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补骨脂素的生物药剂学、药代动力学及药理学

Biopharmaceutics, pharmacokinetics and pharmacology of psoralens.

作者信息

Stolk L M, Siddiqui A H

机构信息

Department of Pharmacy, Academic Medical Centre, Amsterdam, The Netherlands.

出版信息

Gen Pharmacol. 1988;19(5):649-53. doi: 10.1016/0306-3623(88)90122-x.

DOI:10.1016/0306-3623(88)90122-x
PMID:3063592
Abstract

The psoralen derivative 8-methoxypsoralen (8-MOP) and to a lesser extent some other psoralens, including 5-methoxypsoralen (5-MOP) and 4,5',8-trimethylpsoralen (TMP) have acquired a place in the treatment of psoriasis and other dermatoses. They are only active when combined with long-wave ultraviolet light: PUVA therapy (Psoralen plus UVA). Successful PUVA therapy depends on sufficiently high psoralen concentrations coinciding with the time of irradiation. The use of oral or rectal pharmaceutical formulations with 8-MOP dissolved in liquid is preferable to conventional tablets or capsules. Since no formulation of 5-MOP with fast and predictable absorption is available 8-MOP should be preferred in PUVA therapy. The effectiveness of oral TMP is doubtful, because of low serum concentrations, probably due to malabsorption.

摘要

补骨脂素衍生物8-甲氧基补骨脂素(8-MOP)以及在较小程度上的其他一些补骨脂素,包括5-甲氧基补骨脂素(5-MOP)和4,5',8-三甲基补骨脂素(TMP),在银屑病和其他皮肤病的治疗中占据了一席之地。它们只有在与长波紫外线结合时才具有活性:即光化学疗法(补骨脂素加紫外线A)。成功的光化学疗法取决于在照射时补骨脂素浓度足够高。使用将8-MOP溶解在液体中的口服或直肠药物制剂优于传统片剂或胶囊。由于没有可快速且可预测吸收的5-MOP制剂,在光化学疗法中应首选8-MOP。口服TMP的有效性存疑,因为血清浓度较低,这可能是由于吸收不良所致。

相似文献

1
Biopharmaceutics, pharmacokinetics and pharmacology of psoralens.补骨脂素的生物药剂学、药代动力学及药理学
Gen Pharmacol. 1988;19(5):649-53. doi: 10.1016/0306-3623(88)90122-x.
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Psoralens percutaneous permeation across the human whole skin and the epidermis in respect to their polarity (in vitro study).补骨脂素经皮透过人体全皮和表皮的极性研究(体外研究)
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Clinical pharmacokinetics of methoxsalen and other psoralens.
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Psoralens and related compounds in the treatment of psoriasis.补骨脂素及相关化合物在银屑病治疗中的应用
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The evolution of photochemotherapy with psoralens and UVA (PUVA): 2000 BC to 1992 AD.补骨脂素与紫外线A光化学疗法(PUVA)的发展历程:公元前2000年至公元1992年。
J Photochem Photobiol B. 1992 Jun 30;14(1-2):3-22. doi: 10.1016/1011-1344(92)85080-e.
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Photochemotherapy (PUVA) and psoriasis: comparison of 8-MOP and 8-MOP/5-MOP.光化学疗法(补骨脂素加紫外线A,PUVA)与银屑病:8-甲氧基补骨脂素和8-甲氧基补骨脂素/5-甲氧基补骨脂素的比较
Int J Dermatol. 1976 Nov;15(9):688-9. doi: 10.1111/j.1365-4362.1976.tb01829.x.
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Pharmacokinetics and pharmacodynamics of psoralens after oral administration: considerations and conclusions.口服补骨脂素后的药代动力学和药效学:思考与结论
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10
Interstrand crosslinks in DNA of phage lambda after exposure to 8-methoxypsoralen and trimethylpsoralen in the presence of light.在光照条件下,噬菌体λ的DNA在暴露于8-甲氧基补骨脂素和三甲基补骨脂素后形成的链间交联。
J Invest Dermatol. 1979 Sep;73(3):236-8. doi: 10.1111/1523-1747.ep12514302.

引用本文的文献

1
Effects of psoralens as anti-tumoral agents in breast cancer cells.补骨脂素作为乳腺癌细胞抗肿瘤剂的作用。
World J Clin Oncol. 2014 Aug 10;5(3):348-58. doi: 10.5306/wjco.v5.i3.348.
2
5-Methoxypsoralen. A review of its effects in psoriasis and vitiligo.5-甲氧基补骨脂素。其对银屑病和白癜风作用的综述。
Drugs. 1998 Oct;56(4):667-90. doi: 10.2165/00003495-199856040-00015.
3
In vivo activation of human immunodeficiency virus type 1 long terminal repeat by UV type A (UV-A) light plus psoralen and UV-B light in the skin of transgenic mice.
紫外线A(UV-A)光加补骨脂素以及紫外线B(UV-B)光在转基因小鼠皮肤中对人免疫缺陷病毒1型长末端重复序列的体内激活作用
J Virol. 1991 Sep;65(9):5045-51. doi: 10.1128/JVI.65.9.5045-5051.1991.