12. ANTIFUNGAL ANTIBIOTICS

Fungal infections range from mild skin infections to serious systemic diseases, especially in patients with weak immunity. Antifungal antibiotics are medicines used to treat these infections. They act by damaging fungal cell membranes, blocking cell wall synthesis, or interfering with fungal metabolism. Unlike bacteria, fungi are eukaryotic organisms, so antifungal drugs need to be more selective to avoid harming human cells.


Classification of Antifungal Antibiotics

Antifungal agents are broadly classified into:

  • Polyenes
  • Azoles
  • Echinocandins
  • Allylamines
  • Other antifungal agents

POLYENES

Polyenes are powerful antifungal antibiotics that act by binding to ergosterol, a key lipid in fungal cell membranes. This creates pores, leading to leakage of cell contents and fungal death.

1. Amphotericin B

Known as the “ampho-terrible” because of its toxicity but remains the drug of choice for many life-threatening fungal infections.

Uses

  • Systemic fungal infections such as cryptococcosis, histoplasmosis, mucormycosis, and aspergillosis
  • Visceral leishmaniasis

Adverse Effects

  • Fever, chills
  • Kidney damage (major concern)
  • Low potassium and magnesium levels
  • Inflammation at injection site

2. Nystatin

Nystatin is used only for local fungal infections because it is not absorbed from the skin or gut.

Uses

  • Oral candidiasis (thrush)
  • Vaginal candidiasis
  • Skin fungal infections

AZOLES

Azoles inhibit fungal sterol synthesis by blocking the enzyme required to make ergosterol. They are divided into:

  • Imidazoles: ketoconazole, miconazole, clotrimazole
  • Triazoles: fluconazole, itraconazole, voriconazole, posaconazole

Uses

  • Superficial infections (clotrimazole, miconazole)
  • Systemic infections (fluconazole, itraconazole)
  • Cryptococcal meningitis (fluconazole)
  • Aspergillosis (voriconazole)

Side Effects

  • Nausea, vomiting
  • Liver toxicity
  • Hormonal disturbances (ketoconazole)
  • Drug interactions due to CYP450 inhibition

ECHINOCANDINS

Echinocandins inhibit beta-glucan synthesis in fungal cell walls, making them highly effective against Candida and Aspergillus.

Common Drugs

  • Caspofungin
  • Micafungin
  • Anidulafungin

Uses

  • Invasive candidiasis
  • Aspergillosis (when other drugs fail)

Side Effects

  • Fever
  • Rash
  • Mild liver enzyme elevation

ALLYLAMINES

Allylamines block squalene epoxidase, an enzyme needed for ergosterol synthesis.

Common Drugs

  • Terbinafine

Uses

  • Fungal nail infections
  • Skin infections like ringworm

Side Effects

  • GI upset
  • Liver problems

OTHER ANTIFUNGAL AGENTS

1. Flucytosine

Converted into 5-FU inside fungal cells, inhibiting DNA synthesis.

  • Mainly used with amphotericin B

2. Griseofulvin

Used for skin, hair, and nail infections caused by dermatophytes.

3. Tolnaftate

Used topically for ringworm and athlete’s foot.


Superficial vs Systemic Fungal Infections

  • Superficial infections: treated with topical drugs like clotrimazole, miconazole, nystatin
  • Systemic infections: treated with amphotericin B, fluconazole, itraconazole, echinocandins

Detailed Notes:

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