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Pharm > Antiparasitic > Flashcards

Antiparasitic Flashcards

1
Q

How many species of Plasmodium (malaria parasites) infect humans?

A

5

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2
Q

What are the the species of Plasmodium that infect humans?

A

Falciparum
Vivax
Ovale
Malariae
Knowlesi

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3
Q

What is the most common form of malaria?

A

Falciparum malaria

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4
Q

What is the most severe form of malaria?

A

falciparum malaria

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5
Q

What form of malaria is often lethal?

A

Cerebral form

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6
Q

Vivax malaria is…?

A

a milder but common form of malaria

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7
Q

Which form of malaria can relapse due to dormant hypnozoites that remain in the liver and are NOT affected by blood-stage antimalarials?

A

Vivax malaria

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8
Q

What are the two types of antimalarial chemotherapy?

A

Prophylaxis
Treatment of active or latent infection

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9
Q

What antimalarial agents are used for prophylaxis?

A

Cholorquine
Primaquine

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10
Q

What antimalarial agents are used to treat active or latent infections?

A

Chloroquine
Primaquine
Artemether/lumefantrine

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11
Q

What is another term for antimalarials?

A

Schizonticides

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12
Q

What are the two stages of malaria that drugs target?

A

Liver stage
Blood stage

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13
Q

During what stage of malaria do patients experience symptoms?

A

Blood Stage

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14
Q

Malaria drugs that target the blood stage produce a ____ cure

A

Clinical

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15
Q

Malaria drugs that target the liver stage produce a ____ cure

A

radical
(of relapsing malaria)

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16
Q

Are blood stage antimalarial effective against liver stage parasites?

A

No

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17
Q

What antimalarial drugs disrupts disease transmission? And by what activity?

A

Artemether and Primaquine
gametocidial activity

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18
Q

Chloroquine and Artemisinins are antimalarial drugs that target the ____ stage of malaria

A

Blood stage

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19
Q

Primaquine is an antimalarial drug that target the ____ stage of malaria

A

Liver stage

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20
Q

Orally effective, long half-lives and low toxicity are properties of what type of antimalarial agent?

A

Prophylactic

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21
Q

What does chemoprophylaxis treatment for malaria prevent?

A

symptomatic blood stage

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22
Q

How is antimalarial drug for a US traveler selected?

A

dependent on the resistant pattern of the intended destination

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23
Q

Since no regimen is fully protective for malaria, what else is important?

A

prevention of mosquito bites

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24
Q

Chloroquine is a weak organic acid/base?

A

base

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25
Q

inhibition of biocrystalization is the MOA of what antimalarial drug?

A

Chloroquine

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26
Q

what are the therapeutic uses of chloroquine?

A

clinical cure and prophylaxis against sensitive strains

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27
Q

what is used for prophylaxis and treatment of malaria during pregnancy

A

chloroquine

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28
Q

chloroquine is effective/ineffective against most strains of P. falciparum in Africa, Asia and s. America?

A

ineffective

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29
Q

Adverse reactions of chloroquine depend on …

A

low-dose (prophylaxis) vs. high-dose (clinical cure)

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30
Q

Cholorquine targets the blood/liver stage of malaria?

A

blood

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31
Q

True or False: chloroquine is generally well-tolerated at lower doses?

A

true

32
Q

At higher-doses, adverse reactions of chloroquine include:

A

pruritus
headache
GI
CV toxicity

33
Q

Artemether route of administration is…

A

oral

34
Q

artemether is derived from …

A

medicinal Chinese plant quinghao

35
Q

the MOA of artemether is

A

unclear
(drugs may form toxic free radicals in the presence of heme)

36
Q

what property of artemether makes the drug NOT useful for prophylaxis?

A

short half-life

37
Q

what is artemether used with in a fixed-dose combination

A

lumefantrine

38
Q

what is important about lumefantrine?

A

it is long acting, half life of 4.5 days, it sustains antimalarial activity during the frequent sub-therapeutic trough levels or artemether

39
Q

what is an important therapeutic use of artemether-lumefantrine?

A

first line oral of MDR falciparum malaria

40
Q

inactive counterfeits that closely mimic genuine drugs for malaria are common/uncommon

A

common

41
Q

artemether adverse reactions are

A

not well characterized, generally safe

42
Q

adverse reactions of artemether (in animal studies) include

A

neurotoxicity (in animals) and potent embryo toxicity (in animals)

43
Q

artemether is used to treat ____ stage of malaria

A

blood stage

44
Q

Why is it important that chloroquine is a weak organic base?

