在患有Mycobacterium ulcerans感染的患者中延长释放 klarithromycin的药理动力学
Sandor-Adrian Klis1, Ymkje Stienstra1,2, Kabiru M Abass3
1Department of Internal Medicine-Infectious Diseases, University Medical Center Groningen, University of Groningen, Groningen, The Netherlands.
延长释放克拉素 (CLA-ER) 和利芬素 (RIF) 已被用于研究Mycobacterium ulcerans感染. 评估了CLA-ER的药理动力学,显示没有明显的益处超过即时释放的CLA,也没有对RIF水平的影响.
科学领域:
- 药理学 药理学是指药理学的学科.
- 传染性疾病 传染性疾病
- 药物新陈代谢 药物新陈代谢
背景情况:
- 在世卫组织针对Mycobacterium ulcerans感染的试验中,克拉素延长释放剂 (CLA-ER) 与里法素 (RIF) 一起进行了研究.
- 众所周知,利芬素 (RIF) 影响CYP3A4代谢,可能会改变克拉里胺 (CLA) 的血清度.
- 需要对RIF和CLA之间的潜在相互作用进行调查,包括对它们各自的药理动力学特征的影响.
研究的目的:
- 在患有Mycobacterium ulcerans感染的患者中,评估CLA-ER与RIF同时使用时的药理学.
- 为了比较CLA-ER的药理学概况与标准的即时释放CLA.
- 评估CLA同时给药对RIF药理动学的影响.
主要方法:
- 包括一组来自世卫组织药物试验的参与者.
- 对CLA-ER (15 mg/kg) 和RIF (10 mg/kg) 的药理动力学数据是通过连续干燥的血液斑点样本在10小时内收集的.
- 在30名参与者中使用液体染色学-并联质谱法 (LC-MS/MS) 进行了分析.
主要成果:
- 中位数CLA Cmax为0.4 mg/L,AUC为3.9 mg*h/L,用于CLA-ER在15 mg/kg时.
- 与标准CLA (7.5 mg/kg) 相比,CLA-ER显示Cmax下降了58%,AUC增加了30%,不显著.
- 同时服用CLA并没有显著改变RIF Cmax或AUC. 所有参与者都获得了成功的治疗.
结论:
- 药理动力学研究没有揭示CLA-ER对立即释放的CLA在Mycobacterium ulcerans感染治疗中的明显益处.
- 同时服用CLA并没有影响RIF的药理动力学.
- 需要进一步的研究来澄清CLA-ER在这种情况下的临床优势.
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