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阿维A酯在慢性肾衰竭中的药代动力学。对银屑病患者的初步研究。

Etretinate pharmacokinetics in chronic renal failure. A preliminary study in psoriasis patients.

作者信息

Vahlquist A

机构信息

Department of Dermatology, University of Uppsala, Akademiska Hospital, Sweden.

出版信息

Dermatologica. 1987;175(5):224-8. doi: 10.1159/000248908.

DOI:10.1159/000248908
PMID:2960573
Abstract

Chronic renal failure (CRF) interferes with the catabolism of retinol and is frequently associated with hypervitaminosis A. The effect of CRF on the plasma levels of etretinate (Tigason, Tegison), an aromatic retinoid, was therefore studied in 4 patients who were given the drug as part of a maintenance antipsoriatic regimen. The concentrations of the parent compound and its main metabolites (etretin and isoetretin) were monitored for 24 h after receiving a routine dose of the drug. In comparison with 4 non-CRF patients receiving similar maintenance doses of etretinate, although the CRF patients had higher peak levels of the parent compound (p less than 0.01), the levels of the metabolites were similar or lower. The plasma half-lives for all compounds were approximately the same in each group, indicating that the catabolism of the drug was not affected by CRF. However, elevated etretinate concentrations may increase the drug accumulation in fat tissues and thereby prolong the time required for final elimination of the drug.

摘要

慢性肾衰竭(CRF)会干扰视黄醇的分解代谢,且常与维生素A过多症相关。因此,在4例将阿维A酯(银屑灵,Tegison)作为维持性抗银屑病治疗方案一部分的患者中,研究了CRF对其血浆水平的影响。在给予常规剂量药物后,监测母体化合物及其主要代谢产物(阿维A和异阿维A)的浓度24小时。与4例接受相似维持剂量阿维A酯的非CRF患者相比,尽管CRF患者母体化合物的峰值水平较高(p<0.01),但其代谢产物水平相似或更低。每组中所有化合物的血浆半衰期大致相同,表明CRF不影响药物的分解代谢。然而,阿维A酯浓度升高可能会增加药物在脂肪组织中的蓄积,从而延长药物最终消除所需的时间。

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Etretinate pharmacokinetics in chronic renal failure. A preliminary study in psoriasis patients.阿维A酯在慢性肾衰竭中的药代动力学。对银屑病患者的初步研究。
Dermatologica. 1987;175(5):224-8. doi: 10.1159/000248908.
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Pharmacokinetics of etretin and etretinate during long-term treatment of psoriasis patients.依曲替酯和阿维A酯在银屑病患者长期治疗期间的药代动力学
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Int J Dermatol. 1990 May;29(4):270-1. doi: 10.1111/j.1365-4362.1990.tb02559.x.
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[Pharmacokinetics of etretinate, acitretin and 13-cis-acitretin: new results and advantages of blood level oriented clinical use].[依曲替酯、阿维A及13-顺式阿维A的药代动力学:血药浓度导向临床应用的新结果及优势]
Z Hautkr. 1990 Jan;65(1):40-50.
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Teratogenicity of steady-state concentrations of etretinate and metabolite acitretin maintained in maternal plasma and embryo by intragastric infusion during organogenesis in the mouse: a possible model for the extended elimination phase in human therapy.通过在小鼠器官形成期经胃灌注维持母体血浆和胚胎中阿维A酯及其代谢产物阿维A的稳态浓度的致畸性:人类治疗中延长消除期的一种可能模型。
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J Am Acad Dermatol. 1992 Dec;27(6 Pt 2):S8-14. doi: 10.1016/s0190-9622(08)80253-8.

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