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35 Cards in this Set
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What is the MOA of azoles?
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Inhibits CYP 450 leading to impaired synthesis of ergosterol- impaired fungal cell formation
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What is MOA of polyenes?
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Binds to ergosterol in fungal cell
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What is MOA of Flucytosine?
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anti-metabolite works by inhibiting RNA and DNA synthesis
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What is MOA of Echinocandins?
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Inhibits synthesis of B (1,3)-D-glucan (cell wall component
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What is MOA of Griseofulvin?
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Antimitotic
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What is MOA of Terbinafine
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Inhibits squaline epoxidase which blocks ergosterol synthesis
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Name the Triazoles
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Fluconazole
Itraconazole Voriconazole Posaconazole Acronym "Fluconazole IV Push" |
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Name the Imidazoles
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Ketoconazole
Miconazole Clotrimazole "Kathy Makes Candy" |
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What CYP do all azoles inhibit?
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CYP3A4
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What is fluconazole active against?
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Most Candida species, coccidioides and cryptococcus spp. Also histoplasma Capsulatum at higher doses
Acronym- Captain Crunch's Hairy Cocc (idiodes) |
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What is Fluconazole not active against?
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Molds
Krusei Glabrata "Moldy Krusty Glabellas" |
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What is the problem with Ketoconazole?
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LOTs of side effects, anorexia, N/V, rash, teratogenic, hepatic toxicity and basically fucks with all your hormones, makes girls bleed, guys limp and gives them boobs.
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Name drug interactions, concerns with Ketoconazole- What does it inhibit CYP wise?
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CYP3A4. With this there is increased serum concentrations of many other drugs. Absorption is also reduced by drugs that decrease gastric acidity.
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What are adverse effects of Fluconazole?
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Teratogenic, HA, GI distress, facial edema, rash, pruritus, Steven-Johnson sx, qt prolongation
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What CYPs do Fluconazole inhibit?
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Strong- CYP2C9, and 2C19
Moderate CYP3A4 |
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What is Itraconazole active against?
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Know it has broader activity than fluconazole.
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What isn't Itraconazole active against?
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Scedosporium, Scopulariopsis, Fusarium, Zygomycetes
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What do ALL azoles inhibit?
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All inhibit CYP3A4- all cause same side effects
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When is Itraconazole contraindicated?
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Patients with CHF/Ventricular dysfunction.
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Which drug is superior to Amphotericin for invasive aspergillosis?
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Voriconazole
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Which azole has activity twice that as itraconazole?
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Posaconazole- increased activity against Absidia spp.
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What is MOA of Ampho B?
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Binds to ergosterol in fungal cell membrane, disrupting its activity.
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What is the drug of choice for most life-threatening infections?
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Ampho B- Initial therapeutic agent, treatment is continued then with less toxic antifungal
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Describe pharmacokinetics of Ampho B
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Half life of 15 days, concentrates in liver and spleen, metabolism not understood.
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What is MOA of Flucytosine?
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Converted in fungal cytosol to 5-fluorouracil- inhibiting DNA and RNA synthesis- uptook by cytosine permease
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When is Flucytosine used?
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In como with ampho B for cryptococcal meningitis or systemic candidiasis
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What are adverse effects of Flucytosine?
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Dose related bone marrow toxicity
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Name the echinocandins
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Caspofungin
Anidulafungin Micafungin |
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Name pharacokinetics of echinocandins
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Half life 10 hours, hepatic metabolism not by CYP, no significant drug interactions, no dosage adjustment needed for renal issues.
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What are the adverse effects of echinocandins
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rash, fever nausea vomiting HA, hypokalemia mild hepatic toxicity, SJ syndrome, exfoliative dermatitis and teratogenic.
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What is MOA of griseofulvin?
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Antimitotic- interacts with polymerized microtubules lieading to disruption of the mitotic spindle
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What is Griseofulvin for?
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Fungal skin, nail and hair infections.
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What is Terbinafine for, MOA?
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For mucocutaneous fungal infections, inhibits squaline epoxidasee which blocks ergosterol synthesis
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What is pharmacokinetics of Terbinafine?
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Significant first pass metab., highly lipophilic, keratophilic,
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What are adverse effects of Terbinafine?
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No significant drug inte. as does not affect CYP450s, is teratogenic, hepatotoxicity NV, HA rash, diarrhea.
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