Antifungal Drugs Flashcards

1
Q

Amphotericin B

A

Polyene
Most effective drug for most systemic fungal infections
Drug of choice for treating life threatening mycoses

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2
Q

Natamycin (Pimaricin)

A

Polyene

Lipid formulation of amphotericin B

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3
Q

MOA of polyenes

A

Disrupt the cell membrane function

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4
Q

Adverse effect of Amphotericin B (Polyenes)

A

Low therapeutic index

Very careful monitoring

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5
Q

Side effects of Polyenes (Amphotericin B)

A

Nausea and vomiting
Fever, shaking, chills
Headache, malaise, anemia, anorexia

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6
Q

Polyenes (amphotericin B) in eye care

A

Ointment or soluction for topical fungal keratitis
Amphotericin B is the drug of choice to treat patients with fungal keratitis caused by Candida
Administer every 30min first 24hr then every hour for the next 24hr with a slow taper

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7
Q

Drug of choice for endopthalmitis

A

Intravitreal Amphotericin B

Need a compounding pharmacy

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8
Q

Natamycin in eye care

A

A polyene
The only commercially available topical opthalmic antifungal
effective against filamentous fungi particularly for infections caused by Fusarium

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9
Q

Pyrimidines MOA

A

ex: Flucytosine, “5-flurocytosine (5-FC)
Converted to 5-flurouacil (5-FU) and this inhibits DNA synthesis

Fungistatic
Used in combination amphotericin B

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10
Q

Flucytosine Adverse effects

A

Nausea, vomiting, headache, diarrhea, abdominal pain, skin rash
Abnormal liver function tests
Reversible neutropenia and dose related bone marrow derpession

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11
Q

Flucytosine in Eye care

A

A pyrimidine
Rarely used –> resistance
Monotherapy is ineffective

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12
Q

Two classes of Azoles?

A

Imidazoles: Limited to topical for cutanious infections
Triazoles: given systemically or topically for the treatment of cutaneous and systemic fungal infections

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13
Q

Characteristics of Triazoles

A

Given orally or topically
Fungistatic
Blocks the biosynthesis of ergostrol in the cell membrane by inhibiting the CYP450 enzyme (non-specific so also interferes with human CYP450 and others related

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14
Q

Fluconazole

A
a Triazole
First one created 
Limited spectrum to yeast
-no activity against mold
Used as an oral treatment of mucocutaneous candidiasis
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15
Q

Adverse affects of Fluconazole

A

Nausea, vomiting, headache, diarrhea, abdominal pain , skin rash
Can cause hepatotoxicity

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16
Q

Itraconazole

Adverse effects

A

Triazole
Nausea, vomiting, diarrhea
Severe hypokalemia with daily use
Hepatotoxicity

17
Q

Itraconazole in Eye care

A

oral dosage has poor ocular penetration

1% ophtalmic suspension but not very effective on severe fungal infections

18
Q

Voriconazole

A

Triazole
Broad spectrum with high bioavailability when given orally
Replacing amphotericin B for many fungal and yeast systemic infections
FDA approved for first line treatment of aspergillus

19
Q

Efinaconazole

A

A triazole

Used in the topical treatment of onychomycosis

20
Q

Name the 10 Imidazoles

A

Butoconazole, Clotrimazole, Econazole, Ketoconazole, Miconazole, Oxiconazole, Sertazonazole, Sulconazole, Terconazole, Tioconazole

21
Q

Characteristics/Use of Imidazoles

A
Broad spectrum
tinea pedis (athletes foot)
tinea cruris (jock itch)
tinea corporis (ringworm)
tinea capitis (scalp infection)
onychomycosis (nail fungus)
oropharyngeal and vulvo-vaginal candidiasis
22
Q

Clotrimazole

A

also available as a lozenge and miconazole is avaliable as a buccal tablet for the treatment of thrush

23
Q

Imidazoles in eye care

A

Miconazole was availabe as
topical suspenstion
sub conj depot
oral

24
Q

Echinocandins

A

Caspofungin
Micafungin
Anidulafungin

25
Q

MOA of Echinocandins

A

Interfere with fungal cell wall synthesis
they are selective and less toxic

All are used once a day and they are well tolerated

26
Q

Adverse effects of Echinocandins

A

Fever, rash, nausea

27
Q

Echinocandins in eye care

A

Not typically used in eye care

28
Q

Squalene epoxidase inhibitors

A

Oral Terbinafine
Drug of choice for
-Onychomycoses (nail fungus)
-use for tinea capitis (topicals are ineffective)

29
Q

Topical Terbinafine, Naftifine and Buternafine

A

tinea pedis, tinea corporis, and tinea cruris

30
Q

Griseofuvin

A

Stops fungal mitosis
Drug accumulates in hair, nails, skin and adipose issues
Treatment of nail fungus and scalp
Fungstatic - long treatment times 12 weeks

31
Q

Nystatin

A

Like amphotericin B

Used in oral and topical Candidia infections