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Pharmacology > Antimalarials > Flashcards

Antimalarials Flashcards

1
Q

cases of malaria per year

A

300-500 million

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2
Q

cause of plasmodium vivax

A

hypnozoites in the liver

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3
Q

location for plasmodium falciparum

A

tropics

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4
Q

location for plasmodium vivax

A

subtropics and temperate regions

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5
Q

location for plasmodium ovale

A

West Africa

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6
Q

most malarial deaths are due to what plasmodium?

A

falciparum

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7
Q

form of malaria injected by mosquito

A

sporozoite

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8
Q

form of malaria made in the liver

A

merozoite

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9
Q

hypnozoite

A

latent stage of relapsing vivax and ovale cause this form

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10
Q

sexual stages that are taken up by mosquitos

A

gametocytes

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11
Q

Drugs that kill sporozoites

A

none, can’t prevent infection

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12
Q

Chemoprophylaxis can do what?

A

prevent development of symptoms caused by asexual erythrocytic forms

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13
Q

Complete elimination of infection (radical cure)

A

requires more than one drug

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14
Q

Schizonticides tissue, blood act on

A

liver forms, RBC forms

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15
Q

Gametocides

A

kill sexual stages and prevent transmission to mosquitos

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16
Q

Liver exoerythrocytic schizonticides include

A

primaquine, atovaquine, and artemisinins

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17
Q

chloroquine is an

A

aminoquinolone

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18
Q

chloroquine is used for treatment of

A

non-falciparum erythrocytic stage and chemoprophylaxis

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19
Q

chloroquine will NOT eliminate

A

hypnozoites

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20
Q

MOA of chloroquine

A

concentrates in food vacuoles for parasite and limit hemozoin production so cause parasite death through heme toxicity

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21
Q

resistance to chloroquine

A

pfMDR1 esp in vivax and falciparum

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22
Q

some side effects of chloroquine

A

pruritis, nausea, dairrhea

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23
Q

contraindication of chloroquine

A

psoriasis, porphyria, retinal field defects, myopathy

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24
Q

what will influence absorption of chloroquine

A

calcium and magnesium containing antacids and antidiarrheals

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25
Q

artemesinin MOA

A

endoperoxide active group that produces toxic free radicals through interacting with intracellular iron

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26
Q

artemesinin

A

rapidly acting blood schizonticide for all species with no effect on liver stage

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27
Q

limiting factor of artemesinin

A

short half life with recrudescence rate high after short course of treatment

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28
Q

what would you NOT use artemesinin for?

A

chemoprophylaxis

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29
Q

What is a problem you come across in combination therapy with artamesinin

A

short half life means resistance in partner drug becomes a concern

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30
Q

what drugs would you pair with artemesinin

A

meflouquine and lumefantrine

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31
Q

Coartem

A

artemether + lumefantrine

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32
Q

artemesinin administration

A

insoluble, oral admin

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33
Q

artamether administration

A

lipid soluble, oral, IM, rectal admin

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34
Q

artesunate administration

A

water soluble, oral, IM, IV, rectal admin

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35
Q

dihydroartemesinin admin

A

water soluble, oral admin

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36
Q

adverse effect of artemesinin, consequence

A

embryotoxic, no use in first trimester of uncomplicated malaria

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37
Q

quinine and quinidine

A

rapidly acting blood schizonticide against all Plasmodium and babesiosis

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38
Q

quinidine and quinine treatment important for

A

first line alternate drug for falciparum

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39
Q

downside of quinine and quinidine

A

very toxic

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40
Q

sever falciparum malaria, give quinine/ quinidine

A

IV

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41
Q

quinine and quinidine are metabolized by

A

CYP3A4

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42
Q

consequences of quinine and quinidine admin because of liver

A

raise levels of warfarin, digoxin and interacts with antiretroviral drugs

43
Q

adverse effects of quinine

A

cinchonism, cardiotoxicity, mild uterine contractions, blackwater fever, severe hypotension

44
Q

cinchonism

A

tinnitis, headache, nausea, dizziness, flushing, visual disturbances

45
Q

how do you get severe hypotension with quinine treatment?

A

too rapid of infusion

46
Q

mefloquine

A

synthetic 4-quinolone derivative

47
Q

mefloquine treats

A

prophylactic and treatment of erythrocytic falciparum and vivax

48
Q

adverse reaction mefloquine

A

neurological problems, seizures, sleep disturbances

49
Q

mefloquine brand name

A

Lariam

50
Q

Primaquine

A

8 aminoquinolone

51
Q

MOA primaquine

A

ROS involved

52
Q

primaquine treats

A

liver stages of P. vivax and ovale(hypnozoite) and gametocidal to all four

53
Q

primaquine admin how?

