Antifungals

Question 1

Itraconazole = Treatment of choice for

Answer 1

candida, endemic (dimorphic) fungi

Question 2

Nystatin treats

Answer 2

treat oral candidiasis

Question 3

Nystatin is active against

Answer 3

most Candida sp and is most commonly used for suppression of local candidal infections

Question 4

Allylamine subclass?

Answer 4

terbinafine

Question 5

Allylamine

Terbinafine spectrum?

Answer 5

Activity against fungi that cause tinea: trichophyton, epidermophyton, and microsporum

Tera been fine at the MET

Question 6

Allylamine

terbinafine, MOA

Answer 6

• Inhibits squalene epoxidase enzyme
• Causes accumulation of squalene which is toxic to cell

Question 7

Allylamine

terbinafine ( fungicial or fungistatic?)

Answer 7

fungicidal

Question 8

Allylamine

terbinafine, adverse effect?

Answer 8

hepatotoxicity

Question 9

Allylamine

terbinafine, contraindications

Answer 9

Can’t take if you have liver issues

Question 10

Long treatment time with no alcohol use (6-12 wks)

what antibiotic?

Answer 10

terbinafine

Question 11

Inhibits some ____ enzymes for terbinafine

Answer 11

liver

Question 12

Azoles

imidazoles, names

Answer 12

clotrimazole, miconazole, ketoconazole

Question 13

Azoles

imidazoles have __ nitrogens

Answer 13

2 nitrogens

Question 14

Miconazole is used to treat

Answer 14

cutaneous Candida infections

Question 15

Azoles

triazoles have __ nitrogen rings

Answer 15

3

Question 16

Azoles

triazoles, names

Answer 16

fluconazole, itraconazole, voriconazole

Question 17

Azoles

Clotrimazole and miconazole used topically for

Answer 17

vulvovaginal candidiasis

Question 18

Azoles

Oral clotrimazole treat

Answer 18

oral thrush

Question 19

Azoles

Imidazoles treat

Answer 19

• Dermatophytes (tinea) and candida

Question 20

Ketoconazole was used topically for

imdiazole

Answer 20

hair and scalp issues (tinea)

not anymore

Question 21

Fluconazole used for

Triazoles

Answer 21

candida (especially albicans) and cryptococcus

Question 22

Oral fluconazole is the preferred treatment for

triazoles

Answer 22

Candida esophagitis

Question 23

“diflucan”

fluconazole

Triazoles

Answer 23

vaginal yeast infections and thrush

Question 24

reduced bioavailability of itraconazole when taken with

Answer 24

rifamycins (rifampin, rifabutin, rifapentine)

Question 25

Voriconazole treats | triazoles

Answer 25

candida, and more so for aspergillus (less for endemic) - Treatment of choice for aspergilloses

Question 26

Azoles, -cidial or -static?

Answer 26

fungistatic

Question 27

# what antifungal Work on last step in ergosterol formation. lanosterol to ergostreol

Answer 27

azoles

Question 28

# what antifgunal? - Prevents conversion of lanosterol to ergosterol by inhibiting enzyme

Answer 28

azoles

Question 29

Azoles resistance

Answer 29

Resistance: * efflux pumps * target site alteration (mutate enzyme to prevent drug from binding) * bypass pathways * upregulations of lanosterol

Question 30

drug interaction for azoles

Answer 30

- Interfere with liver enzymes that metabolize medications (cP450) - Increased concertation of other medications * Higher risk of toxicity

Question 31

# adverse effects Fluconazole and voriconazole can cause | triazoles ## Footnote azoles

Answer 31

* QT elongation

Question 32

# adverse effects * vision changes and photosensitivy | medication?

Answer 32

Voriconazole | azoles ## Footnote triazoles

Question 33

is the broadest-spectrum member of the azole family, with activity against most species of Candida and Aspergillus

Answer 33

Posaconazole ## Footnote triazoles

Question 34

# adverse effects Edema Exacerbate heart failure

Answer 34

Itraconazole | azoles ## Footnote triazoles

Question 35

# adverse effects Cross blood brain barrier to treat meningitis

Answer 35

Fluconazole and Voriconazole | azoles ## Footnote triazoles

Question 36

Polyenes subclass?

