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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
5- Flucytosine (5-FC) Toxicity lvls
peak 50-100mcg/mL
26
Triazole Antifungals
``` Ketoconazole Fluconazole Itraconazole Voriconazole Posaconazole Isavuconazonium (pro-drug) ```
27
Triazole Antifungal MOA
Inhibit fungal 14-alpha demethylase-blocking ergosterol synthesis Leads to dysfunctional fungal membrane synthesis
28
Fluconazole Spectrum of Activity
``` Candida albicans = + Candida glabrata = +/- Candida Krusei** = -- Aspergillus fumigateurs** = -- Cryptococcus neofromans= ++ Resistant mold Rhizomes Mucor** = -- ```
29
Itraconazole Spectrum of activity
``` Candida albicans = + Candida glabrata = +/- Candida Krusei = +/- (small bump over fluc) Aspergillus fumigateurs** = + Cryptococcus neofromans = + Resistant mold Rhizomes Mucor** = -- ```
30
Voriconazole Spectrum of Activity
``` Candida albicans = + Candida glabrata = + Candida Krusei = +/- Aspergillus fumigateurs** = ++ Cryptococcus neofromans = + Resistant mold Rhizomes Mucor** = -- ```
31
Posaconazole Spectrum of Activity
``` Candida albicans = + Candida glabrata = + Candida Krusei = + Aspergillus fumigateurs = + Cryptococcus neofromans = + Resistant mold Rhizomes Mucor** = ++ ```
32
Isavuconazole Spectrum of Activity
``` Candida albicans = + Candida glabrata = + Candida Krusei = + Aspergillus fumigateurs = + Cryptococcus neofromans = + Resistant mold Rhizomes Mucor = + ```
33
Which Tripazole has most Bioavial?
Fluconazole = ~ 100%, 80% Renal Elim unchanged
34
Fluconazole Dose Adjustments
Req dose adjustment Reduce maintenance doses 50% for CrCl < 50mL/min
35
Fluconazole ADE + Monitoring Paramaters
Hepatotoxicity Monitor AST,ALT, Alk phos * * torsades de pointes ** * * EKG (Prolonged QT Interval) **
36
Itraconazole - Oral Spectrum of Activity
``` Candida albicans Cryptococcus neoformans Aspergillus spp histoplasmosis Blastomycosis Tines unguium (nail fungus) ```
37
Itraconazole admin recommendations
Take with an acidic beverage with drugs reducing gastric acidity anything changing pH in Gut can cause issues
38
Itraconazole Bioavail
Difference between capsules and suspensions
39
Itraconazole ADE
**Hepatotoxicity ** ** Ventricular dysfunction, CI in pts with CHF ** Hypersensitivity Nause Headache Breast tenderness - gynecomastia
40
2nd Gen Triazoles
Voriconazole Posaconazole Isavuconazonium-isavuconazole Ravuconazole - investigational Albaconazole - investigational
41
Voriconazole Spectrum of Activity
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
Dose adjustments req for Voriconazole
Requires Hepatic Dose adjustment Load dose to reach Steady State
43
Notable ADE of Voriconazole
CNS: Hallucinations, agitation, anxiety, delirium Hypersensitivity: Rash & phytotoxicity
44
Posaconazole Spectrum of Activity
Candida - including some fluconazole resistant Aspergillus spp. Resistant mold including Mucor, Rhizopus, Scedosporium, Fusarium
45
Posaconazole Dosing Adjustments
Suspension has erratic absorption, consider alternative dosing in pts with extreme weights Distinc differences between oral suspension & oral delated release tabs/IV
46
Posaconazole ADE + Monitoring
Hepatotoxicity = AST/ALT, Alk Phos torsades de pointes, prolonged QT interval Hypersensitivity = rash + phototoxicity No CNS
47
Isavuconazonium-Isavuconazole Spectrum of Activity
Candida - including some fluconazole resistant Aspergillus spp. Resistant mold including Mucor, Scedosporium, Fusarium
48
Isavuconazonium-Isavuconazole Dose adjustments
IV:PO is 1:1 ratio Hepatic: no adjustment for Child-Pugh score A/B Renal: no adjustment for insufficiency, including ESRD
49
Isavuconazonium-Isavuconazole notable ADE
** Shortens QT, unlike others which prolong ***
50
DI Itraconazole
H2 antagonist PPI Mg, Al, Ca antacid (space 1hr before, 2hrs after) or drink coca-cola or OJ
51
Triazole w/ most CYP interactions
Ketoconazole
52
Triazole w/ least CYP interactions
Fluconazole
53
DI Azoles ( Inhibitors)
HIV Protease Inhib PK boosters 9Cobicistat Will inc lvl of Azole, more tox Interact with all, least with fluconazole
54
DI Azoles (Inducers)
Rifamycins Carbamazepine Phenobarbital Efavirenz, Nevirapine, Rilpivirine Will dec lvl of Azole, leading to potential failure Interact with all, least with fluconazole
55
Ketoconazole MOA
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
Ketoconazole Spectrum of Activity
Not recommended, Systemic - No go = yeasts Oral Salvage ONLY = Endemic Mold Topical ONLY = Dermatophytes
57
Ketoconazole ADE
Hepatotoxicty | Liver function tests: AST, ALT, Alk Phos
58
Ketoconazole used topically for...
