42: antifungals

Question 1

MoA of polyene antibiotics?

Answer 1

bind to ergosterol –> inc. permeabiltiy –> leak content

Question 2

resistance to polyene antibiotics?

Answer 2

reduced ergosterol in membrane

Question 3

amphotericin B ROA:

Answer 3

topical
IV
intrathecal
intraventricular

Question 4

amphotericin B - available in formulation:

Answer 4

lipid formulation

(deoxycholate) - colloid suspension

Question 5

which polyene is broad spectrum?

Answer 5

amphotericin B

Question 6

what will u use for cryptococcal meningitis ?

Answer 6

1. amphotericin B + flucytosine

2. fluconazole

Question 7

amphotericin B is indicated for:

Answer 7

histoplasmosis,
cryptoccal mengitis
candida
coccidiodes 
mucormycosis
fusariosis
blastomyces
aspergillus 
mycotic corneal ulcers
keratitis
fungal arthritis

Question 8

amphotericin B - Adverse effects - infusion related?

Answer 8

fever
chills
muscle spasm
vomiting
headache

Question 9

amphotericin B - increase dose toxicity causes:

Answer 9

nephrotoxicity
acute liver failure
cardiac arrythmias
anemia
leukopenia

Question 10

if amphotericin B is given intrathecally it might cause?

Answer 10

seizures, chemical arachnoiditis

Question 11

what is the route of administeration of Amphotericin B for treatment of meningitis?

Answer 11

IV

Question 12

nystatin ROA:

Answer 12

topical , oral

Question 13

which polyene antibiotic can be given orally and topically?

Answer 13

nystatin

Question 14

oral nystatin is used to treat?

Answer 14

intestinal candidiasis

Question 15

natamycin is available as what type of fomulation ?

Answer 15

ophthalmic suspension

Question 16

natamycin is inidcated for? (3)

Answer 16

blephritis
conjunctivitis
keratitis

Question 17

which group of drugs is acting by inhibiting 14 a-demethylase ?

Answer 17

azole derivatives

Question 18

which azole is least likely to inhibit CYP3A4

Answer 18

fluconazole

Question 19

topical antifungals include?

Answer 19

nystatin
clotrimazole
econazole
amphotericin B
ciclopirox
allylamines (naftafine, terbinafine)
tolnaftate

Question 20

itraconazole ROA?

Answer 20

oral

Question 21

itraconazole formulation

Answer 21

capsule, liquid as cyclodextrin

Question 22

treatment for oncyhomycosis - oral?

Answer 22

1. itraconazole

2. terbinafine

Question 23

chronic use of which antifungal leads to increased risk of birth defects during 1st trimester?

Answer 23

fluconazole

Question 24

which antifungal best penetrates CSF and is used for fungal menigitis treatment?

Answer 24

fluconazole

Question 25

single of dose of which antifungal can eradicate acute vaginal candidiasis ?

Answer 25

fluconazole

Question 26

prophylaxis/treatment of cryptococcal meningitis in AIDS patients we use:

Answer 26

fluconazole

Question 27

if patient was treated with amphotericin B and flucytosine for meningitis he should be given, which drug as followup therapy?

Answer 27

fluconazole

Question 28

which azoles can be given IV?

Answer 28

voriconazole fluconazole posaconazole

Question 29

which azoles require gastric acid for absorption and should not be given with gastric acid inhibitors?

Answer 29

ketoconazole itraconazole posaconazole

Question 30

adverse effects of azoles?

Answer 30

gi distress skin rash hepatotoxicity hematologic toxicity

Question 31

which antifungal is 60-100 times better than fluconazole at treatment of candidiasis?

Answer 31

voriconazole

Question 32

which antifungal has greater fungicidal activity then amphotericin B against invasive aspergillosis?

Answer 32

voriconazole

Question 33

adverse effect of voriconazole

Answer 33

``` visual disturbance (altered light preception, abnormally colored vision, photophobia) hepatic failure ```

Question 34

what is used for treatment of seborrheic dermatidis?

Answer 34

ketoconazole

Question 35

for topical oncyhomycosis?

Answer 35

efinaconazole

Question 36

clortimazole is used for?

Answer 36

topical for: 1. mucocutaneous candida - mouth, throat, vagina. vulva 2. mallasezia furfur - tinear versicolor 3. dermatophyte tinea pedis

Question 37

posaconazole indication?

Answer 37

rhizopus , mucor | fusarium, aspergillus

Question 38

which antifungal acts by inhibiting squalene epoxidase?

Answer 38

allylamine drugs

Question 39

which allylamine is available oral and topical?

Answer 39

terbinafine

Question 40

side effects of terbinafine?

Answer 40

``` steven johnson syndrome toxic epidermal necrolysis liver failure SLE exacerbation neutropenia lymphopenia ```

Question 41

terbinafine indication?

Answer 41

oral: oncyhomycosis topical: superficial dermatophyte infection

Question 42

echinocandin drugs: MOA

Answer 42

inhibit 1,3 B glucan -->inhibit cell wall synthesis

Question 43

casponfungin ROA

Answer 43

IV

Question 44

micafungin indication

Answer 44

prophylaxis/treatment of systemic candidal/ invasive aspergillus

Question 45

which antifungal is a pyrimidine antimetabolite?

Answer 45

flucytosine

Question 46

flucytosine ROA

Answer 46

oral

Question 47

5-fluorouracil is an active form of which drug?

Answer 47

flucytosine

Question 48

cardiopulmonary arrest is an adverse effect of which antifungal?

Answer 48

flucytosine

Question 49

flucytosine is used in combo with amphotericin B for treatment of: (4 clinical indications)

Answer 49

1. pneumonia 2. septicemia 3. meningitis 4. endocarditis - -> by candida, cryptococcus

Question 50

which antifungal is highly lipophilic ?

Answer 50

griseofulvin

Question 51

griseofulvin MOA:

Answer 51

deposits in precursors of keratin cells of skin, hair, nails --> inhibit microtubule formation --> inihibition of mitosis of dermatophytes (it is fungistatic)

Question 52

grisofulvin ROA:

Answer 52

oral

Question 53

griseofulvin acitve against:

Answer 53

dermatophyte (epidermophyton, trichophyton, microsporum)

Question 54

adverse effects of griseofulvin?

Answer 54

1. dizziness 2. headache 3. insomnia 4. GI bleeding 5. hepatitis 6. skin rash 7. leukopenia

Question 55

does griseofulvin inhibit CYP3A4?

Answer 55

yes

Question 56

does caspofungin inhibit CYP3A4?

Answer 56

no

Question 57

ciclopirox ROA?

Answer 57

topical

Question 58

nail lacquer solutions available for fungal nail infections?

Answer 58

ciclopirox, amorolfine

Question 59

which antifungal is a nonprescription thiocarbamate drug?

Answer 59

tolnaftate

Question 60

interesting fact: clotrimazole is used for treatment of tinea versicolor (googled it)

Answer 60

keep in mind: clotrimazole is used for treatment of tinea versicolor (googled it)

Question 61

microtubule formation is associated with MOA of which drug?

Answer 61

griseofulvin ;)