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伊维菌素与血浆蛋白紧密结合。

Ivermectin binds avidly to plasma proteins.

作者信息

Klotz U, Ogbuokiri J E, Okonkwo P O

机构信息

Dr. Margarete-Fischer-Bosch Institut für Klinische Pharmakologie, Stuttgart, FRG.

出版信息

Eur J Clin Pharmacol. 1990;39(6):607-8. doi: 10.1007/BF00316107.

DOI:10.1007/BF00316107
PMID:2095348
Abstract

Human pharmacokinetic data on the new anti-parasitic agent, ivermectin, are scanty. For the evaluation of its disposition a specific HPLC assay with sensitive fluorescence detection was developed. Applying equilibrium dialysis, plasma protein binding of ivermectin was measured in five healthy individuals and it averaged 93.2 +/- 4.4% (SD). Such strong binding should be taken into consideration, especially in patients with malnutrition or with diseases in which a decrease in plasma proteins and consequently a higher free fraction of ivermectin could be expected.

摘要

关于新型抗寄生虫药物伊维菌素的人体药代动力学数据较少。为评估其处置情况,开发了一种具有灵敏荧光检测的特定高效液相色谱法。应用平衡透析法,在五名健康个体中测量了伊维菌素的血浆蛋白结合率,其平均值为93.2±4.4%(标准差)。应考虑到这种强结合情况,尤其是在营养不良患者或患有血浆蛋白减少从而预期伊维菌素游离部分会增加的疾病的患者中。

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本文引用的文献

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The chemotherapy of onchocerciasis X. An assessment of four single dose treatment regimes of MK-933 (ivermectin) in human onchocerciasis.盘尾丝虫病的化疗X. MK-933(伊维菌素)四种单剂量治疗方案治疗人类盘尾丝虫病的评估
Ann Trop Med Parasitol. 1985 Feb;79(1):63-78.
2
The relative systemic availability of ivermectin after administration as capsule, tablet, and oral solution.伊维菌素以胶囊、片剂和口服溶液给药后的相对全身可用性。
Eur J Clin Pharmacol. 1988;35(6):681-4. doi: 10.1007/BF00637608.
伊维菌素、tafenoquine和氯喹在恒河猴中的安全性、药代动力学及潜在神经相互作用
Antimicrob Agents Chemother. 2024 Jun 5;68(6):e0018124. doi: 10.1128/aac.00181-24. Epub 2024 May 14.
4
Nonspecific membrane bilayer perturbations by ivermectin underlie SARS-CoV-2 activity.伊维菌素引起的非特异性膜双层扰动是新冠病毒活性的基础。
bioRxiv. 2023 Oct 24:2023.10.23.563088. doi: 10.1101/2023.10.23.563088.
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Computational Prediction of the Interaction of Ivermectin with Fibrinogen.伊维菌素与纤维蛋白原相互作用的计算预测。
Int J Mol Sci. 2023 Jul 14;24(14):11449. doi: 10.3390/ijms241411449.
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