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Pharm Final > Antifungals > Flashcards

Antifungals Flashcards

1
Q

Superficial mycoses

A

limited to outermost layer of skin and hari

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2
Q

Cutaneous mycoses

A

extended deeper into epidermis, and also include invasive hair and nail diseases; restricted to keratinized layers of skin, hair, nails; “dermatophytes” - athlete’s foot, ringworm, etc.

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3
Q

Subcutaneous mycoses

A

involve dermis, subcutaneous tissues, muscle and fascia; chronic and can be initiated by trauma to skin allowing fungi to enter; difficult to treat and may require surgery

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4
Q

Cause of subcutaneous mycoses

A

trauma to skin allowing fungi to enter

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5
Q

Systemic mycoses due to primary pathogens

A

start in lungs and spread to many organ systems; inherently virulent

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6
Q

Systemic mycoses due to opportunistic pathogens

A

immune deficiencies who would otherwise not be infected (AIDS, abx); ex. Candidiasis, Aspergillosis, Cryptococcosis

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7
Q

Opportunistic pathogens

A

Candidiasis, Aspergillosis, Cryptococcosis

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8
Q

What is the main target of antifungals? what drugs are the exceptions?

A

Cell wall/membrane; Griseofulvin and flucytosine

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9
Q

What is amphotericin B

A

polyene antifungal abx produced by strep nodosus

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10
Q

MOA of amphotericin B

A

interaction with sterol of fungal membrane, ergosterol, that causes depolarization and results in loss of intracellular components – pore formation (CIDAL)

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11
Q

Spectrum of ampho B

A

broad; fungicidal

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12
Q

DOC for systemic infections

A

Ampho B

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13
Q

Ampho B kinetics

A

IV
poor CNS penetration
Excreted slowly by kidney (nephrotoxic)
Detected in urine several weeks after therapy

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14
Q

Toxicities of amphotericin B

A

bind to human membrane sterols leading to toxicities:

Infusion related toxicity (immediate): chills, fever, muscle spasms, vomiting, h/a,; lessened by slowing infusion rate/decreasing dose

Reaction over time (cumulative): NEPHROTOXIC; Azotemia * (elevated BUN and creatinine); renal damage is dose dep. and can lead to irreversible kidney damage
acute hepatic failure, jaundice, anorexia, nausea, weight loss, hypokalemia
Hypersensitivity
Give w/ caution with aminoglycosides (nephrotoxic)
6weeks-4 months of treatment

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15
Q

Ergosterol mimics

A

Cholesterol in humans- leads to toxic side effects of ampho B

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16
Q

Duration of Ampho B

A

use as short a time as you can, then switch to something less; usually 6 weeks-4 months

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17
Q

Flucytosine use

A

great for CNS infections

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18
Q

Flucytosine (5-FC) MOA

A

antagonism of fungal DNA and RNA; flucytosine is converted to 5-fluorouracil which interferes w/ fungal DNA/RNA synthesis

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19
Q

Converts 5-FC to 5-FU

A

cytosine deaminase

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20
Q

Cytosine deaminase

A

bacterial have it; humans do not.

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21
Q

Side effect of flucytosine

A

GI intolerance; only bacterial have cytosine deaminase; won’t convert prodrug to active drug

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22
Q

DOC for cryptococcus

A

flucytosine (CNS) + amphotericin B

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23
Q

Seen in HIV patients

A

TB

Cryptococcus

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24
Q

Spectrum of flucytosine

A

lower than ampho B, cryptococcus*, some strains of candida, aspergillus, sporotrichum

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25
Q

Gets into CNS

A

flucytosine
Fluconazole
Voriconazole (some)

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26
Q

Kinetics of flucytosine

A

absorbed orally
enters CSF and aqueous humor
renal elimination (renal impairment can lead to toxicity)

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27
Q

Toxicity of flucytosine

A

depression of bone marrow (anemia, leukopenia, thrombocytopenia)
GI distrubances
Elevate ALT or AST (reversible upon discontinuation of the drug) (liver function)

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28
Q

Azoles

A 
Ketoconazole
Fluconazole*
Voriconazole
Itraconazole
Isavuconazonium
Posaconazole

(Kate finds veronica in interesting places)

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29
Q

Azole MOA

A

inhibit synthesis of ergosterol- leads to depletion of ergosterol in cell membrane and accumulation of toxic intermediate sterols, causing increased membrane permeability and inhibition of fungal growth (fungistatic)

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30
Q

Cidal

A

Ampho B

Flucytosine

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31
Q

Static

A

Azoles (immune competant individuals)

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32
Q

Ketoconazole spectrum

A

broad antifungal (like ampho B)

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33
Q

Ketoconazole kinetics

A

oral
widely distributed in body, largely bound to plasma albumin, low CNS penetration
extensively metabolized prior to elimination (hepatic)

34
Q

Ketoconazole typically only used as

A

shampoo or topicals

35
Q

Ketocanazole

A

GI upset, pruritus
POTENT INHIBITOR OF P450
Gynecomastia and impotence (inhibition of adrenal and testicular function)
Prolonged QT
elevation of serum enzymes
Dizziness, somnolence, H/a, arthralgia, myalgia, fever/chills, N/v

