Pharmacokinetics of milnacipran in comparison with other antidepressants
Pharmacokinetics of milnacipran in comparison with other antidepressants
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米那普仑与其他抗抑郁药的药代动力学比较
DOI：
10.1097/00004850-199609004-00003
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发表时间：
1996
影响因子：
2.6
通讯作者：
B. Leonard
中科院分区：
文献类型：
--
作者：
C. Puozzo;B. Leonard
尽管目前有大量的抗抑郁药可用，但仍有必要开发新的药物，将老年抗抑郁药的疗效与改进的安全性、耐受性和治疗效果结合起来，使其能够用于老年抑郁症患者或患有心脏、肾脏或肝脏疾病的患者。本文综述了三环类抗抑郁药、选择性5 -羟色胺再摄取抑制剂（SSRIs）和最近推出的抗抑郁药如文拉法辛和奈法唑酮的药代动力学特征。米尔纳西普兰（Ixel）是一种新型药物，结合了抗抑郁功效和一些独特的药代动力学特征。对其药代动力学特征的总结表明，milnacpran具有高生物利用度，低血浆蛋白结合，并且作为母体药物或葡萄糖醛酸盐在尿液中大部分被消除。这些特征表明，与大多数第二代抗抑郁药和三环抗抑郁药同时服用的其他药物发生相互作用的可能性较低。此外，对肝功能障碍患者和老年人的研究表明，对这些患者施用米那西普兰时，不需要调整剂量。milnacpran消除的减少与肾脏损害的程度相关，允许调整时间表。与早期的抗抑郁药相比，milnacpran结合了疗效和相对较低的副作用，并且与其他可能同时服用的药物的相互作用较少。
Despite the large number of antidepressants currently available, it is still necessary to develop new drugs that combine the efficacy of the older antidepressant with improved safety, tolerability and therapeutic profile that will allow them to be used in depressed patients who are elderly or with cardiac, renal or hepatic disease. This article reviews the pharmacokinetic characteristics of the tricyclic antidepressants, the selective serotonin reuptake inhibitors (SSRIs) and more recently introduced antidepressants such as venlafaxine and nefazodone. Milnacipran (Ixel), a novel drug, combines antidepressant efficacy with some unique pharmacokinetic features. A summary of its pharmacokinetic profile shows that milnacipran has a high bioavailability, low plasma protein binding and that it is largely eliminated in the urine as parent drug or as a glucuronide. These features suggest that the likelihood of interactions with other drugs given concurrently is lower than would occur with most second generation antidepressants and the tricyclic antidepressants. Furthermore, studies in patients with liver dysfunction, and in the elderly, suggest that dose adjustment is not necessary when milnacipran is administered to these patients. The decrease in milnacipran elimination is correlated to the degree of renal impairment, allowing adjustment of schedules. In comparison to earlier antidepressants, milnacipran combines efficacy and a relatively low side-effect profile with the added advantage of fewer interactions with drugs that may be given concurrently.