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Anti-Infectives Exam 3 > Lecture 1 - Antifungal Agents > Flashcards

Lecture 1 - Antifungal Agents Flashcards

1
Q

Fungal Categories and which are more resistant to antifungals?

A

Yeasts (Unicellular)
Dimorphics ( Can be yeast or mold)
Molds (Multicellular & more resistant)***

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2
Q

Polyene Macrolide Antifungals

A

Amphotericin B

Nystatin

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3
Q

Polyene Macrolide Antifungal MOA

A
  1. Bind to ergosterol leading to pore formation and leakage of intracellular contents
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4
Q

Low conc of Polyene Macrolide Antifungal

A

selective for ergosterol-rich fungal cell membranes

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5
Q

High conc of Polyene Macrolide Antifungal

A

can damage cholesterol-rich mammalian cells

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6
Q

Amphotericin B Preparations info

A

Deoxycholate = rarely used

Liposomal ones = decrease ADE

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7
Q

Nystatin Preparations

A

Tabs
Suspension
Vag suppositories
Topical cream & powders

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8
Q

Amphotericin B Spectrum of Activity

A

Candida species (Except Lusitanae + auras)

Cryptococcus neoformans

Aspergillus species (Except terries)

Dimetacieous molds (inc rhizomes + mucorlaes)

Endemic fungi ( Blastomycosis, Histoplasma, Coccidiodes)

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9
Q

Liposomal (Ambisome) Dosing Adjustment

A

No adjustment for renal or hepatic insufficiency

Dose: 3-5mg/kg IV every 24hrs, can go higher if needed

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10
Q

Dose-limit toxicity of Amphotericin B?

A

Nephrotoxicity

rehydrate prior to admin

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11
Q

Monitoring for Ambisome

A

AST, ALT, ALP
K & Mg wasting
Acute pulmonary Tox
Infusion reactions

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12
Q

Drug interactions Amphotericin B

A

Nephrotoxicity accelerated by…

Calcineurin inhib (tacrolimus + cyclosporine)
Aminoglycosides
IV contrast
Foscarne
Cidofovir
Tenofovir disoproxil fumarate

Meds that deplete K/Mg = Loop diuretics

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13
Q

Giving Amphotericin B infusion

A

Flush & Mix with D5W, incompatible w/ saline*****

premeditate with Benadryl/ APAP

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14
Q

Amphotericin B Nephrotoxicity Mechanism

A
  1. Reduces pre renal blood flow leading to decrease in GFR
  2. Binds to lipid bilayers of the proximal + distal tubules to cause direct toxicity

Effects Pre/Post Renal blood flow

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15
Q

Mitigating Nephrotoxicty Amphotericin B

A

Hydration, maintain euvolemia

Infuse 250-500ml NaCl 0.9% prior to infusion

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16
Q

Nystatin Spectrum of Activity

A

Candida Species

Tinea

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17
Q

Nystatin Toxicity

A

Limited due to minimal-low absorption

Oral associated with N/V/D

All potential hypersensitivity

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18
Q

Nystatin Oral susp

A

spit for oral candida

swallow for esophageal candida

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19
Q

Nystatin oral tabs

A

non absorbable

used for candida ppx only

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20
Q

5- Flucytosine (5-FC) MOA

A

Converted intracellularly from 5-FC -> 5-FU by fungal cytosine deaminase

Prevents fungal DNA/RNA synthesis

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21
Q

5- Flucytosine (5-FC) should only be used….

A

in combo with other antifungals given rapid resistance to monotherapy

often used corectal cancers

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22
Q

5- Flucytosine (5-FC) dose adjustment

A

Renal cleared

normal: Q6hr

CrCl 10-50 = dosing interval Q12-24hrs
CrCl < 10 = dosing interval Q24-48hrs

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23
Q

5- Flucytosine (5-FC) Spectrum of Activity

A

Candida Spp.

Cryptococcus neoformans

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24
Q

5- Flucytosine (5-FC) ADE

A

CBC w/ Diff (monitor for leukopenia)
N/V
Serum Drug lvls

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25
Q

5- Flucytosine (5-FC) Toxicity lvls

A

peak 50-100mcg/mL

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26
Q

Triazole Antifungals

A 
Ketoconazole
Fluconazole
Itraconazole
Voriconazole
Posaconazole
Isavuconazonium (pro-drug)
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27
Q

Triazole Antifungal MOA

A

Inhibit fungal 14-alpha demethylase-blocking ergosterol synthesis

Leads to dysfunctional fungal membrane synthesis

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28
Q

Fluconazole Spectrum of Activity

A 
Candida albicans = +
Candida glabrata = +/-
Candida Krusei** = --
Aspergillus fumigateurs** = --
Cryptococcus neofromans= ++
Resistant mold Rhizomes Mucor** = --
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29
Q

