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Antifungals
IUSOM Spring 2012
9
Pharmacology
Graduate
04/16/2012

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Cards

Term
Caspofungin
Definition
Use: Invasive candidiasis
MOA: 1,3 B Glucan synth inhibition
Adverse: Well tolerated, GI or flushing
Admin: IV only
Metabolism: hepatic
Term
Amphotericin B (polyenes)
Definition
Use: Broad spectrum anti-fungal. #1 for crypto meningitis. Some protozoa action.
MOA: binds ergosterol and forms pores
Adverse: Renal impairment, infusion rxn, arrhythmia
Admin: IV, oral (thrush), intrathecal, topical
Dist: tissue bound, H/L 15 d. LOW CSF levels
Term
Terbinafine (Lamisil, Allylamines)
Definition
Use: Dermatophytes (Tinea Unguium, cruris, pedis, capitis)
e.g. jock itch, onychomycosis, scalp ringworm, athletes foot
MOA: Inh. squalene epoxidase -> ergosterol synth.
Adverse: Not for preggos or liver/renal failure
Pharm: Oral, topical. Lipophilic, accumulates in skin/nails/fat for long time.
Term
Itraconazole
Definition
Use: ASPERGILLOSIS Broad-spectrum antifungal. Crypto, histo, blasto, onycho. Candidiasis
MOA: Inh. Lanosterol 14a Demethylase (CYP450, ergosterol synth)
Adverse: Not for HF. Otherwise well tolerated, some GI
Inh. CYP3A4 -> drug interactions
Pharm: Most tissues. NO CSF
Mech Resist: C. albicans- mut. drug target, efflux pump, inc. expression drug target
Term
Fluconazole
Definition
Use: Superficial and systemic fungal inf. Crypto, Candidiasis. NOT ASPERGILLOSIS
MOA: Inh. Lanosterol 14a Demethylase (CYP450, ergosterol synth)
Adverse: Well tolerated. Some GI, headache, rash
Admin: IV, oral. CYP3A4 -> drug interactions
Dist: Most tissues, INCLUDING CSF
Term
Flucytosine
Definition
Use: Combine w AmphoB. Crypto meningitis. Systemic fungal ifx- candida, crypto
MOA: Cytosine nucleotide analog -> converted to 5-FU
Adverse: BM supression, liver damage, GI. Adjust for renal impairment
Pharm: Oral, +CSF
Term
Griseofulvin
Definition
MOA: Microtubule mitosis inhibitor
Use: Dermatophytes (hair 1 mo, skin 6-9 mo, nails 1+ yr)
Adverse: Well-tolerated. Check blood count. Photosensitivity, Rash. Teratogen in animals.
Pharm: Oral, topical powder. Depot in keratin precursor cells. Induce CYPs -> ^^warfarin metabolism, reduced OCP efficacy.
Term
TMP-SMX
Definition
Use: PCP
MOA: DHPS inh. (sulfa), DHFR inh. (TMP). Folic acid inhibitor
Adverse: Rash, hepatitis, neutropenia, azotemia, thrombocytopenia
Term
Pentamidine
Definition
Use: Alt. for PCP. Also Leishmania, Trypanosomes
MOA: ???
Adverse: Nephrotoxic, arrhythmias and HF, hypoglycemia, avoid nephrotoxic drugs. Monitor Cr, BUN, Glu, CBC, EKG, BP
Pharm: IM or IV. (-)CNS. Hepatic met. Renal excrete
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