Unit 6-Antifungals

Question 1

Amphotericin B

Drug class

Answer 1

Polyene macrolide

Question 2

Amphotericin B

Mechanism

Answer 2

Pores are formed in the fungal cell membrane, allowing leakage of K+ and Mg+

Question 3

Amphotericin B

Uses

Answer 3

Life-threatening invasive fungal infections; broad antifungal spectrum; (occasionally used with flucytosine in immunocompromised hosts)

Lipid formulations result in better tolerability

Question 4

Amphotericin B

Side effects

Answer 4

Chronic: fall in renal function (may only be partially reversible); K+ Mg+ wasting; renal tubular acidosis
Acute during IV infusion: fever/chillls; potential for hypotension;

Question 5

Nystatin

Drug class

Answer 5

Polyene macrolide

Question 6

Nystatin

Mechanism

Answer 6

Pores are formed in the fungal cell membrane, allowing leakage of K+ and Mg+

Question 7

Nystatin

Uses

Answer 7

Topically (powder) against superficial fungal infections (candidiasis only)

No use against dermatophytes

Question 8

Fluconazole

Drug class

Answer 8

Triazole / Cell membrane synthesis inhibitor

Question 9

Fluconazole

Mechanism

Answer 9

Inhibit ergosterol synthesis by inhibiting lanosterol demethylase

Question 10

Fluconazole

Uses

Answer 10

Candida infections; secondary treatment and prophylaxis of cryptococcal meningitis

Clotrimazole = topical; fluconazole = systemic

Question 11

Fluconazole

Side effects

Answer 11

Hepatotoxicity (rarely), GI side effects, inhibits CYP450

Question 12

Voriconazole; Itraconazole

Drug class

Answer 12

Triazole / Cell membrane synthesis inhibitor

Question 13

Voriconazole; Itraconazole

Mechanism

Answer 13

Inhibit ergosterol synthesis by inhibiting lanosterol demethylase

Question 14

Voriconazole; Itraconazole

Uses

Answer 14

Candida & Aspergillus infections

Question 15

Voriconazole; Itraconazole

Side effects

Answer 15

Hepatotoxicity (rarely), GI side effects, inhibits CYP450

Visual disturbances w/ voriconazole

Question 16

Posaconazole

Drug class

Answer 16

Triazole / Cell membrane synthesis inhibitor

Question 17

Posaconazole

Mechanism

Answer 17

Inhibit ergosterol synthesis by inhibiting lanosterol demethylase

Question 18

Posaconazole

Uses

Answer 18

Candida, Fusarium, Mucorales infections

Question 19

Posaconazole

Side effects

Answer 19

Hepatotoxicity (rarely), GI side effects, inhibits CYP450

Question 20

Efinazonazole (Jublia)

Drug class

Answer 20

Azole / Cell membrane synthesis inhibitor

Question 21

Efinazonazole (Jublia)

Mechanism

Answer 21

Inhibit ergosterol synthesis by inhibiting lanosterol demethylase

Question 22

Efinazonazole (Jublia)

Uses

Answer 22

Candida; Tinea

Question 23

Efinazonazole (Jublia)

Side effects

Answer 23

Application site dermatitis, pain

Question 24

Tolnaftate; Terbinafine

Drug class

Answer 24

Allylamine / Cell wall synthesis inhibitor

Question 25

Tolnaftate; Terbinafine | Mechanism

Answer 25

Inhibit ergosterol synthesis by inhibiting squalene epoxidase

Question 26

Tolnaftate; Terbinafine | Uses

Answer 26

Topical dermatophytes (limited utility against candida) Terbinafine effective against onychomycoses; tolnaftate: oral only; weak agent

Question 27

Tolnaftate; Terbinafine | Side effects

Answer 27

Hepatotoxicity (rarely) | Low side effect profile

Question 28

Capsofungin; Micafungin; Anidulafungin | Drug class

Answer 28

Echinocandin / Cell wall synthesis inhibitor

Question 29

Capsofungin; Micafungin; Anidulafungin | Mechanism

Answer 29

Inhibit synthesis of Beta(1,3)-D-glucan, an essential component of the fungal cell wall

Question 30

Capsofungin; Micafungin; Anidulafungin | Uses

Answer 30

Life-threatening fungal infections unresponsive to older agents (especially candida, aspergillus)

Question 31

Capsofungin; Micafungin; Anidulafungin | Side effects

Answer 31

Low side effect profile Expensive; only available as IV formulation

Question 32

Flucytosine | Drug class

Answer 32

Nucleic acid synthesis inhibitor

Question 33

Flucytosine | Mechanism

Answer 33

Prodrug converted by fungal enzyme to analog inhibitor of pyrimidine nucleotide synthesis

Question 34

Flucytosine | Uses

Answer 34

Used in combo with amphotericin B in life threatening fungal infections in immunocompromised patients.

Question 35

Flucytosine | Side effects

Answer 35

Bone marrow toxicity; Liver dysfunction possible