Mechanisms/Drug Class Flashcards

1
Q

What is the mechanism of action of the antimalarial agents that inhibit heme metabolism?

A

Decrease the metabolism and/or removal of toxic heme products, resulting in increased toxicity to the plasmodia

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2
Q

What is the 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; accumulation of unpolymerized heme leads to oxidative membrane damage

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3
Q

chloroquine

A

antimalarial agent: inhibitor of heme metabolism

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4
Q

What is the mechanism of action of quinine?

A

Similar to chloroquine, but also intercalates into DNA

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5
Q

quinine

A

antimalarial agent: inhibitor of heme metabolism

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6
Q

quinidine

A

antimalarial agent: inhibitor of heme metabolism

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7
Q

What is the mechanism of action of mefloquine?

A

Disrupts polymerization of heme to hemozoin inside intraerythrocytic malarial parasites

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8
Q

mefloquine

A

antimalarial agent: inhibitor of heme metabolism

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9
Q

What is the mechanism of action of artemisinin, artesunate, artemether, and dihydroartemisinin?

A

Form carbon-centered free radicals that alkylate heme

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10
Q

arteminisinin

A

antimalarial agent: inhibitor of heme metabolism

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11
Q

artesunate

A

antimalarial agent: inhibitor of heme metabolism

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12
Q

artemether

A

antimalarial agent: inhibitor of heme metabolism

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13
Q

dihydroartemisinin

A

antimalarial agent: inhibitor of heme metabolism

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14
Q

What is the mechanism of action of the antimalarial agents that inhibit electron transport?

A

Inhibit the plasmodial electron transport chain

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15
Q

What is the mechanism of action of primaquine?

A

Disrupts metabolism in plasmodial mitochondria, likely by inhibiting ubiquinone and by nonspecific oxidative damage

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16
Q

primaquine

A

antimalarial agent: inhibitor of electron transport

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17
Q

atovaquone

A

antimalarial agent: inhibitor of electron transport

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18
Q

What is the mechanism of action of the antimalarial agents that inhibit translation?

A

Inhibit protein synthesis by binding to 30S ribosomal subunit (doxycycline and tetracycline) or 50S ribosomal subunit (clindamycin)

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19
Q

doxycycline

A

antimalarial agent: inhibits translation

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20
Q

tetracycline

A

antimalarial agent: inhibits translation

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21
Q

clindamycin

A

antimalarial agent: inhibits translation

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22
Q

What is the mechanism of action of sulfadoxine and sulfalene?

A

They are PABA analogues that competitively inhibit plasmodial dihydropteroate synthetase

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23
Q

What is the mechanism of action of pyrimethamine?

A

It is a folate analogue that competitively inhibits plasmodial dihydrofolate reductase

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24
Q

sulfadoxine-pyrimethamine

A

antimalarial agent: inhibitor of folate metabolism

25
sulfalene-pyrimethamine
antimalarial agent: inhibitor of folate metabolism
26
What is the mechanism of action of proguanil?
It is a pyrimidine derivative that inhibits plasmodial dihydrofolate reductase
27
proguanil
antimalarial agent: inhibitor of folate metabolism
28
What is the mechanism of action of metronidazole?
It is activated by enzymes in parasites and anaerobic bacteria to form reduced cytotoxic compounds that damage microbial proteins, membranes, and DNA
29
metronidazole
antiprotozoal agent
30
What is the mechanism of action of tinidazole?
A second-generation nitromidazole related to metronidazole; bout better tolerated and requires a shorter duration of treatment
31
tinidazole
antiprotozoal agent
32
What is the mechanism of action of nitazoxanide?
Inhibits the pyruvate-ferredoxin oxidoreductase (PFOR) enzyme that converts pyruvate to acetyl CoA in protozoa and anerobic bacteria
33
nitazoxanide
antiprotozoal agent
34
What is the mechanism of action of pentamidine?
Inhibits DNA, RNA, protein, and phospholipid synthesis, and dihydrofolate reductase activity
35
pentamidine
antiprotozoal agent
36
What is the mechanism of action of suramin?
Inhibits RNA-polymerase and glycerol phosphate dehydrogenase
37
suramin
antiprotozoal agent
38
What is the mechanism of action of melarsoprol?
Inhibits trypanosomal pyruvate kinase, thereby inhibiting glycolysis and decreasing ATP production; also inhibits adenine and adenosine uptake by trypanosomal transporters
39
melarsoprol
antiprotozoal agent
40
What is the mechanism of action of eflornithine?
Selective and irreversible inhibitor of ornithine decarboxylase
41
elfornithine
antiprotozoal agent
42
sodium stibogluconate
antiprotozoal agent
43
meglumine antimonate
antiprotozoal agent
44
What is the mechanism of action of miltefosine?
A synthetic ether phospholipid analogue similar to natural phospholipids in cell membranes; may inhibit enzyme systems associated with plasma membranes; may also inhibit platelet activating factor-induced responses and inosil phosphate formation
45
miltefosine
antiprotozoal agent
46
What is the mechanism of action of the antihelminthic agents?
All mechanisms lead to paralysis and death of worms
47
What is the mechanism of action of ivermectin?
Potentiates both glutamate-gated chloride channels in nematode cell membranes and releases GBA from presynaptic terminals, leads to hyper polarization of neuromuscular cells and pharyngeal paralysis
48
What is the mechanism of action of albendazole, mebendazole, and thiabendazole?
Inhibit tubulin polymerization by binding to beta-tubulin, causing degenerative changes in integumental and intestinal cells of helminths
49
albendazole
antihelminthic agent
50
ivermectin
antihelminthic agent
51
mebendazole
antihelminthic agent
52
thiabendazole
antihelminthic agent
53
What is the mechanism of action of praziquantel?
Increases parasite membrane permeability to calcium, causing contraction and paralysis of worms
54
praziquantel
antihelminthic agent
55
diethylcarbamazine
antihelminthic agent
56
What is the mechanism of action of pyrantel pamoate?
causes constant release of acetylcholine, causing persistent activation of parasite nicotinic acetylcholine receptors, causing tonic parlysis
57
pyrantel pamoate
antihelminthic agent
58
What is the mechanism of action of piperazine?
It is a GABA agonist that causes flaccid paralysis
59
piperazine
antihelminthic agent