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Mechanisms of Action OF Antifungal Agents

This document outlines the mechanisms of action of various classes of antifungal agents. It discusses how polyene antibiotics like amphotericin B insert into fungal cell membranes to form pores, altering permeability and killing cells. It describes how azoles like fluconazole and ketoconazole inhibit ergosterol synthesis in fungal membranes. And it explains that echinocandins inhibit glucan synthesis in fungal cell walls, disrupting the integrity of the wall.

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33 views5 pages

Mechanisms of Action OF Antifungal Agents

This document outlines the mechanisms of action of various classes of antifungal agents. It discusses how polyene antibiotics like amphotericin B insert into fungal cell membranes to form pores, altering permeability and killing cells. It describes how azoles like fluconazole and ketoconazole inhibit ergosterol synthesis in fungal membranes. And it explains that echinocandins inhibit glucan synthesis in fungal cell walls, disrupting the integrity of the wall.

Uploaded by

shaitabligan
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PPTX, PDF, TXT or read online on Scribd
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MECHANISMS OF ACTION

OF
ANTIFUNGAL AGENTS

An antifungal agent is a drug that


selectively eliminates fungal pathogens
from a host with minimal toxicity to the
host.
1. Polyene antibiotics
• A. Amphotericin B
• - is prototype of polyene antibiotics and have high affinity for
ergosterol present in fungal cell membrane.
• - It then gets combined with the membrane and get inserted into the
membrane and several molecules together orient themselves in
such a way as to form the micropore.
• - The hydrophilic side forms the interior of the pore through which
ions, amino acids and other water soluble substances move out.
• - The cell permeability is markedly increased and due to this the cell
death occurs.

• B. Nystatin
• This alters permeability & transport as a result, cell death occurs.
2. Heterocyclic benzofuran Griseofulvin
• - It is active against most dermatophytes including epidermophyton,
trichophyton , microsporum but not against Candida and other fungi
causing mycosis.
• - It is fungistatic in nature. And does not inhibit polymerization of
tubulin but somehow disorients the microtubules.
3. Echinocandins
• - Echinocandins interfere with the synthesis of the fungal cell wall.
• - It is Glucan synthesis inhibitor.
• It inhibits 1,3- beta glucan synthase, an enzyme important in fungal
cell wall synthesis and subsequently inhibit the synthesis of beta
glucan in the fungal cell wall.
• Disruption of the fungal cell wall leads to cellular osmotic instability
and cell death.
4. Azoles
• - The azole antifungal drugs act by inhibiting the synthesis of the sterol
components of the fungal membrane.
• - They inhibit C-14 α-demethylase (a cytochrome P450 [CYP450]
enzyme), thereby blocking the demethylation of lanosterol to ergosterol,
the principal sterol of fungal membranes.
• - This inhibition disrupts membrane structure and function, which then
inhibits fungal cell growth.
Azoles are primarily divided into two groups: imidazoles and triazoles.
• - Clotrimazole, Econazole, Miconazole, Ketoconazole fall under
imidazoles group and Fluconazole, Itraconazole, Posaconazole and
Voriconazole fall under triazoles group
• - They impair ergosterol synthesis leading to cascade of membrane
abnormalities in the fungus.
Nursing considerations
Fluconazole
• Monitor allergic response and hepatic toxicity S and S.
Ketoconazole
• TAKE ORAL DRUG WITH MEALS TO LOWER GI UPSET
• Avoid sunlight exposure
• Don't take antacids
Amphotericin B
• Monitor labs. ESPECIALLY POTASSIUM
• Monitor weight.
• Monitor urine appearance
• Report vertigo, tinnitus or unsteady gait.
Infusion pump
• close monitoring for 1 hr for chills, fever, N/V, headache

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