Itraconazole Spectrum of activity

A 
Candida albicans = +
Candida glabrata = +/-
Candida Krusei = +/- (small bump over fluc)
Aspergillus fumigateurs** = +
Cryptococcus neofromans = + 
Resistant mold Rhizomes Mucor** = --
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30
Q

Voriconazole Spectrum of Activity

A 
Candida albicans = +
Candida glabrata = +
Candida Krusei = +/-
Aspergillus fumigateurs** = ++
Cryptococcus neofromans = +
Resistant mold Rhizomes Mucor** = --
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31
Q

Posaconazole Spectrum of Activity

A 
Candida albicans = +
Candida glabrata = +
Candida Krusei = +
Aspergillus fumigateurs = +
Cryptococcus neofromans = +
Resistant mold Rhizomes Mucor** = ++
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32
Q

Isavuconazole Spectrum of Activity

A 
Candida albicans = +
Candida glabrata = +
Candida Krusei = +
Aspergillus fumigateurs = +
Cryptococcus neofromans = +
Resistant mold Rhizomes Mucor = +
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33
Q

Which Tripazole has most Bioavial?

A

Fluconazole = ~ 100%, 80% Renal Elim unchanged

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34
Q

Fluconazole Dose Adjustments

A

Req dose adjustment

Reduce maintenance doses 50% for CrCl < 50mL/min

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35
Q

Fluconazole ADE + Monitoring Paramaters

A

Hepatotoxicity
Monitor AST,ALT, Alk phos

    • torsades de pointes **
    • EKG (Prolonged QT Interval) **
36
Q

Itraconazole - Oral Spectrum of Activity

A 
Candida albicans
Cryptococcus neoformans
Aspergillus spp
histoplasmosis
Blastomycosis
Tines unguium (nail fungus)
37
Q

Itraconazole admin recommendations

A

Take with an acidic beverage with drugs reducing gastric acidity

anything changing pH in Gut can cause issues

38
Q

Itraconazole Bioavail

A

Difference between capsules and suspensions

39
Q

Itraconazole ADE

A

**Hepatotoxicity **
** Ventricular dysfunction, CI in pts with CHF **
Hypersensitivity
Nause
Headache
Breast tenderness - gynecomastia

40
Q

2nd Gen Triazoles

A

Voriconazole
Posaconazole
Isavuconazonium-isavuconazole

Ravuconazole - investigational
Albaconazole - investigational

41
Q

Voriconazole Spectrum of Activity

A

Candida = including some fluconazole resistant

Aspergillus spp = Drug of choice for therapy for invasive disease

Resistant mold including Scedosporium, Fusarium

Less so other mold, Mucorales, Rhizopus

42
Q

Dose adjustments req for Voriconazole

A

Requires Hepatic Dose adjustment

Load dose to reach Steady State

43
Q

Notable ADE of Voriconazole

A

CNS: Hallucinations, agitation, anxiety, delirium
Hypersensitivity: Rash & phytotoxicity

44
Q

Posaconazole Spectrum of Activity

A

Candida - including some fluconazole resistant
Aspergillus spp.
Resistant mold including Mucor, Rhizopus, Scedosporium, Fusarium

45
Q

Posaconazole Dosing Adjustments

A

Suspension has erratic absorption, consider alternative dosing in pts with extreme weights

Distinc differences between oral suspension & oral delated release tabs/IV

46
Q

Posaconazole ADE + Monitoring

A

Hepatotoxicity = AST/ALT, Alk Phos

torsades de pointes, prolonged QT interval

Hypersensitivity = rash + phototoxicity

No CNS

47
Q

Isavuconazonium-Isavuconazole Spectrum of Activity

A

Candida - including some fluconazole resistant
Aspergillus spp.
Resistant mold including Mucor, Scedosporium, Fusarium

48
Q

Isavuconazonium-Isavuconazole Dose adjustments

A

IV:PO is 1:1 ratio

Hepatic: no adjustment for Child-Pugh score A/B
Renal: no adjustment for insufficiency, including ESRD

49
Q

Isavuconazonium-Isavuconazole notable ADE

A

** Shortens QT, unlike others which prolong ***

50
Q

DI Itraconazole

A

H2 antagonist
PPI
Mg, Al, Ca antacid (space 1hr before, 2hrs after) or drink coca-cola or OJ

51
Q

Triazole w/ most CYP interactions

A

Ketoconazole

52
Q

Triazole w/ least CYP interactions

A

Fluconazole

53
Q

DI Azoles ( Inhibitors)