nail fungus or seborrheic dermatitis
59
Ketoconazole PO only as....
alternative for endemic fungi Blastomycosis coccidioidomycosis histoplasmosis paracoccidioidomycosis
60
Ketoconazole Severe Adverse effects
oral tab potentially fatal liver injury and risk of DI + adrenal gland problems
61
Echinocandins
Caspofungin Micafungin Anidulafungin
62
Echinocandins MOA
Bind to (1,3)-B-D-glucan synthase preventing cell wall synthesis ultimately leading to cell lysis
63
Anidulfungin has Activity for....
Candida albicans Candida glabrata Candida Krusei Candida parapsilopsis = +/-
64
Caspofungin has activity for...
Candida albicans Candida glabrata Candida Krusei Candida parapsilopsis = +/- Aspergillus fumigateurs = +/-
65
Micafungin has activity for...
Candida albicans Candida glabrata Candida Krusei Candida parapsilopsis = +/-
66
Caspofungin Dose adjustment
Dec by 1/2 for Hepatotoxicity None for renal issues
67
Micafungin Dose adjustment
none
68
Anidulagungin Dose adjustment
none
69
Echinocandin with most ADE
Caspofungin > Micafungin > Anidulafungin
70
DI Caspofungin
Rifampin, efavirenz, phenytoin, carbamazepine = dc lvls of caspo Tacrolimus = dc lvl of taco cyclosporine = inc lvl of caspo
71
DI Micafungin
Sirolimus + nifedipine = inc lvls of each
72
DI Anidulafungin
Cyclosporine = inc lvls of Anid, no dose adjust tho
73
Terbinafine MOA
inhibits squalene epoxidase- decrease sterol formation early stage
74
Terbinafine indications
Topical superficial fungal infections Oral use for onychomycosis
75
Terbinafine ADE
Cholestatic Hepatitis ** Onychomycosis, DONT use in pt with chronic or active liver disease **
76
Griseofulvin MOA
Inhibits fungal mitosis Causes production of defective DNA which cannot replicate
77
Griseofulvin Indications
Treatment of ring worm infections of skin, hair and nails
78
Griseofulvin DI
Disulfiram reaction w/ alcohol Decreased effect of oral contraceptives Decrease warfarin effectiveness
79
Terbinafine Elim
Liver metabolism and 70% in urine
80
Griseofulvin Elim
liver metabolism + urine mostly metabolites
81
Ibrexafungerp MOA
inhibits (1,3)-B-D-glucan synthase but at different site than echinocandins
82
Ibrexafungerp Spectrum of activity
Bunch of Candida, including multiple azole-resistant and echinocandin-resistant including C auras + Aspergillus No activity against Mucor + Fusarium
83
Ibrexafungerpy approved for...
Vulvovaginal candidiasis ** high fat meal inc bioavailability **
84
Ibrexafungerp ADE
GiI = D, Ab pain, N, V CNS: Headache, dizziness,fatigue
85
D-Cateslytin Activity
In vitro activity against Candida albicans only Topical only currently Synergy w/ Voriconazole, isavuconazole, Amphotericin
86
APX001A activity
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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