Antifungal drugs Flashcards
What are the pharmacokinetics of Amphoterecin B?
IV, topical, oral and intrathecal admin
**Broad spectrum of action including aspergillus, blastomyces, candida, coccidiodes, cryptococcus, histoplasma
What is the MOA of Amphoterecin B?
Selectively bind fungal ergosterol-> form polyene associated pores in cells membrane -> leakage of intracellular ions and macromolecules
What are the main uses of Amphoterecin B?
- used in all life threatening mycoses
- disseminated infections
- fungal pneumonia and cryptococcal menigitis
- mycoses are rapidly progressing in IC patients
What are the AE of Amphoterecin B?
nephrotoxicity- K+ supplements and normal saline infusions req
What is the MOA of Nystatin?
Selectively bind fungal ergosterol-> form polyene associated pores in cells membrane -> leakage of intracellular ions and macromolecules
What is the pharmacokinetics of flucytosine?
water soluble, oral/IV admin, renal excretions
What is the MOA of flucytosine?
taken up into fungal cells via membrane bound cytosine perm ease -> converted into 5FU will inhibit either DNA synthesis or RNA synthesis
What are the clinical uses of Flucytosine?
Current use is confined to combination therapy
-deep candidal infections, cryptococcal meningitis and chromoblastomycosis
What are the adverse effects of flucytosine?
arise from 5FC metabolism by intestinal flora to toxic antineoplastic 5FU
** black box warning regarding renal impairment
What is the MOA of Fluconazole, Itraconazole, and miconazole?
Inhibition of fungal ergosterol biosynthesis
What are the clinical uses of itraconazole?
scalp ringworm, jock itch, athletes foot
What are the clinical uses of ketoconazole?
tinea versicolor, seborrheic dermatitis
What are the clinical uses of Fluconazole?
candida infections!
What is the MOA of anidulafungin, caspofungin and micafungin?
Resistance?
noncompetitive inhibition of fungal B (1-3) D glucan synthase-> fungicidal effect
***resistance from mutations in FKS1
What are the uses for anidulafungin?
invasive candidiasis, esophageal candidiasis, candidemia
What are the uses for caspofungin?
disseminated and mucocutaneous candidiasis and for invasive aspergillosis
Whata re the uses for micafungin?
prophylaxis for candida infections in BM transplants
What is the MOA of Griseofulvin?
inhibits fungal mitosis (disrupts mitotic spindle by interacting with polymerized microtubules)
**fungistatic
What are the clinical uses Griseofulvin?
Dermatophyte infections of skin, hair and nails
What are the AE of griseofulvin?
hypersensitivity and rash!
What are the pharmacokinetics of griseofulvin?
oral and is distributed in heratinized tissues
What are the pharmacokinetics of terbinafine?
oral and topical
-distributed in keratinized tissue and fat
What is the MOA of Terbinafine?
inhibits ergosterol synthesis by inhibiting squalene epoxidase -> accumulation of squalene is toxic to fungi
*** fungicidal
What are the clinical uses for terbinafine?
fungal infections of skin, hair and nails.
onychomycosis - tinea cruris and tinea corporis
