Fungal Drugs- Exam 2 Flashcards

1
Q

Fungal medications like to bind to _____, which is not present in human cells

A

Ergosterol

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2
Q

Why are Triazoles tend to get used the most? Are they systemic or topical?

A

better distribution
fewer side effects
fewer drug interactions

systemic

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3
Q

______ are primarily topicals

A

Imidazoles

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4
Q

____ Inhibit synthesis of ergosterol

A

Azoles

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5
Q

Name some substances that inhibit Azoles?

A

Grapefruit juice, alcohol (binge), several antibiotics and stomach acid-reducing products

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6
Q

Name some substances that speed up azoles?

A

Alcohol (chronic), several anticonvulsants

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7
Q

_____ may have less DDI than other azoles

A

Fluconazole

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8
Q

What are the SE of azoles?

A

GI upset (N/V/D, abdominal pain); HA; taste changes

Major - hepatotoxicity, prolonged QT, seizures, leukopenia, thrombocytopenia

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9
Q

Azoles needs to be cautious in the certain pt populations, including: ____, ____ and _____

A

hepatic or renal impairment

pregnancy

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10
Q

What trimester of pregnancy should azoles be avoided in?

A

greatest risk with systemic therapy in the FIRST semester

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11
Q

Due to the SE of azoles, which labs would be particularly important to check?

A

Liver function testing

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12
Q

What is the difference between all the azoles?

A

Fluconazole
Itraconazole
Voriconazole
Posaconazole. Increasing spectrum of activity as the list goes down FIVP

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13
Q

______ is the prototype azole drug and has the most limited spectrum of activity among systemic azoles

A

Fluconazole (Diflucan)

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14
Q

_____ is most commonly used in Candida albicans and Cryptococcus infections

A

Fluconazole (Diflucan)

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15
Q

What is Fluconazole (Diflucan) indicated for? Does it penetrate the CSF?

A

superficial fungal infections, uncomplicated systemic infections
Gets into CSF well

Yes! gets into CSF well

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16
Q

_____ is the drug of choice against histoplasmosis, sporotrichosis, blastomycosis. Variable bioavailability

A

Itraconazole (Sporanox)

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17
Q

_____ is the drug of choice for invasive aspergillosis

A

Voriconazole (Vfend)

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18
Q

Very broad-spectrum antifungals
Invasive fungal infections in immunocompromised pts, or resistant infections
What azoles?

A

Posaconazole (Noxafil) and isavuconazole (Cresemba

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19
Q

_____ gets into CSF well; _____
gets into brain tissue, but not CSF

A

Posaconazole

isavuconazole

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20
Q

____ and _____ are available OTC and are inexpensive

A

Clotrimazole and miconazole

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21
Q

What are the topical azoles? Which ones tend to work slightly better?

A

Econazole (Spectazole)
ketoconazole (Nizoral)
sulconazole (Exelderm)

may have slightly more efficacy than

older azoles :clotrimazole and miconazole

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22
Q

_____ bind to ergosterol in the fungal cell membrane, creating pores in the cell and causing leakage of cell contents

A

polyenes

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23
Q

_____ is considered very toxic and is only used topically. What class is it in?

A

nystatin

polyenes

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24
Q

Are polyenes absorbed well in the GI tract?

A

generally not absorbed well via GI tract

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25
Q

____ is mainly administered IV, and is indicated for severe, disseminated mycotic infection with a very broad spectrum of activity

A

Amphotericin B

26
Q

What are some SE of Amphotericin B? What is the major one?

A

Infusion-related - fever, chills, N/V, headache
renal impairment, nephrotoxicity
hypokalemia, hypomagnesemia, hyperchloremic acidosis, anemia, hypotension

27
Q

____ is usually used topical and oral rinse and is indicated for non-invasive candidal infections.

A

Nystatin

28
Q

What are the SE of Nystatin?

A

local irritation, allergic reaction
GI upset (N/V/D, abdominal pain)

29
Q

____ inhibit synthesis of β-(1,3)-d-glucan, needed for fungal cell walls

A

Echinocandins

30
Q

What are the indications for Echinocandins?

A

invasive fungal infections such as:
Disseminated candidiasis
Aspergillosis (especially in HIV+ patients)

31
Q

Echinocandins are given in the ____ setting. What organ system do they impact the most?

A

inpatient setting, IV administered

hepatoxicity

32
Q

Echinocandins have (large/small) effect on the CYP450 system and have (more/less) drug interactions than azoles

A

Minimal effect on CYP 450 and LESS DDI than azoles

33
Q

What are the medications included in the Echinocandins?

