Chapter 36- Antiparasitics Flashcards

1
Q

What is the clinical application of chloroquine

A

Malaria, all species

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2
Q

What are some adverse reactions seen with chloroquine

A

Retinopathy, prolonged QT interval, methemoglobinemia, pruritis

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3
Q

What is a contraindication to chloroquine use

A

Visual field changes

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4
Q

What is the exact mechanism of action of chloroquine

A

Protonated chloroquine accumulates inside the parasite’s food vacuole, where it binds to ferriprotoporphyrin IX (heme) and inhibits its polymerization

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5
Q

What stage of plasmodia infections does chloroquine kill

A

Erythrocytic stage only

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6
Q

What is the clinical application of quinine (quinidine)

A

Malaria, especially P. Falciparum

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7
Q

What antimalarial agent that is an inhibitor of heme metabolism can cause cinchonism (tinnitus, deafness, headaches, nausea, vomiting, visual disturbances)

A

Quinine

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8
Q

What are some contraindications for quinine use

A

G6PD, myasthenia gravis

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9
Q

What specific type of malaria is quinine used for

A

Acute blood-stage malaria, but not used prophylactically

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10
Q

What is the clinical application of mefloquine

A

Chloroquine-resistant malaria

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11
Q

What anti-malarial agent that inhibits heme metabolism has neuropsychiatric symptoms

A

Mefloquine

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12
Q

What are is the proposed mechanism of mefloquine

A

Appears to disrupt polymerization of heme to hemozoin inside intraerythrocytic malarial parasites

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13
Q

What is the mechanism of action of primaquine

A

Disrupts metabolism in plasmodia mitochondria, likely by inhibiting ubiquinone and by non-specific oxidative damage

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14
Q

What is the clinical application of primaquine

A

P. Vivax and P. Ovale (attacks hepatic form)

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15
Q

What is a contraindication for primaquine

A

G6PD- it crosses placenta and DNA induce fatal hemolysis in fetal erythrocytes independent of maternal G6Pd status

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16
Q

What antimalarial drug can also target toxoplasmosis and babesiosis

A

Atovaquone

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17
Q

What is the mechanism of action of atovaquone

A

Inhibits the interaction between reduced ubiquinone and the cytochrome Bc1 complex (disrupts pyrimidine synthesis)

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18
Q

What analogues are sulfadoxine and sulfalene

A

PABA analogues that competitive inhibit plasmodial dihydropteroate synthetase

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19
Q

What analogue is pyrimethamine

A

Folate analogue that competitively inhibits plasmodial dihydrofolate reductase

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20
Q

What stage of P. Falciparum infection is sulfadoxine/sulfalene-pyrimethamine effective against

A

Schizont stage

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21
Q

What is the contraindication for proguanil use

A

Prophylaxis of P. Falciparum malaria in patients with severe renal impairments

22
Q

What does proguanil inhibit

A

Pyrimidine derivative that inhibits plasmodial dihydrofolate reductase

23
Q

What is proguanil primarily effective against

A

Hepatic, pre-erythrocytic forms of P. Falciparum and P. Vivax

24
Q

What is the clinical application of metronidazole and tinidazole

A

Anaerobic bacterial, amebiasis, giardiasis, trichomoniasis

25
Q

What are some adverse reactions seen with metronidazole/tinidazole

A

Disulfiram-like efffect with alcohol; headache, metallic taste, vaginitis

26
Q

What is the clinical application of nitazoxanide in kids

A

Giardiasis

27
Q

What is the clinical application of nitazoxanide in adults

A

Crytosporidiosis

28
Q

What is the mechanism of action of nitazoxanide

A

Inhibits the pyruvate-ferredoxin oxidoreductase (PFOR) enzyme that converts pyruvate to acetyl CoA in Protozoa and anaerobic bacteria

29
Q

What is the clinical application of pentamidine

A

African trypanosomiasis; pneumocystis carinii pneumonia

30
Q

What is the mechanism of action of pentamidine

A

Inhibits DNA, RNA, protein and phospholipid synthesis, and dihydrofolate reductase activity

31
Q

What is the clinical application of suramin

A

Early stage African trypanosomiasis

32
Q

What are some adverse reactions seen with suramin

A

Pruritis, paresthesias, vomiting, nausea

33
Q

What is the mechanism of action of suramin

A

Inhibits RNA polymerase and glycerol phosphate dehydrogenase (interferes with parasite replication)

34
Q

What is the clinical application of metarsoprol

A

Late stage African trypanosomiasis

35
Q

What are some adverse reactions seen with metarsoprol

A

Reactive encephalopathy, death, phlebitis

36
Q

What is the clinical application of eflomithine

A

West African trypanosomiasis (IV); hair removal (topical_

37
Q

What is the mechanism of action of efomithine

A

Selective and irreversible inhibitor of ornithine decarboxylase

38
Q

What is the clinical application of nifurtimox

A

New world trypanosomiasis (chagas disease)

39
Q

What are some adverse reactions seen with nifurtimox

A

Pancytopenia, neuropathy, convulsions memory loss

40
Q

What is the mechanism of action of nifurtimox

A

Generates toxic intracellular oxygen radicals in the parasites

41
Q

What is the clinical application of sodium stibogluconate and meglumine antimonate

A

Leishmaniasis

42
Q

What is the mechanism of action of ivermectin

A

Potentiates both glutamate gated chloride channels in nematode cell membranes and release of GABA from pre-synaptic terminals

43
Q

What is the clinical application of ivermectin

A

Onchocerciasis, lymphatic filariasis, strongyloidiasis, scabies, cutaneous larva migrants

44
Q

What is the mechanism of action of anbendazole, mebendazole, thiabendazole

A

Inhibit tubulin polymerization by binding to beta tubulin

45
Q

What is the clinical application of albendazole, mebendazole, thiabendazole

A

Nematode infections, cysticercosis, echinococcosis

46
Q

What is the mechanism of action of praziquantel

A

Increase parasites membrane permeability to calcium which leads to contraction and paralysis of worms

47
Q

What is the clinical application of diethylcarbamazine

A

Filariasis

48
Q

What excretes diethylcarbamazine

A

Kidney

49
Q

What is the clinical application of pyrantel pamoate

A

Pinworm, roundworm, and hookworm infections

50
Q

What is the mechanism of action of pyrantel pamoate

A

Causes constant release of acetylcholine, leading to persistent activation of parasite nicotinic acetylcholine receptors, leading to tonic paralysis

51
Q

What is the clinical application of piperazine

A

Roundworm infection

52
Q

What is the mechanism of action of piperazine

A

GABA agonist, leading to flaccid paralysis (rarely used)