Fungal Endophthalmitis Medication

Updated: Sep 20, 2018
  • Author: Lihteh Wu, MD; Chief Editor: Hampton Roy, Sr, MD  more...
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Medication

Medication Summary

The best initial therapy for patients with endogenous fungal endophthalmitis has not been established. However, a broad-spectrum systemic antifungal agent, such as amphotericin B or fluconazole, is recommended as first-line therapy.

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Polyene antibiotics

Class Summary

They are classified based on the number of conjugated double bonds. Fungicidal agents bind to sterols in the cell membrane of susceptible fungi and change the permeability of the cell membrane, leading to leakage of cellular constituents and consequently cell death.

Amphotericin B (Amphocin, Fungizone)

Polyene antibiotic produced by a strain of Streptomyces nodosus; can be fungistatic or fungicidal. Binds to sterols, such as ergosterol, in the fungal cell membrane, causing intracellular components to leak with subsequent fungal cell death. Particularly active against Candida, Cryptococcus, and Aspergillus species.

An infectious disease specialist should be consulted regarding the appropriate protocol and dosage.

Several studies have shown poor intravitreal penetration when given systemically.

Special attention is required when making the dilutions and injecting in gas-filled eyes because it has a narrow therapeutic range and can cause retinal toxicity.

Subconjunctival injections of amphotericin B have no role in fungal ocular infections.

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Imidazoles

Class Summary

Bind to the fungal cell membrane and induce permeability changes that alter intracellular electrolyte levels, leading to fungal cell damage. These agents are fungistatic.

Fluconazole (Diflucan)

Fungistatic activity. Synthetic oral antifungal (broad-spectrum bistriazole) that selectively inhibits fungal cytochrome P-450 and sterol C-14 alpha-demethylation, which prevents conversion of lanosterol to ergosterol, thereby disrupting cellular membranes. Effective against Candida, Cryptococcus, and Aspergillus species. Bioavailability following oral administration is comparable to parenteral administration. Good CSF and intravitreal penetration is achieved after systemic administration.

Ketoconazole (Nizoral)

Fungistatic activity. Imidazole broad-spectrum antifungal agent; inhibits synthesis of ergosterol, causing cellular components to leak, resulting in fungal cell death. Active against Blastomyces dermatitidis, C immitis, and Candida and Fusarium species, and exhibits some activity against Aspergillus species.

Itraconazole (Sporanox)

Fungistatic activity. Synthetic triazole antifungal agent that slows fungal cell growth by inhibiting cytochrome P-450–dependent synthesis of ergosterol, a vital component of fungal cell membranes.

Miconazole (Absorbine, Femizol)

Damages fungal cell wall membrane by inhibiting biosynthesis of ergosterol. Membrane permeability is increased, causing nutrients to leak out, resulting in fungal cell death.

The lotion is preferred in intertriginous areas. If the cream is used, apply sparingly to avoid maceration effects.

Administered intravenously due to poor absorption from the gastrointestinal tract.

Used as a second-line drug in the treatment of Candida, Cryptococcus, and Aspergillus species and coccidioidomycosis.

Use in cases that are resistant to treatment with amphotericin B.

Voriconazole (Vfend)

Used for primary treatment of invasive aspergillosis and salvage treatment of Fusarium species or Scedosporium apiospermum infections. A triazole antifungal agent that inhibits fungal cytochrome P-450-mediated 14 alpha-lanosterol demethylation, which is essential in fungal ergosterol biosynthesis.

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Corticosteroids

Class Summary

Some have advocated the use of intravitreal dexamethasone as an adjuvant. Inflammation is believed to play a role in the destructive nature of this disease.

Dexamethasone (Ocu-Dex)

For various allergic and inflammatory diseases. Decreases inflammation by suppressing migration of polymorphonuclear leukocytes and reducing capillary permeability.

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Chemotherapeutic agents

Class Summary

Inhibit cell growth and proliferation.

Flucytosine (Ancobon)

Converted to fluorouracil after penetrating fungal cells. Inhibits RNA and protein synthesis. Active against Candida and Cryptococcus species and generally used in combination with amphotericin B.

A fluorinated pyrimidine that becomes deaminated by susceptible fungi to fluorouracil, which blocks thymidine synthesis.

Effective against Candida and Cryptococcus species and certain strains of Aspergillus species.

Use in combination with another agent because acquired resistance develops frequently when flucytosine is administered alone.

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Echinocandins

Class Summary

Inhibit cell wall synthesis.

Caspofungin (Cancidas)

Used to treat refractory invasive aspergillosis. First of a new class of antifungal drugs (glucan synthesis inhibitors). Inhibits synthesis of beta-(1,3)-D-glucan, an essential component of fungal cell wall.

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