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Antifungal Agents in Ophthalmology
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Antifungal Agents in Ophthalmology

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Fungal infections of eye cause one of the most dangerious infections. Accurate diagnosis and proper institution of anti-fungal therapy is essential. Here we discuss the various anti-fungal agents …

Fungal infections of eye cause one of the most dangerious infections. Accurate diagnosis and proper institution of anti-fungal therapy is essential. Here we discuss the various anti-fungal agents available to be used in ophthalmology.

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  • 1. Dr. Mrinmayee Ghatak Dept of Ophthalmology, K.I.M.S. Hospital, Bangalore (India) [email_address]
  • 2.  
  • 3. Polyenes
    • 1 st effective antifungals
    • Bind preferentially to ergosterol in the fungal plasma membrane > alters membrane permeability > disrupts the fungal cell
    • Use is restricted due to insolubility, irritation on application and instability
  • 4. Nystatin
    • 1 st polyene antibiotic in 1950
    • Derived from Streptomyces noursei
    • Affective against Candida infections
    • Topical ointment 100,000 IU, 4-5 times/day
    • Allergic hypersensitivity reactions
  • 5. Amphotericin B
    • Streptomyces nodosus
    • Insoluble in water, unstable at 37 degree
    • Degrades rapidly is exposed to light
    • Effective against Candida, Aspergillus, Cryptococcus, Coccidioides, Sporothrix, Blastomycosis, Histoplasma, Mucormycosis
    • Topical/s.c./intracameral/i.v.
    • Topical – 0.075%-0.3% hourly
    • S.c. 0.8-1.0mg 1-2 doses
    • i.v. 1-1.5mg/kg/day in 5% dextrose over 4 hrs with pretreatment with hydrosortisone
    • Adverse reactions: anaphylaxis, headache, nausea, vomoting, fever, nephrotoxicity
  • 6. Natamycin
    • Only antifungal commercially available for topical administration
    • Derived from Streptomyces natalenses
    • Most effective against filamentous fungi
    • Also for fusarium, aspergillus and most of other fungi
    • 5% topical suspension drops 4-6 times/day
    • Adverse reactions: irritation, burning, PEK, allergic reactions
  • 7. Imidazoles
    • 1 st imidazole was Clotrimazole
    • Inhibition of fungal ergosterol synthesis
    • Interference with mitochondrial oxidative and peroxisomal enzymes resulting in accumulation of lethal by-products
    • Affinity for fungal cytochrome P450
  • 8. Clotrimazole
    • Chlorinated trityl imidazole
    • Borad antifungal activity
    • Specially for aspergillus
    • Also for Candida, fusarium, penicillium, clasporium and actenomyces
    • 1% eye drops to be used hourly
    • Sckin cream 1% well tolerated by eye
    • Poorly soluble in water
    • Can not be given parenterally
    • Irritation, punctate keratopathy, hepatotoxicity, diarrhoea
  • 9. Miconazole
    • Phenethyl imidazole
    • Broad spectrum
    • Causes alteration in fungal cell wall > induces permeability changes
    • 1% Topical instilled every hourly
    • Sub conj 5-10mg every 48 hrs for 2-3 doses
    • Conjunctival injection, PEE, pruritus, erythema, local irritation
  • 10. Econazole
    • Dichlorimidazole
    • Broad spectrum
    • Low toxicity
    • Interference with membrane sterol formation
    • 1% ointment and drops 4-6times daily
    • Effective in only superficial infections of the eye
  • 11. Ketoconazole
    • Highly effective for treatment of keratomycosis
    • Inhibits ergosterol synthesis
    • More water soluble
    • Enhanced absorption capacity
    • Affective against Candida, Aspergillus, Fusarium
    • Oral: 200-800mg/24hrs single daily dose for a week
    • Topical 1-5% drops
    • Reactions: relatively safe, GIT upset, abnormal LFT, hypersensitivity
    • Reversible hepatotoxicity
    • Topical well tolerated
  • 12. Fluconazole
    • 1 st antifungal with good pharmacokinetic profile & relative low side effect
    • Water soluble
    • Exhibits low binding to proteins
    • Most effective against yeasts.
    • Also few dimorphic fungi
    • Most important application : systemic use in Candida endophthalmitis in combination with Amphotericin B
    • Oral 200-600mg/day for 3 weeks for candida and 10-12 weeks in cryptococcus infection
    • Topically 0.3% eye drop every 4hrly
  • 13. Voriconazole
    • Good bioavailability
    • Good tolerability
    • Good therapeutic concentrations
    • Completely inhibits ergosterol synthesis, more effectively than fluconazole
    • Commonly used for invasive systemic and ocular infections specially aspergillosis and candidiasis
    • 200-400mg BD with maintaininace with half dose
    • Transient visual disturbances, fever, rash, vomiting, headache, abdominal pain, rare but serous hepatotoxicity
  • 14.
    • Faster and deeper penetration
    • Highly effective in fungal keratitis with deep abscess
    • Outclasses all other antifungals
    • IV 100ug at conc of 1000ug/ml in candida endophthalmitis – non-toxic to retina
  • 15. Itraconazole
    • Well distributed in lipid-rich tissues
    • Lack of intravenous preparation
    • Primarily for aspergillus, histoplasma, blastomycosis, onychomycosis
    • Moderate for candida & fusarium
    • Orally 200mg BD for a week
    • Topically – to be freshely prepared
    • Subconj is safe
    • GI upset and hypersensitivity
  • 16. FLUCYTOSINE
    • Fluorinated pyrimidine
    • Effective against Candida, Cryptococcus, Aspergillus, Clasporium, Penicillium
    • Transported across fungal cell membrane by a specific permease
    • In cell it is deaminated to fluorouracil that blocks fungal thymidine synthesis
    • Orally 50-150mg/kg/day divided in 4 doses for a week
    • Topically 1% drops every hourly
    • Not used alone as poor penetration in certain fungal cell membranes
    • Topically causes irritation, itching, burning. Systemically causes nausea, vomiting, diarrhoea
  • 17. Caspofungin
    • Inhibits 1,3 beta glucan synthase
    • Disrupts the integrity of fungal cell wall
    • Administered IV
    • Effective for invasive aspergillosis, candidemia
    • Initial dose 70mg iv-infusion followed by 50mg iv daily
    • Relatively low incidence of side effects including GI disturbances, headache, fever, anemia, hypokalemia, tachycardia, hypersensitivity
  • 18. SILVER COMPOUNDS
    • Silver Sulphadiazine
    • Highly effective against Candida, Aspergillus, Fusarium
    • Topically well tolerated
    • Fungistatic
    • For both superficial and deep infections
    • 1% drops hourly
    • Local irritation, FB sensation, tching
  • 19. NEWER HORIZONS
    • TERBINAFINE (LAMISIL)
      • Allylamine
      • Broad spectrum, highly effective
      • Low toxicity, high cure rates
      • Primary fungicidal action even at low conc
      • Highly selective for single fungal enzyme
      • Highly lipophilic
      • Mycological cure achieved before clinical cure
      • 250mg/day for 2-4 weeks
      • Topical 1% ointment
      • Systemic side effect include GI upset, skin reactions, taste disturbances, liver dynfunction, blood disorders.
      • Topical may cause irritaiton, itching, redness
  • 20. Caspofungin
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