Antifungal Drugs Flashcards
(26 cards)
Amphotericin B
- covers all medically important fungi
- given IV
- cause many SE
- can be given intrathecally
Itraconazole
- given orally
Less serious systemic infections antifungal agents
oral azole drugs i.e. ketoconazole, fluconazole, itraconazole,
tx superficial fungal infections
Griseofulvin, nystatin, azole (clotrimazole, miconazole)
Polyenes (for systemic fungal infections)
nystatin, amphotericin B
MOA of Polyenes
inhibit ergosterol synthesis - fungicidal, nephrotoxic
Griseofulvin microorganism from
penicuillium
- can be systemic/oral
binds to tubulin
MOA Polyenes
Hydrophobic interactions occur between the ergosterol present in fungal membranes and the polyene macrolides leading to enhanced membrane permeability and leakage of intracellular ions
Amphotericin B
Streptomyces nodosus
Nystatin
Streptomycin norsei
Polyenes toxicity caused by:
affinity for cholesterol
Solution for toxicity in Polyenes
Encapsulation of Liposomes in Amphotericin B
Too toxic Polyenes should be topical only
Nystatin
Azoles inhibit what enzyme that involves in ergosterol synthesis
CYP-459
Imidazoles
Ketoconazole
Miconazole
Clotrimazole
Triazoles
Fluconazole
Itraconazole
Voriconazole
Topical Fungal Infections
Clotrimazole
Miconazole
Systemic fungal infections agents, given orally
Ketoconazole
Fluconazole
Itraconazole
block fungal cell-wall synthesis
semisynthetic lipopeptides
produced by various species of fungi and inhibit synthesis of beta (1 - 3) D-glucan
Echinocandins
inhibitors of fungal protein synthesis by interfering with
the action of an enzyme called elongation factor 2.
- factor: unique to yeasts
- can be given IV or oral
Sordarins
inhibit the enzyme squalene epoxidase, which is involved in
the conversion of squalene to squalene epoxide, an
important step in the synthesis of ergosterol
- oral and topically in tx dermatophyte infections of the skin and nails
allylamines
highly lipophilic and keratophilic
- distribute in high conc. in the stratum corneum, sebum, hair, and nail matrix, persist for months
Allylamines
fungistatic antibiotic
- orally active
- accumulates in skin, hair, nails, fat, and skeletal muscles
- tx ringworm of skin, nails, and hair caused by dermatophyte fungi
Griseofulvin
MOA: disrupting the cell’s mitotic spindle, thus arresting the fungal cells in metaphase
+ affect microtubule structure
Griseofulvin
