Pharm - Antifungals Part 2

Question 1

name 3 echinocandins

Answer 1

caspofungin
micafungin
anidulafungin

Question 2

general structure of echinocandins

Answer 2

large, cyclic peptides with long fatty acid chains

Question 3

MOA echinocandins

Answer 3

NONCOMPETITIVE inhibitor of B 1,3-glucan synthase

thus inhibits production of B 1,3 glucan polysaccharide, important component of fungal membrane

Question 4

true or false

echinocandins are competitive inhibitors of B 1,3-glucan synthase

Answer 4

FALSE

noncompetitive

Question 5

route administration echinocandins

Answer 5

IV

Question 6

resistance mechanism to echinocandins

Answer 6

mutation in B 1,3-glucan synthase

Question 7

AE echinocandins

Answer 7

generally well tolerated

can cause GI issues and flushing

Question 8

can echinocandins be used in pregnancy

Answer 8

NO - contraindicated

Question 9

caspfungin ____ the levels of tacrolimus

Answer 9

increases

Question 10

cyclosporine ____ the levels of caspofungin

Answer 10

increases

Question 11

what will rifampin do to caspofungin levels

Answer 11

DECREASE

rifampin is a strong CYP INDUCER

Question 12

2 ORAL drugs for mucocutaneous fungal infections

Answer 12

griseofulvin
terbinafine

Question 13

MOA of griseofulvin

Answer 13

inhibits fungal mitosis (division) by inhibiting spindle formation

does this by binding to tubulin - disrupts mitotic spindle and inhibits fungal mitosis

Question 14

true or false

griseofulvin is fungicidal

Answer 14

FALSE

fungistatic

Question 15

griseofulvin absorption increases with…

Answer 15

fatty foods

Question 16

griseofulvin is used for the systemic treatment of what 2 things

Answer 16

dermatophytosis (ringowrm - skin , hair, nails)
onychomycosis (nails)

Question 17

how does griseofulvin have a stronger affinity for diseased tissues?

Answer 17

bc it’s deposited in keratin precursor cells and gets tightly bound to new keratin - formed in area of fungal infection

Question 18

**DDI concern of griseofulvin

Answer 18

INDUCES CYPS!!!!! decreased levels of warfarin and phenobarbital

Question 19

AE griseofulvin

Answer 19

photosensitivity, rash, allergy

Question 20

MOA terinafine

Answer 20

inhibits the fungal enzyme squalene epoxidase

this prevents the conversion of squalene to squalene 2,3-epoxide, leading to an accumulation of squalene.

NO PROPER ERGOSTEROL SYNTHESIS

FUNGICIDAL

Question 21

terbinafine should not be given to which patients

Answer 21

hepatic and renal dysfunction

Question 22

rifampin will ____ the levels of terbinafine

Answer 22

decrease

Question 23

____ is a polyene macrolide like amphotericin B

Answer 23

nystatin

Question 24

true or false

like amphotericin B, nystatin is also amphipathic

Answer 24

true

Question 25

true or false nystatin can be given orally

Answer 25

FALSE cant be oral or parenteral - too toxic

Question 26

true or false nystatin is active against candida

Answer 26

true

Question 27

which topical antifungal is less selective for fungal CYPS and is thus pretty toxic to humans and no longer used systemically?

Answer 27

ketoconazole

Question 28

what was the first oral azole

Answer 28

ketoconazole but not used orally anymore

Question 29

uses for clotrimazole and miconazole

Answer 29

vulvovaginal candidiasis oral thrush dermatophytic infection seborrheic dermatitis

Question 30

clotrimazole and miconazole are used in which areas

Answer 30

skin and vagina small amt of it will be absorbed -- fungicidal for 2-3 days

Question 31

efinazonazole is used for the topical treatment of _______

Answer 31

onychomycoses (fungal infection of nail bed)

Question 32

AE efinaconazole

Answer 32

ingrown toenails, dermatitis, pain

Question 33

MOA of ciclopirox

Answer 33

inhibits metal-dependent enzymes that are responsible for degrading peroxides in the fungus cell. does this by chelating the di and tri valent cations (metals) necessary for these enzymes to work disrupts the fungal cell membrane

Question 34

MOA tolnaftate

Answer 34

inhibits squalene epoxidase in ergosterol synthesis

Question 35

tolnaftate is INEFFECTIVE against _______

Answer 35

candida

Question 36

tavaborole MOA

Answer 36

inhibits protein synthesis by inhibiting tRNA synthase

Question 37

what molecule is present in fungal cell membranes but NOT in animal cell membranes

Answer 37

ergosterol

Question 38

which antifungal drug inhibits microtubules

Answer 38

griseofulvin

Question 39

miconazole MOA

Answer 39

inhibits ergosterol synthesis by inhibiting 14a-sterol demethylase

Question 40

nystatin MOA

Answer 40

interferese with ergosterol function by binding ergosterol (same as amphotericin b)

Question 41

Terbinafine MOA

Answer 41

inhibits squalene epoxidase

Question 42

amphotercin B MOA

Answer 42

inhibits ergosterol function by binding to it (same as nystatin)

Question 43

flucytosine MOA

Answer 43

inhibits thymidylate synthesis, interfering with DNA production

Question 44

this antifungal is broad spectrum drug of choice for nearly all life threatening mycotic infections

Answer 44

amphotercin B

Question 45

2 toxic pieces of amphotericin B

Answer 45

-shock like fall in BP during IV infusion -renal toxicity (dose dep and may be severe)

Question 46

amphotercin B toxicity seems to be lower with the ____ formulaiton of the drug

Answer 46

lipid

Question 47

true or false metabolic alkalosis and decrease in body temp are common AE of amphotercin B

Answer 47

no - they're not

Question 48

true or false flucyostine works by inhibiting fungal DNA synthesis

Answer 48

true

Question 49

MOA azoles

Answer 49

inhibit the conversion of lanosterol to ergosterol

Question 50

MOA terbenifine

Answer 50

inhibit conversion squalene to lanosterol

Question 51

true or false there is no antifungal drug that inhibits squalene synthesis

Answer 51

true

Question 52

azoles inhibit the conversion of ___ to ___

Answer 52

lanosterol to ergosterol

Question 53

formation of artifical pores in the fungal membrane

Answer 53

amphotericin B

Question 54

Antifungal drug that causes renal toxicity

Answer 54

amphotericin B