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FIU - Anti-Fungal Drugs
Antifungals
23
Pharmacology
Graduate
01/15/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
types of fungi
Definition
yeasts
dimorphic fungi
mold
dermatophyte
Term
yeasts
Definition
-single oval cells
Candida, cryptococcus, trichisporon
Term
dimorphic fungi
Definition
HSBC
-histoplasma
-Sporothrix
-Blastomyces
-Coccidiomyces
Term
molds
Definition
filamentous strands = hyphae
-Aspergillus
-Zygomyces
-Fusarium
Term
Dermatophyte
Definition
-microsporum
-trychophyton
-epidermophyton
Term
Cryptococcus
Definition
-yeast
-from soil contaminated by pigeon or chicken droppings or by inhalation (C. neoformans)
High CNS affinity --> meningitis
high incidence in immunocompromised patients
Term
Aspergillus
Definition
-mold
-widespread in the environment; soil, water, dead leaves, compost
-Acquired through inhalation
Term
Histoplasma
Definition
dimorphic
common to Ohio and Mississippi river valley
90% of residents exposed
Term
Blastomyces and Coccidiomyces
Definition
dimorphic
Blastomyces - Central and SE states
Coccidioides - SW states (San Joaquin Valley Fever)
Term
Microsporum
Definition

anamorphic/dermatophyte

 ringworm disease: tinea corporis

Athletes foot: tinea pedis

Term
Echinocandins; MOA, Use, PK
Definition
-fungins
MOA: inhibit cell wall synthesis by blocking B-(1,3) D-glucan synthase --> cell death
Use: Candida species, Aspergillus spp. (not good for cryptococcus neoformans)
PK: t1/2=15hrs, high protein binding, can cross BBB but low CSF concentration - not good for CNS infections
i.v. only
Term
Azole antifungals; use, MOA
Definition
use: systemic infections
MOA: bind to lanosterol demethylase and inhibit production of ergasterol, a key component in fungal cell membranes
Term
Ketoconazole; use, PK, ADR
Definition
Use: mucosal infections
PK: absorption dependent on pH - give w/ cola or juice, poor CSF penetration, t1/2=2-10hrs, 3A4 metabolized
ADRs: N&V, hepatotoxicity, CYP3A4 and 2C19 inhibition, decreased testosterone synth (gyenecomastia, oligospermia,decreased libido) decreased adrenal cortisol synth
Term
Fluconazole, advantages/disadvantages
Definition
2nd Generation azole
-better tolerated, i.v. or p.o., longer halflife, better PK, better CNS penetration
-fungistatic, resistance is increaseing, narrowing of spectrum
Term
Itraconazole, ADRs
Definition
from i.v. or p.o.
Taste disturbances
N & V
Osmotic diarrhea
Long term compliance low
**but has a broader spectrum
Term
Voriconazole, ADRs
Definition
Visual disturbances (30%) - decreased vision, photphobia, altered color percception and discomfort *are reversible
more in i.v. than p.o.
Also PDE6 inhibition and increased digoxin
Term
What antifungal can't be administered with Azoles? why?
Definition
Amphotericin B
decrease in ergosterol from Azoles will reduce the fungicidal effect of AmphoB
Term
Terbinafine
Definition
"Lamisil"
Allylamine
MOA: inhibits ergosterol synthesis by inhibiting squalene epoxidase
Term
Amphotericin B; use, MOA
Definition
Polyene antibiotic, very efficacious
Use: invaseive fungal infection, not responding to other therapy
MOA: binds to ergosterols in fungal membrane, creates
Term
Amphoteracin B; PK and metabolism
Definition
PK: absorption from GI is negligible, only given i.v.
selective soft tissue distribution
kidney>liver>spleen>lung>heart>skeletal muscle>brain>bone>CSF>eyes
Metabolism: unknown, accumuates in tissue and is slowly released; inverse relationship between age and elimination
Term
Amphotericin B; ADRs
Definition
infusion related cytocine storm - inflammatory response, temp increase, vasodilation, drop in BP nephrotoxicity - decrease RBF and GFR, tubular ischemia, wasting of K, Na and MG Hepatatotoxicity Hypkalaemia
Term
Griseofulvin
Definition
Cytosol antifungal
only fungus selective Microtubule inhibitor
Must accumulate in skin, takes long to kick in
Term
Flucytosine
Definition
Fungistatic
pyrimidine anologue, 5-fluorocytosine
5FC taken up selectively by fungus and converted to 5FU which stops DNA synthesis
Resistance develops quickly, use w/ AmphoB or fluconazole
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