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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
____ is mainly administered IV, and is indicated for severe, disseminated mycotic infection with a very broad spectrum of activity
Amphotericin B
26
What are some SE of Amphotericin B? What is the major one?
Infusion-related - fever, chills, N/V, headache renal impairment, **nephrotoxicity** hypokalemia, hypomagnesemia, hyperchloremic acidosis, anemia, hypotension
27
____ is usually used topical and oral rinse and is indicated for non-invasive candidal infections.
Nystatin
28
What are the SE of Nystatin?
local irritation, allergic reaction GI upset (N/V/D, abdominal pain)
29
____ inhibit synthesis of β-(1,3)-d-glucan, needed for fungal cell walls
Echinocandins
30
What are the indications for Echinocandins?
invasive fungal infections such as: Disseminated candidiasis Aspergillosis (especially in HIV+ patients)
31
Echinocandins are given in the ____ setting. What organ system do they impact the most?
inpatient setting, IV administered hepatoxicity
32
Echinocandins have (large/small) effect on the CYP450 system and have (more/less) drug interactions than azoles
Minimal effect on CYP 450 and LESS DDI than azoles
33
What are the medications included in the Echinocandins?
caspofungin (Cancidas) anidulafungin (Eraxis) micafungin (Mycamine)
34
_____ not well known - may act on cell wall and DNA synthesis
Mitotic Inhibitors :Griseofulvin
35
What are the indications for Griseofulvin?
Dermatophyte (tinea) infections of hair and skin
36
What are the DDI with Griseofulvin?
alcohol, contraceptives, warfarin, barbiturates Can cause “disulfiram”-type reaction with ETOH
37
What are the CI to Griseofulvin? What is the major one?
liver failure, porphyria, *pregnancy*
38
What are the SE of Griseofulvin? What is the most common? What is the most serious?
*HA* ,GI upset, skin rashes, dizziness Serious - hepatotoxicity, teratogenic, *granulocytopenia* Need weekly CBCs
39
What test do you need to order on a pt taking griseofulvin?
weekly CBC to monitor their granulocytes
40
**What is an essential pt education point for griseofulvin?
Absorbed best in the presence of a fatty meal
41
What medication falls under the Allyamines?
Terbinafine (Lamisil)
42
_____ Interfere with ergosterol synthesis
allyamines Terbinafine (Lamisil)
43
What are the indications of Terbinafine (Lamisil)?
Oral - onychomycosis, dermatophyte (tinea) infections of hair and skin Topical - Dermatophyte (tinea) infections of hair and skin
44
What are the DDI of Terbinafine (Lamisil)?
numerous - certain beta-blockers, certain TCAs, tamoxifen, tramadol
45
What are the CI to Terbinafine (Lamisil)?
liver disease
46
What are the SE of terbinafine (Lamisil)? Which one is most common? Which one is the most serious?
*HA*, GI upset, skin rashes, taste disturbances *Serious - hepatotoxicity, neutropenia*
47
What test do you need to monitor on a pt taking Terbinafine (Lamisil)?
Monitor LFTs and CBC before and during tx Liver damage usually reversible, but case reports of liver failure and death
48
______ enters cells and is converted to 5-fluorouracil, which inhibits fungal RNA and protein synthesis
flucytosine (Ancobon)
49
What is the indication for flucytosine (Ancobon)?
Adjunct treatment - used in combination with amphotericin B For severe candidal or cryptococcal infections (immunocompromised pts)
50
What is the BBW with flucytosine (Ancobon)?
about use in pts with renal impairment
51
What are some SE of flucytosine (Ancobon)? What are the major ones?
increased renal function testing, *renal failure* hepatic injury, hepatotoxicity, GI upset *pancytopenia/aplastic anemia* CNS - peripheral neuropathy, confusion, psychosis, dizziness, ataxia
52
_____ inhibits glucan synthase, used to make part of the cell wall
ibrexafungerp (Brexafemme)
53
What is the drug class for ibrexafungerp (Brexafemme)?
triterpenoids
54
What is the indication for ibrexafungerp (Brexafemme)?
Vulvovaginal candidiasis (single-day treatment option)
55
What is the CI to ibrexafungerp (Brexafemme)? What are the SE?
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
____ and ____ are available OTC - indicated for dermatophytes (tineas)
Butenafine (Lotrimin) Tolnaftate (Tinactin)
57
____ 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)
Naftifine (Naftin)
58
______ are expensive , but now generic, more effective than clotrimazole and miconazole Indicated for dermatophytes, onychomycosis, seborrheic dermatitis
Ciclopirox (Loprox, Penlac)
59
____ is expensive, but has a generic version; equally effective as ciclopirox Indicated for onychomycosis
Tavaborole (Kerydin)
60
_____ is expensive and has no generic More effective than clotrimazole, miconazole, and even ciclopirox Indicated for onychomycosis
Efinaconazole (Jublia)
61

Infectious Disease (16 decks)

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