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82 Cards in this Set

  • Front
  • Back
amphotericin B

MOA
Spectrum
ADE
binds ergosterol creating pores in membrane= cell permeability and cell death
Broad spectrum, no antibacterial
Fever and renal toxicity
Capsofungin
Class
MOA
ADE
Interactions
Echinocandin
Inhibits beta-glucan synthase= inhibited cell wall sx= cell death
Preg Cat C
Phlebitis, histamine mediated effects
Micafungin
Class
MOA
ADE
Interactions
Echinocandin
Inhibits beta-glucan synthase= inhibited cell wall sx= cell death
Preg Cat C
Mild CYP3A4 inhibitor
Anidulafungin
Class
MOA
ADE
Interactions
Echinocandin
Inhibits beta-glucan synthase= inhibited cell wall sx= cell death
Preg Cat C
Ketoconazole
MOA
ADE
Interactions
Inhibits 14-a-sterol demethylase= reduced ergosterol sx= less membrane integrity = inhibited growth
GI distress, liver abnormalities
Inhibits CYP3A4
Itraconazole
MOA
ADE
Interactions
Inhibits 14-a-sterol demethylase= reduced ergosterol sx= less membrane integrity = inhibited growth
GI distress, liver abnormalities
Substrate and inhibitor of CYP3A4
Fluconazole
MOA
ADE
Interactions
Inhibits 14-a-sterol demethylase= reduced ergosterol sx= less membrane integrity = inhibited growth
GI distress, liver abnormalities
Inhibits CYP3A4 and CYP2C9
Voriconazole
MOA
ADE
Interactions
Inhibits 14-a-sterol demethylase= reduced ergosterol sx= less membrane integrity = inhibited growth
GI distress, liver abnormalities
Substrate and inhibitor of CYPs 2C9, 2C19, 3A4
Posaconazole
MOA
ADE
Interactions
Inhibits 14-a-sterol demethylase= reduced ergosterol sx= less membrane integrity = inhibited growth
GI distress, liver abnormalities
Inhibits 3A4
Terbinafine
MOA
Spectrum
ADEs
inhibits squalene epoxidase= reduces ergosterol sx and accumulation of squalene= fungicidal
Spectrum: skin and nail
Preg Cat B
Hepatotoxicity
GI side effects
Flucytosine
MOA
ADEs
metabolized by cytosine deaminase and then incorporated in RNA and inhibits protein sx. Also inhibits thymidylase synthase and inhibits DNA sx.
Bone marrow toxicity: leukocytopenia, thrombocytopenia
Amphotericin B
Administration?
IV infusion over 2-4 hours
Pre-treat with fluids, NSAIDS, APAP for side effects
Nystatin
administration?
DOC for?
Topical
3-5x per day
GI and vaginal candidiasis
Itraconazole
administration?
Capsules: need acid-food, cola, OJ, no PPIs
Liquid: need empty stomach, no food or drink for 10 min
Voriconazole
Administration?
Empty stomach, avoid high fat foods
acid neutral- can be on PPIs
also IV
Posaconzole
Administration?
Must take with food, fatty foods have more bioavailability
Suspension only
Crytococcal meningitis
DOC
Fluconazole
Histoplasmosis
DOC
itraconazole
Aspergillus
DOC
voriconazole
Superficial skin infections
DOC
terbinafine
Caspofungin
DOC for
invasive candidiasis and aspergilosis
IV only, histamine rxns
Mycafungin
DOC for
esophageal candidiasis
prophylaxis in stem cell transplants
IV only, histamine rxns
Anidulafungin
DOC for
esophageal candidiasis
intra-abdominal abscess

IV only, histamine rxns (infuse slowly)
Griseofulvin
DOC for
treatment of ringworm in children
tinea versicolor treatment
1. topical slenium sulfide or nizoral cream x 2weeks
2. oral ketaconazole or fluconazole 1 dose
Oral thrush treatment
topical clotrimazole or nystatin 5x/day
oral fluconazole (itracon. or capofungin, ampho for severe)
Esophagitis (fungal) treatment
NO topical
fluconazole 14-21 days past improvement (alt. voriconzole, ampho, caspo)
Candida vaginitis treatment
DO NOT SELF TREAT IF 1st INFECTION
topical (faster sx relief): miconazole, teraconazole, clotrimazole
oral: fluconazole 1 dose (also weekly for 6 months for prophylaxis)
Non-nail ringworm treatment
terbinafine or butenafine at least 7 days or 7-10 days past when rash clears.
alt: clotrimazole, miconazole, longer treatment duration
Nail ringworm treatment
NO TOPICALS
Terbinafine oral 250 mg x 6 weeks (finger) or 12 weeks (toe)
Itraconazole oral 200 mg x 6wk or 12 wks
Fluconazole: 6-12 months
Subcutaneous mycoses
Ex. sporotrichosis
treatment
Itraconazole 200 mg 3-6 months
Blastomycosis treatment
Severe: amphotericin
Switch to
Itraconazole oral at least 6 months
Coccidioidomycosis treatment
fluconazole
Cryptococcosis treatment
ampho + flucytosine
then fluconazole
Acyclovir
Class
MOA
Activating enzyme?
