anti helminthic/protozoal drugs Flashcards
1. List the prototype drugs used to treat helminth infections, describe their mechanism of action, their clinical activity, and list their major side effects. 2. List the prototype drugs used to treat amebiasis, describe their clinical activity and their mechanism of action, and list their significant side effects. 3. List the prototype drugs used to treat giardiasis, leishmaniasis, trypanosomiasis and trichomoniasis infections, describe their mechanism of action and clinical activity, and lis
Drugs against nematodes (roundworms)
albendazole Diethylcarbamazine ivermectin mebendazole pyrantel
drugs active against tremadotes (flukes)
praziquentel
bithionol
metrifonate
oxaniquine
drugs against cestodes (tapeworms)
nilosamine
praziquentel
albendazole
mebendazole
DOC for tapeworms
niclosamide
MOA of niclosamide
uncoupling of oxidasive phosphorylation, or by activating ATPases
result of niclosamide
detachment of bug from intestinal wall and evacuation
SE of niclosamide
slight abdominal discomfort
niclosamide will not work on
ova
way to remove tapeworm ova from GI
purging of tract, drugs will not usually kill
DOC for cestode AND trematode
praziquantil
MOA of praziquantil
increases permability of worm cell membrane to Ca++ ions.
results of praziquantil
massive contracture of worm body and impairs it’s ability to attach to intestinal wall
At high doses, can activate host immune reponse
SE of V
abdominal discomfort, fever, sedation, headache
anti-hemlith that has extensive first-pass metabilism
praziquantil
DOC for roundworms
-dazoles
very wide spectrum -dazole (nematodes and cestodes)
albendazole
MOA of albendazole
larvicidal effect due to inhibition of microtubule activity
SE of albendazole
reversible leukopenia, alopecia, eleveted liver enzymes, bone marrrow suppression in LTT
DOC for most GI nematodes
mebendazole
MOA for mebendazole
inhibition of hemlitnth glucose uptake, inhibition of microtuble polymerization
drug that lethal effect extends to adults and ova
mebendazole
DOC for pinworms
mebendazole
drug given to all household members
mebendazole for pinworm
SE of mebendazole
abdominal disomfort, diarrhea
why does mebendazole have a large conentration in the colon
very poorly absorbed by SI
contraindicated in pregancy
mebendazole, pyrantel pamoate, metronidazole
ALt drug for nematodes
thiabendazole
MOA for thiabendazole
inhibition of glucose uptake, AND inhibition of fumarate reductase (needed for anaerobic metabolism)
larve that are not affected by thiabendazole
trichnella spiralis (porkworm) in muscle
causes stevens-johnson syndrome
thiabendazole
SE of thiabendazole
N/V, diarrhea, vertigo, crystalluria, leukopenia, SSJ
major use for thiabendazole
creeping skin eruptions with strongylodies sercoralis
DOC for hookworm and roundworm
pyrantel pamoate
MOA of pyrantel pamoate
depolarises the myneural junction of helmith muscle
results of pyrantel pamoate
spastic paralysis in porkworm
SE of pyrantel pamoate
GI sx, fever, CNS effects
contraindicated in kids less than 1 yr of age
pyrantel pamoate
used with pyrantel pamoate
piperazine
use of piperazine
Alt drug for nematodes
contraindications of piperazine
epilepsy
DOC for O vululus (river blindness) and S stercoralis (threadworm)
mectizan
treatment for urinary shistosomiasis in africa
metrifonate
DOC for sheep liver fluke
bithionol
DOC for trichomoniasis, SI and Hepatic amebiasis and giardiasis
metronidazole
MOA of metronidazole
functions as electron sink in protazoa, ROS then disrupts DNA
contraindications of metronidazole
alchohol use, CNS disease, preggers
IV or sub Q alt drug for amebiasis
emetine and dehydroememtine
used for acute chagas
nifurtimox
DOC for leishmaniasis
sodium stibogluconate
onlyeffective drug for crypto
nitazoxanide
MOA of nitazoxanide
interferes with pyruvate enzyme deoendant electron transfer