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Progress in the National Schistosomiasis Control Programme of Iran
Published in Max J. Miller, E. J. Love, Parasitic Diseases: Treatment and Control, 2020
Chemotherapy with niridazole often produced side effects on the 3rd and 4th day of treatment, as a result of which some patients, particularly children, refused to complete the prescribed course. From 1981, metrifonate was used in the treatment of infected persons in the area with a much higher cure rate and minor side effects. The cure rate with metrifonate varied between 80 to 93%, which was significantly higher than with niridazole. Repeated annual chemotherapy in the area proved to be highly effective. Among subjects who continued to excrete schistosome eggs after treatment, the mean concentration was reduced from 15,700 eggs per liter of urine in 1967,3 to 11,800 per liter in 1976,1 and to 1,000 per liter in 1986.
An Overview of Helminthiasis
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Leyla Yurttaș, Betül Kaya Çavușoğlu, Derya Osmaniye, Ulviye Acar Çevik
Metrifonate (15), originally developed as an insecticide, is an alternative drug for the therapy of urinary schistosomiasis including Schistosoma haematobium and S. mansoni. It is an organophosphate inhibitor of acetylcholinesterase. Side effects include nausea, vomiting, vertigo, headache, lethargy, abdominal pain and diarrhea. It has largely been replaced by praziquantel as primary therapy. Metrifonate is made by the condensation of dimethyl phosphite with 2,2,2-trichloroacetaldehyde (Akgün et al. 2013, Kuhlmann and Fleckenstein 2017). Synthesis of Metrifonate (15).
Oxamniquine and Metrifonate
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
Metrifonate was initially used as an insecticide, which then led to the treatment of the ectoparasites of farm animals. Initial in vitro studies suggested activity against schistosomes, hookworm, Ascaris spp., and Trichuris spp. (Holmstedt et al., 1978). The vast majority of information obtained on the human use of metrifonate comes from the treatment of schistosomiasis—in particular, S. haematobium infection.
Treating organophosphates poisoning: management challenges and potential solutions
Published in Critical Reviews in Toxicology, 2020
Maria Alozi, Mutasem Rawas-Qalaji
Despite their high toxicity profiles, smaller doses of certain OP have shown some therapeutic benefits. As a long-acting inhibitor, echothiophate iodide (Phospholine®) eye drop formulation is approved for treating glaucoma. Phospholine® helps treat glaucoma by sustaining ACh levels to mitigate intraocular pressure (Phospholine Iodide® Ophthalmic 2018). Additionally, the short-term safety of metrifonate for treating schistosomiasis led researchers to investigate its efficacy for treating dementia by enhancing central cholinergic neurotransmission. Despite its proven efficacy, its long-term use during phase III clinical trials was found to induce respiratory paralysis and led to the discontinuation of the clinical trial and subsequent FDA withdrawal (Sharma 2019).
Non-conventional compounds with potential therapeutic effects against Alzheimer’s disease
Published in Expert Review of Neurotherapeutics, 2019
Alexandre A. de Castro, Flávia V. Soares, Ander F. Pereira, Daniel A. Polisel, Melissa S. Caetano, Daniel H. S. Leal, Elaine F. F. da Cunha, Eugenie Nepovimova, Kamil Kuca, Teodorico C. Ramalho
Alzheimer’s disease (AD) is a kind of pathology that is widespread, becoming a serious public health problem at a global level. Several researchers around the world have dedicated efforts in the search for alternative therapies for AD treatment, but to date, there is no therapy or therapeutic agent capable of inducing reversal of the disease. Current drugs in use bring about symptomatic benefits, but without reversing the pathological process. In this context, the discovery of novel remediation methods is crucial to an attempt of providing better and more efficient treatments of AD. Interestingly, there are non-conventional compounds and/or tools that bring about significant results in the control of the disease. Methylene blue, for example, is described in the literature as having important outcomes in AD therapy, along with the potential benefits from natural products and those from traditional Chinese medicine. The incredible diversity of active substances found from these approaches allows for a range of possibilities with practical applications on AD treatment. Finally, among the organophosphorus compounds, despite the high toxicity present in most of them, there are some compounds with therapeutic potential for use in the treatment of NDs, such as AD. In this line, trichlorfon, also called metrifonate, is described in the literature as one of these beneficial compounds. On the other hand, further investigations are required to better understand its performance and action mechanism within the human body. Furthermore, this compound should be used with caution due to reports of severe side effects in some occasions.
Pyridostigmine bromide and its relation to Gulf War illness
Published in Toxin Reviews, 2020
Jana Zdarova Karasova, Milos Hroch, Miroslav Pohanka, Vendula Hepnarova, Jaroslav Pejchal, Kamil Kuca
The overview of blood biochemical markers corresponds with the results of basic oxidative stress markers. Decreased TBARS values measured in the 2 and 3h intervals suggest suppression of basal metabolism as discussed earlier for metrifonate, another AChE inhibitor (Lu et al. 2018).