diloxanide furoate
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Diloxanide is a medication used to treat amoeba infections. In places where infections are not common, it is a second line treatment after
paromomycin Paromomycin is an antimicrobial used to treat a number of parasitic infections including amebiasis, giardiasis, leishmaniasis, and tapeworm infection. It is a first-line treatment for amebiasis or giardiasis during pregnancy. Otherwise it is g ...
when a person has no symptoms. For people who are symptomatic, it is used after treatment with
metronidazole Metronidazole, sold under the brand name Flagyl among others, is an antibiotic and antiprotozoal medication. It is used either alone or with other antibiotics to treat pelvic inflammatory disease, endocarditis, and bacterial vaginosis. It i ...
or
tinidazole Tinidazole is a drug used against protozoan infections. It is widely known throughout Europe and the developing world as a treatment for a variety of anaerobic amoebic and bacterial infections. It was developed in 1972 and is a prominent member ...
. It is taken
by mouth Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are i ...
. Diloxanide generally has mild side effects. Side effects may include
flatulence Flatulence, in humans, is the expulsion of gas from the intestines via the anus, commonly referred to as farting. "Flatus" is the medical word for gas generated in the stomach or bowels. A proportion of intestinal gas may be swallowed environm ...
, vomiting, and itchiness. During
pregnancy Pregnancy is the time during which one or more offspring develops ( gestates) inside a woman's uterus (womb). A multiple pregnancy involves more than one offspring, such as with twins. Pregnancy usually occurs by sexual intercourse, but ca ...
it is recommended that it be taken after the
first trimester Pregnancy is the time during which one or more offspring develops ( gestates) inside a woman's uterus (womb). A multiple pregnancy involves more than one offspring, such as with twins. Pregnancy usually occurs by sexual intercourse, but ca ...
. It is a luminal amebicide meaning that it only works on infections within the
intestines The gastrointestinal tract (GI tract, digestive tract, alimentary canal) is the tract or passageway of the digestive system that leads from the mouth to the anus. The GI tract contains all the major organs of the digestive system, in humans ...
. Diloxanide came into medical use in 1956. It is on the
World Health Organization's List of Essential Medicines The WHO Model List of Essential Medicines (aka Essential Medicines List or EML), published by the World Health Organization (WHO), contains the medications considered to be most effective and safe to meet the most important needs in a health ...
. It is not commercially available in much of the
developed world A developed country (or industrialized country, high-income country, more economically developed country (MEDC), advanced country) is a sovereign state that has a high quality of life, developed economy and advanced technological infrastruct ...
as of 2012.


Medical uses

Diloxanide furoate works only in the digestive tract and is a lumenal amebicide. It is considered second line treatment for infection with amoebas when no symptoms are present but the person is passing cysts, in places where infections are not common.
Paromomycin Paromomycin is an antimicrobial used to treat a number of parasitic infections including amebiasis, giardiasis, leishmaniasis, and tapeworm infection. It is a first-line treatment for amebiasis or giardiasis during pregnancy. Otherwise it is g ...
is considered the first line treatment for these cases. For people who are symptomatic, it is used after treatment with ambecides that can penetrate tissue, like
metronidazole Metronidazole, sold under the brand name Flagyl among others, is an antibiotic and antiprotozoal medication. It is used either alone or with other antibiotics to treat pelvic inflammatory disease, endocarditis, and bacterial vaginosis. It i ...
or
tinidazole Tinidazole is a drug used against protozoan infections. It is widely known throughout Europe and the developing world as a treatment for a variety of anaerobic amoebic and bacterial infections. It was developed in 1972 and is a prominent member ...
. Diloxanide is considered second-line, while paromomycin is considered first line for this use as well.


Adverse effects

Side effects include flatulence, itchiness, and hives. In general, the use of diloxanide is well tolerated with minimal toxicity. Although there is no clear risk of harm when used during pregnancy, diloxanide should be avoided in the first trimester if possible. Diloxanide furoate is not recommended in women who are breast feeding, and in children <2 years of age.


Pharmacology

Diloxanide furoate destroys
trophozoites A trophozoite (G. ''trope'', nourishment + ''zoon'', animal) is the activated, feeding stage in the life cycle of certain protozoa such as malaria-causing '' Plasmodium falciparum'' and those of the '' Giardia'' group. (The complement of the tropho ...
of ''E. histolytica'' and prevents amoebic cyst formation. The exact mechanism of diloxanide is unknown. Diloxanide is structurally related to chloramphenicol and may act in a similar fashion by disrupting the
ribosome Ribosomes ( ) are macromolecular machines, found within all cells, that perform biological protein synthesis (mRNA translation). Ribosomes link amino acids together in the order specified by the codons of messenger RNA (mRNA) molecules to ...
The
prodrug A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug ...
, diloxanide furoate, is metabolized in the gastrointestinal tract to release the active drug, diloxanide. 90% of each dose is excreted in the urine and the other 10% is excreted in the feces.


Society and culture

It is on the
World Health Organization's List of Essential Medicines The WHO Model List of Essential Medicines (aka Essential Medicines List or EML), published by the World Health Organization (WHO), contains the medications considered to be most effective and safe to meet the most important needs in a health ...
. The drug was discovered by
Boots UK Boots UK Limited (formerly Boots the Chemists), trading as Boots, is a British health and beauty retailer and pharmacy chain in the United Kingdom and other countries and territories including Ireland, Italy, Norway, the Netherlands, Thailand an ...
in 1956, and introduced as ''Furamide''; it was not available in much of the developed world as of 2012.


References


External links

* {{portal bar, Medicine Anilides Antiprotozoal agents 2-Furyl compounds Organochlorides World Health Organization essential medicines Wikipedia medicine articles ready to translate