A

it becomes ionized in acidic environment which allows ion trapping in parasite food vacule (an infected RBC)

45
Q

what is the food source for malaria parasites?

A

globin from hemoglobin

46
Q

hematin is ____ to malaria parasites

A

toxic

47
Q

what is biocrystallization and why is it important for malaria parasites?

A

malaria parasites:
hematin —(biocrystallization) —> non-toxic hemozoin

48
Q

resistance to chloroquine is due to ….

A

mutated efflux transporter (PfCRT) that prevents drug accumulation

49
Q

Primaquine targets ____ stage of malaria

A

liver stage

50
Q

what is the MOA of primaquine?

A

it is unknown

51
Q

what are the three therapeutic uses of primaquine (oral)?

A
  1. with chloroquine to achieve clinical and radical cure of vivax/ovale malaria
  2. for terminal prophylaxis AFTER completion of travel to vivax/ovale endemic areas
  3. for primary prophylaxis against all species if other agents are inappropriate
52
Q

what are the two types of prophylaxis that are uses of primaquine?

A

primary and terminal

53
Q

primaquine is well tolerated but causes hemolytic anemia in _____ deficient patients

A

G6PD

54
Q

Besides G6PD-deficient patients, primaquine is contraindicated for

A

pregnant females (fetal G6PD status cannot be determined)

55
Q

What is a common genital STI protozoal infection in the US?

A

trichomoniasis

56
Q

giardiasis, amebiasis and cryptosporidiosis are …

A

all GI protozoal infections that are common in the US

57
Q

amebiasis infection occurs mainly in the GI and the infection can ….

A

be asymptomatic, mild-mod (colitis) or severe (dysentery)

58
Q

antiprotozoal agents for GI protozoal infections are classified as ____ or ______

A

systemic or GI luminal

59
Q

what is a systemic antiprotozoal agent?

A

metronidazole

60
Q

what is a luminal antiprotozoal agent?

A

paromomycin

61
Q

metronidazole MOA

A

prodrug converted to DNA-damaging metabolite in anaerobic organisms

62
Q

two therapeutic uses of metronidazole are …

A
  1. treat amebiasis (given in combo with a luminal amebicide to eradicate luminal survivors)
  2. anaerobic bacterial infections
63
Q

why is metronidazole given in combination with a luminal amebicide?

A

to eradicate luminal survivors because metronidazole levels in the GI tract are low due to its complete oral absorption

64
Q

what class is parmomycin?

A

aminoglycoside

65
Q

MOA of paromomycin

A

binds to 30S subunit to inhibit protein synthesis

66
Q

is paromymycin absorbed from the GI tract?

A

No, it is a luminal antiprotozoal agent

67
Q

what is the prototype drug for benzimidazoles?

A

albendazole

68
Q

MOA of albendazole

A

inhibits polymerization of parasite B-tubulin, preventing formation of cytosolic microtubules

69
Q

Antihelminthics include …

A

albendazole, ivermectin

70
Q

uses for albendazole and how is it used?

A
  1. enterobiasis infection, single 400 mg dose repeated 2 weeks later
  2. cestode and roundworm infections
71
Q

adverse effects of albendazole

A

teratogenic effect in animal, long term–liver toxicity, bone marrow suppression

72
Q

immobilization by tonic muscle paralysis is the MOA of what antihelminthic drug?

A

Ivermectin

73
Q

how does ivermectin cause tonic muscle paralysis in helmniths?

A

(+) glutamate-gated Cl- channels only found in invertebrate neurons, causes hyperpolarization of neuronal membrane

74
Q

how is ivermectin kept out of the CNS in the host?

A

P-glycoprotein efflux transporter in host BBB

75
Q

three uses of ivermectin include:

A
  1. broad spectrum agent to treat ticks, fleas, mites in vet medicine
  2. onchocerciasis (river blindness)
  3. scabies, head lice
76
Q

adverse effects of ivermectin

A

mazzotti reaction
teratogenic potential (cleft palate in animals)

77
Q

what is a mazzotti reaction and when does it occur?

A

adverse reaction of ivermectin that occurs in onchocerciasis. It is an immune reaction to drying worms. Includes: pruritus, rash, fever, lymphedema

Pharm (6 decks)

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