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IBI Test 3 > B3.046 - Antifungal and Antiparasitic Therapy > Flashcards

B3.046 - Antifungal and Antiparasitic Therapy Flashcards

1
Q

Why are fungi so hard to target selectively

A

they are eukaryotes

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2
Q

Targets for antifungal chemo

A
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3
Q

what does Amphotericin B do and what is it

A

Its a polyene antibiotic
Binds to Ergosterol in fungal membranes

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4
Q

Amphotericin B is given how, where is it distributed and what is the half life

A

IV or Intrathecal

Widely dist. except CNS

t1/2 2 weeks

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5
Q

what is a required component of the lipid membrane of fungi and what drug targets it

A

Ergosterol, Amphotericin B

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6
Q

What is the resivoir for amphotericin B

A

liposomes

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7
Q

Rank what has the highest affinity for amphotericin between fungal membrane, human membrane, liposome

A

Fungal membrane 10 >Liposome 1 >Human membrane 0.1

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8
Q

Clincal uses of Amphotericin B

A

Most important available durg for severe systemic mycoses

Wide range of fungal infections

Use for initial intervention, then switch to other antifungals for maintenence, cure

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9
Q

Name the drug:

Most important available durg for severe systemic mycoses

Wide range of fungal infections

Use for initial intervention, then switch to other antifungals for maintenence, cure

A

Amphotericin B

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10
Q

Adverse effects of amphotericin B

A

Usually: Chills, fever, nausea, vomiting, headache almost always

Nephrotoxicity common often irreversible

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11
Q

Mechanism of 5-Fluorocytosine

A

Activated by fungal cystosine deaminase

Blocks DNA and RNA synthesis

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12
Q

pharmacokinetics of flucytosine

A

orally effective, widely distributed inlcuding CNS

excreted in urine

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13
Q

adverse effects flucytosine

A

low toxicity to patient (not activated in human cells)

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14
Q

clinical use of flucytosine

A

narrow specturm, cryptococus some candida

resistance develops rapidly, have to administer with other drugs like amphotericin B or intraconazole

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15
Q

Mechanism of azoles

A

inhibit ergesterol synthesis (fungal CYPs)

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16
Q

Ketonazole used for and given

A

oral antifungal for systemic disease

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17
Q

does ketoconazole go to CNS

A

no

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18
Q

adverse effects of ketoconazole

A

nausea, vomiting, anorexia

hepatotoxicity

blocks adrenal steroidoenesis

inhibits drug metabolism

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19
Q

what is a distinct effect of ketoconazole

A

gynecomastia - abnormal breast development in males

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20
Q

itraconazole administration, uses

A

oral, IV

less effect on mammalian CYPs than ketoconazole

used for histoplasma, blastomyces, sporothrix

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21
Q

fluconazole administration

A

oral, topical, IV

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22
Q

distribution of fluconazole

A

gets into CNS!

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23
Q

voriconazole admin, location of metabolization, uses

A

IV or oral, metabolized in liver, little mam. CYP inhibtion,

active againts candida, dimorphic fungi

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24
Q

AEs of voriconazole

A

visual distrubances

color vision, accuity

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25
Q

which drug is better tolerated, more effective against aspergillus than amphecillin B

A

Voriconazole

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26
Q

how does caspofungin work

A

inhibtits cell wall synthesis by inhibiting beta(1-3) glucan for cell wall

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27
Q

how is caspofungin administered/excreted

A

IV, urine and feces

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28
Q
A
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29
Q

AEs of caspofungin

A

GI effects, flushing

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30
Q

uses of caspofungin

A

candida, empiric anti-fungal, salvage therapy for aspergillus

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31
Q

topical antifungal agent

A

nystatin, similar to amphotericin B

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32
Q

systemic drugs for topical infection

A

Griseofulvin

Terbinafine

33
Q

how is griseofulvin administered, and what is it used for

A

orally, ringworm for athletes foot

34
Q

terbinafine administration, use

A

orally, can be topically

inhibits squalene epoxidase (ergosterol synthesis)

