Chapter 188 - Antifungals

Question 1

Mainstay treatment of tinea capitis and onychomycosis

Answer 1

Systemic antifungals

Question 2

Main target of both systemic and topical antifungals is

Answer 2

Ergosterol

Question 3

All antifungals block the biosynthesis of ergosterol, except for ____ creating cell membrane pores

Answer 3

Polyenes

Question 4

Azoles exhibit ___ activity against yeasts and ___ activity against dermatophytes compared to allylamines.

Answer 4

Superior

Less

Question 5

Allylamine is ___ against Candida species and ___ aginst dermatophytes

Answer 5

Fungistatic

Fungicidal

Question 6

MOA of allylamine

Answer 6

Inhibition of squalene epoxidase enzyme

Question 7

The fungistatic effect of allylamine is due to ___ while fungicidal activity is due to ____

Answer 7

Deficiency of ergosterol

Buildup of squalene

Question 8

Aside from antifungal activity, naftifine has (2) more additional properties

Answer 8

Antibacterial

Antiinflammatory (suppress synthesis of LT and PGs)

Question 9

Lipophilic properties of naftifine persist in stratum corneum up to ___ days

Answer 9

5

Question 10

Absorption of oral terbinafine is not influenced by food intake
True or False

Answer 10

True

Question 11

Topical terbinafine is efficacious in treatment of all superficial mycoses.
True or False

Answer 11

True

Question 12

FDA approved treatment for tinea capitis

Answer 12

Terbinafine

Griseofulvin

Question 13

Terbinafine is lipophilic and can persist in keratinized tissue up to ___ mos after last dose

Answer 13

6

Question 14

SJS/TEN has been reported within __ weeks of treatment

Answer 14

4-5

Question 15

Most unique side effect of terbinafine (3)

Answer 15

Ageusia (altered taste)
Loss of smell
Tongue discoloration

Question 16

Most serious side effect of terbinafine (2)

Answer 16

Hepatotoxicity

Hematologic disorders

Question 17

FDA approved indications of terbinafine (2)

Answer 17

Tinea unguium

Tinea capitis

Question 18

Off label indications for terbinafine (2)

Answer 18

Tinea pedis, cruris, corporis

Seborrheic dermatitis

Question 19

All oral antifungals are category C except

Answer 19

Terbinafine Category B

Question 20

Terbinafine is a CYP 2C9 inducer and should not be given ___ which may increase risk of thrombosis

Answer 20

Warfarin

Question 21

Terbinafine is a CYP 2D6 inhibitor and should not be given with

Answer 21

TCA
SSRI
Haloperidol

Question 22

Pregnancy Category of Butenafine

Answer 22

C

Question 23

Examples of triazoles (4)

Answer 23

Fluconazole
Itraconazole
Efinaconazole
Isavuconazole

Question 24

MOA of azole

Answer 24

Inhibition of lanosterol demethylase

14 alpha-demethylase

Question 25

Azoles can be fungicidal in hugh concentrations. | True or False

Answer 25

True

Question 26

First developed topical imidazole that can disrupt mycotic phospholipids resulting in leakage of intracellular iron, degradation of nucleic acids, suppression of cell respiration

Answer 26

Clotrimazole

Question 27

Clotrimazole can be used for all superficial mycoses, achieveing mycological cure rates ranging from ___ in dermatophytosis and ___ in cutaneous candidiasis

Answer 27

60-100% | 80-100%

Question 28

__% of ketoconazole reaches hair keratin ___ hours from first shampoo

Answer 28

5%, 12

Question 29

2% antifungal prep

Answer 29

Sertaconazole Ketoconazole Miconazole

Question 30

Has androgen opposing properties resulting to impotence, gynecomastia, and decreased libido

Answer 30

Ketoconazole

Question 31

Serious side effects of ketoconazole (3)

Answer 31

Liver toxicity Anaphylaxis Marked depression

Question 32

Blocks mycotic peroxidase enzyme resulting to accumulation of toxic peroxide

Answer 32

Miconazole

Question 33

Most recently developed imidazoles

Answer 33

Luliconazole | Sertaconazole

Question 34

Binds to nonsterol lipids in mycotic cell wall resulting in cell lysis

Answer 34

Sertaconazole

Question 35

In addition to antifungal properties, sertaconazole has (2) properties

Answer 35

Antibacterial | Antipruritic

Question 36

Sertaconazole can persist up ti __ hours after the last dose

Answer 36

48

Question 37

In EU, sertaconazole is approved for all dermatophytoses but in the Us its limited to ___