A

caspofungin (Cancidas)
anidulafungin (Eraxis)
micafungin (Mycamine)

34
Q

_____ not well known - may act on cell wall and DNA synthesis

A

Mitotic Inhibitors :Griseofulvin

35
Q

What are the indications for Griseofulvin?

A

Dermatophyte (tinea) infections of hair and skin

36
Q

What are the DDI with Griseofulvin?

A

alcohol, contraceptives, warfarin, barbiturates

Can cause “disulfiram”-type reaction with ETOH

37
Q

What are the CI to Griseofulvin? What is the major one?

A

liver failure, porphyria, pregnancy

38
Q

What are the SE of Griseofulvin? What is the most common? What is the most serious?

A

HA ,GI upset, skin rashes, dizziness

Serious - hepatotoxicity, teratogenic, granulocytopenia
Need weekly CBCs

39
Q

What test do you need to order on a pt taking griseofulvin?

A

weekly CBC to monitor their granulocytes

40
Q

**What is an essential pt education point for griseofulvin?

A

Absorbed best in the presence of a fatty meal

41
Q

What medication falls under the Allyamines?

A

Terbinafine (Lamisil)

42
Q

_____ Interfere with ergosterol synthesis

A

allyamines

Terbinafine (Lamisil)

43
Q

What are the indications of Terbinafine (Lamisil)?

A

Oral - onychomycosis, dermatophyte (tinea) infections of hair and skin

Topical - Dermatophyte (tinea) infections of hair and skin

44
Q

What are the DDI of Terbinafine (Lamisil)?

A

numerous - certain beta-blockers, certain TCAs, tamoxifen, tramadol

45
Q

What are the CI to Terbinafine (Lamisil)?

A

liver disease

46
Q

What are the SE of terbinafine (Lamisil)? Which one is most common? Which one is the most serious?

A

HA, GI upset, skin rashes, taste disturbances

Serious - hepatotoxicity, neutropenia

47
Q

What test do you need to monitor on a pt taking Terbinafine (Lamisil)?

A

Monitor LFTs and CBC before and during tx

Liver damage usually reversible, but case reports of liver failure and death

48
Q

______ enters cells and is converted to 5-fluorouracil, which inhibits fungal RNA and protein synthesis

A

flucytosine (Ancobon)

49
Q

What is the indication for flucytosine (Ancobon)?

A

Adjunct treatment - used in combination with amphotericin B

For severe candidal or cryptococcal infections (immunocompromised pts)

50
Q

What is the BBW with flucytosine (Ancobon)?

A

about use in pts with renal impairment

51
Q

What are some SE of flucytosine (Ancobon)?
What are the major ones?

A

increased renal function testing, renal failure

hepatic injury, hepatotoxicity, GI upset

pancytopenia/aplastic anemia

CNS - peripheral neuropathy, confusion, psychosis, dizziness, ataxia

52
Q

_____ inhibits glucan synthase, used to make part of the cell wall

A

ibrexafungerp (Brexafemme)

53
Q

What is the drug class for ibrexafungerp (Brexafemme)?

A

triterpenoids

54
Q

What is the indication for ibrexafungerp (Brexafemme)?

A

Vulvovaginal candidiasis (single-day treatment option)

55
Q

What is the CI to ibrexafungerp (Brexafemme)? What are the SE?

A

pregnancy

GI - abdominal pain, nausea, diarrhea in 10-17%
Rare - elevated AST/ALT, flatulence, vomiting
GU - vaginal bleeding, dysmenorrhea
Other - rash, dizziness, back pain

56
Q

____ and ____ are available OTC - indicated for dermatophytes (tineas)

A

Butenafine (Lotrimin)

Tolnaftate (Tinactin)

57
Q

____ is prescription only, newly generic but still may be a little expensive
Some studies suggest more effective than clotrimazole and miconazole
Indicated for dermatophytes (tineas)

A

Naftifine (Naftin)

58
Q

______ are expensive , but now generic, more effective than clotrimazole and miconazole
Indicated for dermatophytes, onychomycosis, seborrheic dermatitis

A

Ciclopirox (Loprox, Penlac)

59
Q

____ is expensive, but has a generic version; equally effective as ciclopirox
Indicated for onychomycosis

A

Tavaborole (Kerydin)

60
Q

_____ is expensive and has no generic
More effective than clotrimazole, miconazole, and even ciclopirox
Indicated for onychomycosis

A

Efinaconazole (Jublia)

61
Q
A