A

HIV Protease Inhib
PK boosters 9Cobicistat

Will inc lvl of Azole, more tox

Interact with all, least with fluconazole

54
Q

DI Azoles (Inducers)

A

Rifamycins
Carbamazepine
Phenobarbital
Efavirenz, Nevirapine, Rilpivirine

Will dec lvl of Azole, leading to potential failure

Interact with all, least with fluconazole

55
Q

Ketoconazole MOA

A

Alters permeability of fungal cell wall, blocks CYP450 leading to build-up of toxic conc of hydrogen peroxide.
inhibits biosynthesis of phospholipids for cell membrane

56
Q

Ketoconazole Spectrum of Activity

A

Not recommended, Systemic - No go = yeasts
Oral Salvage ONLY = Endemic Mold
Topical ONLY = Dermatophytes

57
Q

Ketoconazole ADE

A

Hepatotoxicty

Liver function tests: AST, ALT, Alk Phos

58
Q

Ketoconazole used topically for…

A

nail fungus or seborrheic dermatitis

59
Q

Ketoconazole PO only as….

A

alternative for endemic fungi

Blastomycosis
coccidioidomycosis
histoplasmosis
paracoccidioidomycosis

60
Q

Ketoconazole Severe Adverse effects

A

oral tab

potentially fatal liver injury and risk of DI + adrenal gland problems

61
Q

Echinocandins

A

Caspofungin
Micafungin
Anidulafungin

62
Q

Echinocandins MOA

A

Bind to (1,3)-B-D-glucan synthase preventing cell wall synthesis ultimately leading to cell lysis

63
Q

Anidulfungin has Activity for….

A

Candida albicans
Candida glabrata
Candida Krusei

Candida parapsilopsis = +/-

64
Q

Caspofungin has activity for…

A

Candida albicans
Candida glabrata
Candida Krusei

Candida parapsilopsis = +/-
Aspergillus fumigateurs = +/-

65
Q

Micafungin has activity for…

A

Candida albicans
Candida glabrata
Candida Krusei

Candida parapsilopsis = +/-

66
Q

Caspofungin Dose adjustment

A

Dec by 1/2 for Hepatotoxicity

None for renal issues

67
Q

Micafungin Dose adjustment

A

none

68
Q

Anidulagungin Dose adjustment

A

none

69
Q

Echinocandin with most ADE

A

Caspofungin > Micafungin > Anidulafungin

70
Q

DI Caspofungin

A

Rifampin, efavirenz, phenytoin, carbamazepine = dc lvls of caspo

Tacrolimus = dc lvl of taco

cyclosporine = inc lvl of caspo

71
Q

DI Micafungin

A

Sirolimus + nifedipine = inc lvls of each

72
Q

DI Anidulafungin

A

Cyclosporine = inc lvls of Anid, no dose adjust tho

73
Q

Terbinafine MOA

A

inhibits squalene epoxidase- decrease sterol formation

early stage

74
Q

Terbinafine indications

A

Topical superficial fungal infections

Oral use for onychomycosis

75
Q

Terbinafine ADE

A

Cholestatic Hepatitis

** Onychomycosis, DONT use in pt with chronic or active liver disease **

76
Q

Griseofulvin MOA

A

Inhibits fungal mitosis

Causes production of defective DNA which cannot replicate

77
Q

Griseofulvin Indications

A

Treatment of ring worm infections of skin, hair and nails

78
Q

Griseofulvin DI

A

Disulfiram reaction w/ alcohol

Decreased effect of oral contraceptives

Decrease warfarin effectiveness

79
Q

Terbinafine Elim

A

Liver metabolism and 70% in urine

80
Q

Griseofulvin Elim

A

liver metabolism + urine mostly metabolites

81
Q

Ibrexafungerp MOA

A

inhibits (1,3)-B-D-glucan synthase but at different site than echinocandins

82
Q

Ibrexafungerp Spectrum of activity

A

Bunch of Candida, including multiple azole-resistant and echinocandin-resistant including C auras + Aspergillus

No activity against Mucor + Fusarium

83
Q

Ibrexafungerpy approved for…

A

Vulvovaginal candidiasis

** high fat meal inc bioavailability **

84
Q

Ibrexafungerp ADE

A

GiI = D, Ab pain, N, V

CNS: Headache, dizziness,fatigue

85
Q

D-Cateslytin Activity

A

In vitro activity against Candida albicans only

Topical only currently

Synergy w/ Voriconazole, isavuconazole, Amphotericin

86
Q

APX001A activity

A

in Vitor against Candida, including….

Auris
Cryptococcus
Aspergillus
Scedosporium
Fusarium
Mucor
Coccidiomycosis

Synergy w/ Fluconazole

Anti-Infectives Exam 3 (7 decks)

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