Antiparistics Flashcards

1
Q

Antimalarials

A

Chloroquine, primaquine, artemether

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2
Q

Prophylactic antimalarials

A

Chloroquine and primaquine

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3
Q

Treatment antimalarials

A

Artemether/lumefantrine
Chloroquine
Primaquine

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4
Q

Blood stage antimalarials

A

Chloroquine

Artemether

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5
Q

Liver stage antimalarials

A

Primaquine

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6
Q

3 characteristics of prophylactic agents

A

Low toxicity
Orally effective
Long half-life

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7
Q

Prophylaxis prevents what stage of malaria?

A

Blood stage

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8
Q

Chloroquine MOA

A

Weak base trapped in acidic parasite
Inhibits biocrystallization to increase heme concentration in food vacuole

Heme toxic to parasite

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9
Q

Chloroquine uses

A

Clinical cure & Prophylaxis against sensitive strains

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10
Q

Is chloroquine safe for pregnancy?

A

Yes

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11
Q

Chloroquine side effects

A

CV toxicity

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12
Q

Chloroquine resistance due to…

A

Mutated vacuole efflux transporter (PfRCT)

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13
Q

Chloroquine does not work for…

A

P. Falciparum in Asia, Africa, S. America

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14
Q

Artemether MOA

A

Maybe converted to toxic free radicals by heme

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15
Q

Artemether Uses

A

Fixed dose w/ lumefantrine
Oral drug for MDR falciparum

Artesunate (IV)

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16
Q

Artemether side effects

A

Neurotoxicity & embryotoxicity

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17
Q

Artemether PK (when not w/ lumefantrine)

A

Absorbed from GI tract —> short half-life

Does NOT work as prophylactic

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18
Q

Artemether Fun Fact

A

Inactive counterfeit to mimic drug

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19
Q

Liver Antimalarial

A

Primaquine

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20
Q

Primaquine MOA

A

Unknown

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21
Q

Primaquine Uses

A

Clinical & radical cure of vivax/ovale (take w/ chloroquine)

Terminal prophylaxis for vivax/ovale regions

Primary prophylaxis if other drugs inappropriate

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22
Q

Primaquine side effects

A

Mild cyanosis in normal G6PD

Hemolytic anemia in G6PD deficiency

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23
Q

Primaquine contraindications

A

G6PD deficiency

Pregnancy

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24
Q

Antiprotozoal Drugs

A

Metronidazole

Paromomycin

25
Q

Common protozoans in USA

A

Trichomoniasis
Giardiasis
Amebiasis
Cryptosporidiosis

26
Q

Classifications of antiprotozoal agents

A

Systemic

Luminal - agents not absorbed

27
Q

Metronidazole classification

A

Systemic

28
Q

Metronidazole MOA

A

Prodrug

DNA damaging metabolite by anaerobic organism

29
Q

Metronidazole Uses

A

Amebiasis, giardiasis, trichomoniasis, anaerobic bacteria

For amebiasis, add luminal amebicide to eradicate luminal “survivors”

30
Q

Metronidazole side effects

A

Metallic taste
Red/brown urine
Carcinogenic

31
Q

Nitazoxanide uses

A

Diarrhea caused by cryptosporidiosis or giardiasis

32
Q

Nitazoxanide MOA

A

Pyruvate Ferrell in oxidoreductase inhibitor

33
Q

Paromomycin classification

A

Luminal antiprotozoal

34
Q

Paromomycin MOA

A

Binds 30s subunit of S hisolytica

Inhibits protein synthesis (not absorbed by GI, so can’t treat systemic infections)

35
Q

Paromomycin uses

A

Asymptomatic amebiasis (solo)

Amebic colitis/dysentery (combo w metro)

1st trimester pregnant pts w/ giardiasis

36
Q

Antihelminthics

A

Albendazole
Praziquantel
Ivermectin

37
Q

Nematodes

A

Round worms

38
Q

Cestodes

A

Tapeworms

39
Q

Trematodes

A

Flukes

40
Q

How do humans get worms?

A

Ingestion of eggs/larvae in food or soil to skin

Worms lodge in digestive tissue

41
Q

Neurocysticercosis

A

Ingestion of undercooked pork or feces contaminated w/ Taenia solium tapeworm eggs

Cysts in brain cause seizures

42
Q

Most common infection in kids in USA age 5-10 years old

A

Enterobiasis (pinworm)

43
Q

Single dose antihelminthic

A

Expels worms from GI tract

44
Q

Extended treatment antihelminthic

A

Systemically eradicate adults or developmental forms in other tissues

45
Q

Antihelminthic prototype

A

Albendazole

46
Q

Albendazole MOA

A

Block polymerization of B-tubulin, disrupts nematode motility and uptake of glucose

Cell death in ~3 days

47
Q

Best way to improve albendazole absorption

A

Take with fatty meal

48
Q

Active form of albendazole

A

Albendazole sulfoxide

49
Q

Albendazole uses

A

Cestode infections
Roundworm infections
Pinworm (400mg dose, two weeks apart)

50
Q

Albendazole side effects

A

Teratogenic
Liver toxicity
Bone marrow suppression

51
Q

Albendazole contraindications

A

Pregnancy

52
Q

Praziquantel MOA

A

Increases perm of trematode & cestode membrane to Ca, causes paralysis, dislodgement, and worm death

53
Q

Praziquantel use

A

Schistosomiasis
Most trematodes and cestodes
Cysticerosis

54
Q

Praziquantel side effects

A

Fever, rash, itching associated w/ protein release from dying worms

55
Q

Ivermectin MOA

A

Tonic muscle paralysis, activates glutamate gated Cl channels, hyperpolarization of cell

56
Q

Why does Ivermectin not effect human cells?

A

Human cells have p-glycoprotein efflux transporters

57
Q

Ivermectin uses

A

Fleas, ticks, mites
Onchocerciasis (river blindness)
Strongyloidiasis
Scabies, head lice

58
Q

Ivermectin side effects

A

Mazzotti reaction

Cleft palate

59
Q

Ivermectin contraindications

A

Pregnancy