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NAME MOA PHARMAKOKINETICS ADVERSE EFFECTS THERAPEUTIC USES MISC.

Amphotericin B (a polyene Punches holes in ergosterol: 1. No oral absorption: so give it 1. Nephrotoxic (reversible) Severe systemic fungal 1. Monitor BUN and creatinine
antibiotic) increases membrane IV 2. Acute febrile reaction infections: levels daily to follow kidney
permeability, resulting in cell 2. Does NOT cross blood brain 3. Anemia 1. Systemic candida infections dysfunction
death barrier: so must give 4. Phlebitis at IV site 2. Cryptococcal meningitis 2. New lipid preparations are
intrathecally to reach CSF 3. Excellent for blastomycosis, less nephrotoxic: ABLC
3. Excreted via biliary tract and histoplasmosis, and amphocil, and ambiosome
kidney (clearance is not coccidioides
affected by kidney 4. Invasive aspergillosis
dysfunction) 5. Invasive sporotrichosis
6. Mucormycosis
Flucytosine Converted to 5-fluorouracil, 1. Oral absorption 1. Bone marrow suppression 1. Cryptococcal meningitis (in The reason for these adverse
which inhibits fungal DNA & RNA 2. Excreted in urine A. Leukopenia combination w/ amphotericin B) effects is that flucytosine inhibits
synthesis 3. Penetrates CSF well B. Thrombocytopenia 2. Candidal endocarditis (in DNA synthesis, which occurs
2. Nausea, vomiting and combination w/ amphotericin B) rapidly dividing cells such as
diarrhea bone marrow cells & GI epithelial
cells
Ketoconazole (an imidazole) Blocks ergosterol synthesis by 1. Oral absorption 1. Nausea, vomiting, and Chronic mucocutaneous
inhibiting cytochrome P450 2. Absorbed better at low pH anorexia candidiasis
enzymes. This causes depletion so worse absorption when 2. Hepatotoxic
of ergosterol, resulting in taken w/ antacids or H2 3. Inhibits CYP450 system,
disruption of the permeability of blockers resulting in decreased
the cell membrane 3. Extensive hepatic androgen & testosterone
metabolism synthesis:
A. Gynecomastia
B. Impotence
C. Decreased sex drive
D. Decreased sperm
production
4. Rash/pruritus
Miconazole and clotrimazole Blocks ergosterol synthesis by 1. Topical usage Low toxicity when used topically A. Topical fungal infections
(imidazoles) inhibiting cytochrome P450 2. Oral (not absorbed 1. Tinea versicolor
enzymes systematically) 2. Cutaneous candidiasis
3. Dermatophytosis
B. Oral troches for thrush (oral
candidiasis)
C. Vaginal suppositories for
candida vaginitis
Fluconazole (a triazole) Blocks ergosterol synthesis by 1. Oral absorption Less toxic than ketoconazole 1. Oral, vaginal, and
inhibiting cytochrome P450 2. Can also be administered IV No interference w/ testosterone esophageal Candida
enzymes synthesis 2. Alternative to amphotericin B
1. Nausea for treatment of:
2. Skin rash A. Systemic candidiasis
3. Headache (second choice, behind
amphotericin B)
B. Cryptococcal meningitis
C. Pulmonary and
Extrapulmonary
coccidioidomycosis (but
fluconazole us is not
used to treat
coccidioides meningitis)
Itraconazole (a triazole) Blocks ergosterol synthesis by 1. Oral absorption Less toxic than ketoconazole Shows promise in treating
inhibiting cytochrome P450 2. Metabolized and excreted No interference w/ testosterone systemic fungal infections (safer
enzymes via liver synthesis alternative for amphotericin)
3. Available IV 1. Nausea 1. Blastomycosis
2. Skin rash 2. Histoplasmosis
3. Headache 3. Coccidioidomycosis
4. Sporotrichosis
5. Chromomycosis
6. Invasive aspergillosis
Voriconazole Blocks ergosterol synthesis by 1. Oral absorption 1. Photophobia Highly active against a broad
inhibiting cytochrome P450 2. Can also be administered IV 2. Rash range of fungi. May be useful in
enzymes 3. Liver enzyme increases patients with Aspergillosis w/
therapy-limiting toxicity
associated w. conventional
regimens
Nystatin Punches holes in ergosterol: 1. Not absorbed from GI tract. Highly toxic if given IV 1. Oral, esophageal or gastric Order as nystatin, swish and
increases membrane Oral administration results in candidiasis (oral swallow
permeability, resulting in cell topical treatment along the administration)
death GI tract 2. Vaginal Candidiasis (apply
2. Apply topically to skin and topically)
vaginal infections
3. Too toxic to give IV
Griseofulvin Inhibits mitosis of cells by 1. Oral absorption 1. Headache, nausea, Dermatophytosis of the skin, Works very slowly
disrupting spindle formation vomiting, hair, and nails
2. Absorbed better w/ fatty photosensitivity, and
foods mental confusion
3. Deposits in keratin 2. Bone marrow
4. Excreted in feces unchanged suppression
Potassium iodide Skin rash Cutaneous sporotrichosis You get sporotrichosis while
potting plants