Diloxanide furoate : It is a highly effective luminal amoebicide: directly kills trophozoites responsible for production of cysts.
AMIDES
Diloxanide furoate
It is a highly
effective luminal amoebicide: directly kills trophozoites responsible for
production of cysts. The furoate ester is hydrolysed in intestine and the
released diloxanide is largely absorbed. Diloxanide is a weaker amoebicide than
its furoate ester : no systemic antiamoebic activity is evident despite its absorption.
It is primarily metabolized by glucuronidation and is excreted in urine.
Diloxanide furoate
exerts no antibacterial action. It is less effective in invasive amoebic
dysentery, because of poor tissue amoebicidal action. However, a single course
produces high (80–90%) cure rate in mild intestinal amoebiasis and in
asymptomatic cyst passers.
Dose: 500 mg TDS for 5–10
days; children 20 mg/kg/ day.
FURAMIDE 0.5 g tab; in
TINIBADF 250 mg + 150 mg tinidazole and TINIBADF FORTE 500 mg + 300 mg tabs; in
ENTAMIZOLE 250 mg + 200 mg metronidazole and ENTAMIZOLE FORTE 500 mg + 400 mg
tabs.
Diloxanide furoate is very well tolerated; the only side effects
are flatulence, occasional nausea, itching and rarely urticaria. It is the drug
of choice for mild intestinal/asymptomatic amoebiasis, and is given after any
tissue amoebicide to eradicate cysts. Combined use with metronidazole/
tinidazole is quite popular. Some chronic cases require repeat courses for
eradication.
Nitazoxanide
This salicylamide congener
of the anthelmintic
niclosamide, recently introduced for the treatment of giardiasis is also active
against E. histolytica, T. vaginalis,
Cryptosporidium, H. pylori, Ascaris, H. nana and some other protozoa and helminths. It is a prodrug which on
absorption is converted to the active form tizoxanide,
an inhibitor of PFOR enzyme that is an
essential pathway of electron transport energy metabolism in anaerobic organisms.
Activity against metronidazole-resistant Giardia
has also been demonstrated. Tizoxanide produced in the body is conjugated and
excreted in urine and bile.
Nitazoxanide is indicated in giardiasis, cryptosporidiasis, as
well as in amoebic dysentery as luminal amoebicide. Abdominal pain, vomiting
and headache are mild and infrequent side effects.
Dose: 500 mg (children 7.5
mg/kg) BD × 3 days NITACURE, TITCOL,
NITARID 200 mg, 500 mg tabs, 100 mg/5 ml dry syrup.
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