- inhibition of lanoserol > ergosterol synthesis - disrupts sterol content in cell membrane

- caspifungin - micafungin - anidulafungin

Fitz - Antifungal Drugs Flashcards by Erin Kretovics

MOA: Amphoterecin B

insert into yeast membrane, physical association w/ ergosterol to form hydrophilic pores in cell membrane > disruption of membrane integrity

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AEs: Amphotericin B Deoxycholate

-at infusion: chills, fever, anemia, hypotension
-later onset: nephrotoxicity
(mostly ass’d with the deoxycholate)

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polyene drug

amphotericin B

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mechanism of nephrotoxicity caused by amphotercin B

direct damage to distal tubule
Na, Mg, K wasting > hypokalemia
decreased GFR> arteriole constriction
further concentration of drug in tubule > inc damage

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pts at increased risk for nephrotoxicity caused by amphotericin B

transplant pt
HIV pts
pts with serious inf (gm(-), MRSA)

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triazole drugs - 1st gen

fluconazole

- utraconazole

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triazole drugs - 2nd gen

voriconazole

- posaconazole

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MOA: fluconazole

inhibition of lanoserol > ergosterol synthesis

- disrupts sterol content in cell membrane

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what yeast CYP450 enzyme does fluconazole target?

14-alpha-demethylase

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Fluconazole indications

candida albicans

- cyptococcus (w/ AmpB)

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Fluconazole limitations

aspergillus

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Fluconazole clearance

75% renal

-good for candiduria

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Itraconizole indications

candida albicans
other candida
histo*
coccidioides*
blastomycoses*

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voriconisol indications

candida albicans
other candida
aspergillus

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echinocandins

caspifungin
micafungin
anidulafungin

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MOA: echinocandins

inhibition of beta-(1,3)-glucan synthase leading to osmotic fragility of the fungal cell wall

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metabolism of caspofungin

hepatic - good for renal pts

what type of pts do you worry about caspofungin drug interactions with?

immunocomp pts d/t cyclocporine or tacrolimus

caspofungin indications

-serious opportunistic infections (candidiasis, aspergillosis)

how long can it take to see results of antifungals?

up to 8 days!

what would you use in an HIV pt with cadidiasis who failed fluconazole, amphotericin B, and itraconazole

caspofungin

caspofungin limitations

histoplasmosis
coccidiomycosis
fusarium spp

histoplasmosis has been ass’d with what type of therapy?

anti-TNFalpha therapy

most common pulmonary and systemic mycosis in humans

histoplasmosis

triazole opportunistic indications

- aspergilllus - candida - rhizopus - cryptococcus

triazole pathogenic indications

- histoplasma - coccidioides - blastomyces - paracoccidiodies

intraconizole is front line tx for

- histoplasmosis - coccidioides - blastomycoses

tx of oral candidiasis in HIV pts

- oral fluconazole | - can also use itraconazole

drug of choice for invasive aspergillosis

voriconazole

what do you use for candidiasis resistant to fluconasole (C. krusi, c. galbrata)

voriconazole

AEs: ketoconazole

- inhibition of adrenal and gonadal steroid synthesis - gynecomastia - decreased libido

2 triazoles with wide dist including the CSF

- voriconazole | - fluconazole

what would impair the absorption of itraconazole?

antacids - needs gastric acidity to dissolve

2 triazoles that inhibit hepatic CYP450 and enhance renal toxicity

- voriconazole | - itraconazole

why do you avoid voriconazole in kids?

vision disturbances

rare fungal infection ass'd with tornado-related wounds

zygomycosis

tx of mucormycosis (zygomycosis)

amphotericin B

drug of choic for crytoccal meningitis

amphotericin B + 5-FC

MOA: 5-FC

inhibition of DNA & protein synthesis

intrinsic resistance to 5-FC is caused by

mutated cytosine permease (can't cross cell membrane)

acquired resistance to 5-FC is caused by

mutated cytosine deaminase (can't be converted to active form, 5-FU)

role of amphotericin B in tx of cryptococcal meningitis

creates ergosterol pores for 5-FU to enter in the case of resistance