Antifungal Drugs

Question 1

Amphotericin B

Answer 1

• covers all medically important fungi
• given IV
• cause many SE
• can be given intrathecally

Question 2

Itraconazole

Answer 2

• given orally

Question 3

Less serious systemic infections antifungal agents

Answer 3

oral azole drugs i.e. ketoconazole, fluconazole, itraconazole,

Question 4

tx superficial fungal infections

Answer 4

Griseofulvin, nystatin, azole (clotrimazole, miconazole)

Question 5

Polyenes (for systemic fungal infections)

Answer 5

nystatin, amphotericin B

Question 6

MOA of Polyenes

Answer 6

inhibit ergosterol synthesis - fungicidal, nephrotoxic

Question 7

Griseofulvin microorganism from

Answer 7

penicuillium
- can be systemic/oral
binds to tubulin

Question 8

MOA Polyenes

Answer 8

Hydrophobic interactions occur between the ergosterol present in fungal membranes and the polyene macrolides leading to enhanced membrane permeability and leakage of intracellular ions

Question 9

Amphotericin B

Answer 9

Streptomyces nodosus

Question 10

Nystatin

Answer 10

Streptomycin norsei

Question 11

Polyenes toxicity caused by:

Answer 11

affinity for cholesterol

Question 12

Solution for toxicity in Polyenes

Answer 12

Encapsulation of Liposomes in Amphotericin B

Question 13

Too toxic Polyenes should be topical only

Answer 13

Nystatin

Question 14

Azoles inhibit what enzyme that involves in ergosterol synthesis

Answer 14

CYP-459

Question 15

Imidazoles

Answer 15

Ketoconazole
Miconazole
Clotrimazole

Question 16

Triazoles

Answer 16

Fluconazole
Itraconazole
Voriconazole

Question 17

Topical Fungal Infections

Answer 17

Clotrimazole
Miconazole

Question 18

Systemic fungal infections agents, given orally

Answer 18

Ketoconazole
Fluconazole
Itraconazole

Question 19

block fungal cell-wall synthesis
semisynthetic lipopeptides
produced by various species of fungi and inhibit synthesis of beta (1 - 3) D-glucan

Answer 19

Echinocandins

Question 20

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

Answer 20

Sordarins

Question 21

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

Answer 21

allylamines

Question 22

highly lipophilic and keratophilic
- distribute in high conc. in the stratum corneum, sebum, hair, and nail matrix, persist for months

Answer 22

Allylamines

Question 23

fungistatic antibiotic
- orally active
- accumulates in skin, hair, nails, fat, and skeletal muscles
- tx ringworm of skin, nails, and hair caused by dermatophyte fungi

Answer 23

Griseofulvin

Question 24

MOA: disrupting the cell’s mitotic spindle, thus arresting the fungal cells in metaphase
+ affect microtubule structure

Answer 24

Griseofulvin

Question 25

inhibit RNA synthesis

Answer 25

Flucytosine

Question 26

Microogranism of Griseofulvin

Answer 26

Penicillium griseofulvum