China
Africa
Explore chapters and articles related to this topic
The Challenge of Parasite Control
Published in Eric S. Loker, Bruce V. Hofkin, Parasitology, 2023
Eric S. Loker, Bruce V. Hofkin
The threat of drug resistance is not the only reason to welcome the arrival of new anti-parasitic drugs. As previously discussed, the difficulty of achieving selective toxicity against eukaryotic parasites is an important reason that we have so few safe and effective anti-parasitic drugs to begin with. In certain cases, available drugs carry substantial baggage in the form of side effects or complex treatment regimens. All the drugs currently used to treat the later stages of African trypanosomiasis, for instance, require either injection or intravenous administration, sometimes for as long as 2 weeks. They also cause serious side effects. The problem is almost as grim when considering treatment options for American trypanosomiasis (Chagas disease). Currently, there are only two available drugs, both of which can cause adverse reactions. Nifurtimox can cause symptoms ranging from anorexia to nerve damage. Benznidazole may sometimes cause severe skin inflammation. New treatment options against these and other parasitic diseases have been slow in coming, but at least some new and safer drugs are at least in trials, offering hope that new treatment options may be on the horizon.
Curcumin and Neglected Infectious Diseases
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Francesca Mazzacuva, Agostino Cilibrizzi
The use of nitrocompounds (e.g., benznidazole (22) and nifurtimox (23), Figure 6) represents the common treatment in the event of infection from Trypanosoma cruzi (Muñoz et al. 2011, Diniz et al. 2013, Oliveira 2015),which is the etiological agent of Chagas disease. However, there is a lack of specific and effective therapies, since several disadvantages are associated to the use of nitrocompounds, including elevated toxicity (mainly due to the production of reactive oxygen and nitrogen species in the host through cytochrome P450 metabolism) and limited efficacy in the latest stages of the infection (i.e., once the parasites are diffused in multiple organs and tissues) (Rassi et al. 2010, Novaes et al. 2015).
Trypanosoma cruzi
Published in Dongyou Liu, Handbook of Foodborne Diseases, 2018
Paula Andrea Jiménez, Jesus Eduardo Jaimes, Juan David Ramírez
Doses for patient treatment vary from the drug used to the age of the patient. Treatment with benzonidazole is done at any age at doses of 5–7 mg/kg/day in two doses for 60 days. Nifurtimox is used in children under 10 years of age at a dose of 15–20 mg/kg/day, from 11 to 16 years of age, 12.5–15 mg/kg/day is used in three to four doses per 90 days, and in adults a dose of 8–10 mg/kg/day in three to four doses per 90–120 days [75].
Repurposing of rabeprazole as an anti-Trypanosoma cruzi drug that targets cellular triosephosphate isomerase
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Itzhel García-Torres, Ignacio De la Mora-De la Mora, Gabriel López-Velázquez, Nallely Cabrera, Luis Antonio Flores-López, Ingeborg Becker, Juliana Herrera-López, Roberto Hernández, Ruy Pérez-Montfort, Sergio Enríquez-Flores
Currently, Benznidazol (Bzn) and nifurtimox with over 40 years of use, are the only relatively effective treatments for acute CD. However, their efficacy against the chronic stage of the disease is uncertain in some cases, and their therapeutic regimens can extend for several months with common toxic side effects7. One of the most reported adverse effects for Bzn are dermatological alterations and gastrointestinal complications8 with a higher incidence in females and young adults. A study involving patients with established Chagas cardiomyopathy suggested that Bzn treatment may be less effective in those with chronic CD9. Regarding nifurtimox, a CDC report between 2001 and 2021 indicates that the patients’ most common adverse effects were nausea, anorexia, weight loss, headache, and abdominal pain, with some reporting severe adverse events as depression, peripheral neuropathy, paresthaesia, dizziness/vertigo10. Moreover, treatment-refractory strains of parasites are frequently observed11–13. The absence of approved and efficient drugs to combat CD has contributed to the disease’s increasing incidence. Consequently, research efforts have increased over the past decades to identify new anti-chagasic compounds and therapeutic targets.
How effective are rapid diagnostic tests for Chagas disease?
Published in Expert Review of Anti-infective Therapy, 2021
Maria-Jesus Pinazo, Joaquim Gascon, Julio Alonso-Padilla
There are two trypanocidal drugs available to treat Chagas disease: benznidazole (BNZ) and nifurtimox (NFX). They have a very good efficacy when administered early in the initial acute phase of the disease, especially in neonates under the age of one year, who also tolerate the treatment very well [3]. However, this acute phase is mostly asymptomatic and often goes undiagnosed and thus untreated. If host immunity and/or treatment do not clear the parasite during it, the infection becomes chronic. By then, it is estimated that about a third of those chronically infected will develop cardiac, digestive, or cardio-digestive tissue damage, which can be life-threatening [1]. In the chronic phase, the efficacy of the anti-parasitic drugs is diminished, and their long-term administration regimens involve frequent side effects [4]. Yet, until more efficacious and safer drugs, or new regimens of already existing ones become available, BNZ and NFX are the best and only options. Moreover, despite their limitations, the results of several observational studies with chronically infected adults conclude that treatment when clinical symptomatology is absent or incipient has benefits [5,6].
Synthesis, antiproliferative and antitrypanosomal activities, and DNA binding of novel 6-amidino-2-arylbenzothiazoles
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Livio Racané, Valentina Rep, Sandra Kraljević Pavelić, Petra Grbčić, Iva Zonjić, Marijana Radić Stojković, Martin C. Taylor, John M. Kelly, Silvana Raić-Malić
Preliminary screening of 2-arylbenzimidazole amidines 6a–6c, 7a–7c, 8, 14a–18a, 14b–18b, and 14c–18c against bloodstream-form T. brucei in vitro was performed at a range of concentrations to select compounds with the highest inhibition for further evaluation (Table S1, Supplementary material). Thus, compounds, 10a–10c, 11a–11d, 12b, 12c, 13a, 13b, 14a–14d, and 15b, were submitted for more detailed evaluation and the concentrations that inhibited growth by 50% (IC50) and 90% (IC90) were determined (Table 2). Nifurtimox was included as a reference drug. Cytotoxicity was assessed using the rat myoblast cell line L6.