Answer 36

(amphotericin B)

Question 37

amphotericin B, spectrum

Answer 37

Very broad and kill lots of different fungi

Question 38

- Used for severe fungal infection initially and then switched to another medication due to side effects | what antifungal?

Answer 38

Polyenes (amphotericin B)

Question 39

Amphotericin B is used to treat

Answer 39

systemic Candida infections

Question 40

amphotercin b, -cidial or -static?

Answer 40

fungicidal

Question 41

resistance for Polyenes (amphotericin B)

Answer 41

- Uses ergosterol to kill fungal cells * Binds to ergosterol and make a membrane pore - Not much resistance

Question 42

- Given only IV * Poorly bioavailable * Has a formulation with a liposome that makes it less toxic (nephrotoxic) | what antifungal

Answer 42

Polyenes (amphotericin B)

Question 43

# adverse effect Immediate onset: muscle spasms, headache, fever & chills (rigors), hypotension, electrolyte imbalance, nausea and vomiting | what antifungal?

Answer 43

Polyenes (amphotericin B)

Question 44

Delayed adverse effects for Polyenes (amphotericin B)

Answer 44

severe nephrotoxicity long term

Question 45

drug interactions for amphotericin b?

Answer 45

Vancomycin and aminoglycosides (antibiotics) | - Nephrotoxic drugs

Question 46

- Not great to use for pregnant women contraindications | 3 drugs

Answer 46

* Polyenes (amphotericin B) * Flucytosine * Echinocandins (micafungin, caspofungin, anidulafungin)

Question 47

Flucytosine is effective against

Answer 47

- Only effective against cryptococcus and some candida

Question 48

converted by cytosine deaminase to 5-flurouracil (active form) which inhibits DNA/RNA synthesis, what drug and why?

Answer 48

Flucytosine, Humans don’t have cytosine deaminase

Question 49

Amphotericin B make pore for flucytosine to

Answer 49

get into the fungi cell

Question 50

Flucytosine Resistance:

Answer 50

alteration of metabolic pathway to avoid activation step

Question 51

# what antifungal? Synergy: Always used with another drug (never used as monotherapy due to quick resistance)

Answer 51

Flucytosine

Question 52

# adverse effect of - Non-selective activation causes Bone marrow toxicity (decreases in blood cells) from amphotercin b

Answer 52

Flucytosine

Question 53

# Flucytosine Nephrotoxicity (bad when used with ___

Answer 53

amphotericin B

Question 54

Flucytosine is given

Answer 54

Orally bioavailable

Question 55

# Flucytosine Contraindication:

Answer 55

pregnancy especially in first trimester

Question 56

Echinocandins, 3 drugs

Answer 56

(micafungin, caspofungin, anidulafungin)

Question 57

Echinocandins treats? | (micafungin, caspofungin, anidulafungin)

Answer 57

- Candida and Aspergillus

Question 58

Echinocandins is used to treat | (micafungin, caspofungin, anidulafungin)

Answer 58

systemic candida infections

Question 59

Echinocandins is used as salvage therapy for | (micafungin, caspofungin, anidulafungin)

Answer 59

aspergillosis after voriconazole

Question 60

Echinocandins, -cidal or -static? | (micafungin, caspofungin, anidulafungin)

Answer 60

fungicidal

Question 61

Inhibits enzyme beta-1,3 glucan synthase | what antifungal?

Answer 61

Echinocandins | (micafungin, caspofungin, anidulafungin)

Question 62

Echinocandins they work on cell wall by | (micafungin, caspofungin, anidulafungin)

Answer 62

preventing the synthesis of Beta-1,3-glucans

Question 63

Echinocandins Resistance: | (micafungin, caspofungin, anidulafungin)

Answer 63

mutation of the glucan synthase so it cannot bind to echinocandin

Question 64

Echinocandins is not orally bioavailable so must be given | (micafungin, caspofungin, anidulafungin)

Answer 64

must be given IV

Question 65

is the agent most commonly used for the treatment of mucocutaneous candidiasis

Answer 65

Fluconazole