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
What are some adverse reactions seen with metronidazole/tinidazole
Disulfiram-like efffect with alcohol; headache, metallic taste, vaginitis
26
What is the clinical application of nitazoxanide in kids
Giardiasis
27
What is the clinical application of nitazoxanide in adults
Crytosporidiosis
28
What is the mechanism of action of nitazoxanide
Inhibits the pyruvate-ferredoxin oxidoreductase (PFOR) enzyme that converts pyruvate to acetyl CoA in Protozoa and anaerobic bacteria
29
What is the clinical application of pentamidine
African trypanosomiasis; pneumocystis carinii pneumonia
30
What is the mechanism of action of pentamidine
Inhibits DNA, RNA, protein and phospholipid synthesis, and dihydrofolate reductase activity
31
What is the clinical application of suramin
Early stage African trypanosomiasis
32
What are some adverse reactions seen with suramin
Pruritis, paresthesias, vomiting, nausea
33
What is the mechanism of action of suramin
Inhibits RNA polymerase and glycerol phosphate dehydrogenase (interferes with parasite replication)
34
What is the clinical application of metarsoprol
Late stage African trypanosomiasis
35
What are some adverse reactions seen with metarsoprol
Reactive encephalopathy, death, phlebitis
36
What is the clinical application of eflomithine
West African trypanosomiasis (IV); hair removal (topical_
37
What is the mechanism of action of efomithine
Selective and irreversible inhibitor of ornithine decarboxylase
38
What is the clinical application of nifurtimox
New world trypanosomiasis (chagas disease)
39
What are some adverse reactions seen with nifurtimox
Pancytopenia, neuropathy, convulsions memory loss
40
What is the mechanism of action of nifurtimox
Generates toxic intracellular oxygen radicals in the parasites
41
What is the clinical application of sodium stibogluconate and meglumine antimonate
Leishmaniasis
42
What is the mechanism of action of ivermectin
Potentiates both glutamate gated chloride channels in nematode cell membranes and release of GABA from pre-synaptic terminals
43
What is the clinical application of ivermectin
Onchocerciasis, lymphatic filariasis, strongyloidiasis, scabies, cutaneous larva migrants
44
What is the mechanism of action of anbendazole, mebendazole, thiabendazole
Inhibit tubulin polymerization by binding to beta tubulin
45
What is the clinical application of albendazole, mebendazole, thiabendazole
Nematode infections, cysticercosis, echinococcosis
46
What is the mechanism of action of praziquantel
Increase parasites membrane permeability to calcium which leads to contraction and paralysis of worms
47
What is the clinical application of diethylcarbamazine
Filariasis
48
What excretes diethylcarbamazine
Kidney
49
What is the clinical application of pyrantel pamoate
Pinworm, roundworm, and hookworm infections
50
What is the mechanism of action of pyrantel pamoate
Causes constant release of acetylcholine, leading to persistent activation of parasite nicotinic acetylcholine receptors, leading to tonic paralysis
51
What is the clinical application of piperazine
Roundworm infection
52
What is the mechanism of action of piperazine
GABA agonist, leading to flaccid paralysis (rarely used)