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