anti-fungal drugs Flashcards
1. List the prototype drugs used to treat systemic, mucocutaneous, and topical fungal infections, describe their mechanism of action, list their clinical uses, and list their significant side effects.
MOA of flucyosine
inhibits fungal nucleic acid by interfereing with fungal thymidylate
MOA of griseofulvin
inhibits mitosis by binding to tubilin
Polyenes MOA
destabylizes fungal membrane
drugs that inhibit squalene expoxidase
allyl- and benzyl-amines
drugs that inhibit 14 alpha demethylase
Tri-, imid-azoles
MOA of echinocandins
inhibits cell wall synthesis
can cause bone marrow suppression
flucytosine
use of flucytosine
used with Ampotercin B to treat systemic candida and cyptococcal infections
accumultes in keratin precursor cells
griseofulvin,
use of griseofulvin
syperficial mycoses
must be used for 6 months to a year
griseofulvin
SE of griseofulvin
headache, hepatic enzyme induction , and disulfrim reactions
MOA of terbinafine and butenafine
prevent formation of lanosterol by squalene epoxidase inhibition, and produce accumulation of toxic squalene metabolite
accumulates in hair, skin and nails
terbinafine
cures most nail mycoses
terbinafine
SE of terbinafine
GI upset, headache, rare hepatic toxicity
300 hr half life drug
terbinafine
use of butenafine
superficial mycoses
-azole MOA
inhibit 14a demathylase, decreasing ergosterol formation and increasing accumulation of toxic 14a-methyl sterole
inhibits hepatic P450 and can cause drug interactiions
-azole
broad spectrum fungistatic at low doses, fungicidal at high doses
-azole
SE of ketoconazole
inhibiton of P450 n/v, endocrine abnormalities
DOC for systemic blastomyces, sporothix, and SQ chromoblastomycosis
itraconazole
azoles that do not cross the BBB
intra, keto,
azoles that DO cross BBB
fluco
used as a single dose for vaginal candida
fluconazole
absorption not effected by gastric pH
fluconazole
used for phrolylaxis of crytococcal meningitis
fluconazole
DOC for esophgeal and oropharyngel candidasis
fluconazole
only azole used for mucormycosis
posaconazole
DOC for invasic aspergillosis
vericonazole
can cause visual disturbances
vericonazole
inhibits CYP3A4
posaconazole
form of posacanzole
oral
broadest spectrum -azole
posaconazole
topical OTC -azoles with significant systemic toxicity
clotrimazole and miconazole
DOC for serious systemic mycosis
amphotericin
MOA of amhpotericin B
binds to fungal erosterol to form a pore, distrupting membrane stability
reason amphotericin B has low toxicity
affinity is 500 times higher for fungal erosterol than human
does amphotercin B cross the BBB?
no
way amphocerterin must be administered
IV (highly insolulabe)
dose related SE of amphotericin
kidney damage, anemia
infusion related SE of amphotericin
fever, chills, muscle spasma, vomiting, hypotension
way to treat infusion related SE of amphotericin
infuse slowly or pretreat with antihistamines
formulation of ampotericin B that reduces toxity
lipid formulation
MOA of echinocandins
target fungal cell wall sythesis
caspofungin class
echinocandins
use of caspofungin
IV for esophageal candiadis and spergillus
used IV for esiphageal and invasive candidias
anidulafungin
used Iv for mucocutaneous candidiadsis and prophalyxis for candida in BM transplant pts
micofungin
can produce histamine release and flushing
micofungin and echinocandins