A

short term orally

54
Q

contraindication of primaquine

A

G6PDH deficiency, granulocytopenia, methemoglobinemia, patients on myelosuppressive drugs

55
Q

Why should you not use primaquine in pregnant patients?

A

fetus is G6PDH deficient

56
Q

if an individual has G6PDH and you give primaquine, what happens

A

hemolytic anemia

57
Q

Fansidar consists of

A

pyremethamine + sulfodoxine

58
Q

what does sulfodoxine do?

A

inhibits dihydropteroate synthase (PABA > dihydrofolic acid)

59
Q

what does pyrmethamine do?

A

inhibits dihydrofolate reductase (dihydrofolate > tetrahydrofolate)

60
Q

Fansidar treats

A

erythrocytic schizonticides and toxoplasmosis

61
Q

sulfadiazine can be replaced by what drug in Fansidar?

A

clindamycin

62
Q

What would you treat pneumocystis with?

A

trimethoprim + sulfamethoxazole

63
Q

why should you not use single antifolates?

A

Resistance develops easily

64
Q

when synergistically used, what happens to the dose of each component

A

20 fold reduction

65
Q

half life of pyrmethamine

A

90 hours

66
Q

half life of sufadoxine

A

170 hours

67
Q

proguanil?

A

antifolate drug

68
Q

Atavaquone?

A

disrupts mitochondrial electron transport

69
Q

Malarone

A

proguanil + atavaquone

70
Q

why dont you use atavaquone on its own?

A

develops resistance really quickly

71
Q

Atavaquone treatment for what else?

A

P. jiroveci

72
Q

What do you use malarone for primarily?

A

chemoprophylaxis and falciparum treatment

73
Q

what antibiotics are used as antimalarials?

A

tetracycline, doxycycline, clindamycin

74
Q

what do antibiotics in malaria target?

A

components of the apicoplast as blood schizonticide

75
Q

what is an apicoplast?

A

plant like organelle that carries out many biochemical processes

76
Q

What do you tend to pair doxycycline with in malaria tx?

A

quinine/ quinidine for falciparum malaria, chemoprophylaxis

77
Q

metronidazole is the drug of choice for what

A

extraintestine E. histolytica, giardiasis, and trichomoniasis

78
Q

what does metronidazole kill?

A

trophozoites, not cysts

79
Q

what do you follow metronidazle with?

A

luminal drug to eliminate asymptomatic infection

80
Q

what is the brand name of metronidazole?

A

Flagyl

81
Q

what is the antabuse effect related to?

A

metronidazole and alcohol ingestion

82
Q

what is metronidazole going to inhibit that causes the antabuse effect?

A

acetaldehyde dehydrogenase

83
Q

Iodoquinol

A

luminal amecide used in conjunction with metronidazole to kill trophozoites

84
Q

problem with iodoquinol?

A

low bioavailability

85
Q

where does iodoquinol act?

A

GI lumen

86
Q

pentamidine

A

aromatic diamidine

87
Q

how to admin pentamidine

A

parenteral

88
Q

what to use pentamidine for

A

trypanosomiasis in West Africa

89
Q

problem with pentamidine

A

highly toxic!

90
Q

Nifurtimox

A

commonly used in T. cruzi

91
Q

MOA nifurtimox

A

reduction, oxidation, ROS production

92
Q

what does nifurtimox do to illnesses?

A

reduces severity of acute phase

93
Q

Limitation of nifurtimox

A

no complete elimination of parasite, no prevention of disease progression

94
Q

toxicity issues with nifurtimox

A

hypersensitivity, GI

95
Q

how long does nifurtimox tend to be used?

A

3-4 months

96
Q

miltefosine used for

A

anti cancer, anti leshmaniasis (visceral)

97
Q

miltefosine

A

phospholipid analog

98
Q

miltefosine cure rate in visceral leshmaniasis

A

100% after 28 daily doses

99
Q

main side effect of miltefosine

A

teratogenic

100
Q

nitazoxanide treats

A

giardia, cryptosporidium

101
Q

Early stage of West African Sleeping Sickness treated iwth

A

Pentamidine

102
Q

Late stages of West African Sleeping Sickness treated with

A

Eflornithine

103
Q

East African Sleeping Sickness Early stages

A

Suramin

104
Q

Late stage East African Sleeping Sickness

A

melarsoprol

Pharmacology (3 decks)

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