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D&D Infectious Disease FINAL > Pharm - Antifungals Part 2 > Flashcards

Pharm - Antifungals Part 2 Flashcards

1
Q

name 3 echinocandins

A

caspofungin
micafungin
anidulafungin

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2
Q

general structure of echinocandins

A

large, cyclic peptides with long fatty acid chains

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3
Q

MOA echinocandins

A

NONCOMPETITIVE inhibitor of B 1,3-glucan synthase

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

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4
Q

true or false

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

A

FALSE

noncompetitive

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5
Q

route administration echinocandins

A

IV

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6
Q

resistance mechanism to echinocandins

A

mutation in B 1,3-glucan synthase

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7
Q

AE echinocandins

A

generally well tolerated

can cause GI issues and flushing

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8
Q

can echinocandins be used in pregnancy

A

NO - contraindicated

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9
Q

caspfungin ____ the levels of tacrolimus

A

increases

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10
Q

cyclosporine ____ the levels of caspofungin

A

increases

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11
Q

what will rifampin do to caspofungin levels

A

DECREASE

rifampin is a strong CYP INDUCER

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12
Q

2 ORAL drugs for mucocutaneous fungal infections

A

griseofulvin
terbinafine

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13
Q

MOA of griseofulvin

A

inhibits fungal mitosis (division) by inhibiting spindle formation

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

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14
Q

true or false

griseofulvin is fungicidal

A

FALSE

fungistatic

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15
Q

griseofulvin absorption increases with…

A

fatty foods

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16
Q

griseofulvin is used for the systemic treatment of what 2 things

A

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

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17
Q

how does griseofulvin have a stronger affinity for diseased tissues?

A

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

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18
Q

**DDI concern of griseofulvin

A

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

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19
Q

AE griseofulvin

A

photosensitivity, rash, allergy

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20
Q

MOA terinafine

A

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

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21
Q

terbinafine should not be given to which patients

A

hepatic and renal dysfunction

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22
Q

rifampin will ____ the levels of terbinafine

A

decrease

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23
Q

____ is a polyene macrolide like amphotericin B

A

nystatin

24
Q

true or false

like amphotericin B, nystatin is also amphipathic

A

true

25
Q

true or false

nystatin can be given orally

A

FALSE

cant be oral or parenteral - too toxic

26
Q

true or false

nystatin is active against candida

A

true

27
Q

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

A

ketoconazole

28
Q

what was the first oral azole

A

ketoconazole

but not used orally anymore

29
Q

uses for clotrimazole and miconazole

A

vulvovaginal candidiasis
oral thrush
dermatophytic infection
seborrheic dermatitis

30
Q

clotrimazole and miconazole are used in which areas

A

skin and vagina

small amt of it will be absorbed – fungicidal for 2-3 days

31
Q

efinazonazole is used for the topical treatment of _______

A

onychomycoses (fungal infection of nail bed)

32
Q

AE efinaconazole

A

ingrown toenails, dermatitis, pain

33
Q

MOA of ciclopirox

A

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

34
Q

MOA tolnaftate

A

inhibits squalene epoxidase in ergosterol synthesis

35
Q

tolnaftate is INEFFECTIVE against _______

A

candida

36
Q

tavaborole MOA

A

inhibits protein synthesis by inhibiting tRNA synthase

37
Q

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

A

ergosterol

38
Q

which antifungal drug inhibits microtubules

A

griseofulvin

39
Q

miconazole MOA

A

inhibits ergosterol synthesis by inhibiting 14a-sterol demethylase

40
Q

nystatin MOA

A

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

41
Q

Terbinafine MOA

A

inhibits squalene epoxidase

42
Q

amphotercin B MOA

A

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

43
Q

flucytosine MOA

A

inhibits thymidylate synthesis, interfering with DNA production

44
Q

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

A

amphotercin B

45
Q

2 toxic pieces of amphotericin B

A

-shock like fall in BP during IV infusion

-renal toxicity (dose dep and may be severe)

46
Q

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

A

lipid

47
Q

true or false

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

A

no - they’re not

48
Q

true or false

flucyostine works by inhibiting fungal DNA synthesis

A

true

49
Q

MOA azoles

A

inhibit the conversion of lanosterol to ergosterol

50
Q

MOA terbenifine

A

inhibit conversion squalene to lanosterol

51
Q

true or false

there is no antifungal drug that inhibits squalene synthesis

A

true

52
Q

azoles inhibit the conversion of ___ to ___

A

lanosterol to ergosterol

53
Q

formation of artifical pores in the fungal membrane

A

amphotericin B

54
Q

Antifungal drug that causes renal toxicity

A

amphotericin B

55
Q
A

D&D Infectious Disease FINAL (21 decks)

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