antifungal drugs Flashcards

1
Q

Flucytosine

MOA

A

inhibits DNA, RNA, synthesis

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2
Q

Flucytosine

clinical use and side effects

A

Flucytosine

CU: systemic infection d/t cryptococcus neoformans and some candida spp. excellent CNS penetration- meningitis caused by cryptococcus

Side effects: Bone marrow suppression leading to leukopenia and thrombocytopenia

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3
Q

Griseofulvin

MOA

A

Griseofulvin

inhibits microtubule function, disrupt mitosis

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4
Q

Griseofulvin

Clinical use

A

Griseofulvin

Not for systemic infection- used systemically (oral) for treating dermatophytosis (ringworm, tinea) of the scalp, torso, inguinal, foot, and nail.

terfinabine is the DOC for tinea infections, azoles are the alternative

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5
Q

Griseofulvin

Side effects

A

serious reactions are rare

GI- N/V/D/bleeding

Hepatotoxicity: avoid in a patient with compromised liver fuction

photosensativity

CYP450 drug inducer

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6
Q

Terbinafine

MOA

A

Terbinafine

ergosterol synthesis inhibitor

Inhibits the synthesis of squalene epoxide by inhibiting the enzyme “squalene epoxidase”

this leads to the accumulation of squalene which is toxic to fungal cells

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7
Q

Terbinafine

Side effects

A

well tolerated

Pregnancy category B

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8
Q

Terbinafine

Clinical Use

A

Terbinafine

DOC for treating dermatophytosis (tinea infections): topical use for cruris and corporis

Onychomycosis (tinea unguinum- nail fungus)

oral administration and prolonged therapy

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9
Q

“-azoles”

MOA

A

“-azoles”

ergosterol synthesis inhibitors

inhibit the synthesis of ergosterol from lanosterol by inhibiting CYP450 enzymes

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10
Q

“-azoles”

Clinical Use

A

“-azoles” broad spectrum of action including candida spp, cryptococcus neoformans, endemic mycoses, dermatophytes, even aspergillus

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11
Q

Ketoconzole:

Clinical Use

Side effects

A

Ketoconzole:

dermatophytosis

not for systemic use dt its narrow therapeutic index and side effects.

Side effects:

potent CYP450 inhibition

inhibits adrenal steroidogenesis causing adreanal insufficiency

hepatotoxicity

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12
Q

Fluconazole

major clinical use

A

Fluconazole

Cryptococcal meningitis (good CSF penetration)

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13
Q

Itraconazole

Major clinical use

A

Itraconazole:

candida, cryptococcus, blastomycosis

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14
Q

vorconazole

A

Vorconazole

DOC Aspergillus

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15
Q

Amphotericin B/Nystatin

MOA

A

Amphotericin B/Nystatin

Cell membrane integrity inhibitors

bind to ergosterol and forms pores in membrane to allow the leakage of electrolytes

Polyenes

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16
Q

Amphotericin B:

Clinical Uses

A

Amphotericin B:

DOC for most severe and/or life-threatening infections, systemic infections

topical use for candida albicans infection

17
Q

Amphotericin B:

Side Effects

A

Amphotericin B:

Side effects

immediate toxicity: fever/chills, muscle spasms, vomiting, headache, hypotension. Treated by slowing infusion or prevent with antipyretics, antihistamine, meperidine, corticosteroids

cumulative toxicity: renal toxicity dt constriction of afferent arterioles and disruption of the membrane permeability. Renal tubular acidosis and renal wasting of K+ and Mg+

18
Q

Nystatin:

Clinical Use

A

Nystatin

topical use only (too toxic for systemic use)

cutaneous, mucocutaneous, and oral infections normally caused by candida spp.

“swish and swallow” for thrush

topical for diaper rash or vaginal candidiasis

19
Q

Nystatin

Side effects

A

Nystatin

Not absorbed from GI, skin, or vagina so has little toxicity

20
Q

Echinocandins

Suffix

MOA

A

Echinocandins “-fungin”

Inhibit cell wall synthesis

inhibit synthesis of beta- glucan a component of the cell wall

21
Q

Echinocandins

Clinical use

A

Echinocandins

Candida and Aspergillus

emperic antifungal therapy during febrile neutropenia

22
Q

Echinocandins

Side effects

A

Echinocandins

Minor GI upset and flushing

v. expensive ($400/day)