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8th > Chapter 188 - Antifungals > Flashcards

Chapter 188 - Antifungals Flashcards

1
Q

Mainstay treatment of tinea capitis and onychomycosis

A

Systemic antifungals

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2
Q

Main target of both systemic and topical antifungals is

A

Ergosterol

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3
Q

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

A

Polyenes

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4
Q

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

A

Superior

Less

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5
Q

Allylamine is ___ against Candida species and ___ aginst dermatophytes

A

Fungistatic

Fungicidal

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6
Q

MOA of allylamine

A

Inhibition of squalene epoxidase enzyme

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7
Q

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

A

Deficiency of ergosterol

Buildup of squalene

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8
Q

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

A

Antibacterial

Antiinflammatory (suppress synthesis of LT and PGs)

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9
Q

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

A

5

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10
Q

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

A

True

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11
Q

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

A

True

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12
Q

FDA approved treatment for tinea capitis

A

Terbinafine

Griseofulvin

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13
Q

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

A

6

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14
Q

SJS/TEN has been reported within __ weeks of treatment

A

4-5

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15
Q

Most unique side effect of terbinafine (3)

A

Ageusia (altered taste)
Loss of smell
Tongue discoloration

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16
Q

Most serious side effect of terbinafine (2)

A

Hepatotoxicity

Hematologic disorders

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17
Q

FDA approved indications of terbinafine (2)

A

Tinea unguium

Tinea capitis

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18
Q

Off label indications for terbinafine (2)

A

Tinea pedis, cruris, corporis

Seborrheic dermatitis

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19
Q

All oral antifungals are category C except

A

Terbinafine Category B

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20
Q

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

A

Warfarin

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21
Q

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

A

TCA
SSRI
Haloperidol

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22
Q

Pregnancy Category of Butenafine

A

C

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23
Q

Examples of triazoles (4)

A

Fluconazole
Itraconazole
Efinaconazole
Isavuconazole

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24
Q

MOA of azole

A

Inhibition of lanosterol demethylase

14 alpha-demethylase

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25
Q

Azoles can be fungicidal in hugh concentrations.

True or False

A

True

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26
Q

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

A

Clotrimazole

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27
Q

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

A

60-100%

80-100%

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28
Q

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

A

5%, 12

29
Q

2% antifungal prep

A

Sertaconazole
Ketoconazole
Miconazole

30
Q

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

A

Ketoconazole

31
Q

Serious side effects of ketoconazole (3)

A

Liver toxicity
Anaphylaxis
Marked depression

32
Q

Blocks mycotic peroxidase enzyme resulting to accumulation of toxic peroxide

A

Miconazole

33
Q

Most recently developed imidazoles

A

Luliconazole

Sertaconazole

34
Q

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

A

Sertaconazole

35
Q

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

A

Antibacterial

Antipruritic

36
Q

Sertaconazole can persist up ti __ hours after the last dose

A

48

37
Q

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

A

Tinea pedis

38
Q

FDA licensed for topical treatment of onychomycosis

A

Efinaconazole 10% OD for 48 weeks

39
Q

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

A

True

40
Q

Only Category B in azoles

A

Clotrimazole

Oxiconazole

41
Q

Main route of elimination of fluconazole

A

Kidney

42
Q

Fluconazole is efficacious against all Candida except

A

C. Krusei

43
Q

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

A

Astemizole
Cisapride
Pimozide
Terfenadine

44
Q

FDA - approved indications for Fluconazole (3)

A

Esophageal candidiasis
Vaginal candidiasis
Cutaneous mucocutaneous candidiasis

45
Q

Most common side effects of fluconazole

A

HA
Myalgia
Dizziness
GIT upset

46
Q

Most serious side effects of Fluconazole (3)

A

Cardiac abnormalities
Exfoliative skin reactions
Anaphylactic reactions

47
Q

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

A

6-9 mos

48
Q

Best choice in the treatment of candida and nondermatophyte onychomycosis

A 
Itraconazole 200 mg daily for 6 weeks or 12 weeks
Or 
400 mg pulse dose
2 pulses - fingers
3 pulses - toes
49
Q

FDA approved indication for Itraconazole (2)

A

Onychomycosis

Oropharyngeal candidiasis

50
Q

Most unique side effect of Itraconazole

A

Triad of edema
Hyperkalemia
Hypertension

51
Q

Most serious side effect of itraconazole

A

Negative inotropic
Fulminant hepatitis
SJS
Anaphylaxis

52
Q

Most common side effect of itraconazole

A

GI upset with cyclodextrin solution

53
Q

Itraconazole is CyP 3A4 inhibitor hence contraindicated with

A

Digoxin

Quinidine

54
Q

Antifungal derived from Streptomyces

A

Nystatin

55
Q

MOA of polyene

A

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

56
Q

Nystatin is commonly used for

A

Candidiasis

57
Q

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

A

Potassium

Aluminum, Iron

58
Q

Treatment for onychomycosis

A

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

59
Q

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

A

Amorolfine

60
Q

Pregnancy category of amorolfine 5% nail lacquer

A

D

61
Q

Topica imidazoles are Category C, except

A

Clotrimazole, Oxiconazole

Category B

62
Q

Ciclopirox 8% nail lacquer are pregnancy category

A

B

63
Q

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

A

Tavaborole

64
Q

MOA of tavaborole

A

Inhibits aminoacyl transfer RNA synthetase

65
Q

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

A

Griseofulvin

66
Q

FDA approved indications for griseofulvin (3)

A

Tinea capitis
Tinea cruris
Tinea pedis

67
Q

Most serious side effect of griseofulvin

A

Hepatotoxicity

Pancytopenia

68
Q

Most common side effect of griseofulvin

A

GI upset

8th (28 decks)

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