Hosam Mohamed-
binds to ergosterol to form pores & channels that lead to the leakage of intracellular ions
What is the MOA of Polyenes?
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Nystatin, Amphotericin
What are our Polyenes? (2)
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fever, chills, thrombophlebitis, HA, malaise
What are infusion-related reactions that can occur when administering Polyenes?
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acetaminophen, steroids
What can be taken prior to avoid the infusion-reactions of Polyenes?
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b
Which one is Amphotericin B Lipid Complex?
a) C-AmB
b) ABLC
c) ABCD
d) L-AmB
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c
Which one is Amphotericin B Colloidal Dispersion?
a) C-AmB
b) ABLC
c) ABCD
d) L-AmB
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a
Which one is Conventional Amphotericin B?
a) C-AmB
b) ABLC
c) ABCD
d) L-AmB
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d
Which one is Liposomal Amphotericin B?
a) C-AmB
b) ABLC
c) ABCD
d) L-AmB
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a
Which amphotericin formulation causes the most cases of azotemia & anemia?
a) C-AmB
b) ABLC
c) ABCD
d) L-AmB
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pre-treatment of fluids
How do we prevent renal tubular acidosis from occurring when administering amphotericin?
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ABCD, C-Amb, ABLC, L-AmB
In regards to infusion-related reactions, rank our formulations from worst to best in terms of toxicity.
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candida only
Nystatin spectrum?
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topically only; severe toxicity when administered PO or IV
How is Nystatin administered? Why?
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meningitis, zygomycosis, neutropenic fever
What are the clinical uses for Amphotericin B? (3)
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potassium, magnesium
Which ions are wasted when Polyenes are administered?
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a pyrimidine analog that is converted from 5-FU and inhibits DNA/RNA synthesis
What is the MOA for Flucytosine?
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d
Which anti-fungal agent has good penetration and is primarily used for Cryptococcal meningitis?
a) polyenes
b) azoles
c) echinocandins
d) flucytosine
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d
Which anti-fungal agent is ONLY available orally?
a) polyenes
b) azoles
c) echinocandins
d) flucytosine
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cryptococcus; some candida
Flucytosine spectrum?
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d
Which anti-fungal class can cause bone marrow toxicity?
a) polyenes
b) azoles
c) echinocandins
d) flucytosine
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d
Which anti-fungal class can cause liver enzyme alterations?
a) polyenes
b) azoles
c) echinocandins
d) flucytosine
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inhibits 14-a-sterol demethylase to impair the biosynthesis of ergosterol; disrupting the packing of phospholipids and impairing the enzyme systems
Azoles MOA?
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metabolized slower; less effect on human sterol synthesis
Why are triazoles preferred over standard azoles?
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candida, blastomyces, histoplasma, coccidioides
Azole spectrum? (4)
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b
Which antifungal class is mostly fungistatic?
a) polyenes
b) azoles
c) echinocandins
d) flucytosine
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f; can be cidal at high concentrations
Azoles are never cidal. T/F?
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b
Which antifungal class can cause drug interactions in the CYP450 pathway?
a) polyenes
b) azoles
c) echinocandins
d) flucytosine
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b
Which Azole is ONLY available orally?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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b
Which Azole requires stomach acid to be absorbed?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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a
Which Azole has excellent GI absorption & renal excretion?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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cryptococcus meningitis, transplant prophylaxis, candidasis
What are the clinical roles of Fluconazole? (3)
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b
Which Azole is teratogenic/ CI in pregnancy?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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blastomyces, histoplasma, coccidioides, onychomycosis
What are the clinical roles of Itraconazole? (4)
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a
Which Azole has the least drug interactions?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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aspergillus, febrile neutropenia, candidemia, salvage therapy
What are the clinical roles of Voriconazole? (4)
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prophylaxis-neutropenia, salvage therapy-mucormycosis
What are the clinical roles of Posaconazole? (2)
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c
Which Azole can lead to an accumulation of SBECD when administered IV?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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d,e
Which Azole has greater activity in vitro?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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d
Which Azole has significantly altered absorption with food?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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e
Which Azole is a prodrug?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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e
Which Azole is new and still has an unclear clinical role?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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IV & PO
How are Azoles administered?
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febrile neutropenia, salvage therapy, mucormycosis
What are the clinical roles of Isavuconazole? (3)
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b
Which azole has a black box warning for Coronary Heart Failure (CHF)?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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a
Which azole can cause rashes and sometimes lead to SJS?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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a
Which azole can cause heart attacks?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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c
Which Azole can cause visual side effects such as hallucinations?
a) fluconazole
b) itraconazole
c) voriconazole
d) posaconazole
e) isavuconazole
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N&V, diarrhea, abdominal pain, hepatotoxicity, QT prolongation
What are the general SE's of Azoles? (5)
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inhibits cell wall synthesis by binding 1,3-B-D- glucan synthase
What is the MOA of Echinocandins?
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candida, aspergillus
What is the spectrum for Echinocandins? (2)
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c
Which class of antifungals are only available via IV?
a) polyenes
b) azoles
c) echinocandins
d) flucytosine
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lack oral bioavailability, poor concentration in kidneys, high protein binding, hepatic clearance
What are some common PK features associated with Echinocandins? (4)
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c
Which do we adjust when there is hepatic impairment?
a) andiulafungin
b) micafungin
c) caspofungin
d) rezafungin
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d
Which one has an extremely long half-life that requires per week dosing?
a) andiulafungin
b) micafungin
c) caspofungin
d) rezafungin
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invasive candidiasis; salvage-therapy aspergillus
What are the clinical roles of Caspofungin, Micafungin, and Anidulafungin? (2)
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infusion site reaction, histamine-like effects w/rapid infusion, cardiac toxicity
What are AE's associated with Echinocandins? (3)
