Anti-Fungal Agents

Question 1

Bacterial derivative of Amphotericin B

Answer 1

Streptomyces nodosus

Question 2

MOA of Amphotericin B

Answer 2

Binding to ergosterol to create pores leading to increased cell permeability and lysis

Question 3

Therapeutic uses of amphotericin B

Answer 3

Used as induction regime and treatment of all life-threatening mycotic infections; immunosuppressed individuals

Question 4

Adverse effects of amphotericin B

Answer 4

Nephrotoxicity (decreased EPO) causing anemia; infusion related toxicity

Question 5

New AMB Formulations

Answer 5

AMB Lipid Complex (ABLC)
AMB colloidal dispersion (ABCD)
Liposomal AMB

Question 6

Drug of choice for nearly all life-threatening mycotic infections

Answer 6

New AMB formulations

Question 7

New AMB formulation that deliver AMB to reticuloendothelial cells in the liver and spleen

Answer 7

Liposomal AMB

Question 8

These drugs produce lower AMB levels

Answer 8

ABLC and ABCD

Question 9

Polyene macrolide active against Candida spp.

Answer 9

Nystatin

Question 10

Therapeutic usage of nystatin

Answer 10

Oropharyngeal thrush, vaginal candidiasis and intertriginous candidal infections

Question 11

Pharmacokinetics of nystatin

Answer 11

use only as topical agent “swish and spit or swish and swallow”

Question 12

MOA of azoles

Answer 12

inhibit lanosterol 14-demethylase leading to decreased ergosterol synthesis

Question 13

Azole type with lesser degree of specificity causing higher drug interactions and side effects

Answer 13

Imidazole

Question 14

Azole type with lower toxicity and less propensity to inhibit mammalian sterol synthesis

Answer 14

Triazole

Question 15

Common effect of azole groups

Answer 15

Both groups affect CYP450 causing a drug-drug interaction

Question 16

Azole with 3 nitrogen atoms with good oral absorption and high propensity to inhibit mammalian CYP450

Answer 16

Ketoconazole

Question 17

Adverse effects of Ketoconazole

Answer 17

Reduction in testosterone synthesis and suppression of estradiol synthesis

Question 18

Drugs that decrease absorption of ketoconazole

Answer 18

H2 blockers, PPI, and antacids

Question 19

Drugs that decrease efficacy and induce metabolism of ketoconazole

Answer 19

Rifampicin
Phenobarbital
Carbamazepine
Phenytoin

Question 20

Drugs that cause torsades des pointes with Ketoconazole

Answer 20

Terfenadine
Astemizole
Cisapride

Question 21

Fluorinated bistriazole that does not require an acidic environment

Answer 21

Fluconazole

Question 22

Only renal triazole

Answer 22

Fluconazole

Question 23

Therapeutic use of Fluconazole

Answer 23

Treatment and secondary prophylaxis of cryptococcal meningitis

Question 24

Adverse effects of fluconazole

Answer 24

reversible alopecia

Question 25

Synthetic triazole with 2 enantiomeric pairs each possessing 3 chiral centers

Answer 25

Itraconazole

Question 26

Therapeutic use for Itraconazole

Answer 26

For aspergillus; most systemic mycosis not associated with meningitis

Question 27

Drug of choice for paracoccidioidomycosis and chromomycosis

Answer 27

Itraconazole

Question 28

MOA of flucytosine

Answer 28

Inhibits thymidylate synthesis which is an important component of DNA

Question 29

Therapeutic use of flucytosine

Answer 29

Used as part of combination regimen with: Amphotericin B for cryptococcal meningitis Itraconazole for chromoblastomycosis

Question 30

Adverse effect of flucytosine

Answer 30

Bone marrow toxicity

Question 31

This anti-fungal drug is derived from Penicillium and is active against dermatophytes

Answer 31

Griseofulvin

Question 32

MOA of griseofulvin

Answer 32

Binds to microtubules leading to defective cell wall formation and binds to keratin protecting the skin from new infection

Question 33

Therapeutic use of griseofulvin

Answer 33

Oral fungistatic agent used in systemic treatment of dermatophytosis

Question 34

Water-soluble, semisynthetic lipopeptide synthesized from the fermentation product of Glurea lozonensis

Answer 34

Terbinafine

Question 35

MOA of terbinafine

Answer 35

noncompetitive inhibition of squalene monooxygenase to prevent ergosterol synthesis; squalene accumulation

Question 36

Adverse effect of terbenafine

Answer 36

Steven-Johnson Syndrome

Question 37

Topical used for ringworm, tinea versicolor, and mucocutaneous candidiasis

Answer 37

Triazoles

Question 38

Ketal triazole similar to ketoconazole and clotrimazole

Answer 38

Terconazole and Butoconazole

Question 39

Topical anti-fungal used for Candida vulvovaginitis

Answer 39

Tioconazole

Question 40

Topical anti-fungal used for common pathogenic dermatophytes

Answer 40

Oxiconazole, Sulconazole, Sertaconazole

Question 41

Topical anti-fungal that penetrates the stratum corneum and is found in effective concentration down to the mid-dermis

Answer 41

Econazole

Question 42

Topical anti-fungal where fungicidal concentration remains in the vagina for as long as 3 days

Answer 42

Clotrimazole

Question 43

Close chemical congener of econazaole that penetrates stratum corneum for more than 4 days

Answer 43

Miconazole

Question 44

Drug used to treat seborrheic dermatitis of the scalp

Answer 44

Ciclopirox olamine

Question 45

Halogenated phenolic ether used to treat tinea pedis, cruris, manuum, and versicolor

Answer 45

Haloprogin

Question 46

Thiocarbamate fungicidal ineffective against Candida and is associated with pruritus

Answer 46

Tolnaftate

Question 47

An allylamine that inhibits squalene 2,3-epoxidase that inhibits synthesis of ergosterol

Answer 47

Naftifine

Question 48

Drug used for treatment of tinea cruris and tinea corporis

Answer 48

Naftifine