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Anti-fungal Drugs
VM 607 Final
21
Veterinary Medicine
Professional
02/24/2012

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Cards

Term
Griseofulvin Characteristics
Definition
natural product
oral tx for treating dermatophytes
Term
Griseofulvin Mechanism of Action
Definition
inhibits growth by disrupting mitotic spindle structure
normal mitosis cannot proceed
concentration in newly formed cells of skin, hair, nails
stops infection from spreading
fungi are shed as infected hair, skin, nails are replaced
Term
Polyenes Characteristics
Definition
natural product from some streptomyces species
Amphotericin B and Nystatin
Term
Polyenes Mechanism of Action
Definition
binds to ergosterol in fungal membrane
distorts membrane which alters permeability
causes leakage of ions
Term
Amphotericin B Characteristics
Definition
from streptomyces nodosus
used IV to treat deep-seeded fungal infections
Term
Amphotericin B Mechanism of Action
Definition
several molecules insert into cytoplasmic membrane of fungi
forms cylindrical channel that pentrates membrane
pore causes leakage from cell
must cross cell wall to access membrane
Term
Amphotericin B Adverse Reactions
Definition
nephrotoxic
binds to other sterols (cholesterol)
Term
Amphotericin B Resistance
Definition
alterations in membrane sterol composition creates resistance
Term
Flucytosine Characteristics
Definition
originally created as anticancer
aka 5-flurocytosine or 5-FC
inhibits growth of Candida and Cryptococcus
used for treating fungal meningitis
Term
Flucytosine Mechanism of Action
Definition
disrupts DNA and RNA synthesis to inhibit fungal growth by two mechanisms
1)enters cell and is converted inside the cell
replaces uracil in pyrimidine pool
distorts normal RNA structure
2) enters cell and is converted
competitively inhibits thymidylate synthetase which makes thymidine for DNA synthesis
Term
Flucytosine Adverse Reactions
Definition
cannot be used directly as antifungal
not taken up by fungal cells and is toxic to mammalian cells
Term
Flucytosine Resistance
Definition
secondary resistance: develop resistance during treatment
decreased permeability, deficiency in enzymes to convert, synthesis of metabolites to compete?
develops more rapidly when used alone
use with amphotericin B
Term
Azoles Characteristics
Definition
synthetic compounds
lower toxicity and broad spectrum
systemic and topical drugs
Term
Azoles Mechanism of Action
Definition
interfere with ergosterol biosynthesis
depletes ergosterol to alter plasma membrane structure
damage of membrane makes cell susceptible for other damage
inhibits fungal growth
Term
Azoles Resistance
Definition
develops through long-term use
Term
Imidazole Characteristics
Definition
Ketoconazole
oral or topical
Term
Itraconazole Characteristics
Definition
broad range of antifungal activity
treats dermatophytes
Term
Fluconazole Characteristics
Definition
lower toxicity
penetrates CSF
treats Candida and Cryptococcus
ineffective against Aspergillus
Term
Voriconazole Characteristics
Definition
effective against Aspergillus
Term
Echinocandins Mechanism of Action
Definition
inhibits B1,3-glucan synthesis in fungal cell wall
Term
Echinocandins Characteristics
Definition
Caspofungin, Micafungin, Anidulafungin
treats Candida and Aspergillus if doesn't respond to other agents
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