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52 Cards in this Set
- Front
- Back
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What drug is amphociterin related to?
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nystatin
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What are the chemical properties of amphociterin?
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it is a polyene that is amphipathic meaning that it has both hydrophillic and lipophilic properties
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What is the MOA of amphociterin?
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it binds to ergosterol and forms pores
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What is the most important drug for systemic mycoses?
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amphoterecin B
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What is the drug of choice to treat systemic aspergillus? What other organisms is this drug first line for?
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1) amphoterecin
2) balstomyces (itraconazole), C albicans, Cryptococcus, Histoplasma, and Mucor |
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What antifungal has the widest spectrum of action?
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amphoticerin
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What adverse effects can result from infusing amphotecerin B? What can be given to ameliorate these effects?
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1) shocklike fall in BP, fever, chills, spasms
2) Give antihistamines, antipyretics, meperidine, glucocorticoids |
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What is the effect of amphotercin on the kidneys?
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decreases filtration, tubular acidosis, Mg and K wasting, decreased EPO leading to anemia,
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What is another name for 5-FC
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flucytosine
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What does 5-FC resemble structurally?
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a pyrimidine and the anticancer drug 5-fluorouracil
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What is the MOA of flucytosine?
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it is accumulated in fungal cells via a permease and converted by cytosine deaminase to 5-FU which is an inhibitor of thymidylate synthase
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Is the spectrum of action large or narrow with flucytosine? What all is it actively used against?
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narrow, used primarily against cyrptococcus neoformans and only in conjunction with amphoticerin or triazole
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A person taking an antifungal has bone marrow depression, alopecia and liver dysfunction. Which drug are they taking?
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5-FC, bone marrow depression is reversible
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What are the azoles that are used in systemic mycoses?
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ketoazole, fluconazole, itraconazole, and voriconazole
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What is the main imidazole?
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ketoconazole
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What are the triazoles?
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fluconazole, itraconazole, voriconazole
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What is the MOA of azoles?
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inhibit ergosterol synthesis by acting at the step of 14alpha-demethylation of lanosterol catalyzed by a fungal P450 enzyme
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Which azole has a narrow spectrum and the most side effects?
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ketoconazole
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What does ketoconazole continue to be used for?
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chronic mucocutaneous candidiasis and dermatophytes
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What is the drug of choice for esophageal and oropharyngeal candidiasis and infections with coccidiodes?
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fluconazole
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What is the choice treatment of cryptococcal meningitis?
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fluconazole
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What is the drug of choice to treat blastomyces and sporothrix and subcutaneous chromobalsatomycosis?
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itraconazole
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Which triazole has the widest spectrum of action?
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voriconazole
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What is voriconazole the treatment of choice for?
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invasive aspergillosis
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What is ketoconazole notorious for?
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inhibiting hepatic P450 enzymes which increases plasma levels of oral hypoglycemics, phenytoin, warfarin
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What are the sexual side effects of ketoconazole?
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interferes with P450 enzymes in adrenal and gonadal cells leading to gynecomastia, menstrual irregularities and infertility
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What should be done in someone taking voriconazole that experiences visual disturbances?
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tell them these are immediate adverse effects that will go away with time
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What are examples of echinocandins?
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caspofungin, anidulafungin and micafungin
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What is the MOA of echinocandins?
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inhibit beta(1-2)glycan a component of cell walls
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When is caspofungin used?
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disseminated and mucocutaneous Candida and in aspergillosis that doesn't respond to amphotecerin B
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When is anidulafungin used?
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Esophageal and invasive candiasis
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Someone is infused with caspofungin and immediately turns red. What should be done?
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tell them this a common reaction because caspofungin causes histamine release. Note micofungin also causes histamine release
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What is the MOA of griseofulvin?
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interferes with microtubule function in dermatophytes and polymerization of nucleic acids
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Is Griseofulvin fungocidal or static?
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static
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When is griseofulvin prescribed?
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it is only an oral formulation given for dermatophytes of skin and hair
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Why can't people drink while taking griseofulvin?
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it has disulfuram effects
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What is the MOA of terbinafine?
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inhibits squalene epoxidase causing elevated toxic levels of squalene which interferes with ergosterol synthesis
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Is terbinafine fungicidal or static?
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cidal
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Where do griseofulvin and terbinafine accumulate?
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in keratin
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All of the azoles can be used to treat dermatophytoses except?
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voriconazole
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When is nystatin used?
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topically for C albicans and dermatophytes
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What is the MOA of nystatin?
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binds ergosterol
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What agent is used for oral candidal infections?
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nystatin
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mycotic corneal ulcers and keratitis and be treated locally with what antifungal?
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amphotericin B
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What does intrathecal administration of amphotercin B cause?
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seizures and neurlogic damage
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What other drug is equivalent to amphotercin B in treating candidemia?
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fluconazole
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What drug is especially useful in treating onychomycosis?
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itraconazole
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What antifungal is given systemically but goes to stratum corneum where it binds keratin?
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griseofulvin and terbinafine
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What are the adverse effects of griseofulvin?
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headaches, confusion, GI irritation, photosensitivity, liver function changes, disulfuram effects, contraindicated in people with porphyria
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What patients is griseofulvin contraindicated in?
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porphyria
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What are the adverse effects of terbinafine?
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GI upsets, rash, headache, taste disturbance
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What are two topical azole compounds in use?
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miconazole and clotrimazole
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