Antifungal Agents Flashcards
Amphotericin B
Fungizone
Amphotericin B MOA
Binds ergosterol of cell membrane, creates pores that leads to spilling of intracellular contents
Fungicidal.
Can bind human cholesterol component of mamillian cells
Amphotericin B Kinetics
Poor PO ABS
IV or topical
very slow excretion - T1/2 is 15 days
Amphotericin B uses
Broad spectrum - opportunistic and systemic.
Drug of choice for systemic fungal infections seen in immunocompromized patients
Amphotericin B ADR
Very toxic drug
Nephrotoxic majorly, also anemia
infusion related-toxicity - fever, chills, N/V…. pretreat with tylenol, benadryl or steroids
Nystatin
Mycostatin
Nystatin MOA
similar to Amphotericin B
Nystatin kinetics
Toxicity limits use to topical only
No absorption from GI tract
Nystatin uses
Treatment of topical candidal infections of skin, mucus membranes and GI tract
Triazoles
Fluconazole (Diflucan)
Itraconazole (Sporanox)
Terconazole (Terazole)
Triazole MOA
Highly selective inhibition of fungal cytochrome p450, reducing sterol use
Fungistatic
Triazole kinetics
Cleared mainly be renal excretion, renal dosing necessary in renal impaired patients
(Itraconazole mostly hepatic)
Fluconazole can enter CNS for tx of meningitis
Fluconazole use
Vaginal candidiasis, once failure of topical agents happens
Oropharyngeal and esophageal candidiasis
May be used for cryptococal meningitis because is able to get into CNS
Itraconazole use
Onychomycoses
Imidazoles
Ketoconazole (Nizoral) - systemic and topical
Clotrimazole (Lotrimin/Mycelex) - topical
Miconazole (Monistat) - topical
