ANTI FUNGAL DRUGS

Pharm. Ezekiel Efeobhokhan

CLASSES
Antifungal, or antimycotic, drugs are used to treat fungal infections.
They include:

• polyenes
• flucytosine
• ketoconazole
• synthetic triazoles
• glucan synthesis inhibitors
POLYENES
• The polyenes include amphotericin B and nystatin. The potency of
amphotericin B has made it the most widely used antifungal drug for
severe systemic fungal infections.
• Nystatin is used only topically or orally to treat local fungal infections
because it’s extremely toxic when administered parenterally.
GRISEOFULVIN
Griseofulvin is used to treat fungal infections of the:
• • skin (tinea corporis)
• • feet (tinea pedis)
• • groin (tinea cruris)
• • beard area of the face and neck (tinea barbae)
MICONAZOLE
• Available as miconazole or miconazole nitrate, this imidazole
derivative is used to treat local fungal infections, such as vaginal and
vulvar candidiasis, and topical fungal infections such as chronic
candidiasis of the skin and mucous membranes.
CLOTRIMAZOLE
An imidazole derivative, clotrimazole is used:
• topically to treat dermatophyte and Candida albicans infections
• orally to treat oral candidiasis
• vaginally to treat vaginal candidiasis
FLUCYTOSINE
• Flucytosine, a fluorinated pyrimidine analogue, is the only
antimetabolite (a substance that closely resembles one required for
normal physiologic functioning and that exerts its effect by interfering
with metabolism) that acts as an antifungal.
• Flucytosine is a purine and pyrimidine inhibitor.
GLUCAN SYNTHESIS INHIBITORS
• Caspofungin acetate is a drug in a class known as glucan synthesis
inhibitors (also known as echinocandins).
• Caspofungin is primarily used when other antifungal therapies
haven’t been successful
SYNTHETIC TRIAZOLES
• The synthetic triazoles include fluconazole, itraconazole, and
voriconazole
KETOCONAZOLE
• Ketoconazole, a synthetic imidazole derivative, is an effective oral
antifungal drug with a broad spectrum of activity
Mechanism of Action
• Within the fungal cells, ketoconazole interferes with sterol synthesis,
damaging the cell membrane and increasing its permeability. This leads
to a loss of essential intracellular elements and inhibition of cell growth.

• Ketoconazole usually produces fungistatic effects but can also produce

fungicidal effects under certain conditions.

• When given orally, ketoconazole is absorbed variably and distributed

widely. It undergoes extensive liver metabolism and is excreted in bile
and feces.
Uses
• Ketoconazole is used to treat topical and systemic infections caused by
susceptible fungi, which include dermatophytes and most other fungi.

Adult Dose
• 200mg once daily
• Children older than 2 years. 3.3 to 6.6 milligrams (mg) per kilogram
(kg) of body weight per day.
Nursing Consideration
• Because of the risk of serious hepatotoxicity, the drug shouldn’t be
used for less serious conditions, such as fungal infections of the skin or
nails.

• To minimize nausea, divide the daily amount into two doses and give
the drug with meals.

• Monitor the patient’s hydration status if adverse GI reactions occur.

Adverse reactions
The most common adverse reactions to ketoconazole are
• nausea and vomiting.

Less frequent reactions include:

• anaphylaxis • joint pain • chills • fever • tinnitus • impotence •
photophobia • hepatotoxicity (rare; reversible when the drug is stopped).