Answer 37

Tinea pedis

Question 38

FDA licensed for topical treatment of onychomycosis

Answer 38

Efinaconazole 10% OD for 48 weeks

Question 39

Less efinaconazole is biund to keratin compared to amorolfine and ciclopirox which allows more drug to penetrate the nail plate. True or False

Answer 39

True

Question 40

Only Category B in azoles

Answer 40

Clotrimazole | Oxiconazole

Question 41

Main route of elimination of fluconazole

Answer 41

Kidney

Question 42

Fluconazole is efficacious against all Candida except

Answer 42

C. Krusei

Question 43

Fatal arrythmias can result when fluconazole is administered with (4)

Answer 43

Astemizole Cisapride Pimozide Terfenadine

Question 44

FDA - approved indications for Fluconazole (3)

Answer 44

Esophageal candidiasis Vaginal candidiasis Cutaneous mucocutaneous candidiasis

Question 45

Most common side effects of fluconazole

Answer 45

HA Myalgia Dizziness GIT upset

Question 46

Most serious side effects of Fluconazole (3)

Answer 46

Cardiac abnormalities Exfoliative skin reactions Anaphylactic reactions

Question 47

Itraconazole has high affinity to nail form a drug reservoir for ____ after DC of drug

Answer 47

6-9 mos

Question 48

Best choice in the treatment of candida and nondermatophyte onychomycosis

Answer 48

``` Itraconazole 200 mg daily for 6 weeks or 12 weeks Or 400 mg pulse dose 2 pulses - fingers 3 pulses - toes ```

Question 49

FDA approved indication for Itraconazole (2)

Answer 49

Onychomycosis | Oropharyngeal candidiasis

Question 50

Most unique side effect of Itraconazole

Answer 50

Triad of edema Hyperkalemia Hypertension

Question 51

Most serious side effect of itraconazole

Answer 51

Negative inotropic Fulminant hepatitis SJS Anaphylaxis

Question 52

Most common side effect of itraconazole

Answer 52

GI upset with cyclodextrin solution

Question 53

Itraconazole is CyP 3A4 inhibitor hence contraindicated with

Answer 53

Digoxin | Quinidine

Question 54

Antifungal derived from Streptomyces

Answer 54

Nystatin

Question 55

MOA of polyene

Answer 55

Generation of pores in cell membrane with subsequent leakage of essential fungal intracellular components resulting in cell death

Question 56

Nystatin is commonly used for

Answer 56

Candidiasis

Question 57

High drug concentrations of ciclopirox (>50ug/ml) lead to leakage of ___ ions and chelating ___

Answer 57

Potassium | Aluminum, Iron

Question 58

Treatment for onychomycosis

Answer 58

Ciclopirox 8% OD- BID for 48 weeks Amorolfine 5% nail lacquer weeky for 6 months fingernails 12 months toenails Tavaborole 5% OD for 48 weeks

Question 59

Interrupts the ergosterol synthesis at the 14 reduction and 7-8 isomerization in ergosterol pathway resulting in accumulation if 24- methylene igsterol

Answer 59

Amorolfine

Question 60

Pregnancy category of amorolfine 5% nail lacquer

Answer 60

D

Question 61

Topica imidazoles are Category C, except

Answer 61

Clotrimazole, Oxiconazole | Category B

Question 62

Ciclopirox 8% nail lacquer are pregnancy category

Answer 62

B

Question 63

Novel oxaborole antifungal drug that encloses a fluorine atom which inhibits fungal peptide synthesis

Answer 63

Tavaborole

Question 64

MOA of tavaborole

Answer 64

Inhibits aminoacyl transfer RNA synthetase

Question 65

Binds to tubulin and microtubule associated protein (MAPs) suppressing the G2/M phase of cell cycle

Answer 65

Griseofulvin

Question 66

FDA approved indications for griseofulvin (3)

Answer 66

Tinea capitis Tinea cruris Tinea pedis

Question 67

Most serious side effect of griseofulvin

Answer 67

Hepatotoxicity | Pancytopenia

Question 68

Most common side effect of griseofulvin

Answer 68

GI upset