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Hits and Lead Discovery in the Identification of New Drugs against the Trypanosomatidic Infections
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Theodora Calogeropoulou, George E. Magoulas, Ina Pöhner, Joanna Panecka-Hofman, Pasquale Linciano, Stefania Ferrari, Nuno Santarem, Ma Dolores Jiménez-Antón, Ana Isabel Olías-Molero, José María Alunda, Anabela Cordeiro da Silva, Rebecca C. Wade, Maria Paola Costi
The disease usually evolves from an acute to a chronic phase. The acute phase arises just after the infection and can last from a few weeks to several months and is characterized by non-specific signs (i.e., fever, swelling of skin and mucosa). Thereafter, the disease enters an asymptomatic chronic stage and only 20–30% of the infected people manifest lethal complications after several years (Bern et al. 2011). The treatment of both the acute and chronic stages of Chagas disease is based on chemotherapy. For almost 50 years, benznidazole and nifurtimox (Figure 2) were the two first-line drugs for the treatment of Chagas disease (Rodriques Coura and de Castro 2002). Unfortunately, their efficacy is limited, and more frequently the side effects that the two drugs elicit during the treatment of the chronic stage induce the patients to quit the therapy. Nifurtimox treatment is discontinued in up to 75% of all cases, and benznidazole, which is better tolerated, is discontinued in 9 to 29% of the cases. Besides chemotherapy, serological cure is recommended for acute congenital Chagas during the first year of life, and for chronically infected children under 14 years (Pérez-Molina and Molina 2018). Drugs currently in use for the treatment of Chagas disease and Human African Trypanosomiasis.
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].
Benznidazole
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Ralph K. Junckerstorff, Ronan J. Murray
Benznidazole is an antiparasitic agent active against Trypanosoma cruzi, the causative organism of American trypanosomiasis or Chagas disease. Benznidazole (N-benzyl-2-nitroimidazole acetamide) is a nitroimidazole. Its chemical formula is C12H12N4O3 and its chemical structure is shown in Figure 192.1.
Why do few drug delivery systems to combat neglected tropical diseases reach the market? An analysis from the technology’s stages
Published in Expert Opinion on Therapeutic Patents, 2022
Jabson Herber Profiro de Oliveira, Igor Eduardo Silva Arruda, José Izak Ribeiro de Araújo, Luise Lopes Chaves, Mônica Felts de La Rocca Soares, José Lamartine Soares-Sobrinho
Cyclodextrins were also among the systems found in this study [272,276,280,281,291,297]. Cyclodextrins allow the alteration of the physicochemical characteristics of drugs, including the improvement of water solubility [341–347]. Although its oral administration demonstrates good results, its parenteral administration is considered nephrotoxic and has hemolytic activity [345,348]. However, polymer-conjugated cyclodextrins have been reported to be low in toxicity and very soluble in aqueous solutions [346,349–352]. In particular, in the literature, we highlight the reduction in benznidazole toxicity [353]. Among the patents found, we highlight: increase in solubility for benznidazole [276]; increase in oral absorption and bioavailability of antimony [281]; and increased bioavailability of antimony by oral route [280].
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].
An evaluation of benznidazole as a Chagas disease therapeutic
Published in Expert Opinion on Pharmacotherapy, 2019
Ivo S. Caldas, Elda G. Santos, Rômulo D. Novaes
Over decades of research and use of benznidazole in clinical practice, the pharmacokinetic profile of this drug has not been consistently considered in the treatment of patients with Chagas disease. In addition to hampering the development and evaluation of the pharmacological characteristics of novel benznidazole formulations [27], the paucity of pharmacokinetic evidence often encourages the application of adult dosages to children by using simple and inadvisable weight-based adjustments [23]. However, understand the pharmacokinetic profile of benznidazole can contribute to the rational design of specific protocols for adult and pediatric populations [23,24]. In this sense, information about absorption and elimination half-life, maximal concentrations, and total clearance are useful for adjusting the doses administered and reduce the risk of bioaccumulation and systemic toxicity [23,24], which are factors known to be associated with treatment discontinuation and lower therapeutic efficacy [8,27].