Boddu Sai H S, Kumari Sneha
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Ajman University, Ajman P.O. Box 346, UAE.
Center of Medical and Bio-allied Health Sciences Research, Ajman University, Ajman P.O. Box 346, UAE.
Pharmaceutics. 2020 Nov 30;12(12):1167. doi: 10.3390/pharmaceutics12121167.
Benzodiazepines such as diazepam, lorazepam and midazolam remained the mainstay of treatment for acute repetitive seizures (ARS). The immediate care for ARS should often begin at home by a caregiver. This prevents the progression of ARS to prolonged seizures or status epilepticus. For a long time and despite social objections rectal diazepam gel remained only FDA-approved rescue medication. Intranasal administration of benzodiazepines is considered attractive and safe compared with rectal, buccal and sublingual routes. Intranasal delivery offers numerous advantages such as large absorptive surface area, bypass the first-pass metabolism and good patient acceptance as it is needle free and painless. Recent clinical studies have demonstrated that diazepam nasal spray (NRL-1; Valtoco, Neurelis Inc.,San Diego, CA, USA) showed less pharmacokinetic variability and reliable bioavailability compared with the diazepam rectal gel. Diazepam nasal spray could be considered as a suitable alternative for treating seizure emergencies outside the hospital. This review summarizes the treatment options for ARS and findings from clinical studies involving intranasal diazepam for treating seizure emergencies.
地西泮、劳拉西泮和咪达唑仑等苯二氮䓬类药物仍然是急性重复性癫痫发作(ARS)治疗的主要药物。ARS的即时护理通常应由护理人员在家中开始。这可防止ARS进展为长时间癫痫发作或癫痫持续状态。长期以来,尽管存在社会反对意见,但直肠用地西泮凝胶仍然是唯一获得美国食品药品监督管理局(FDA)批准的急救药物。与直肠、颊部和舌下给药途径相比,苯二氮䓬类药物的鼻内给药被认为具有吸引力且安全。鼻内给药具有诸多优点,如吸收表面积大、绕过首过代谢以及患者接受度高,因为它无需针头且无痛。最近的临床研究表明,与地西泮直肠凝胶相比,地西泮鼻喷雾剂(NRL-1;Valtoco,Neurelis公司,美国加利福尼亚州圣地亚哥)显示出较小的药代动力学变异性和可靠的生物利用度。地西泮鼻喷雾剂可被视为治疗院外癫痫紧急情况的合适替代药物。本综述总结了ARS的治疗选择以及涉及鼻内地西泮治疗癫痫紧急情况的临床研究结果。