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Antiprotozoal Effects of Wild Plants
Published in Mahendra Rai, Shandesh Bhattarai, Chistiane M. Feitosa, Ethnopharmacology of Wild Plants, 2021
Muhammad Subbayyal Akram, Rao Zahid Abbas, José L. Martinez
Until recently, metronidazole, and its derivatives secnidazole and tinidazole, was the only drug of choice for the treatment of trichomoniasis (Wendel and Workowski 2007). However, it’s not safe to use metronidazole in pregnancy as it may result in fetal malformation, and increase the risk of preterm birth, specifically when used in the first trimester (Klebanoff et al. 2001). Persistent and overuse of metronidazole and its derivatives result in the development of drug-resistant strains of T. vaginalis; chiefly, parasite develops resistance against 5-nitomidazole derivatives, which was observed in up to 20% of patients (Krashin et al. 2010). The resistance of metronidazole and tinidazole in T. vaginalis were 9.6% and 0.56%, respectively (Schwebke and Barrientes 2006). In this scenario, development and research of new drugs is a necessity and wild plants’ extracts show promising results against resistant strains of T. vaginalis.
Clinical Spectrum of Amebiasis in Children
Published in Roberto R. Kretschmer, Amebiasis: Infection and Disease by Entamoeba histolytica, 2020
The diarrheic-dysenteric form of amebiasis must in principle be treated like any other acute infectious diarrhea in children: i.e., oral hydration and normal diet or breast feeding, and when present, control of fever and vomiting, the latter with short fasting periods. In addition, any of the two following therapeutic schedules should lead to complete recovery7: (1) oral metronidazole or related compounds (secnidazole, nimorazole), 30 to 40 mg/kg/ day, t.i.d. for 5 to 10 days, with a daily dose not exceeding 2.0 g; or (2) intramuscular emetine hydrochloride, 1 mg/kg/day, maximal daily dose 65 mg, or dehydroemetine, 1.5 mg/kg/day, maximal daily dose 90 mg, for 5 to 10 days. The latter drugs are not to be administered to patients with heart disease. Metronidazole and emetine or dehydroemetine at the recommended doses may be administered simultaneously in particularly severe cases. Metronidazole may be administered intravenously if vomiting is persistent, in cases of gastric intolerance to the drug or when the oral route cannot be used for other reasons. Emetine can cause cardiac arrythmias or pain at the site of application. However, at correct doses, no cardiotoxic effects will arise. Metronidazole is mutagenic for bacteria and carcinogenic for mice but not in humans, at least not at therapeutic doses.64,65 Metronidazole causes nausea and vomiting and may behave like disulfiram when alcohol is ingested.
Dientamoeba fragilis Infection
Published in Dongyou Liu, Handbook of Foodborne Diseases, 2018
Candela Menéndez Fernández-Miranda, Jonathan Fernández Suarez, Noelia Moran Suarez, Javier Fernández Domínguez, María Martínez Sela, Mercedes Rodríguez Pérez, Azucena Rodríguez-Guardado
Secnidazole and ornidazole are 5-nitroimidazole derivatives. They have a longer half-life than metronidazole, so they can be administered in a single oral dose per day, and they have less side effects. Girginkardesler et al.72 studied the treatment of D. fragilis with secnidazole in 35 patients, being eradicated in 34 of them (97%). Ornidazole was used by Kurt et al.107 for the treatment of D. fragilis infection, and comparing with metronidazole, 112 patients were enrolled and randomized in two treatment groups: the first was treated with ornidazole in a single oral dose, and the second with metronidazole three times a day. They achieved parasitological eradication in 52 of 56 (92.9%) patients treated with ornidazole, and 39 of 56 (69.6%) patients treated with metronidazole. The four remaining patients of the ornidazole group were treated again with this drug, demonstrating parasite eradication. In the second group only 8 of the 17 remaining patients were cured with a second regimen, and the other nine had to receive a single oral dose of ornidazole to achieve eradication.
Successes, failures, and future prospects of prodrugs and their clinical impact
Published in Expert Opinion on Drug Discovery, 2019
Antimicrobials of the 5-nitroimidazole class are the first line choice in the treatment of protozoal and some bacterial infections. Metronidazole and tinidazoleare are prodrugs with a similar proposed mechanism of action: the parent compound diffuses into the target organism and is reduced to several intermediates which cause cytotoxicity. Tinidazole is commonly prescribed for giardiasis, bacterial vaginosis, and H. pylori. Metronidazole, though, undergoes heavy hepatic metabolism producing 5 metabolites. Hydroxy-metronidazole, is an active metabolite with 30–65% of the antimicrobial activity of metronidazole [62]. Secnidazole is a second generation 5-nitroimidazole commonly prescribed for bacterial vaginosis. It is oxidized hepatically to an active hydroxyethyl metabolite. Both parent compound and its metabolite are clinically significant [61,63]. The mechanism of action of both secnidazole and its active metabolite is similar to that of metronidazole.
Bacterial vaginosis: a primer for clinicians
Published in Postgraduate Medicine, 2019
Suzanne Reiter, Susan Kellogg Spadt
Secnidazole (SYM-1219) is a novel granular formulation member of the family of 5-nitroimidazoles that was approved in the United States in 2017 for the treatment of BV [100]. This granular formulation is designed to be sprinkled into applesauce, yogurt, or pudding and consumed without chewing the granules. Prior to US approval, secnidazole was used in Europe and Asia to treat BV, trichomoniasis, and other conditions. In vitro studies with secnidazole demonstrated clinical and microbiologic evidence of activity against many anaerobic Gram-positive and Gram-negative bacteria implicated in BV [101] and limited activity against beneficial lactobacilli species [92,102,103]. Pharmacokinetic/pharmacodynamic studies of secnidazole have been favorable, showing rapid absorption, high bioavailability, low intersubject variability, longer half-life, high potency, and minimal potential for interactions with CYP450 substrates, inhibitors, or inducers, supporting its use as a single-dose treatment for BV [104,105]. Additionally, the results of a thorough QT/QTc evaluation of the cardiac safety of secnidazole at therapeutic and supratherapeutic doses in healthy individuals demonstrated that secnidazole does not have any clinically concerning effect on ECG parameters, including QT interval [106].