Pharmacology: Antifungals

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Fungal infection groupings

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1. Systemic mycoses
2. Subcutaneous mycoses
3. Superficial mycoses

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Systemic mycoses

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Include soft tissue infections, UTI, pneumonia, meningitis or septicemia; more likely to occur in immunocompromised patients

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Subcutaneous mycoses

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Caused by puncture wounds contaminated with soil funig

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Superficial mycoses

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- Infection of nail, skin and mucous membranes usually cause by dermatophytes or yeasts
- Dermatophytes include all tinea infections
- Yeasts include candida albicans

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Classification of antifungal drugs

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1. Polyene class
2. Azole derivatives
3. Allylamine drugs
4. Echinocandin class
5. Miscellaneous

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Amphotericin B

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- Fungizone
- In the polyene class of drugs
- Not absorbed PO
- Very broad spectrum
- Poor penetration into CNS, so not effective for cryptococcal meningitis
- ADRs - chills, fever, vomiting, renal and hepatic impairment, anemia, hypokalemia, hypotension, phlebitis
- High cost and difficult to administration; usually not first line drug and usually used in combination with other drugs

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Other polyenes

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1. Nystatin - available in topical form only; best medication for superficial candida
2. Natamycin - used in opthalmic suspensions for tx of fungal blepharitis, conjunctivitis or keratitis caused by Aspergillus and candida

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Azole derivatives

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- MOA - inhibits synthesis of fungal lipid ergosterol
- Active against a wide range of fungi
- Well absorbed PO
1. Clotrimazole
2. Econazole
3. Fluconazole
4. Ketoconazole

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Clotrimazole

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Effective for oral, topical or vaginal candidiases and come forms of tinea

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Econazole

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Used topically for tinea and candidal infections; can be used once daily

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Fluconazole

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- Used to treat candida and cryptococcal meningitis because it can cross the BBB
- Used for prophylaxis of fungal infections in patients undergoing BMT or solid organ transplant
- Can be given as single oral doe or recurrent vaginal dose

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Ketoconazole

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- Used for a variety of systemic fungal infections but does not enter CNS
- Has anti-adrenergic properties
- Requires acedic medium to be absorbed

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Other azoles

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1. Itraconazole
2. Miconazole
3. Posaconazole
4. Voriconazole

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Azole derivatives ADR's

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- The 2 most common ADRs of all systemic azoles are hepatotoxicity and GI effects
- Must monitor the patients liver function

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Azole derivatives DDI's

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- Inhibits CYP450 system - caution with drugs such as phenytoin, warfarin, hypoglycemics
- Decreased absorption of azoles (mainly ketoconazole and itraconazole) w/ drugs that decrease gastric acidity

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Allyamine class

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- MOA - inhibit ergosterol synthesis
1. Terbinafine - used to treat dermatophytoses (tinea); fungal nail infections usually require 6-12 weeks of PO therapy; ADRs include liver toxicity

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Echinocandin class

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- MOA - inhibit cell wall synthesis
- Very good activity against candida and aspergillus and not as broad
- ADRs include histamine-like reactions
1. Capsofungin
2. Micafungin
3. Anidulafungin

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Flucytosine

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- Pregnancy category X
- MOA - inhibits DNA synthesis as a result of its conversion to 5-FU
- Most often used in combination with amphotericin for treatment of systemic candida or cryptococcus
- Prolonged high dose may suppress bone marrow and cause alopecia

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Griseofulvin

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Treatment of choice for tinea capitis
- Must be taken with high fat food to maximize absorption
- Rarely used today because other agents are more effective and faster

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Tolnaftate

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Topical treatment for dermatophytosis - tinea

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Ciclopirox

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Topical treatment for nails