Diloxanide in amoebiasis management: Unravelling the mechanism of action and effectiveness

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Samuel Inshutiyimana, Michael Matiop Aleu, Mustaf Aden Abdinoor, Mariyah Murtaza Janoowalla, Norhayati Norhayati
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Abstract

Although diloxanide is a drug of choice for treating asymptomatic amoebiasis, its mechanism of action (MOA) remains unclear. This review aims to shed light on the current understanding of the effectiveness and MOA of diloxanide in treating amoebiasis . It involves analysis of articles, retrieved from PubMed, Google Scholar and EBSCOhost, on diloxanide and the treatment of Entamoeba histolytica infection. Diloxanide is used in an ester form, which allows its high luminal concentration and greater efficacy than metronidazole in the management of asymptomatic amoebiasis. The current understanding of the action of diloxanide is based on its structural similarity to chloramphenicol at dichloroacetamide group. It acts against protein synthesis in E. histolytica trophozoites, blocking their conversion to more virulent and invasive cyst forms. Furthermore, it has a parasite clearance rate of 81–96% and treats amoebic abscesses when combined with metronidazole and chloroquine. Nevertheless, it is associated with adverse events such as flatulence, anorexia, headache and urticaria. Diloxanide is efficacious against amoebiasis but there is a need to explore its structure–activity relationship.The study suggests future directions, including novel drug formulations, diagnostic improvements, and combination regimens to enhance treatment outcomes and mitigate relapse associated with the use of diloxanide.

Abstract Image

地洛沙尼在阿米巴病治疗中的应用:揭示作用机制和有效性。
尽管地洛沙尼是治疗无症状阿米巴病的首选药物,但其作用机制(MOA)仍不明确。本综述旨在阐明目前对地洛沙尼治疗阿米巴病的有效性和作用机制的认识。文章分析了从 PubMed、Google Scholar 和 EBSCOhost 上检索到的有关地洛沙尼和治疗组织溶解恩塔米巴虫感染的文章。地洛沙内酯以酯类形式使用,在治疗无症状阿米巴病时,其腔内浓度高,疗效优于甲硝唑。目前对地洛沙内酯作用的了解是基于它与氯霉素在二氯乙酰胺基团上的结构相似性。它能抑制组织溶解埃希氏菌滋养体的蛋白质合成,阻止其转化为毒性更强的侵袭性包囊形式。此外,它的寄生虫清除率高达 81-96%,与甲硝唑和氯喹合用可治疗阿米巴脓肿。不过,该药也有不良反应,如胀气、厌食、头痛和荨麻疹。该研究提出了未来的发展方向,包括新型药物制剂、诊断改进和联合疗法,以提高治疗效果并减少与使用地洛沙尼相关的复发。
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来源期刊
CiteScore
5.60
自引率
6.50%
发文量
126
审稿时长
1 months
期刊介绍: Basic & Clinical Pharmacology and Toxicology is an independent journal, publishing original scientific research in all fields of toxicology, basic and clinical pharmacology. This includes experimental animal pharmacology and toxicology and molecular (-genetic), biochemical and cellular pharmacology and toxicology. It also includes all aspects of clinical pharmacology: pharmacokinetics, pharmacodynamics, therapeutic drug monitoring, drug/drug interactions, pharmacogenetics/-genomics, pharmacoepidemiology, pharmacovigilance, pharmacoeconomics, randomized controlled clinical trials and rational pharmacotherapy. For all compounds used in the studies, the chemical constitution and composition should be known, also for natural compounds.
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