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两性霉素B:内脏利什曼病的首选药物。

Amphotericin B: A drug of choice for Visceral Leishmaniasis.

作者信息

Kumari Shobha, Kumar Vikash, Tiwari Ritesh Kumar, Ravidas Vidyanand, Pandey Krishna, Kumar Ashish

机构信息

Department of Biochemistry, Rajendra Memorial Research Institute of Medical Sciences, Agamkuan, Patna, Bihar 800007, India.

Department of Clinical Medicine, Rajendra Memorial Research Institute of Medical Sciences, Agamkuan, Patna, Bihar 800007, India.

出版信息

Acta Trop. 2022 Nov;235:106661. doi: 10.1016/j.actatropica.2022.106661. Epub 2022 Aug 20.

DOI:10.1016/j.actatropica.2022.106661
PMID:35998680
Abstract

Visceral leishmaniasis or Kala-azar is a vector-borne disease caused by an intracellular parasite of the genus leishmania. In India, Amphotericin B (AmB) is a first-line medication for treating leishmaniasis. After a large-scale resistance to pentavalent antimony therapy developed in Bihar state, it was rediscovered as an effective treatment for Leishmania donovani infection. AmB which binds to the ergosterol of protozoan cells causes a change in membrane integrity resulting in ions leakage, and ultimately leading to cell death. The treatment effect of liposomal AmB can be seen more quickly than deoxycholate AmB because, it has some toxic effects, but liposomal AmB is significantly less toxic. Evidence from studies suggested that ABLC (Abelcet) and ABCD (Amphotec) are as effective as l-AmB but Liposomal form (Ambisome) is a more widely accepted treatment option than conventional ones. Nevertheless, the world needs some way more efficient antileishmanial drugs that are less toxic and less expensive for people living with parasitic infections caused by Leishmania. So, academics, researchers, and sponsors need to focus on finding such drugs. This review provides a summary of the chemical, pharmacokinetic, drug-target interactions, stability, dose efficacy, and many other characteristics of the AmB and their various formulations. We have also highlighted the clinically significant aspects of PKDL and VL co-infection with HIV/TB.

摘要

内脏利什曼病或黑热病是一种由利什曼原虫属细胞内寄生虫引起的媒介传播疾病。在印度,两性霉素B(AmB)是治疗利什曼病的一线药物。在比哈尔邦对五价锑疗法产生大规模耐药性后,它被重新发现是治疗杜氏利什曼原虫感染的有效药物。与原生动物细胞的麦角固醇结合的AmB会导致膜完整性改变,导致离子泄漏,最终导致细胞死亡。脂质体两性霉素B的治疗效果比脱氧胆酸盐两性霉素B出现得更快,因为它有一些毒性作用,但脂质体两性霉素B的毒性明显较小。研究证据表明,ABLC(Abelcet)和ABCD(Amphotec)与脂质体两性霉素B(l-AmB)一样有效,但脂质体形式(安必素)比传统剂型更被广泛接受。然而,对于感染利什曼原虫引起的寄生虫病的人来说,世界需要更高效、毒性更小且更便宜的抗利什曼药物。因此,学者、研究人员和赞助商需要专注于寻找此类药物。本综述总结了两性霉素B及其各种制剂的化学、药代动力学、药物靶点相互作用、稳定性、剂量疗效和许多其他特性。我们还强调了PKDL以及与HIV/TB共感染VL的临床重要方面。

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