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Infectious disease
Published in Kaji Sritharan, Jonathan Rohrer, Alexandra C Rankin, Sachi Sivananthan, Essential Notes for Medical and Surgical Finals, 2021
Kaji Sritharan, Jonathan Rohrer, Alexandra C Rankin, Sachi Sivananthan
Amoebiasis (Entamoeba histolytica): often insidious onset with few or mild symptoms but may lead to a fulminant colitis. Complications: toxic megacolon, amoeboma in colon and liver abscess. Treatment: with metronidazole +/- diloxanide furoate.
The management of Babesia, amoeba and other zoonotic diseases provoked by protozoa
Published in Expert Opinion on Therapeutic Patents, 2023
Clemente Capasso, Claudiu T. Supuran
Although there are ongoing studies, there is currently neither a vaccine nor a wide range of medications that are effective against amebiasis, which remains one of the most severe enteropathogens worldwide [38]. Patients with the clinical disease can be treated with an amoebicidal tissue-active agent or a luminal cysticidal agent to stop the infection and avoid further infections [47,48]. The amoebicidal drug includes the nitroimidazole agents, such as metronidazole 13 and tinidazole 14 (Figure 3), which are the treatment of choice for amebic colitis and amebic liver disease due to their potency against the parasites’ reproductive stages (trophozoites) [47,48]. Tinidazole has a longer half-life and is better tolerated, although metronidazole kills the parasites more efficiently [47,48]. It is necessary to use a luminal agent after using nitroimidazole because it does not eradicate luminal cysts [49–51]. The aminoglycoside paromomycin 15 is utilized as a luminal cysticidal agent, which should not be provided concurrently with the nitroimidazole agent [52]. Alternatives include diloxanide furoate 16 and iodoquinol 17 (Figure 3) [38]. Recently, auranofin, a gold compound used to treat particular cases of rheumatoid arthritis, has entered early clinical drug development as an antiparasitic agent [53]. However, more research is needed to evaluate if auranofin would be a successful treatment of amebiasis and if its usage will be limited by known safety issues such as diarrhea, rash, and bone marrow suppression [53].
Diloxanide furoate binary complexes with β-, methyl-β-, and hydroxypropyl-β-cyclodextrins: inclusion mode, characterization in solution and in solid state and in vitro dissolution studies
Published in Pharmaceutical Development and Technology, 2018
Carolina Aloisio, Marcela Longhi
Pathogenic intestinal protozoa are responsible for clinically important infections in both the developed and the developing world. Amoebiasis affects around 480 million people worldwide, with an annual mortality of 40 000–110 000 persons. These organisms are responsible for both acute and chronic diarrhea, and Entamoeba histolytica, which affects the colon, can spread to involve the liver. Acute amebic colitis ranges from mild to severe, and can be fulminant, leading to colon perforation. The infection can spread from the liver by direct extension into the pleuropulmonary cavity and the pericardial cavity. Occasionally, and most often in immuno-suppressed individuals, the infection might be widely disseminated and affect other organs, including bones and the brain (Farthing 2006). Diloxanide furoate (DF) (Figure 1(a)) is one of the drugs of choice for the treatment of amebic colitis caused by Entamoeba histolytica (Budal et al. 2004; Mishal and Sober 2005; Farthing 2006). DF acts on organisms in the intestinal lumen (Farthing 2006). For this reason, high concentrations of this drug in the intestinal fluids are substantially related to the effectiveness of the drug. Orally administered drugs must have sufficient water solubility to ensure their bioavailability and pharmacological activity (Ojarinta et al. 2017). However, DF presents little solubility in water, which can affect its action against Entamoeba histolytica (Budal et al. 2004). Accordingly, the use of suitable strategies to increase water solubility of DF and dissolution rate in the intestinal fluids may reduce the possibility of the drug precipitating in the lumen, and this would lead to a loss in effectiveness.
Anti-infective treatment of brain abscess
Published in Expert Review of Anti-infective Therapy, 2018
Jacob Bodilsen, Matthijs C. Brouwer, Henrik Nielsen, Diederik Van De Beek
In patients infected with E. histolytica, cerebral amoebiasis has been documented at autopsy among 1.2–2.5%, but in clinical studies this proportion remains less than 0.1%. Treatment includes metronidazole for the brain abscess and diloxanide furoate for clearance of the intestinal stages [103].