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antifungals
antifungals
12
Health Care
Professional
12/05/2010

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Cards

Term
amphotericin B
Definition
POLYENE - ANTIFUNGAL
USE: tx of systemic fungal infections, IV intrathecal for meningitis, severe life threating infections
Mechanism: target cell membrane, fungistatic, disrupt membrane through a pore and K+ ions lost, does not kill bacteria, binds ergosterol in cell membranes
Side Effecets: nephrotoxicity, increased creatinine and anemia and decreased potassium, acute fever, chills, rigors, aches, vomit, thrombocytopenia, leukopenia, hepatocellular and renal impairment, decreased bp, electrolyte balance, toxic
Other: forms pores, weakly water solubele , unstable at body temp, admin as complex with doxycholate, now have lipid formulations to decrease toxicity but more $, IV, does not cross BBB, inherent resistance only
Term
nystatin
Definition
POLYENE ANTIFUNGAL
USE: candida infections of skin, mucous, bowel
mechanism: target cell membrane, same as amphotericin B, fungistatic, disrupt membrane through a pore and K+ ions lost, does not kill bacteria, binds ergosterol in cell membranes
OTAHER: not ORAL, too toxic for IV, given topically
Term
clotrimazole
Definition
ANTIFUNGAL - IMIDAZOLE
USE: oral, vaginal or cutaneous candidiasis
machnism: target cell membranes, target cell membranes, inhibit fungal ergosterol synthesis, cidal or static dose dependent
Other: not ORAL, too toxic for IV,topical
Term
ketoconazole
Definition
ANTIFUNGAL - IMIDAZOLE
USE: chronic mucocutaneous candidiasis and paracoccidiodomycosis, non-life threating infections, not first choice, NOT for esophageal candidiasis
machnism: target cell membranes, inhibit fungal ergosterol synthesis, cidal or static dose dependent
Other: orall with food, avoid antacids, cimetidine, does not cross BBB, CP metabolism, sex adverse affects
Side effects: nausea, vomit, skin rash, reversible hepatotoxicity, gynecomastia, menstrual irregularity, drug interactions, resistance, C?I in renal impairment
Term
miconazole
Definition
ANTIFUNGAL - IMIDAZOLE
USE: oral, vaginal or cutaneous candidiasis
Term
fluconazole
Definition
ANTIFUNGAL - TRIAZOLE
USE: oropharyngeal and esophageal candidiasis
mechanism: target cell membrane, fungistatic inhibitor of ergosterol biosynthesis
Other: ORAL, excreted unchanged in urine, distribute well and in CNS
Side effects: well tolerated, GI, nausease, vomit, bloating, reversible alopecia, rare reversible thrmobocytopenia, increases cyclopsorine, warfarin
Term
virconazole
Definition
ANTIFUNGAL - TRIAZOLE
mechanism: target cell membrane
Term
terbinafine
Definition
ANTIFUNGAL - ALLYLAMINE
USE: tx of cutaneous infections, oncychomycosis of toenail and fingernal due to dermatophytes
mechanism: target cell membrane, fungicidal or static inhibitor of squalene epoxidase
Other: ORAL, topical, hepatic metabolism, renal elim, accumulate in hair, naisl, secreted in sebum, resistance not a problem yet, new
Term
caspoungin
Definition
ANTIFUNGAL - DNA SYNTHESIS ANTIMETABOLITE
USE: effective against Aspergillus and Candida, intra-abdominal abscess, peritonitits
machnism: targets cell replication/division, fungicidal, blocks cell wall biosyntehsis enzyme beta (1,3) D_glucan synthas
Other: NOT ORAL, IV ONLY< renal and hepatic elim, adjust dosage for HEPATIC insufficiency
Side effects: histamine mediated sys, better tolerated than amphotericin B
Other: resistance no yet
Term
flucytosine
Definition
ANTIFUNGAL - DNA SYNTHESIS ANTIMETABOLITE
USE: in conjunction with amphotericin B or triazole, tx of candida and cyrptococcal organisms
machnism: targets cell replication/division, fungistatic, activated to 5-FU and fdUMP, inhibits DNA synthesis by blocking thymidylate syntehtase
Other: ORAL, widely distributed even to CNS, excreted unchanged in kidney
BLACK BOX WARNING - use with caution in renal insufficiency
Side Effects: nausea, vomit, skin rash, reversible leukopenia and thrombocytopenia, syngergy with amphotericin B but fatal in AIDS with greater bone marrow suppression
Other: resistance is a big problem
Term
grseofulvin
Definition
USE: not against candida, good for epidermophyton, microsporum, trchophyton
mechanism: target cell replication and difivions - mitotic spindle, inhibits mitotic function, fungicidal
Other: ORAL aided by high fat food, increased affinity for skin and binds to keratin, given for a long time, not used topically, inactivated by liver by demethylation, excreted slowly in urine
side effects: increase anticoag metabolism, related to penicillins immunologically, replaced by triazoles and terbinafine
Term
tolnaftate
Definition
ANTIFUNGAL
USE: superficial skin, gut, oral, eye infections
- not systemically absorbed, too toxic for IV use
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