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Wrap Up Block > Antiparasitic Drugs 1 > Flashcards

Antiparasitic Drugs 1 Flashcards

1
Q

MoA of Albendazole?

A

inhibits microtubule assembly

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2
Q

MoA of Diethylcarbamazine?

A

immobilizes microfilariae by unknown mechanism, renders them more susceptible to host defenses

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3
Q

MoA of Ivermectin?

A

intensifies GABA neurotransmission in nematodes and causes immobilization, facilitating removal by RES

(selective toxicity b/c GABA is only in CNS in humans and ivermectin doesn’t cross BBB)

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4
Q

MoA of Mebendazole?

A

inhibiting microtubule synthesis and glucose uptake in nematodes

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5
Q

MoA of Piperazine?

A

paralyzes ascaris by acting as agonist at GABA receptors.

paralyzes roundworms are expelled live by normal peristalsis

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6
Q

MoA of Pyrantel pamoate?

A

stimulates nicotinic receptors present at NMJ of nematodes. contraction of muscles occurs, followed by depolarization-induced paralysis.

no actions on flukes or tapeworms

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7
Q

MoA of Thiobendazole?

A

structural congener of mebendazole. inhibits microtubule assembly

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8
Q

MoA of Praziquantel?

A

increases membrane permeability to Ca++

marked contraction initially and then paralysis of trematode and cestode muscles. this is followed by vacuolization and parasite death

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9
Q

MoA of Bithionol?

A

unknown.

codrug of choice (w/ triclabendazole) for treatment of fascioliasis and alternative for paragonimiasis

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10
Q

MoA of Metrifonate?

A

organophosphate prodrug. converted in the body to the cholinesterase inhibitor dichlorvos.

the active metabolite acts only on Schistosoma haematobium.

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11
Q

MoA of Oxamniquine?

A

causes paralysis of Schistosoma mansoni by unknown mechanism.

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12
Q

MoA of Niclosamide?

A

uncouples oxidative phosphorylation or possibly activates ATPases

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13
Q

MoA of Chloroquine?

A

accumulates in food vacuole of plasmodia and prevents polymerization of the hemoglobin breakdown product heme into hemozoin

intracellular accumulation of heme is toxic to the parasite

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14
Q

MoA of quinine?

A

complexes w/ dsDNA to prevent strand separation, resulting in block of DNA replication and transcription to RNA.

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15
Q

MoA of Mefloquine?

A

unknown

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16
Q

MoA of Primaquine?

A

quinolone-quinone metabolites that are electron-transferring redox compounds that also act as cellular oxidants.

17
Q

MoA of Proguanil?

A

sulfonamide. blocks folic acid synthesis…

proguanil is activated to cycloguanil which is selective inhibitor of dihydrofolate reductase

18
Q

Antimalarial drugs with QT prolongation?

A

halofantrine

19
Q

MoA of Artemisinins?

A

metabolized in food vacuole to form free radicals

20
Q

Prevent malaria in travelers?

A

Chloroquine weekly is doc in places w/o resistance
Mefloquine weekly in places w/ resistance
in places w/ MDR malaria, use Malarone (proguanil + atovaquone)

21
Q

MoA of emetines?

A

block ribosomal movement along messenger RNA, thus inhibiting ameobal protein synthesis

22
Q

MoA of melarsoprol?

A

inhibits enzyme sulfhydryl groups

drug of choice in African trypanosomiasis

23
Q

DoC in African sleeping sickness?

A

Melarsoprol

inhibits enzyme sulfhydryl groups

24
Q

DoC in American trypanosomiasis?

A

Nifurtimox

inhibits parasite-unique enzyme trypanothione reductase

25
Q

MoA of Nifurtimox?

A

inhibits parasite-unique enzyme trypanothione reductase

drug of choice in America trypanosomiasis

26
Q

Drug of choice for Leishmaniasis?

A

sodium stibogluconate

appears to kill parasite by inhibition of glycolysis or effects on nucleic acid metabolism

27
Q

MoA of Paromomycin?

A

aminoglycoside antibiotic
(30S subunit -> inhibit protein synthesis)

(used as a luminal amebicide)

28
Q

MoA of Eflornithine?

A

suicidal substrate of ornithine decarboxylase

effective in some forms of African trypanosomiasis

29
Q

Antimalarial that can precipitate porphyria attacks?

A

chloroquine

30
Q

What is cinchonism?

A

caused by quinine/quinidine:

tinnitus, vertigo, h/a, GI distress, blurred vission

severe overdose can result in cardiotoxicity (torsades?)

31
Q

Antimalarial that can cause Blackwater Fever?

A

quinine

Blackwater fever is a rare intravascular hemolysis

32
Q

Antimalarial that can cause methemoglobinemia?

A

Primaquine

also causes hemolysis in G6PD deficiency

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