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13 Cards in this Set
- Front
- Back
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Amphotericin B
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Mech: (an amphipathic molecule) binds to ergosterol, Intercalates into pm, forms pores and disrupts pm
Fungicidal Broadest spectrum of use and often used as initial drug or when you don't know what organism is causing infection SE-Renal Toxity =>Amphoterror |
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Voriconazole
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*shown to be superior to AmB in treatment of invasive aspergillosis.
*excellent activity against candida sp. (including fluconazole- resistant candida) SE: blurred vision, sensitivity to light Low affinity for P450 enzymes |
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imidazoles
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Older class of Azoles
Includes: ketoconazole, miconazole, clotrimazole Mech: inhibit ergosterol synthesis by inhibiting Erg11 (lanosterol demethylase), a cytochrome P450 protein |
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triazoles
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Newer class of Azoles
itraconazole, fluconazole voriconazole Mech: inhibit ergosterol synthesis by inhibiting Erg11 (lanosterol demethylase), a cytochrome P450 protein |
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Fluconazole
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#1 choice for C. neoformans;
no activity against Aspergillus spp. High bioavailability, excellent penetration of the CSF |
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Ketoconazole
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not used much due to its high affinity
for human P450 proteins. |
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Itraconazole
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- prone to drug interactions - reduced bioavailability when taken with rifamycin
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Posaconazole
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New hot drug
prevented invasive fungal infections more effectively than fluconazole or itraconazole More GI side effects |
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Flucytosine
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Fungistatic. NEVER USE ALONE, always use in combination with another drug.
Effective against cryptococcal meningitis Mech: Inhibits thymidylate synthase and substitutes for uracil in RNA. Taken up by cytosine permease (unique to fungi) Note: Obligate renal excretion |
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Echinocandins
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Ex. (caspofungin, micafungin, anidulafungin)
Mech: Inhibition of ß(1,3) glucan synthase disrupts cell wall and leads to cell death (fungicidal) |
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Caspofungin
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*Effective in treatment of oropharyngeal and esophageal
candidiasis and invasive aspergillosis with resistance/intolerance to AmpB -IV administered -Fungicidal No activity against Cryptcoccus neoformans or Histoplasma capsulatum |
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Griseofulvin
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Only used in the systemic
treatment of dermatophytosis Mech: Disrupts mitotic spindle resulting in multinucleated cells (fungistatic) |
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Terbinafine
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Largely replaced Griseofulvin
Used treatment of onychomycosis (fungal infection of the nail) Mech: Inhibits squalene epoxidase (ERG1) activity resulting in ergosterol depletion and accumulation of toxic sterol squalene => Fungicidal |
