脂质体两性霉素B:临床药理学、药代动力学和药效学

IF 1.5 4区 生物学 Q4 MYCOLOGY Revista Iberoamericana De Micologia Pub Date : 2021-04-01 DOI:10.1016/j.riam.2021.02.004
José Ramón Azanza Perea
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引用次数: 1

摘要

脂质体两性霉素B是抗真菌药物两性霉素B的脂质制剂,其药理行为具有一些独特的特征,引起了一些临床差异的极大兴趣。系统和肾脏耐受性的显著改善就是其中之一。这一事实与脂质体的巨大稳定性有关,这种稳定性是由它的负电荷、胆固醇的存在和组成它的剩余脂质的显著的热稳定性所促进的。在这种情况下,两性霉素B似乎不是自发地从脂质体中释放出来,而是当脂质体与真菌细胞膜中的麦角甾醇结合时释放出来的。因此,血浆或组织中几乎没有游离两性霉素B,尽管在真菌感染时它的可用性似乎更大。因此,当研究药代动力学行为时,两性霉素B脂质体的浓度和可用性非常高,与其他制剂相比,其分布体积减小。
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Anfotericina B liposomal: farmacología clínica, farmacocinética y farmacodinamia

Liposomal amphotericin B is a lipid formulation of the antifungal drug amphotericin B with some distinguishing characteristics in its pharmacological behavior that entail some clinical differences of great interest. The significant improvement in the systemic and renal tolerability is one of them. This fact is related to the great stability of the liposome, promoted by its negative charge, the presence of cholesterol and the remarkable thermo-stability of the remaining lipids that compose it. In this situation, amphotericin B seems to be released from the liposome not spontaneously but when the liposome binds to the ergosterol in the fungal cell membrane. For this reason, there is almost no free amphotericin B in plasma or tissues, although it seems that its availability is greater when there is fungal infection. As a consequence, when the pharmacokinetic behavior is studied, the concentration and availability of liposomal amphotericin B are very high, and its volume of distribution is reduced in comparison with the other formulations.

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来源期刊
CiteScore
1.90
自引率
0.00%
发文量
17
审稿时长
81 days
期刊介绍: Revista Iberoamericana de Micología (Ibero-American Journal of Mycology) is the official journal of the Asociación Española de Micología, Asociación Venezolana de Micología and Asociación Argentina de Micología (The Spanish, Venezuelan, and Argentinian Mycology Associations). The Journal gives priority to publishing articles on studies associated with fungi and their pathogenic action on humans and animals, as well as any scientific studies on any aspect of mycology. The Journal also publishes, in Spanish and in English, original articles, reviews, mycology forums, editorials, special articles, notes, and letters to the editor, that have previously gone through a scientific peer review process.
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