anti-parasitics Flashcards
DOC for invasive amebiasis
metronidazole
Metronidazole use
giardia trichomonas anaerobic cocci anaerobic gram - bacili h. pylori in combo tx
metronidazole MOA
reduced by reacting with reduced ferredoxin = produces cytotoxic compounds
these bind proteins and DNA = unstable molecules - cell death
metronidazole PK
hepatic oxidation
glucuoronidation
CYP P450s
metronidazole AE
GI distress
**disulfiram with alcohol
leukopenia
unpleasant metallic taste
safety in pregnancy not established
Tinidazole
2nd generation nitroimidazole
better tolerated and shorter duration that metronidazole
Tinidazole AE
same as metronidazole
diloxanide furoate
luminal antiamebics
iodoquinol
luminal antiamebics
paraymomycin
luminal antiamebics
What can be used by itself to tx asymptomatic ameobiasis
diloxanide furoate
Iodoquinol use
orally against luminal trophozoite and cyst forms of entamobea
alternative to diloxanide furoate for mild-severe infections
Iodoquinol AE
Adverse: with long term use - risk of optic neuritis
rash, diarrhea, dose related peripheral neuropathy
Paramomycin
aminoglycside antibiotic
only effected against luminal forms of E. histolytica and tapeworm
alternative agent for cryptosporidiosis in AIDS pt
paromycin MOA
amebicidal = cell membranes become leaky
interferes with bacterial protein synthesis - binds to 30s ribosomal subunits
reduces intestinal flora population
chloroquine use
combo: metroniazole, diloxanite furoate
eliminates trophozites in liver abscesses
emetine/dihydroemetine
back up drugs for tx of severe intestinal or hepatic amebiasis
MOA: inhibit protein synthesis by bloking ribosomal movement along mRNA
albendazole MOA
tx of cestodal infections (t. solium, e. granulosis)
inhibits microtubule synthesis and glucose uptake
ATP production is decreased = worm immobilization and death
albendazole AE
1-3 days of tx: HA, nausea
3 months/hydatid tx: hepatotoxicity, agranulocytosis/pancytopenia
CONTRAINDICATED in pregnancy/children
DOC for trichuris trichuria
mebendazole (or albendazole)
DOC for enterobius vermicularis
mebendazole (or pyrantel pamoate)
DOC for hookworms/n. americanus and a. duodenale:
mebendazole (pyrantel pamoate or albendazole)
roundworm/ascariasis lumbricoides DOC:
mebendazole (albendazole, pyrantel pamoate)
mebendazole MOA
inhibts formation of helminth microtubules
blocks glucose tuptake
affects parasitse that are expelled with feces
mebendazole AE
contraindic in preg
caution in children <2 or with cirrhosis
Thiabendazole
tx: strongyloidiasis, cutaneous larva migrans, early stage of trichinosis
MOA: affects microtubular aggregation
thiabendazole AE
more toxic than other benzimidazoles
CNS disturbance
contraindic in pregnacy
erythema multiforme - stevens johnson
not used in presence of liver or kidney disease
doc for onchoceriasis
ivermectin
doc for CLM
ivermectin
doc for strongyloides
ivermectin
ivermectin MOA
GABA agonist
Cl- influx = inc hyperpolarization - death occurs later
does not cross BBB
Ivermectin AE
mazotti reactions with onchoceriasis: fever, dizzy, somnolence, hypotension
contraindic in pregnacy and meningitis
DONT give with drugs that enhance GABA: barbiturates and benzos
piperazine
alt drug for tx of pinworm and roundworm
piperaize MOA
GABA agonist -
explusion of worm by peristalsis
contraindicated in seizure pt’s
pyrantel pamoate
tx roundworms, pinworms, hookworms
pyrantel pamoate MOA
depolarizing , NM blocker = persistent activation of parasite nicotinic-r = release of Ach and inhibition of cholinesterase
