Monti Jaime M, Spence David Warren, Buttoo Kenneth, Pandi-Perumal Seithikurippu R
Department of Pharmacology and Therapeutics, University of the Republic School of Medicine, Montevideo, Uruguay.
652 Dufferin Street, Toronto, ON M6K 2B4, Canada.
Asian J Psychiatr. 2017 Feb;25:79-90. doi: 10.1016/j.ajp.2016.10.006. Epub 2016 Oct 12.
Zolpidem is a short-acting non-benzodiazepine hypnotic drug that belongs to the imidazopyridine class. In addition to immediate-release (IR) and extended-release (ER) formulations, the new delivery forms including two sublingual tablets [standard dose (SD) and low dose (LD)], and an oral spray form have been recently developed which bypass the gastrointestinal tract. So far, Zolpidem has been studied in several clinical populations: cases poor sleepers, transient insomnia, elderly and non-elderly patients with chronic primary insomnia, and in comorbid insomnia. Peak plasma concentration (Tmax) of zolpidem-IR occurs in 45 to 60min, with the terminal elimination half-life (t½) equating to 2.4h. The extended-release formulation results in a higher concentration over a period of more than 6h. Peak plasma concentration is somewhat shorter for the sublingual forms and the oral spray, while their t½ is comparable to that of zolpidem-IR. Zolpidem-IR reduces sleep latency (SL) at recommended doses of 5mg and 10mg in elderly and non-elderly patients, respectively. Zolpidem-ER at doses of 6.25mg and 12.5mg, improves sleep maintenance in elderly and non-elderly patients, respectively, 4h after its administration. Sublingual zolpidem-LD (5mg) and zolpidem oral spray are indicated for middle-of-the-night (MOTN) wakefulness and difficulty returning to sleep, while sublingual zolpidem-SD (10mg) is marketed for difficulty falling asleep. With their array of therapeutic uses and their popularity among physicians and patients; this review describes the clinical pharmacology, indications and uses, identifying withdrawal symptoms, abuse and dependence potentials, and adverse drug reactions are discussed.
唑吡坦是一种短效非苯二氮䓬类催眠药物，属于咪唑吡啶类。除了速释（IR）和缓释（ER）制剂外，最近还开发了包括两种舌下片[标准剂量（SD）和低剂量（LD）]以及口服喷雾剂型的新给药形式，这些剂型可绕过胃肠道。到目前为止，唑吡坦已在多个临床人群中进行了研究：睡眠不佳者、短暂性失眠患者、患有慢性原发性失眠的老年和非老年患者以及共病性失眠患者。唑吡坦速释制剂的血浆峰浓度（Tmax）在45至60分钟出现，终末消除半衰期（t½）为2.4小时。缓释制剂在超过6小时的时间段内会产生更高的浓度。舌下剂型和口服喷雾的血浆峰浓度稍短，而它们的t½与唑吡坦速释制剂相当。唑吡坦速释制剂在老年和非老年患者中分别以5毫克和10毫克的推荐剂量可减少睡眠潜伏期（SL）。唑吡坦缓释制剂在6.25毫克和12.5毫克的剂量下，分别在给药4小时后可改善老年和非老年患者的睡眠维持情况。舌下唑吡坦低剂量（5毫克）和唑吡坦口服喷雾适用于半夜觉醒和难以重新入睡，而舌下唑吡坦标准剂量（10毫克）用于治疗入睡困难。鉴于其一系列治疗用途以及在医生和患者中的受欢迎程度；本综述描述了临床药理学、适应症和用途，识别戒断症状、滥用和依赖潜力，并讨论了药物不良反应。
