Antifungals Flashcards
Amphotericin B
Broad spectrum, limited b/c of toxitcity, standard of treatment for most serious mycoses
Mucocutaneous
Yeast infection in mouth, Thrush
Fungi MOR
Efflux pumps, impaired ergosterol binding, reduced permeabilty of cell membrane, alter P450 enzymes, overproduction of enzymes
Amphotericin B available products
Funigizone, Abelcet, Amphotec, AmBisome
Amphotericin B
fungicidal, ergosterol (cholesterol in fungus membrane), causes cell to be very leaky and die
Amp-B Spectrum of coverage
Yeasts, Molds, resistance shown with some species as well.
Amp-B ADR
Infusion related rxn’s or toxicity. (fever, chills, muscle spasms, vomiting, HA and hypotension) premedicate ADR symptoms to reduce ADR, slow infusion, give via central line (minimal-anemia/neurotoxic)
Amp-B
risk increases with increased dose, give 1-2 grams, give w/ NS
L-AmB (lipid version)
least nephrotoxicity, least infusion rxn’s
Flucytosine
taken up by cell, converted to 5-FU and other metabolites, oral, inhibits DNA and RNA synthesis
Flucytosine
rarely used, Cryptococcal meningitis and Chromoblastomycosis, NOT as a mono-therapy
Flucytosine ARD
Bone marrow toxicity w/ anemia, leukopenia, thrombocytopenia (decrease in platelets), incr. LFT, enterocolitis
Diflucan
Fluconazole
Sporanox
Itraconazole
Nizoral
Ketoconazole
Vfend
Voriconazole
Noxafil
Posaconazole
Imidazoles
ketoconazole, miconazole, clotrimazole, older, more drug-drug interactions
Triazoles
Fluconazole, voriconazole, posaconazole, itraconazole
Azole MOA
inhibit enzyme that eventually leads to ergosterol synthesis, inhibits fungal P450 enzymes
Azole Spectrum of Activity
Broad, Candida, Aspergillus, Dermatophytes
Azole ADR
NVD
Ketoconazole
shampoo for dandruff, absorption is pH dependent, metabolized in liver, increase LFT, excreted in bile
Ketoconazole
IMPOTENCE, rash, pruritis, alopecia, menstrual irregularities,
Itraconzaole
pH dependent, oral, WF that is acidic, for onychomycosis
Itraconazole Drug Interactions
antacids, H2 blockers, PPI’s, rifampin decreases itraconazole
Fluzonazole
Candida, absorption NOT pH dependent, good CSF penetration (60-80%), NOT for aspergilius
Fluconazole ADR
less of the common ADR 100-800mg daily
Vfend
treatment of choice for Aspergillosis, on empty stomach, 30% GET VISUAL DISTURBANCES W/IN 30MIN, LASTS FOR 30 MIN
Vfend ADR
QTc prolongation, more interactions than other newer azoles, Loading dose required
Poscanazole
broadest spectrum of all, suspension, tablet, IV, give w/ full high fat meal
Poscanazole
broadest spectrum of all, suspension, tablet, IV, give w/ full high fat meal
Miconazole/Clotrimazoel
for thrush, dermatophytic infections (Tinea corporis, pedis, cruris)
Know MOA for all
Echinocandins- inhibit component of cell wall
Echinocandins
overall well tolerated w/ minor GI side effects and flushing
Candidas
Capsofungin, for neutropenic therapy, slow rate of infusion and pre-medicate with antihistamine, DOES NOT INHIBIT CYP450, load w/ 70mg then continue w/ 50mg daily
Mycamine
(Micafungin), similar to Candidas, 150mg daily for esophageal candidiasis, 50mg prophylaxis
Eraxis
(anidulafungin), invasive or deep-tissue candidiasis, NO SIGNIFICANT DRUG INTERACTIONS, IV
Others
Griseofulvin (must use for 2-6 weeks), Terbinafine (Lamisil) for at least 12 weeks, Nystatin- for oral thrush
