Institute of Translational Biomedicine (ITBM), St. Petersburg State University, St. Petersburg 199034, Russia.
Institute of Experimental Medicine, Almazov National Medical Research Centre, Ministry of Healthcare of Russian Federation, St. Petersburg 197341, Russia.
ACS Chem Neurosci. 2024 Nov 6;15(21):3848-3862. doi: 10.1021/acschemneuro.4c00505. Epub 2024 Oct 15.
Antihistaminic drugs are widely used clinically and have long been primarily known for their use to treat severe allergic conditions caused by histamine release. Antihistaminic drugs also exert central nervous system (CNS) effects, acting as anxiolytics, hypnotics, and neuroleptics. However, these drugs also have multiple serious neuropharmacological side-effects, inducing delirium, hyperarousal, disorganized behavior, and hallucinations. Due to their robust CNS effects, antihistamines are also increasingly abused, with occasional overdoses and life-threatening toxicity. Here, we discuss chemical and neuropharmacological aspects of antihistaminic drugs in both human and animal (experimental) models and outline their current societal and mental health importance as neuroactive substances.
抗组胺药物在临床上被广泛应用,长期以来主要因其用于治疗由组胺释放引起的严重过敏病症而被人们所熟知。抗组胺药物还具有中枢神经系统 (CNS) 作用,具有抗焦虑、催眠和神经安定作用。然而,这些药物也具有多种严重的神经药理学副作用,引起意识混乱、过度警觉、行为紊乱和幻觉。由于其强大的中枢神经系统作用,抗组胺药物也越来越被滥用,偶尔会出现过量用药和危及生命的毒性。在这里,我们讨论了人类和动物(实验)模型中抗组胺药物的化学和神经药理学方面,并概述了它们作为神经活性物质的当前社会和精神健康重要性。