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Antifungal Agents
N/A
30
Pharmacology
Graduate
03/02/2010

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Cards

Term
Mechanism of Polyene antimycotics?
Definition
Bind to ergosterol and poke holes in the membrane
Term
Which are the polyene antimycotics?
Definition
Nystatin, Amphotericin B, Natamycin
Term
Which polyene is used in the eye?
Definition
Natamycin
Term
Which antimycotics are used topically?
Definition
Polyene antimycotics (Nystatin, Amphotericin B, Natamycin), Tolnaftate, Ciclopirox, Terbinafine, Imidazoles (Miconazole, Clotrimazole)
Term
Which antimycotics are used topically for ringworm?
Definition
Tolnaftate, Ciclopirox, Terbinafine, Miconazole, other "-azoles"
Term
Which antimycotic agents are used for candida?
Definition
Miconazole and other "-azols"
Term
Which antimycotics are given systemically for skin infections (mainly nail)?
Definition
Griseofulvin and Terbinafine
Term
What is the mechanism of Griseofulvin?
Definition
Binds to microtubules and inhibits mitosis
Term
Is Griseofulvin fungistatic or fungicidal?
Definition
Fungistatic
Term
What are the side effects of Griseofulvin?
Definition
Headache, photosensitive, induces P450, cross-reacts for PCN allergy
Term
What is the mechanism of Terbinafine?
Definition
Inhibits ergosterol synthesis and causes a buildup of toxic squalene by inhibiting squalene epoxidase, which is necessary to convert squalene to squalene 2,3 oxide
Term
What are the side effects of Terbinafine?
Definition
Liver damage, inhibits P450
Term
Which antimycotics are used for systemic infections?
Definition
Amphotericin B, Triazoles (Fluconazole, Itraconazole, Voriconazole), Imidazoles (ketoconazole), Flucytosine, Echinocandins
Term
What is the mechanism of Amphotericin B?
Definition
Forms pores in ergosterol-containing membranes
Term
Is Amphotericin B fungistatic or fungicidal?
Definition
Fungicidal
Term
How is Amphotericin B adminstered, and why?
Definition
IV for 2-4 months; it is insoluble in water
Term
What are the side effects of Amphotericin B?
Definition
Impaired (irreversible) renal function in 80% of patients, thrombophlebitis, fever, chills, convulsions, anemia
Term
What are the Imidazoles?
Definition
Miconazole, Clotrimazole, Ketoconazole
Term
What is the mechanism of the Imidazoles?
Definition
Inhibits fungal cyp450 (lanasterol demethylase), preventing conversion of lanasterol to 14 demethyl lanosterol
Term
What are the side effects of Ketoconazole?
Definition
Can inhibit host cyp450, can inhibit cortisol and testosterone synthesis
Term
What are the Triazoles?
Definition
Fluconazole, Itraconazole, Voriconazole
Term
What is the mechanism of the Triazoles?
Definition
Inhibits fungal CYP450 (lanasterol demethylase), preventing conversion of lanasterol to 14 demethyl lanosterol
Term
Side effects of Itraconazole?
Definition
Decreases heart contractility
Term
What are the side effects of Voriconazole?
Definition
Causes visual disturbances
Term
What is the mechanism of Flucytosine?
Definition
It is a prodrug that is converted to 5 fluorouracil by fungi; inhibits thymidine synthesis
Term
What are the side effects of Flucytosine?
Definition
GI upset, bone marrow depression
Term
What is Flucytosine used in combination with, and why?
Definition
Few targets are sensitive to Flucytosine alone; used in combination with Amphotericine B
Term
What is the mechanism of the Echinocandins?
Definition
Inhibit the synthesis of beta (1,3) glucan, a cell wall component of fungi
Term
How are Echinocandins adminstered?
Definition
Intravenously
Term
What are the targets of Echinocandins?
Definition
Aspergillus, Candida
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