Burkin: Parasitic Pharmacology Flashcards

1
Q

What are these drugs used for?

Quinine
Chloroquine
Primarquine
Antimetabolites

A

Malaria

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2
Q

What are other drugs used to treat protozoan parasites?

A

metronidazole
diloxanide
nifurtimox
suramin

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3
Q

Which antimalarial drug is active against malaria when it is NOT in RBCs? What about when it is in RBCs?

A

primaquine; chloroquine and quinine

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4
Q

Different antimalarial drugs act at different stages of the malarial parasite’s life cycle. Which drug works when the parasite is NOT within RBCs?

A

paraquine

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5
Q

What is the method of action of quinine? What is it used to treat?

A

blocks heme polymerization so that heme concentrations are at toxic levels to parasites; used to treat chloroquine resistant Plasmodium falciparum

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6
Q

What is an adverse reaction caused by quinine?

A

cinchonism (similar to salicylate toxicity), curare effect, myocardial depression

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7
Q

How does chloroquine work? What is it used to treat?

A

blocks polymerization of heme, leading to toxic heme concentrations (toxic to parasites); works against ERYTHROCYTIC forms - used for acute malarial attacks, prophylaxis (prevention)

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8
Q

What are the effects of chloroquine if used for prophylaxis? If used acutely? If used in large doses?

A

little toxicity; anorexia, vomiting, nausea, headache; photosensitivity, retinopathy, leukopenia

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9
Q

How does primaquine work?

A

binds to DNA –> damages mitochondria via oxidative stress –> inhibits protein synthesis

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10
Q

What is primaquine used for?

A

liver forms of P. vivax and P. ovale

**not very effective against P. falciparum or P. malariae

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11
Q

Adverse reactions for primaquine?

A

same as chloroquine + hemolytic anemia

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12
Q

What types of patients are particularly prone to hemolytic anemia while taking primaquine?

A

those with G6PDH deficiency

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13
Q

How does pyrimethamine-sulfadoxine work?

A

inhibits dihydrofolate reductase (in PABA/DHF/THF pathway) - no folic acid synthesis - can’t form DNA

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14
Q

What is the pathway that takes PABA to DNA and RNA?

A

PABA –> DHF acid via sulfadoxine
DHF –> THF via pyrimethamine
THF –> DNA and RNA

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15
Q

What is pyrimethamine-sulfadozine used to treat?

A

cholorquine-resistant P. falciparum

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16
Q

What is the mechanism of action of metronidazole?

A

prodrug that is activated by electron transport proteins in ANAEROBES and PROTOZOANS –> produces cytotoxic metabolites that damage DNA

17
Q

What is metronidazole used for?

A

amebiasis
trichomoniasis
giardiasis
anaerobic bacterial infections

18
Q

What is one adverse effect to keep in mind when talking about metronidazole?

A

potentially mutagenic to fetus

19
Q

What is the mechanism of action of Nifurtimox? What is it used for?

A

oxidative damage to DNA; Chagas disease

20
Q

What is the mechanism of action of suramin? What is it used for?

A

inhibits multiple enzymes, esp enzymes important for energy metabolism; African trypanosomiasis (pre-CNS)

21
Q

What is the most common helminthic parasite infection?

A

ancylostoma and necator (hookworms)

22
Q

What is praziquantel used for? Method of action?

A

broad spectrum for cestodes (tapeworm) and flukes; massive Ca++ influx causes muscle contraction of parasite

23
Q

Side effects of praziquantel?

A

nausea
vomiting
abdominal pain

24
Q

What is bithionol used for? Adverse effects?

A

alternative to praziquantel - uncouples oxidative phosphorylation - used for lung and liver fluke infections; causes nausea, vomiting, diarrhea, rashes, photosensitivity

25
Q

This drug us useful in treating chloroquine and Fansidar-resistant strains of malaria

A

mefloquine

26
Q

What are two antimetabolites used to treat malaria

A

chloroguanide

pyrimethamine-sulfadozine (fansidar)

27
Q

Three drugs used to treat Entamoeba histolytica

A

Paramomycin
Iodoquinol
Diloxanide furoate

28
Q

List four very important nematodes

A

Tricuris trichuria - whipworm
Ascaris lumbricoides - roundworm
Ancylostoma duodenale - hookworm
Strongyloides stercoralis - threadworm

29
Q

How does mebendazole work? What is it used for?

A

binds to tubulin and disrupts microtubules; used broad spectrum - for trichuriasis, hookworms, enterobiasis, ascariasis

30
Q

Should mebendazole/albendazole be taken during pregnancy?

A

no - potential teratogen

31
Q

How does albendazole work? What is it used to treat?

A

disrupts microtubules; used for Strongyloidiasis; trichurasis; capillariasis, ascariasis, filariasis, toxocariasis; Taenium Solium and Cysticercus cellulosis; Echinococcosis (hydatid disease)

32
Q

How does thiabendazole work? What is it used to treat?

A

binds to tubulin, also blocks helminth specific enzyme fumarate reductase; used to treat Strongyloidiasis

33
Q

What are the filarial worms, or roundworms?

A

Trichinella spiralis
Wucheria bancrofti
Onchocerca volvulus
Brugia malayi

34
Q

What drug is used for tissue and blood nematodes (filariasis)?

A

diethylcarbamazine

35
Q

How does Ivermectin work? What is it used to treat?

A

tonic paralysis of musculature via Cl- channels opening; used for nematodes (Onchocerciasis, enterobius, strongyloides, trichuris, ascaris)