Ronda-Roca Gerard, Caballero-Bermejo Antonio F, Cantillana-Barrenas José, Ruiz-Antorán Belén
Clinical Pharmacology Department, Hospital Universitario Puerta de Hierro Majadahonda, Majadahonda, Madrid, Spain.
Emergency Department, Hospital Universitario Puerta de Hierro Majadahonda, Majadahonda, Madrid, Spain.
Toxicol Rep. 2025 Jul 28;15:102098. doi: 10.1016/j.toxrep.2025.102098. eCollection 2025 Dec.
We report two cases of acute imepitoin overdose, a partial GABA-A receptor agonist. The first case involved a caucasian women of 22-year-old patient who ingested 20-24 g of imepitoin in a suicide attempt, presenting with central nervous system depression and mydriasis. The second case involved a caucasian male of 31-year-old patient who ingested 6-8 g of imepitoin along with other psychiatric medication, paracetamol, and ibuprofen. This patient presented with somnolence and bradylalia. Both patients received supportive care, including airway protection, intravenous fluids, activated charcoal, and cardiac monitoring. In the second case, flumazenil was administered and later discontinued. Both patients recovered fully within hours without complications. Imepitoin acts at the benzodiazepine binding site of the GABA-A receptor, approved for canine epilepsy and scarcely studied in humans, producing anxiolytic and anticonvulsant effects with reduced risk of sedation, dependence, or tolerance. It has a rapid absorption profile (T 0.5-2 h) and a variable half-life, shorter in smokers due to CYP1A2 induction.
我们报告了两例急性氨己烯酸过量中毒的病例,氨己烯酸是一种部分GABA - A受体激动剂。第一例涉及一名22岁的白人女性患者,她为自杀而摄入了20 - 24克氨己烯酸,出现中枢神经系统抑制和瞳孔散大。第二例涉及一名31岁的白人男性患者,他摄入了6 - 8克氨己烯酸以及其他精神科药物、对乙酰氨基酚和布洛芬。该患者表现为嗜睡和言语缓慢。两名患者均接受了支持性治疗,包括气道保护、静脉输液、活性炭和心脏监测。在第二例中,给予了氟马西尼,随后停药。两名患者均在数小时内完全康复,无并发症。氨己烯酸作用于GABA - A受体的苯二氮䓬结合位点,已被批准用于犬癫痫,在人类中的研究很少,具有抗焦虑和抗惊厥作用,同时降低了镇静、依赖或耐受性的风险。它具有快速吸收的特点(T 0.5 - 2小时),半衰期可变,由于CYP1A2诱导,吸烟者的半衰期较短。