35
Q

what drug deposits/concentrations in keratinized tissues

A

griseofulvin

36
Q

what is the only drug that affects tissue schizonts

A

Primaquine

37
Q

where does malaria mature in the body

A

liver

38
Q

why has malaria incidence gone down

A

insectside developments

39
Q

what plasmodium have to be killed in liver as well as blood

A

vivax and ovale

40
Q

chloroquine is an anti

A

malarial

41
Q

mechanism of chloroquine

A

alters metabolism/detoxification of heme by parasite

42
Q

how is cholorquine given, distributed, excreted

A

orla or PE

Rapid, wide distribution

excreted in urine

43
Q

clinical uses of choroquine what does it do/to what

A

highly effective blood schizonticide

ONLY in blood bourne disease

acutely kills parasite from all 4 sp

curative for pl malaria, p. knowlsi sn. p fallciparum

44
Q

what do you combine chloroquien with to kill ovale and vivax

A

primaquine

45
Q

why do you give chloroquine prophylactively and after return

A

to kill all through lifecycle

46
Q

adverse effects of chloroquine

A

pruitis, GI, resistance esp in falciparum

47
Q

mechanism of resistacne to chloroquine

A

p-glycoprotien mumping mechanism

48
Q

mefloquine pharmacokinetics

A

only oral, well absorbed, metabolized in liver, excreted in feces

49
Q

adverse effects of mefloquine

A

GI, CNS, possible psychotropic effects

50
Q

clinical uses of mefloquine

A

prophylaxis for chloroquine resistant areas

51
Q

quinine how its given, distribution, metabolism

A

oral, doesnt cross BBB, metabolized by CYp3A4

52
Q

adverse effects of quinine

A

cinchonism - headache, sweating, nausea, tinnitus, dizzines, blurred vision

QT prolongation

53
Q

use of quinine

A

acute treatment when chloroquine resistance is present and adverse effects are tolerable

54
Q

malarone is a combo of what

A

atovaquone/proguanil

55
Q

what does atovaquone do, how is it given, half life

A

inhibits ETC, mit fxn

oral

2-3 day half life

56
Q

proguanil

what does it do, half life

A

12 hr, inhibits protozoal dihydrofolate reductase

57
Q

what is malarone used for

A

prophylaxis or treatment

58
Q

what is resistant to malarone

A

p. falciparum

59
Q

fansidar is a combo of what

A

pyrimethamine-sulfadoxine

60
Q

what does fansidar do

A

anti-folate combination

blocks synthesis/utilization of folic acid

61
Q

what does arteminisinin do and what is it used for

A

traditional chinese medicine activated by oxidative metabolism, rapidly acting blood schizonticide useful for p. falciparum

62
Q

how is artemisinin administered

A

IV artesunate

63
Q

what is better about artesinate IV than artemisinin

A

lnger half life and IV if oral isnt possible

64
Q

what is theonly drug that can target liver part of malaria

A

primaquine

65
Q

primaquine is used in combo with what and for what

A

chloroquine for phrophylaxis or cure of p. vivax, p. ovale

66
Q

mtronidazole is a

A

tissue ameabocide

67
Q

how is metronidazole activated and whats it used for

A

electron donation

anaerobic/hypoxic site, used for anarobic infections

68
Q

pharmacokinetics/adverse effects of metronidazole

A

oral/IV, goes everyhwere including CNS, cleared in urine

nausea, headache, dry mouth, disulfiram effect

69
Q

what is a disulfram effect

A

used in alcoholism to make you feel bad bc you make a lot of acetaldehyde, you get it with metronidazole too

70
Q

nitozoxanide mech, pharmacokinetics, AE, uses

A

inhibits electron transport system (PFOR)

oral, well absorebed, most secreted into bile

Giardia lamblia, crpytosporidia parvum

few AEs

71
Q

pentamidine given, clinical uses, AEs

A

IV, IM or Aerosol

Doesnt enter CNS

pneumocystis - inhaled version of drug most common

Resp stimulation/depression, hypotension

72
Q

mebendazole is what type of drug

A

anti helminth chemo

73
Q

mebendazole is given how and why

A

Orally, GI bugs are target

74
Q

mech of mebendazole

A

blocks microtubue synthesis of helminths

75
Q

AEs of mebendazole

A

possibly embryotoxic

76
Q

albendazole mech

A

interferes with microtubule structures of helminths

77
Q

ivermectin/avermectin are

A

antihelmithics

78
Q

ivermectin uses

A

oral treatment for intestical strongyloidiasis and onchocercasias

79
Q

how does ivermectin work, AEs

A

inhibits chloride channels, no BBB crossing so its ok

headache, dizziness

IBI Test 3 (16 decks)

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