Amides

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Chapter: Essential pharmacology : Antiamoebic And Other Antiprotozoal Drugs

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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