence to ganciclovir? |
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| mutation in UL97 phosphotransferase |
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| What are the side effects of ganciclovir/valganciclovir? |
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| myelosuppression |
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| What is the difference between valganciclovir and ganciclovir? |
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| valg is a monovalyl ester prodrug of gancyclovir that is metabolized by intestinal and hepatic esterases when administered orally |
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| What is cidofovir/how does it work? |
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| a cytosine analog whose phosphorylation is NOT dependent on viral enzymes (therefore resistance is due to mutation in DNA polymerase gene) |
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| What are the side effects of cidofovir? |
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| nephrotoxicity (prevented by probenecid |
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| What is Foscarnet/how does it work? |
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| inorganic pyrophosphate that inhibits viral DNA pol, RNA pol, and HIV RT. DOESN"T HAVE TO BE PHOSPHORYLATED |
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| How do you form resistence to foscarnet? |
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| mutations in DNA pol |
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| What are the side effects of foscarnet? |
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| hypo or hypercalcemia and phosphatemia, renal failure, genital ulcers |
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| What are the different types of antiretroviral agents? |
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| NRTIs, NNRTIs, protease inhibitors, fusion inhibitors, CCR5 co-receptor inhibitors, integrase inhibitors |
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| What is zidovudine? |
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| AZT; NRTI nucleoside |
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| What is stavudine? |
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| NRTI nucleoside that can cause peripheral neuropathy |
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| What is lamivudine? |
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| NRTI nucleoside that can be used for HBV. Can rarely cause pancreatitis |
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| What is emtrimcitabine? |
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| NRTI nucleoside with HBV action; rarely causes pancreatitis |
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| What is abacavir? |
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| NRTI nucleoside, hypersensitivity esp in HLA B5701 |
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| What is didanosine? |
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| NRTI nucleoside that can cause pancreatitis |
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| What is entecavir? |
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| NRTI nucleoside with HBV action only |
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| What is telbivudine? |
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| NRTI nucleoside with HBV action only |
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| What is tenofovir? |
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| NRTI nucleotide that can rarely cause renal dysfunction; has HBV action |
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| What is adefovir? |
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| NRTI nucleotide that rarely causes renal dysfunction and has HBV action ONLY |
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| What is nevirapine? |
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| NNRTI that causes hepatic dysfunction |
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| What is efavirenz? |
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| NNRTI that causes CNS dysfunction and rarely hepatic dysfunction. Also is a teratogen |
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| What is the mechanism of action of AZT (zidovudine)? |
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| deoxythymidine analog that enters the cell via passive diffusion and then is converted to triphosphate by mammalian thymidine kinase. Causes chain termination |
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| What is the mechanism of resistance against zidovudine? |
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| mutations in RT gene |
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| What diseases can you usezidovudine against? |
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| HIV1, HIV2 and HTLVs |
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| T/F AZT helps prevent mother to newborn transmission of HIV. |
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| true |
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| What are the side effects of zidovudine? |
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| GI intolerance, headaches and insomnia |
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| NNRTIs are substrates and inhibitors of ___. |
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| CYP3A4 |
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| Which NNRTI do you use to prevent transmission of HIV from mother to newborn? |
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| nevirapine (not efavirenz because its teratogenic) |
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| Which NNRTI do you use to prevent transmission of HIV from mother to newborn? |
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| nevirapine (not efavirenz because its teratogenic) |
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| Which NNRTI do you use to prevent transmission of HIV from mother to newborn? |
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| nevirapine (not efavirenz because its teratogenic) |
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| Indinavir, ritonavir, saquinavir, nelfinavir, fos-amprenavir, lopinavir/ritonavir, tipranavir, darunaivr are all exampels of... |
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| protease inhibitors |
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| How do protease inhibitors work? |
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| inhibits proteases that cleave precursor molecules to produce mature, infectious virions, |
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| What are the side effects of protease inhibitors? |
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| syndrome of altered body fat distribution, insulin resistance and hyperlipidemia |
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| What are contraindications for protease inhibitors? |
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| it is an inhibitor/substrate for CPY3A4; careful with other drugs |
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| What is the name of the drug that is a CCR5 antagonist? |
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| Maraviroc |
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| How does enfuvitide work? How is it given to the patient? |
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| efurvitide (T-20) binds to the gp41 subunit of gp 160 preventing the conformational changes required for fusion of the viral and cellular membranes; given via subq injection |
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| What type of drug is raltegravir? |
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| integrase inhibitor |
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| What are the drugs for hep B? |
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| polymerase inhibition (lamivudine or emtricabine, entecavir, telbuvidine, tenofovir or adefovir) pegylated interferon alpha |
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| What is the treatment for hep C? |
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| pegylated interferon alpha + ribavirin +/- protease inhibitors (boceprevir, telaprevir) |
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| What is the mechanism of interferon alpha to treat viral infection? |
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| induce host cell enyzmes that inhibit viral RNA translation and cause degradation of viral mRNA and tRNA bind to membrane receptors on cell surface May also inhibit viral penetration, uncoating, mRNA synthesis and translation and virion assembly release |
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| Why is interferon alpha pegylated? |
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| a linear or branched polyethylene glycol (PEG) is attached covalently to increase half-life and steady drug concentrations. Allows less frequent dosing |
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| What is ribavirin/how does it work? |
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| a guanosine analog that is phosphorylated intracellularly by host enzymes. Inhibits capping of viral messenger RNA, viral RNA dependent RNA polymerase, and replication of DNA and RNA viruses |
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| What are the oral NS3 protease inhibitors? |
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| boceprevir and telaprevir |
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| How do NS3 protease inhibitors work? |
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| inhibit a nonstructural hep C protein responsible for proteolytic processing of other non-structural proteins |
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| NS3 protease inhibitors are generally used in combination with... |
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| interferon alpha and ribavirin |
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| List the anti-influenza agents. |
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| amantidine, rimantadine, zanamivir, oseltamivir |
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| How do amantadine and rimantidine work? |
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| they are cyclic amines that inhibit the uncoating of viral RNA. |
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| How do viruses get resistant to amantadine/rimantadine? |
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| mutations in the RNA sequence coding for the structural M2 protein |
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| How do zanamivir and oseltamivir work? |
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| inhibit the enzyme neuraminidase by inhibiting the replication of influenza A and B (most avian strains too) |
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