diethylcarbamazine
immobilizes microfilarier - makes suscpetible t ohost defense
DOC lymphatic filarisis
diethycarbamazine
diethylcarbamazine MOA
immobilizes microfilariae - susceptible to host defense
Doxycycline MOA
macrofilaricidal against wuchereria bancrofti
active against onchoceriasis
MOA - indirectly kills wolbachia - intracellular bacterial symbiont of parasite
Praziquantel
shisto, trematode, cestode, cysticerosis
DOC for schistomasiasis
Praziquantel
Praziquantel MOA
inc perm of cell membrane to calcium causing contracture and paralysis of worm = detachment of suckers from BV walls
DOC for cysticerosis
albendazole (praziquantel has similar efficacy)
praziquantel PK
extensive 1st pass metabolism
praziquantel AE
contraindicated in pregnancy, nursing mothers, and OCULAR CYSTICERCOSIS - destroying organism may damage eye
drug interactions (CYP P450)
bithionol
fasciolosis
alternative tx for pulmonary paragonimiasis
bithionol MOA
inhibition of helminth electron transport chain
DOC fasciolosis
bithionol
niclosamide
2nd line drug for most cestodes
uncommon b/c of effectiveness of praziquantel
niclosamide MOA
inhibition of parasite’s mitochondrial phosphorylation of ADP
Lethal for cestode’s scolex and segments - BUT not for ova
Niclosamide PK
laxative given prior to niclosamide to purge bowel of dead segments - in order to preclude digestion and liberation of ova
alcohol should NOT be given within 1 day of dose
tinidazole use
amebiasis
amebic liver abscess
giardiasis
trichomoniasis
diloxanide furoate MOA
converted in gut to diloxanide freebase active form
DOC for luminal amebicide
diloxanide furoate - not available in US
paromycin AE
GI distress - diarrhea
HA, dizzy, rash, arthralgia
systemic antiamebics
chloroquine
emetine
dehydroemetine
tx liver abscesses or intestinal wall infections
emetine/dihydroemetine AE
**pain at site of infection
cardiotoxicity
NM weakness
nausea
DOC asymptomatic intestinal infection
diloxanide furoate
alternative: iodoquinol, paromycin
DOC mild to mod intestinal infection
metronidazole + diloxanide furoate
alternatives: tinidazole or tetracycline or erythromycin + diloxanide furorate
DOC severe intestinal infection
metronidazole/tinidazole + diloxanide furoate
alternatives: tetracycline/emetine/dihydroemetine + diloxanide furoate
DOC hepatic abscesses and other extraintestinal disease
metronidazole/tinidazole + diloxanide furoate
alternatives: emetine/dihydroemetine + chloroquine + diloxanide furoate
DOC loiasis
diethylcarbamazine
DOC tropical eosinophilia
diethylcarbamazine
diethylcarbamazine AE
d/t host response following parasite death:
- fever, malaise, myalgias
- leukocytosis
can use anti-histamines/steroids to resolve AE
DOC visceral larva migrans (toxocariasis)
albendazole
DOC trichinosis (trichinella spiralis)
albendazole or mebendazole
DOC clonorchis sinesis
praziquantel
DOC paragonimus westermani
praziquantel
DOC echinococcosis
albendazole
DOC taeniasis solium/saginata
praziquantel or niclosamide
cysticercosis DOC
albendazole or praziquantel
diphyllobothriasis DOC
praziquantel or niclosamide
DOC giardia
metronidazole
DOC trichomonas vaginalis
metronidazole
DOC trypanosomiasis
melarsoprol or suramin
DOC hemolymphatic stage of trypanosomiasis and PCP infection
pentamidine
toxoplasmosis encephalitis DOC
pyrimethamine + clindamycin or sulfadiazine or folinic acid
DOC leishmaniasis (all stages)
sodium stibogluconate/amphoteracin B
DOC cystercosis with taenia solium larva
albendazole or praziquantel