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治疗银屑病患者的麦考酚酸的药物监测。

Therapeutic drug monitoring of mycophenolic acid in patients with psoriasis.

机构信息

Dermatology Department, Hospital de la Princesa, Diego de León street, 62, 28006 Madrid, Spain.

出版信息

Eur J Dermatol. 2010 May-Jun;20(3):321-2. doi: 10.1684/ejd.2010.0899. Epub 2010 Feb 10.

DOI:10.1684/ejd.2010.0899
PMID:20146966
Abstract

Mycophenolate mofetil (MMF) has been shown to be effective in the treatment of psoriasis. MMF is the morpholinoethyl ester of mycophenolic acid (MPA), the active compound. Our objective was to characterize the pharmacokinetic profile of MPA in patients with psoriasis treated with MMF and to examine its correlation with effectiveness and toxicity. Eleven patients with moderate-to-severe chronic plaque psoriasis were treated with oral MMF 30 mg kg-1 daily over a period of 16 weeks. Patients were reviewed at 3, 8 and 16 weeks, checking the Psoriasis Area and Severity Index (PASI) and possible adverse events, and performing MPA C0 (trough) and C1 (1-hour post-dose) plasma levels. The reduction in PASI was statistically significant in all our patients. The drug was well tolerated. There was no significant correlation between C0 and C1 MPA levels and the reduction of PASI, improvement rates of PASI from baseline, weight of the patients and total dosage of MMF. Nevertheless, the highest detected mean levels of MPA C1 were observed in two of the patients with the highest improvement rate of PASI at the end of the study. Although C1 levels do not seem to strongly correlate with the effectiveness of the drug, the finding that the highest detected mean levels of MPA C1 were observed in two of the patients with the highest improvement rate of PASI suggests that the monitoring of C1 could be useful in some individual cases.

摘要

霉酚酸酯(MMF)已被证明在治疗银屑病方面有效。MMF 是霉酚酸(MPA)的吗啉乙酯,是一种活性化合物。我们的目的是描述接受 MMF 治疗的银屑病患者中 MPA 的药代动力学特征,并研究其与疗效和毒性的相关性。11 名中重度慢性斑块型银屑病患者接受 MMF 30mg/kg 每日 1 次治疗,疗程为 16 周。患者在第 3、8 和 16 周进行复查,检查银屑病面积和严重程度指数(PASI)和可能出现的不良反应,并进行 MPA 的 C0(谷值)和 C1(给药后 1 小时)血浆水平检测。所有患者的 PASI 评分均有显著下降。该药物具有良好的耐受性。MPA 的 C0 和 C1 水平与 PASI 的降低、PASI 从基线的改善率、患者体重和 MMF 的总剂量之间均无显著相关性。然而,在研究结束时,两名 PASI 改善率最高的患者中检测到的 MPA C1 平均水平最高。尽管 C1 水平似乎与药物疗效没有强烈相关性,但 C1 水平在 PASI 改善率最高的两名患者中观察到的最高检测均值提示在某些情况下监测 C1 可能有用。

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Int J Mol Sci. 2015 Nov 6;16(11):26654-66. doi: 10.3390/ijms161125985.
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Clinical pharmacokinetics and pharmacodynamics of mycophenolate in patients with autoimmune disease.自身免疫性疾病患者麦考酚酸的临床药代动力学和药效学。
Clin Pharmacokinet. 2013 May;52(5):303-31. doi: 10.1007/s40262-013-0039-8.