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Pharmacology Chapter 36 > Mechanisms/Drug Class > Flashcards

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
Q

sulfalene-pyrimethamine

A

antimalarial agent: inhibitor of folate metabolism

26
Q

What is the mechanism of action of proguanil?

A

It is a pyrimidine derivative that inhibits plasmodial dihydrofolate reductase

27
Q

proguanil

A

antimalarial agent: inhibitor of folate metabolism

28
Q

What is the mechanism of action of metronidazole?

A

It is activated by enzymes in parasites and anaerobic bacteria to form reduced cytotoxic compounds that damage microbial proteins, membranes, and DNA

29
Q

metronidazole

A

antiprotozoal agent

30
Q

What is the mechanism of action of tinidazole?

A

A second-generation nitromidazole related to metronidazole; bout better tolerated and requires a shorter duration of treatment

31
Q

tinidazole

A

antiprotozoal agent

32
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 anerobic bacteria

33
Q

nitazoxanide

A

antiprotozoal agent

34
Q

What is the mechanism of action of pentamidine?

A

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

35
Q

pentamidine

A

antiprotozoal agent

36
Q

What is the mechanism of action of suramin?

A

Inhibits RNA-polymerase and glycerol phosphate dehydrogenase

37
Q

suramin

A

antiprotozoal agent

38
Q

What is the mechanism of action of melarsoprol?

A

Inhibits trypanosomal pyruvate kinase, thereby inhibiting glycolysis and decreasing ATP production; also inhibits adenine and adenosine uptake by trypanosomal transporters

39
Q

melarsoprol

A

antiprotozoal agent

40
Q

What is the mechanism of action of eflornithine?

A

Selective and irreversible inhibitor of ornithine decarboxylase

41
Q

elfornithine

A

antiprotozoal agent

42
Q

sodium stibogluconate

A

antiprotozoal agent

43
Q

meglumine antimonate

A

antiprotozoal agent

44
Q

What is the mechanism of action of miltefosine?

A

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
Q

miltefosine

A

antiprotozoal agent

46
Q

What is the mechanism of action of the antihelminthic agents?

A

All mechanisms lead to paralysis and death of worms

47
Q

What is the mechanism of action of ivermectin?

A

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
Q

What is the mechanism of action of albendazole, mebendazole, and thiabendazole?

A

Inhibit tubulin polymerization by binding to beta-tubulin, causing degenerative changes in integumental and intestinal cells of helminths

49
Q

albendazole

A

antihelminthic agent

50
Q

ivermectin

A

antihelminthic agent

51
Q

mebendazole

A

antihelminthic agent

52
Q

thiabendazole

A

antihelminthic agent

53
Q

What is the mechanism of action of praziquantel?

A

Increases parasite membrane permeability to calcium, causing contraction and paralysis of worms

54
Q

praziquantel

A

antihelminthic agent

55
Q

diethylcarbamazine

A

antihelminthic agent

56
Q

What is the mechanism of action of pyrantel pamoate?

A

causes constant release of acetylcholine, causing persistent activation of parasite nicotinic acetylcholine receptors, causing tonic parlysis

57
Q

pyrantel pamoate

A

antihelminthic agent

58
Q

What is the mechanism of action of piperazine?

A

It is a GABA agonist that causes flaccid paralysis

59
Q

piperazine

A

antihelminthic agent

Pharmacology Chapter 36 (1 decks)

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