Alcantara-Montero A
Hospital Comarcal Don Benito-Villanueva, 06400 Don Benito, Espana.
Rev Neurol. 2017 Mar 1;64(5):219-226.
Desvenlafaxine is the third antidepressant within the group of serotonin-norepinephrine reuptake inhibitors. The latest clinical practice guidelines consulted agree that tricyclic antidepressants, dual (venlafaxine/duloxetine) and gabapentin/pregabalin antiepileptics, are the first-line drugs in the treatment of neuropathic pain, being tramadol, lidocaine 5% patches and capsaicin 8% patches of second-line drugs, while strong opioids constitute a third line treatment. The interaction between the binomial pain and depression is very frequent, being the psychological complication more frequent in patients with chronic pain.
Following a literature search, this article summarizes the most relevant pharmacological data of desvenlafaxine and its usefulness in clinical practice, as well as the specific literature of this drug in neuropathic pain and chronic pain.
Although evidence of desvenlafaxine in neuropathic pain is scarce, it presents some interesting pharmacokinetic properties, as it is not substrate or have activity on P-glycoprotein, and have a metabolism which practically does not depend on cytochrome P450 system, which limits the risk of pharmacokinetic interactions and potential problems associated tolerability when administered with drugs that are CYP2D6 moderate or potent inhibitors or other substrates of this isoenzyme. These characteristics make desvenlafaxine a different antidepressant especially useful in some subgroups of patients with chronic pain (as polypharmacy and patients with liver failure), where comorbid depression is frequent.
去甲文拉法辛是5-羟色胺-去甲肾上腺素再摄取抑制剂类中的第三种抗抑郁药。最新查阅的临床实践指南一致认为,三环类抗抑郁药、双重作用(文拉法辛/度洛西汀)和加巴喷丁/普瑞巴林类抗癫痫药是治疗神经性疼痛的一线药物,曲马多、5%利多卡因贴剂和8%辣椒素贴剂为二线药物,而强效阿片类药物则构成三线治疗。疼痛与抑郁之间的相互作用非常常见,是慢性疼痛患者中较为常见的心理并发症。
通过文献检索,本文总结了去甲文拉法辛最相关的药理学数据及其在临床实践中的效用,以及该药物在神经性疼痛和慢性疼痛方面的具体文献。
尽管去甲文拉法辛在神经性疼痛方面的证据较少,但它具有一些有趣的药代动力学特性,因为它不是P-糖蛋白的底物或对其无活性,并且其代谢几乎不依赖细胞色素P450系统,这限制了与CYP2D6中度或强效抑制剂或该同工酶的其他底物合用时药代动力学相互作用的风险以及与耐受性相关的潜在问题。这些特性使去甲文拉法辛成为一种不同的抗抑郁药,在一些慢性疼痛患者亚组(如联合用药患者和肝功能衰竭患者)中特别有用,这些患者中合并抑郁症很常见。