36
Q

Contraindications of ketoconazole

A

acute/chronic hepatic disease

37
Q

Oral ketoconazole

A

only used when no other antifungal tx can be used

38
Q

Fluconazole

A

oral/IV

penetrates body fluids, CSF

39
Q

DOC for fungal meningitis

A

Fluconazole

40
Q

Use of fluconazole

A

fungal meningitis

suppressive and/or prophylactic therapy in HIV patients (+ bactrim)

41
Q

Toxicity of fluconazole

A

less toxic than ampho B/flucytosine, better tolerated than keto
less drug interactions, but potent inhibitor of CYP2C9
H/A*, GI

42
Q

Voriconazole kinetics

A

IV/oral
Modest CSF penetration
hepatic elimination

43
Q

DOC for aspergillus

A

Vorizonazole + ampho B

44
Q

Voriconazole use

A

Aspergillus

Esophageal candidiasis

45
Q

Voriconazole toxicity

A

Drug interactions (metabolized by p540 and inhibits P450- drug interaction w/ itself; metabolized by 2C19, inhibits 2C19 the least); 2C19 genetic polymorphism (extensive/poor metabolizer: changes drug concentration)

Visual impairment: reversible; acuity, photophobia, changes in color/ligh; take off drug

46
Q

Itraconazole spectrum

A

similar to ketoconazole and fluconaole but greater activity against Aspergillus (but voriconazole is DOC for Asp- itraconazole has drug interactions)

47
Q

Itraconazole kinetics

A

Oral, IM;

oral bioavailability: capsules higher than oral solution; two dosage forms should not be used interchangeably!!!

48
Q

Least drug interactions

A

fluconazole

49
Q

2C9 inhibitors

A

fluconazole

voriconazole

50
Q

Isavuconazonium

A

azole; little toxicity - nephrotoxicity, QT, CYP3A4 inhibitor

51
Q

Posaconazole

A

drug interactions; asperigillus/candida

52
Q

Echinocandin drugs

A

Caspofungin
Micafungin
Anidulafungin

53
Q

Echinocandin MAO

A

inhibits the synthesis of major fungal cell wall component, beta-1,3-D-glucan, which is not present in mammalian cells

54
Q

PCN if antifungals

A

Echinocandins

55
Q

Caspofungin properties

A

IV, slow infusion
Cidal “PCN of antifungals”
lack of nephrotoxicity and few drug interactions = attractive tx

56
Q

Caspofungin use

A

invasive Aspergillosis in refractory patients (azole or ampho B resistant; esophageal candidiasis

57
Q

Caspofungin toxicity

A

elevated liver enzymes (AST, ALT), histamine release, H/A, chills, GI side, effects occur

58
Q

Micafungin and Anidulafungin

A

similar to caspofungin, altered pharmacokinetic properties

59
Q

Local/Topical tx

A

Griseofulvin
Terbinafine
Nystatin

60
Q

Dermatophytosis

A

Fungal infection that infects diff parts of the body; caused by group of fungi known as dermatophytes; invade and feed on keratin, outer layer of skin, hair, nails

61
Q

Onychomycosis

A

dermatophytic onychomycosis “ringworm of the nail”

62
Q

Caused of onychomycosis

A

dermatophytes, candida, and nondermatophytic molds

63
Q

Griseofulvin MOA

A

bind to microtubules of certain fungi and destroys the mitotic spindle structure; fungiSTATIC

64
Q

DOC onychomycosis

A

Griseofulvin

65
Q

Griseofulvin use

A

onychomycosis; dermatophytosis infections of skin, hair, nails

66
Q

Griseofulvin kinetics

A

STATIC
ORAL ONLY - no topical; poor solubility/asorption
Binds to keratin; prevents infection in new skin structures
excreted uncahnged in feces

67
Q

Tx time for griseofulvin

A

6mo-1 year to allow for replacement of infected keratin

68
Q

Griseofulvin toxicity

A

H/A*, GI, disulfiram-like effect *, CNS

Hematological distrubances, skin rash, photosensitivity, angioedema, albuminuria, hepatotoxicity, leukopenia

69
Q

Contraindications of griseofulvin

A

Acute intermittent porphyria (increase attacks and heme production)
hepatocellular failure
Pregnancy and men 6 months prior to fathering child!!!!!!

70
Q

Terbinafine

A

oral/topical

CIDAL

71
Q

Terbinafine use

A

onychomycosis (not DOC), less active against candida

72
Q

Terbinafine MOA

A

interferes w/ sterol biosynthesis; inhibits squalene monooxygenase; build-up of swualene is toxic to fungi

73
Q

Nystatin

A

polyene antibiotic (like ampho B)
oral; topical
not absorbed appreciably from Gi, skin or mucous membrane

74
Q

Nystatin use

A

candidal infections (oral for GI candida infections, topically for other candida infections)

75
Q

Nystatin toxicity

A

N/V, diarrhea (oral)

76
Q

Polyene antiobiotics

A

Amphotericin B

Nystatin

77
Q

Efinaconazole

A

newest TOPICAL antifungal

78
Q

DOC for candida

A

Nystatin

79
Q

Efinaconazole use

A

onychomycosis caused by Trichophytan rubrum and Trichophyton mentagrophytes

80
Q

DOC for Trich. rubrum and Trich

A

Efinaconazole topical solution daily for 48 weeks (probs not on test)

81
Q

Efinaconazole MOA

A

forms bonds and causes pores to form and leakage (like ampho B)

Pharm Final (6 decks)

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