Shared Flashcard Set

Details

anti fungals
pharmacology, med chem, thera
24
Pharmacology
Graduate
11/11/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
fungal kingdom includes
Definition
yeast, mold, rust, mushrooms
Term
saprophytic
Definition
living on dead organic matter
Term
yeast can cause infections if
Definition
introduced via wounds or inhalation
Term
obligate intracellular parasite and fungi
Definition
only a few
candida albicans-gi flora
dermatophytes- living on/in keratin can cause ringworm/athlete's foot
Term
fungi are eukaryotes with
Definition
-lipid rich membrane
-DNA organized in chromosomes in nucleus
-cytoplasmic organelles (ER, golgi apparatus, mitochondria, storage vacuoles)
Term
unlike mammalian cells, fungi have
Definition
cell wall that functions like bacterial cell wall
Term
differences btw fungi and human cells
Definition
fungi have cell walls
diffrences in cell membrane, genetics, biosynthetic pathways
Term
echinocandins
Definition
EX-caspofungin and Micafungin,
moa-inhibit -(1,3)-D-glucan synthase, and thus disrupt cell-wall integrity in much the same way b-lactam antibiotics disrupt bacterial cell walls.
Term
5-flucytosine
Definition
moa-selectively taken up by fungal cells via the enzyme “cytosine permease” into fungal cell cytosol and converted to 5-fluorouracil, a potent inhibitor of DNA and RNA synthesis.
Term
polyenes
Definition
ex-amphotericin B
moa-binds to the cell membrane sterol ergosterol, thereby forming pores in the membranes.
Term
azoles
Definition
Ex-fluconazole, voriconazole, posaconazole
moa-specifically inhibit the fungal enzyme lanosterol 14-alpha-demethylase and blocks the production of ergosterol causing the accumulation of a toxic sterol intermediate, which results in cell membrane stress.
Term
azoles inhibit enzyme
Definition
CYP450 14DM= lanosterol 14alpha demethylase
Term
polyenes lead to cell
Definition
osmotic lysis
Term
flucytosine gets metabolized and leads to
Definition
blocking of thymidylate synthase and interferes with DNA synthesis; 5-fluorouracil is also converted into 5-fluorouridine triphosphate, which disrupts RNA synthesis. Note: Human cells do not contain cytosine permease or cytosine deaminase.
Term
Sterols account for approximately
Definition
25% of the weight of the cell membrane.
Term
the predominant sterol in many pathogenic fungi
Definition
ergosterol
Term
imidazoles
Definition
2 nitrogen atom containing ring system),
Ketoconazole
Miconazole
Clortrimazole
Term
triazoles
Definition
3 nitrogen atom containing ring system)
Itraconazole
Fluconazole
Voriconazole
Posaconazole
Term
Triazoles are more selective than
Definition
imidazoles
Term
Extensively and rapidly metabolized via
Definition
first pass effect
Term
azole resistance occurs due to
Definition
mutations in the cyp51A gene that encodes the target of azoles, lanosterol 14α-demethylase.
Term
azole clinical uses
Definition
broad
used topically to treat superficial dermatophytic and yeast infections.
orally for systemic fungal infections
Term
Because azoles are substrates for and thus potent inhibitors of the CYP3A4 enzyme pathway,
Definition
sometimes life threatening drug interactions occur
Term
azole adv effect
Definition
minor GI disturbances
May cause abnormalities in liver enzymes
Rare but may cause hepatitis
Supporting users have an ad free experience!