Tuesday 20 January 2015

ANTI FUNGAL DRUGS: MUST KNOW POINTS




* Most antifungal agents interfere with fungal cell wall synthesis and are fungistatic.

Here are few important points and dosages of important antifungal agents classwise:

1. Polyenes

NATAMYCIN

  • Broad spectrum
  • 5% topical suspension
AMPHOTERICIN B
  • Highly effective against yeast.
  • Topical 0.15%
  • Subconjunctival 0.5-1 mg
  • Intracameral 7.5 -10 micrograms/0.1 ml
  • Intravitreal 5 micrograms/0.1 ml
Natamycin and Amphotericin B are not preferred for subconjunctival administration baecause of significant toxicity.

2. Triazoles

FLUCONAZOLE
  • Most effective against Yeast.
  • oral dose 400mg/day upto 4-6 weeks
  • Topical 0.2%
  • Subconjunctival 1-2mg. 
ITRACONAZOLE
  • Supposed to have good corneal permeability and aqueous levels.
  • Oral 200 mg/day.
  • Topical 1%
  • Subconjuntival 100mg twicw daily injection.
VORICONAZOLE
  • Broad spectrum
  • Topical 1%
  • Subconjunctival 10 mg.
  • Oral 100mg/day. 98% bioavailability with peak action in 2-3 hours.
3. Imidazoles
  • This group of drugs have poor corneal penetration.
  • Useful in superficial infections.
 KETOCONAZOLE
  • Oral 200-400mg/day.
  • topical 5% (oil based).
MICONAZOLE
  • Topical 1% suspension
  • Subconjunctival 5-10 mg.
CLOTRIMAZOLE
  • Topical 1%.
4. Pyrimidines

FLUCYTOSINE
  • Rapid resistance.
  • Effective against Candida sp.
  • Oral 50-150 mg/kg/day.
  • Topical 2%. 
NEWER ANTIFUNGAL AGENTS
  • Ravuconazole : Triazole, oral, effective against Candida and Aspergillus.
  • PosaconazoleTriazole, oral, effective against Candida and Aspergillus.
  • Caspofungin: Echinocandin group. Effective against Candida (fungicidal) with some activity against Aspergillus.
  • Micofungin: Echinocandin group. Effective against Candida (fungicidal). Available for oral and subconjunctival administration.
  • Echinocandins are the safest antifungals available with lowest hepatic and renal toxicity profiles.
INDICATIONS OF ORAL ANTIFUNGAL THERAPY:
  • Large ulcer >6mm.
  • Severe deep keratitis (endothelial plaque, AC penetration)
  • Scleritis
  • Post penetrating keratoplasty
  • Endophthalmitis
  • Diabetes Mellitus
  • Immunocompromised
Liver function profiles should be repeated every 15 days in patients taking oral antifungals.




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