Antifungal Agents Flashcards
For many years _____ drug was the only efficacious antifungal drug available for systemic use
Amphotericin B
Azole drugs comes with what formations?
Oral and parenteral
The only available route of administration of echinocandins
Parenteral administration
___ drugs are antifungal antibiotics produced by streptomyces nodosus
Amphotericin A and B
Amphotericin A is not in clinical use
___ is an amphoteric polyene macrolide.
Amphotericin B
Is effective only on fungi within the lumen of the tract an cannot be used for treatment of systemic disease
Oral amphotericin B
___ is a cell membrane sterol, is found in the cell membrane of fungi
Ergosterol
The predominant sterol of bacteria and human cell is?
Cholesterol
In what sterol does amphoericin B binds to?
Ergosterol
MOA of the drug:
Binds to ergosterol and alters the permeability of the cell by forming amphotericin B-associated pores in the cell membrane. The pore allows the leakage of intracellular ions and macromolecules, eventually leading to cell death
Amphotericin B
A drug that remains as the anti fungal agent with the broadcast spectrum of action. Has activity against candida albicans, cryptococcus neoformans, pathogenic molds.
Amphotericin B
A drug that remains a useful agent for all nearly life-threatening mycotic infections
Amphotericin B
Topical drops as well as direct subconjunctival injection of amphotericin B can cure?
Mycotic corneal ulcer and keratitis
Two broadcast categories of toxicity in amphotericin B
Infusion-related toxicity
- nearly universal and consists of fever, chills, muscle spasms, vomiting, headache
Cumulative toxicity
- renal damage, most significant toxic reaction
A potent antifungal agent that was discovered in 1957 during a search for novel antineoplastc agents. Its spectrum of action is much NARROWER that that of amphotericin B
Flucytosine
ROA of flucytosine
Only in oral formulation
MOA
Taken up by fungal cells via the enzyme cytosine permease. It is converted intracellularly first to 5-FU and then to 5-fluorodeoxyuridine monophosphate and fluoridine triphosphate, which inhibit DNA and RNA synthesis
Flucytosine
Enzyme that takes up flucytosine
Fungal cells via enzyme cytosine permease.
Conversion of flucytosine
- 5-fluroacil
- 5-fluorodeoxyuridine monophosphate (FdUMP)
- Fluorouridine triphosphate
Spectrum of activity of ____ is restricted to C neoformans and some candida sp
Flucytosine
Bone marrow toxicity, with anemia, leukopenia and thrombocytopenia
What drug has this kinds of common adverse effect?
Flucytosine
Are systemic compounds that can be classified as either imidazole or triazoles according to the number of nitrogen atoms in the five-membered azole ring
Azoles
Examples of imidazole
Ketoconazole
Miconazole
Clotrimazole