GI pharmacology (Fitz) Flashcards

1
Q

albendazole and mebendazole are used for these helminths:

A

nematodes and cestodes

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2
Q

praziquantel is used for these helminths:

A

cestodes and trematodes

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3
Q

pyrantel pamoate, diethylcarbamazine, and ivermectin are used for these helminths

A

nematodes

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4
Q

niclosamide used for this hleminth

A

cestodes

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5
Q

these soil-transmitted helminths are among most prevalent worldwide

A

ascaris, hookworm, trichuris

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6
Q

list the anti-helminthic Benzimidazoles

A

albendazole and mebendazole

thiabendazole (cutaneous only)

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7
Q

MOA of Benzimidazoles?

A

disrupt microtubule dynamics

bind to parasite B-tubulin, disrupt microtubule polymerization and microtubule dependent processes

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8
Q

this Benzimidazole has poor solubility, POOR ABSORPTION, plus efficient metabolism and protein binding which leads to LOW SYSTEMIC EXPOSURE

A

Mebendazole

safe and effective: single dose (child > 2 and adult)

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9
Q

This Benzimidazole has modest absorption, EFFICIENT METABOLISM, low systemic exposure to parent drug

A

Albendazole

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10
Q

this Benzimidazole’s systemic toxicity limits its use and is for CUTANEOUS USE ONLY (For larval migrans)

A

Thiabendazole

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11
Q

this drug is for Enterobius vermicularis-Pinworm

A

Mebendazole

Pinworm a common infx in US children

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12
Q

this drug for Necator americanus and Ancylostoma duodenale-Hookworm

A

Albendazole

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13
Q

these drugs for Ascaris lumbricoides

A

Albendazole

Mebendazole

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14
Q

these drugs for Trichuris trichiura-Whipworm

A

Mebendazole: 3 day course most effective

Albendazole

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15
Q

this drug for Toxocara spp, Larval migrans

A

Albendazole

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16
Q

a single dose of oral albendazole, mebendazole, and pyrantel pamoate show high cure rates against ___

A

A lumbricoides

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17
Q

for __ infx, albendazole was more efficacious than mebendazole and pyrantel pamoate

A

hook worm

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18
Q

are albendazole and mebendazole teratogens?

A

yes

embryotoxic and teratogenic and not recommended for use in pregnancy (category C)

19
Q

This alternative or adjuntive nematode therapy is effective against hookworm, pinworm, and roundworm but ineffective against Trichuris trichuria

A

Pyrantel pamoate

20
Q

how does Pyrantel cause spastic paralysis of the worm?

A

it is a depolarizing NM blocking agennt. Causes persistent activation of N-AChRs

21
Q

this nematode/helminth drug is used against intestinal strongloidyiasis (thread worm) and Onchocerciasis (river blindness)

A

Ivermectin

22
Q

this anti-helminth activated glutamate-gated Cl channels which causes Cl current, hyperpolarization, and paralysis of the body wall and pharyngeal muscle in nematodes with no impact on mammals since it cannot cross BBB

A

Ivermectin

23
Q

Ivermectin can act on this channel in humans and is contraindicated when the BBB is disrupted

A

GABA-gated Cl channels

24
Q

the most extensive use for ivermectin in humans has been for ___

A

onchorcerciasis control in africa

river blindness

also useful for lymphatic filiariasis –> Wuchereria bancrofti and Brugia malayi

25
Q

this drug is only available via CDC in the US for lymphatic filiariasis and Loasis. it has signficiant toxicity d/t host response following death of parasites

A

diethylcarbamazine

26
Q

this is the drug of choice for all adult form tapeworm infx

A

Praziquantel

T solium-pork
T saginata-beef
D latum-fish

27
Q

This is the drug of choice for larval forms of tapeworm infx

A

Albendazole

cysticercosis
Echinococcus granulosus (cystic hydatid disease)

Longer tx duration 1-6 months, risk of hepatotoxicity

28
Q

drug of choice for Cysticercosis: Taenia solium tapeworm

A

albendazole

29
Q

this drug is contra-indicated for tx of ocular cysticercosis-destruction of the org in the eye may damage th eeye

A

praziquantel

30
Q

this is the drug of choice for cystic hydatid disease d/t Echinococcus granulosus (dog tapeworm in human)

A

Albendazole-3 month tx or longer

31
Q

this is the drug of choice for all forms of schistosomiasis

A

praziquantel

eggs in intestine, flukes in liver

32
Q

Absorption of praziquantel?
Distribution?
Metabolism?

A

Rapidly absorbed
Distributes into CF
short 1/2 life (1-3 hrs), extensive protein binding, inactive metabolites

33
Q

MOA of praziquantel?

A

interfere with Ca homeostasis and causes flaccid paralysis in adult flukes

causes Ags within the parasite to be exposed to the action of host Abs

34
Q

List anti-protozoal agents

A

metronidazole
tinidazole
nitazoxanide

35
Q

list anti-amebic agents

A

iodoquinol
diloxanide furoate
paromomycin

36
Q

__ is extensively used to tx infx caused by anaerobic orgs including protozoa/amoebas such as Entamoeba histolytica and Giardia lamblia

A

metronidazole

also bacteria such as Enterococcus spp and clostridium spp

37
Q

how are metronidazole and tinidazole selectively toxic toward microaerophilic pathogens?

A

these orgs rely on metabolism by pyruvate-ferredoxin oxidoreductase (PFOR) complex –> This activates Metronidazole

38
Q

___ is the drug of choice for amebiasis

A

Metronidazole

39
Q

__ is approved for the tx of giardiasis as a single 2-g dose and is appropriate 1st line therpay, considered superior to metronidazole

A

tinidazole

40
Q

adverse effects of metronidazole and tinidazole?

A

Metallic taste

Disulfiram-like rxn

41
Q

symptomatic, or invasive colitis is treated with ___

A

metronidazole, followed by a luminal amebicide such as paromomycin, diiodohydroxyquin, or diloxanide furoate to eliminate intraluminal cysts

42
Q

this is the drug of choice for colonization of intestine with E histolytica and an alternative to metronidazole for E histolytica infx during pregnancy

A

Paromomicin

43
Q

symptomatic pts with giardiasis should be tx with __ as drugs of choice

A

TINIDAZOLE, metronidazole, or nitazoxanide