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Treatment of Human Mansoni Schistosomiasis: Comparison Between Praziquantel and Oxamniquine in Brazil
Published in Max J. Miller, E. J. Love, Parasitic Diseases: Treatment and Control, 2020
The treatment of schistosomiasis mansoni has markedly advanced during the last decade as a corollary of the development of two drugs — oxamniquine1–5 in the early seventies and praziquantel6–11 in the late seventies. It should be pointed out that whereas the former is solely active against Schistosoma mansoni, the latter displays a broad spectrum of antihelmintic activity comprising not just all schistosoma species pathogenic to man12–20 but also a variety of other trematode, as well as cestode, infections.21–23
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
Oxamniquine (8) is a tetrahydroquinoline derivative used in the treatment of worm infections. Oxamniquine is effective against Schistosoma mansoni at all stages, from acute toxaemic to chronic and complicated infections. Besides, it has no effect on S. haematobium and S. japonicum. Its mode of action is to shift worms from the mesenteric veins to the liver and thereby cause their death. The adverse effects of the oxamniquine are similar to praziquantel and commonly include headache, dizziness, drowsiness, and abdominal pain (Akgün et al. 2013). In the synthesis of oxamniquine, 2,6-dimethylquinoline is chlorinated to give 2-chloromethyl-6-methylquinoline. After replacing the chlorine with isopropylamine, the heterocyclic quinoline ring is reduced via catalytic hydrogenation. Finally, nitration and microbiologically oxidation of the methyl group with Aspergillus sclerotium afford oxamniquine (Vardanyan and Hruby 2006) (Scheme 5). The synthesis of Oxamniquine (8).
Gastrointestinal and liver infections
Published in Michael JG Farthing, Anne B Ballinger, Drug Therapy for Gastrointestinal and Liver Diseases, 2019
The treatment of choice is praziquantel given orally as a single 40 mg/kg dose.128 Improved cure rates for all forms of schistosomiasis have been obtained by giving praziquantel 60 mg/kg as three divided doses over an 8-h period. This is, however, a more difficult regimen to administer in the field. An alternative regimen is oxamniquine given as a single dose of 15 mg/kg up to a total 60 mg/kg over 2-3 days. Metriphonate is only effective against S. haematobium.
Preparation of stabilized submicron fenofibrate crystals on niacin as a hydrophilic hydrotropic carrier
Published in Pharmaceutical Development and Technology, 2020
Rasha A. Alshaikh, Ebtessam A. Essa, Gamal M. El Maghraby
The equilibrium solubility of fenofibrate in different niacin concentration is shown in Table 2. Fenofibrate has limited aqueous solubility in absence of niacin (0.18 μg/ml). The solubility increased progressively by increasing niacin concentration (Table 2). These data indicated significant increase in the solubility of fenofibrate in presence of high concentration of niacin highlighting the possible hydrotropic effect of niacin. Nicotinamide, a structurally related to niacin is widely used as a hydrotropic agent in the pharmaceutical field (Saleh and El-Khordagui 1985; Sanghvi et al. 2007; Kim et al. 2010). Sodium nicotinate and sodium isonicotinate were also employed as hydrotropes for solubilization of oxamniquine (Ammar and Khalil 1996). This effect can influence the dissolution rate of fenofibrate (to be researched in the proceeding sections).
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
Schistosomiasis (Bilharzia) is an infectious disease caused by worms of the family Schistosomatidae (S. mansoni, S. guineensis, S. intercalatum, S. japonicum, S. mekongi. and S. haematobium), mainly the Schistosoma mansoni, associated with poor living and hygiene conditions [20]. Its transmission occurs through snails (mollusks) that come into contact with man in polluted rivers containing feces infested with the larval forms of these worms [20,21]. Two main forms of the disease are described, intestinal schistosomiasis and urogenital schistosomiasis. Intestinal schistosomiasis is characterized mainly by abdominal pain, diarrhea and an increase in the volume of the belly as a result of the enlargement of the size of the liver and spleen [20,22,23]. In turn, urogenital schistosomiasis, can cause damage or injury in the urinary and reproductive system [20]. In addition, the disease can also occur with the involvement of the central nervous system (neuroschistosomiasis), requiring more complex and expensive treatment [24]. Although an avoidable disease, schistosomiasis affects about 240 million people worldwide. In addition, more than 700 million live in endemic areas and, in 2010, schistosomiasis was associated with 3.31 million DALYs [15,21]. In 2019, it was associated with around 1.6 million DALYs with approximately a rate of 21.18 (per 100 thousand peoples) in the world [18]. According to the World Health Organization (WHO), the disease is present in 78 countries and about 90% of people in need of treatment live in Africa. Current data on schistosomiasis mortality are inaccurate. Praziquantel is the main drug used in the treatment of the disease, being recommended by the WHO because it is effective against all species of the parasite [20]. In some cases, oxamniquine and triclabendazole may also be indications for treatment [25]. Praziquantel is a drug that has had its cost of production lowered over the years. It is currently produced mainly in Korea and China, being strategic for combating schistosomiasis in these countries [26–29] and in mass treatment programs in African [30–34].