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82 Cards in this Set
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amphotericin B
MOA Spectrum ADE |
binds ergosterol creating pores in membrane= cell permeability and cell death
Broad spectrum, no antibacterial Fever and renal toxicity |
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Capsofungin
Class MOA ADE Interactions |
Echinocandin
Inhibits beta-glucan synthase= inhibited cell wall sx= cell death Preg Cat C Phlebitis, histamine mediated effects |
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Micafungin
Class MOA ADE Interactions |
Echinocandin
Inhibits beta-glucan synthase= inhibited cell wall sx= cell death Preg Cat C Mild CYP3A4 inhibitor |
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Anidulafungin
Class MOA ADE Interactions |
Echinocandin
Inhibits beta-glucan synthase= inhibited cell wall sx= cell death Preg Cat C |
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Ketoconazole
MOA ADE Interactions |
Inhibits 14-a-sterol demethylase= reduced ergosterol sx= less membrane integrity = inhibited growth
GI distress, liver abnormalities Inhibits CYP3A4 |
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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 |
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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 |
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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 |
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Posaconazole
MOA ADE Interactions |
Inhibits 14-a-sterol demethylase= reduced ergosterol sx= less membrane integrity = inhibited growth
GI distress, liver abnormalities Inhibits 3A4 |
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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 |
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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 |
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Amphotericin B
Administration? |
IV infusion over 2-4 hours
Pre-treat with fluids, NSAIDS, APAP for side effects |
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Nystatin
administration? DOC for? |
Topical
3-5x per day GI and vaginal candidiasis |
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Itraconazole
administration? |
Capsules: need acid-food, cola, OJ, no PPIs
Liquid: need empty stomach, no food or drink for 10 min |
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Voriconazole
Administration? |
Empty stomach, avoid high fat foods
acid neutral- can be on PPIs also IV |
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Posaconzole
Administration? |
Must take with food, fatty foods have more bioavailability
Suspension only |
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Crytococcal meningitis
DOC |
Fluconazole
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Histoplasmosis
DOC |
itraconazole
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Aspergillus
DOC |
voriconazole
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Superficial skin infections
DOC |
terbinafine
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Caspofungin
DOC for |
invasive candidiasis and aspergilosis
IV only, histamine rxns |
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Mycafungin
DOC for |
esophageal candidiasis
prophylaxis in stem cell transplants IV only, histamine rxns |
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Anidulafungin
DOC for |
esophageal candidiasis
intra-abdominal abscess IV only, histamine rxns (infuse slowly) |
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Griseofulvin
DOC for |
treatment of ringworm in children
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tinea versicolor treatment
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1. topical slenium sulfide or nizoral cream x 2weeks
2. oral ketaconazole or fluconazole 1 dose |
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Oral thrush treatment
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topical clotrimazole or nystatin 5x/day
oral fluconazole (itracon. or capofungin, ampho for severe) |
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Esophagitis (fungal) treatment
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NO topical
fluconazole 14-21 days past improvement (alt. voriconzole, ampho, caspo) |
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Candida vaginitis treatment
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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) |
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Non-nail ringworm treatment
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terbinafine or butenafine at least 7 days or 7-10 days past when rash clears.
alt: clotrimazole, miconazole, longer treatment duration |
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Nail ringworm treatment
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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 |
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Subcutaneous mycoses
Ex. sporotrichosis treatment |
Itraconazole 200 mg 3-6 months
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Blastomycosis treatment
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Severe: amphotericin
Switch to Itraconazole oral at least 6 months |
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Coccidioidomycosis treatment
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fluconazole
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Cryptococcosis treatment
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ampho + flucytosine
then fluconazole |
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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 |
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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 |
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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 |
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Famciclovir
Class MOA Activating enzyme |
base analog viral DNA polymerase inhibitor. inactive prodrug gets converted to penciclovir
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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.
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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 |
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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
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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 |
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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 |
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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 |
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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 |
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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 |
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Foscarnet
Class MOA |
Does not req activation. inhibits DNA polymerase and HIV reverse transcriptase.
Herpes viruses, HIV, CMV Toxicity: nephrotoxic, hypocalcemia, mutagenic |
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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 |
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Docosanol
Class MOA |
Inhibits HSV attachment. inhibits attachment of enveloped viruses to cells.
Topical against oral herpes. Spectrum- DNA and RNA viruses |
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Imiquimod
Class MOA |
Immune enhancer- induces interferon. Spectrum: wart treatment HPV, genital HSV 1 &2
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Podofilox
Class MOA |
Spindle poison for infected cells, blocks replication, may kill them
Wart treatment |
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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 |
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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 |
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Zanamivir
Class MOA |
Blocks release of virus by blocking neuraminidase
neuraminidase inhibitor Spectrum: influenza A & B |
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Oseltamivir
Class MOA |
Blocks release of virus by blocking neuraminidase
neuraminidase inhibitor Spectrum: influenza A & B |
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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 |
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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 |
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Zidovudine
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Nucleos(t)ide reverse transcriptase inhibitor. HIV
phosphorylated by cellular enzymes, do not combine with stavudine |
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Stavudine
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Nucleos(t)ide reverse transcriptase inhibitor. HIV
Do not combine with didanosine, zalcitabine or zidovudine. Toxicities: periph sensory neuropathy, pancreatitis |
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Lamivudine
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Nucleos(t)ide reverse transcriptase inhibitor. HIV
Effective in Hep B pts- inhibits HBV DNA polymerase |
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Emtricitabine
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Nucleos(t)ide reverse transcriptase inhibitor. HIV
effective in Hep B |
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Zalcitabine
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Nucleos(t)ide reverse transcriptase inhibitor. HIV
Do not combine with didanosine, or stavudine Toxicities: periph sensory neuropathy, pancreatitis |
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Didanosine
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Nucleos(t)ide reverse transcriptase inhibitor. HIV
Do not combine with stavudine, or zalcitabine Toxicities: periph sensory neuropathy, pancreatitis |
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Abacavir
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Nucleos(t)ide reverse transcriptase inhibitor. HIV
Effective in children. hypersensitivity req DC of drug |
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Tenofovir
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Nucleos(t)ide reverse transcriptase inhibitor. HIV
Nucleotide, does not req phosphorylation for activity. Active against HIV, Hep B and herpes virus |
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Nevirapine
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non-nucleoside reverse transcriptase inhibitor. 1st generation, lacks teratogenic effects - prevention of transmission from mother to newborn
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Delaviridine
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non-nucleoside reverse transcriptase inhibitor. 1st generation, lacks teratogenic effects - prevention of transmission from mother to newborn
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Efavirenz
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non-nucleoside reverse transcriptase inhibitor. 1st generation, lipid soluble, crosses BBB (CNS effects)
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Etravirine
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non-nucleoside reverse transcriptase inhibitor. 2nd generation.
RASH- steven johnson |
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Rilpivirine
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non-nucleoside reverse transcriptase inhibitor. 2nd generation.
Toxicity: depression |
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Ritonavir
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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 |
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Saquinavir
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Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
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Indinavir
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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 |
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Fosamprenavir
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Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
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Lopinavir
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Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
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Atazanavir
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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 |
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Darunavir
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Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
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Nelfinavir
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Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
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Tipranavir
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Protease inhibitor. HIV protease cleaves gag-pol polyprotein producing active enzymes. Inhibition prevents viral maturation.
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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 |
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Maraviroc
|
CCR5 antagonist
selective, reversible CCR5 coreceptor antagonist. Prevents gp120 conformation change, inhibiting HIV entry |
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Raltegravir
|
integrase inhibitor
inhibits integrase reaction |