Base analog inhibitor of viral DNA polymerase. TriPO4 competes w/dGTP, lacks 3'OH, causing DNA chain termination. Irreversibly inactivates viral DNA poly.
Activated by viral thymidine kinase
DOC for herpes. also prophylaxis for CMV
Valacyclovir
Class
MOA
Activating enzyme
L-valine ester prodrug converted to acyclovir- better absorption. Base analog inhibitor of viral DNA polymerase; TriPO4 incorporated into DNA, lack of 3'OH causes chain termination. Activated by viral thymidine kinase.
herpes treatment or CMV prophylaxis
Penciclovir
Class
MOA
Activating enzyme
base analog inhibitor of viral DNA poly. doesn't cause chain termination, 100x less potent DNA pol inhibitor. high conc accumulates, longer half-life. fewer daily doses, shorter neuralgia
activated by viral thymidine kinase
Famciclovir
Class
MOA
Activating enzyme
base analog viral DNA polymerase inhibitor. inactive prodrug gets converted to penciclovir
Ganciclovir
Class
MOA
activating enzyme
base analog viral DNA polymerase inhibitor. competitively inhibits dGTP on DNA poly, inhibits elongation. UL97 kinase phosphorylates drug. more conc. activated drug in CMV infected cells.
Valganciclovir
Class
MOA
Activating enzyme
L-val ester prodrug of ganciclovir. oral produces concs similar to ganciclovir.
Base analog viral DNA polymerase inhibitor, competitively inhibits dGTP and elongation. UL97 kinase phosphorylates it
Vidarabine
Class
MOA
Activating enzyme
purine analog of adenosine, competes for dATP. incorporates into human and viral DNA, but more selective for viral. wide spectrum
Idoxuridine
Class
MOA
Activating enzyme
pyrimidine analog of thymidine. TriPO4 incorporated into viral and human DNA= mutation= chromosome breaks.
Opthalmic only, used for herpes and pox
Trifluridine
Class
MOA
Activating enzyme
pyrimidine analog of thymidine, monoPO4 irreversibly inhibits thymidylate synthase, TriPO4 incorporates into viral and cellular DNA= chromosome break
Too toxic for systemic use
Cidofovir
Class
MOA
Activating enzyme
Pyrimidine analog of cytosine, cellular enzymes activate into diPO4 which competitively inhibits dCTP use by viral DNA pol.
**Can be used in zcyclovir resistant virus w/ mutant viral thymidine kinase b/c activated by cellular enzymes.
CMV> HSV, adenovirus
Adefovir
Class
MOA
Activating enzyme
analog of adenosine, activated to diPO4. inhibits viral DNA poly and reverse transcriptase. Terminates chain if incorporated into DNA.
Hep B, herpes, HIV. can develop HIV resistance if co-infected w/ hep B and HIV
Entecavir
Class
MOA
activating enzyme
analog of guanosine, cellular kinases phosphorylate to make triPO4,, competes w/ dGTP to inhibit DNA pol and reverse transcriptase.
Hep B
Foscarnet
Class
MOA
Does not req activation. inhibits DNA polymerase and HIV reverse transcriptase.
Herpes viruses, HIV, CMV
Toxicity: nephrotoxic, hypocalcemia, mutagenic
Ribavirin
Class
MOA
Activating Enzyme
Affects RNA- phophorylated by cellular enzymer. RMP- inhibits GTP synthesis. RTP- inhibits usage of mRNA by interfering w/ GTP capping of 5' end of mRNA. Inhibits RNA polymerase, decreasing mRNA and protein synthesis
Broad spectrum- DNA and RNA viruses
Docosanol
Class
MOA
Inhibits HSV attachment. inhibits attachment of enveloped viruses to cells.
