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Flashcards in antihelminths/antiprotozoals Deck (26):

Albendazole (Albenza®) MOA

~5% absorbed orally
-Bind with high affinity to free β-tubulin of the parasite-->*inhibition of microtubule polymerization and an inhibition of microtubule-dependent glucose uptake* (good selectivity, does not bind well to human β–tubulin)
-txs GI and systemical symptoms


Albendazole (Albenza®) SEs

-GI: N/V/D/abd. pain
-hepatotoxicity, increases in liver enzymes (~16 % of patients) -do LFTs
-Leukopenia (


Pyrantel (Antiminth®, Pin-X®)

Broad-spectrum OTC drug that is effective against a variety of nematodes
*activation of cholinergic nicotinic recs in the muscles of the nematode resulting in a depolarizing NM blockade-->worm becomes paralyzed (similar to succinylcholine in humans) and is expelled from the GIT during peristalsis


Pyrantel (Antiminth®, Pin-X®) SEs

-GI: N/V/cramps
-CNS: ha, dizziness, drowsiness
-caution w. pre-ex. hepatic failure
-Use in pregnancy only when needed; Use in children


Praziquantel (Biltricide®)

Broad spectrum drug with activity against shistosomes (trematodes) as well as tapeworms (cestodes), effective against neuroschistosomiasis
-ppx for travelers to endemic areas (Africa)
*induces muscle contraction then spastic paralysis of the musculature of worms by causing an increase in calcium ion influx-->With cestodes, this action causes the suckers to become dislodged. (good selectivity; little effect on human muscle)


Praziquantel (Biltricide®)

-CNS: dizziness, drowsiness, headache, decreased mental alertness
-GI: N/V/abd. pain
-hepatic: inc. liver enzymes
-urticaria, rash, low-grade fever, arthralgia, myalgia
-Avoid with pregnancy if possible


Metronidazole (Flagyl®)

-good oral absorption, only used if symptomatic: GI, amebic liver abscess
MOA: cidal, drug gets reduced and binds to IC macromolecules (e.g. DNA)-->*inhibition of DNA synthesis*
-anaerobic bac: B. fragilis, C. diff
-protozoa: E. histo, Trich vag*, Giardia


Metronidazole (Flagyl®) SEs



Iodoquinol (Yodoxin®)



Iodoquinol (Yodoxin®)



Paromomycin (Humatin®)



Nitazoxanide (Alinia®)



Nitazoxanide (Alinia®)



Paromomycin (Humatin®)



know drugs and MOA

know spp best tx by drug
he will go over biology but will not be tested


preferred drugs for Enterobius vermicularis
(most common helminth infection in US)

Albendazole (Albenza)
Pyrantel (Antiminth, Pin-X)
-need strict personal hygiene control


preferred drugs for Ascaris lumbricoides

(2nd most common helminth inf. in US, most common WW, only inf. humans, egg is resistant ("night soil", "wandering worms"))

2nd most common helminth inf. in US, most common WW, only inf. humans, egg is resistant ("night soil")
Asymptomatic or mild infections: albendazole
Heavy infections: pyrantel (sx may be required i.e. if reach common bile duct), causes more paralysis, reduces wandering


Taenia solium (pork tapeworm) Taenia saginata (beef tapeworm)

Helminth: Cestodes: (Tapeworms)
Adult worms can cause GI upset, loss of appetite, and larvae (cysticerci) can become encysted in visceral organs causing the disease cysticercosis (T. solium)
both tx w. Praziquantel (Biltricide)
T. solium tx may cause the disintegration of gravid segments of T. solium that can result in the release of embryos from the eggs and cysticercosis; give a purgative (magnesium sulfate 15 to 30 g) 2 hrs after praziquantel tx


Necator americanus

Helminth: Nemotode: hookworm, feed on blood, cause iron-def. anemia (mental dullness)
-inf. thru skin (foot), don't need to eat
Albendazole: also tx "creeping eruptions" as parasite moves under skin


Entamoeba histolytica

Amebiasis; 1 – 5% USA; 10 % World’s population
-ingest cysts, typ. contaminated water, oral-anal contact
-cause sev. bloddy diarrhea, may spread to liver and cause hepatic abscess


Entamoeba histolytica tx

asymptomatic carrier tx: (Luminal acting drugs):
iodoquinol, paramomycin

symtomatic tx: (e.g. gastrointestinal symptoms, amebic liver abscess) Tissue Amebicide + Luminal acting drugs:
Metronidazole followed by Iodoquinol or Paromomycin


Giardia lamblia – Giardiasis

-Most commonly reported pathogen for causing infectious diarrhea in US
-contaminated water, sexual practices, poor hand washing
-causes profuse watery foul-smelling Diarrhea, abd. distension and cramping,
anorexia and nausea, constipation


Giardia tx



Trichomonas vaginalis – trichomoniasis

5 - 10% in women in the general population; 50
– 70% in prostitutes
-sexually transmitted, treat the sexual partner(s) of the
infected individual to prevent recurrence
tx: Metronidazole


Cryptosporidium parvum (Cryptosporidiosis)

GI protozoal infection, contaminated water
-affects liver, biliary system, pancreas, lymphatics, and lungs
-large amounts of watery diarrhea with vomiting, cramping and flatulence.


Crypto tx