Nishino Seiji, Okuro Masashi
Sleep and Circadian Neurobiology Laboratory, Center for Narcolepsy, Stanford University School of Medicine, Palo Alto, CA 94304-5489, USA.
Drugs Today (Barc). 2008 Jun;44(6):395-414. doi: 10.1358/dot.2008.44.6.1195861.
Armodafinil is the (R)-enantiomer of the wakepromoting compound modafinil (racemic), with a considerably longer half-life of 10-15 hours. Armodafinil (developed by Cephalon, Frazer, PA, USA) was approved in June 2007 for the treatment of excessive sleepiness associated with narcolepsy, obstructive sleep apnea syndrome and shift work disorder, and the indications are the same as those for modafinil. Like modafinil, the mechanisms of action of armodafinil are not fully characterized and are under debate. Clinical trials in these sleep disorders demonstrated an enhanced efficacy for wake promotion (wake sustained for a longer time period using doses lower than those of modafinil). The safety profile is consistent with that of modafinil, and armodafinil is well tolerated by the patients. Like modafinil, armodafinil is classified as a non-narcotic Schedule IV compound. Many patients with excessive sleepiness may prefer the longer duration of effect and may have better compliance (with low doses) with armodafinil. The commercial challenge to armodafinil may come from generic modafinil, which may become available in 2012, as well as from classical amphetamine and amphetamine-like compounds (for the treatment of narcolepsy).
阿莫达非尼是促醒化合物莫达非尼（外消旋体）的（R）-对映体，半衰期长得多，为10 - 15小时。阿莫达非尼（由美国宾夕法尼亚州弗雷泽的 Cephalon 公司研发）于2007年6月获批用于治疗与发作性睡病、阻塞性睡眠呼吸暂停综合征和倒班工作障碍相关的过度嗜睡，其适应症与莫达非尼相同。与莫达非尼一样，阿莫达非尼的作用机制尚未完全明确，仍存在争议。针对这些睡眠障碍的临床试验表明，其促醒效果有所增强（使用低于莫达非尼的剂量就能使清醒状态持续更长时间）。其安全性与莫达非尼一致，患者对阿莫达非尼耐受性良好。与莫达非尼一样，阿莫达非尼被归类为非麻醉性的IV类化合物。许多过度嗜睡的患者可能更喜欢其更长的药效持续时间，并且（低剂量时）对阿莫达非尼的依从性可能更好。阿莫达非尼面临的商业挑战可能来自2012年可能上市销售的莫达非尼仿制药，以及传统的苯丙胺和苯丙胺类化合物（用于治疗发作性睡病）。