Topical against oral herpes. Spectrum- DNA and RNA viruses
Imiquimod
Class
MOA
Immune enhancer- induces interferon. Spectrum: wart treatment HPV, genital HSV 1 &2
Podofilox
Class
MOA
Spindle poison for infected cells, blocks replication, may kill them
Wart treatment
Amantadine
Class
MOA
Prevents uncoating of influenza A virus after viral entry into host cell and release
Binds and inhibits action of viral M2 protein ion channel which inhibits acidification of internal vesicle
Inhibits dissociation of ribonucleoprotein complex
Inhibits acid-induced hemagglutinin conformation changes that would allow binding of virus to cellular receptors
Treats Influenza A
Rimantadine
Class
MOA
Prevents uncoating of influenza A virus after viral entry into host cell and release
Binds and inhibits action of viral M2 protein ion channel which inhibits acidification of internal vesicle
Inhibits dissociation of ribonucleoprotein complex
Inhibits acid-induced hemagglutinin conformation changes that would allow binding of virus to cellular receptors
Treats Influenza A
Zanamivir
Class
MOA
Blocks release of virus by blocking neuraminidase
neuraminidase inhibitor
Spectrum: influenza A & B
Oseltamivir
Class
MOA
Blocks release of virus by blocking neuraminidase
neuraminidase inhibitor
Spectrum: influenza A & B
Telaprevir
Class
MOA
NS3-4A protease inhibitor used in combo with INF-α and ribavirin. NS3-4A (a serine protease) cleaves HCV polyprotein precursor at 4 sites producing several enzymes and structural proteins for the virus. Inhibiting it prevents assembly of hep C virus
Hep C serine protease inhibitor
Boceprevir
Class
MOA
NS3-4A protease inhibitor used in combo with INF-α and ribavirin. NS3-4A (a serine protease) cleaves HCV polyprotein precursor at 4 sites producing several enzymes and structural proteins for the virus. Inhibiting it prevents assembly of hep C virus
Hep C serine protease inhibitor
Zidovudine
Nucleos(t)ide reverse transcriptase inhibitor. HIV
phosphorylated by cellular enzymes, do not combine with stavudine
Stavudine
Nucleos(t)ide reverse transcriptase inhibitor. HIV
Do not combine with didanosine, zalcitabine or zidovudine.
Toxicities: periph sensory neuropathy, pancreatitis
Lamivudine
Nucleos(t)ide reverse transcriptase inhibitor. HIV
Effective in Hep B pts- inhibits HBV DNA polymerase
Emtricitabine
Nucleos(t)ide reverse transcriptase inhibitor. HIV
effective in Hep B
Zalcitabine
Nucleos(t)ide reverse transcriptase inhibitor. HIV
Do not combine with didanosine, or stavudine
Toxicities: periph sensory neuropathy, pancreatitis
Didanosine
Nucleos(t)ide reverse transcriptase inhibitor. HIV
Do not combine with stavudine, or zalcitabine
Toxicities: periph sensory neuropathy, pancreatitis
Abacavir
Nucleos(t)ide reverse transcriptase inhibitor. HIV
Effective in children. hypersensitivity req DC of drug
Tenofovir
Nucleos(t)ide reverse transcriptase inhibitor. HIV
Nucleotide, does not req phosphorylation for activity. Active against HIV, Hep B and herpes virus
Nevirapine
non-nucleoside reverse transcriptase inhibitor. 1st generation, lacks teratogenic effects - prevention of transmission from mother to newborn
Delaviridine
non-nucleoside reverse transcriptase inhibitor. 1st generation, lacks teratogenic effects - prevention of transmission from mother to newborn
Efavirenz
non-nucleoside reverse transcriptase inhibitor. 1st generation, lipid soluble, crosses BBB (CNS effects)
Etravirine
non-nucleoside reverse transcriptase inhibitor. 2nd generation.
RASH- steven johnson
Rilpivirine
non-nucleoside reverse transcriptase inhibitor. 2nd generation.
Toxicity: depression
Ritonavir
Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
used at low doses to inhibit metabolism of other protease inhibitors. High GI side effects
Saquinavir
Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
Indinavir
Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
10x more inhibition of HIV-1 protease over HIV-2
Fosamprenavir
Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
Lopinavir
Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
Atazanavir
Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
If resistant to other protease inhibitors, usually cross resistance to atazanavir. if used 1st, no cross resistance to other protease inhibitors
Darunavir
Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
Nelfinavir
Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
Tipranavir
Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
Enfuvirtide
fusion/adhesion inhibitor
synthetic peptide corresponding to a repeat seq in HIV gp41. Competes w/ endogenous HR2 for binding to HR1, antagonizing folding of gp41
Maraviroc
CCR5 antagonist
selective, reversible CCR5 coreceptor antagonist. Prevents gp120 conformation change, inhibiting HIV entry
Raltegravir
integrase inhibitor
inhibits integrase reaction