Antifungal Drugs Flashcards
Amphotericin B
Polyene
Most effective drug for most systemic fungal infections
Drug of choice for treating life threatening mycoses
Natamycin (Pimaricin)
Polyene
Lipid formulation of amphotericin B
MOA of polyenes
Disrupt the cell membrane function
Adverse effect of Amphotericin B (Polyenes)
Low therapeutic index
Very careful monitoring
Side effects of Polyenes (Amphotericin B)
Nausea and vomiting
Fever, shaking, chills
Headache, malaise, anemia, anorexia
Polyenes (amphotericin B) in eye care
Ointment or soluction for topical fungal keratitis
Amphotericin B is the drug of choice to treat patients with fungal keratitis caused by Candida
Administer every 30min first 24hr then every hour for the next 24hr with a slow taper
Drug of choice for endopthalmitis
Intravitreal Amphotericin B
Need a compounding pharmacy
Natamycin in eye care
A polyene
The only commercially available topical opthalmic antifungal
effective against filamentous fungi particularly for infections caused by Fusarium
Pyrimidines MOA
ex: Flucytosine, “5-flurocytosine (5-FC)
Converted to 5-flurouacil (5-FU) and this inhibits DNA synthesis
Fungistatic
Used in combination amphotericin B
Flucytosine Adverse effects
Nausea, vomiting, headache, diarrhea, abdominal pain, skin rash
Abnormal liver function tests
Reversible neutropenia and dose related bone marrow derpession
Flucytosine in Eye care
A pyrimidine
Rarely used –> resistance
Monotherapy is ineffective
Two classes of Azoles?
Imidazoles: Limited to topical for cutanious infections
Triazoles: given systemically or topically for the treatment of cutaneous and systemic fungal infections
Characteristics of Triazoles
Given orally or topically
Fungistatic
Blocks the biosynthesis of ergostrol in the cell membrane by inhibiting the CYP450 enzyme (non-specific so also interferes with human CYP450 and others related
Fluconazole
a Triazole First one created Limited spectrum to yeast -no activity against mold Used as an oral treatment of mucocutaneous candidiasis
Adverse affects of Fluconazole
Nausea, vomiting, headache, diarrhea, abdominal pain , skin rash
Can cause hepatotoxicity