Fungal Drugs- Exam 2 Flashcards
Fungal medications like to bind to _____, which is not present in human cells
Ergosterol
Why are Triazoles tend to get used the most? Are they systemic or topical?
better distribution
fewer side effects
fewer drug interactions
systemic
______ are primarily topicals
Imidazoles
____ Inhibit synthesis of ergosterol
Azoles
Name some substances that inhibit Azoles?
Grapefruit juice, alcohol (binge), several antibiotics and stomach acid-reducing products
Name some substances that speed up azoles?
Alcohol (chronic), several anticonvulsants
_____ may have less DDI than other azoles
Fluconazole
What are the SE of azoles?
GI upset (N/V/D, abdominal pain); HA; taste changes
Major - hepatotoxicity, prolonged QT, seizures, leukopenia, thrombocytopenia
Azoles needs to be cautious in the certain pt populations, including: ____, ____ and _____
hepatic or renal impairment
pregnancy
What trimester of pregnancy should azoles be avoided in?
greatest risk with systemic therapy in the FIRST semester
Due to the SE of azoles, which labs would be particularly important to check?
Liver function testing
What is the difference between all the azoles?
Fluconazole
Itraconazole
Voriconazole
Posaconazole. Increasing spectrum of activity as the list goes down FIVP
______ is the prototype azole drug and has the most limited spectrum of activity among systemic azoles
Fluconazole (Diflucan)
_____ is most commonly used in Candida albicans and Cryptococcus infections
Fluconazole (Diflucan)
What is Fluconazole (Diflucan) indicated for? Does it penetrate the CSF?
superficial fungal infections, uncomplicated systemic infections
Gets into CSF well
Yes! gets into CSF well
_____ is the drug of choice against histoplasmosis, sporotrichosis, blastomycosis. Variable bioavailability
Itraconazole (Sporanox)
_____ is the drug of choice for invasive aspergillosis
Voriconazole (Vfend)
Very broad-spectrum antifungals
Invasive fungal infections in immunocompromised pts, or resistant infections
What azoles?
Posaconazole (Noxafil) and isavuconazole (Cresemba
_____ gets into CSF well; _____
gets into brain tissue, but not CSF
Posaconazole
isavuconazole
____ and _____ are available OTC and are inexpensive
Clotrimazole and miconazole
What are the topical azoles? Which ones tend to work slightly better?
Econazole (Spectazole)
ketoconazole (Nizoral)
sulconazole (Exelderm)
may have slightly more efficacy than
older azoles :clotrimazole and miconazole
_____ bind to ergosterol in the fungal cell membrane, creating pores in the cell and causing leakage of cell contents
polyenes
_____ is considered very toxic and is only used topically. What class is it in?
nystatin
polyenes
Are polyenes absorbed well in the GI tract?
generally not absorbed well via GI tract
____ is mainly administered IV, and is indicated for severe, disseminated mycotic infection with a very broad spectrum of activity
Amphotericin B
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
____ is usually used topical and oral rinse and is indicated for non-invasive candidal infections.
Nystatin
What are the SE of Nystatin?
local irritation, allergic reaction
GI upset (N/V/D, abdominal pain)
____ inhibit synthesis of β-(1,3)-d-glucan, needed for fungal cell walls
Echinocandins
What are the indications for Echinocandins?
invasive fungal infections such as:
Disseminated candidiasis
Aspergillosis (especially in HIV+ patients)
Echinocandins are given in the ____ setting. What organ system do they impact the most?
inpatient setting, IV administered
hepatoxicity
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
What are the medications included in the Echinocandins?
caspofungin (Cancidas)
anidulafungin (Eraxis)
micafungin (Mycamine)
_____ not well known - may act on cell wall and DNA synthesis
Mitotic Inhibitors :Griseofulvin
What are the indications for Griseofulvin?
Dermatophyte (tinea) infections of hair and skin
What are the DDI with Griseofulvin?
alcohol, contraceptives, warfarin, barbiturates
Can cause “disulfiram”-type reaction with ETOH
What are the CI to Griseofulvin? What is the major one?
liver failure, porphyria, pregnancy
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
What test do you need to order on a pt taking griseofulvin?
weekly CBC to monitor their granulocytes
**What is an essential pt education point for griseofulvin?
Absorbed best in the presence of a fatty meal
What medication falls under the Allyamines?
Terbinafine (Lamisil)
_____ Interfere with ergosterol synthesis
allyamines
Terbinafine (Lamisil)
What are the indications of Terbinafine (Lamisil)?
Oral - onychomycosis, dermatophyte (tinea) infections of hair and skin
Topical - Dermatophyte (tinea) infections of hair and skin
What are the DDI of Terbinafine (Lamisil)?
numerous - certain beta-blockers, certain TCAs, tamoxifen, tramadol
What are the CI to Terbinafine (Lamisil)?
liver disease
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
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
______ enters cells and is converted to 5-fluorouracil, which inhibits fungal RNA and protein synthesis
flucytosine (Ancobon)
What is the indication for flucytosine (Ancobon)?
Adjunct treatment - used in combination with amphotericin B
For severe candidal or cryptococcal infections (immunocompromised pts)
What is the BBW with flucytosine (Ancobon)?
about use in pts with renal impairment
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
_____ inhibits glucan synthase, used to make part of the cell wall
ibrexafungerp (Brexafemme)
What is the drug class for ibrexafungerp (Brexafemme)?
triterpenoids
What is the indication for ibrexafungerp (Brexafemme)?
Vulvovaginal candidiasis (single-day treatment option)
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
____ and ____ are available OTC - indicated for dermatophytes (tineas)
Butenafine (Lotrimin)
Tolnaftate (Tinactin)
____ 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)
______ are expensive , but now generic, more effective than clotrimazole and miconazole
Indicated for dermatophytes, onychomycosis, seborrheic dermatitis
Ciclopirox (Loprox, Penlac)
____ is expensive, but has a generic version; equally effective as ciclopirox
Indicated for onychomycosis
Tavaborole (Kerydin)
_____ is expensive and has no generic
More effective than clotrimazole, miconazole, and even ciclopirox
Indicated for onychomycosis
Efinaconazole (Jublia)
