safetyriskБезопасность и риск фармакотерапииSafety and Risk of Pharmacotherapy2312-78212619-1164Federal State Budgetary Institution ‘Scientific Centre for Expert Evaluation of Medicinal Products’ of the Ministry of Health of the Russian Federation (FSBI ‘SCEEMP’)safetyrisk-315Research ArticleОБЗОРЫ И ОРИГИНАЛЬНЫЕ СТАТЬИREVIEWS AND ORIGINAL ARTICLESТрансформация взглядов на тератогенность противоэпилептической терапииTransformation of views on the teratogenic effects of antiepileptic drugsПастернакЕ. Ю.АляутдинР. Н.AlyautdinR. N.РомановБ. К.RomanovB. K.Федеральное государственное бюджетное учреждение «Научный центр экспертизы средств медицинского применения» Министерства здравоохранения Российской Федерации, МоскваРоссияScientific Centre for Expert Evaluation of Medicinal Products Russian FederationRussian Federation201402062022041217Copyright © Пастернак Е.Ю., Аляутдин Р.Н., Романов Б.К., 20222022Пастернак Е.Ю., Аляутдин Р.Н., Романов Б.К.Пастернак Е.Ю., Alyautdin R.N., Romanov B.K.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://www.risksafety.ru/jour/article/view/315

В статье представлена история развития взглядов на применение противоэпилептических средств при беременности и нежелательные реакции у плода, рассматриваются причины снижения рождаемости у женщин, страдающих эпилепсией. Статистика разделяет пациентов на 3 условные группы: здоровые пациентки, женщины с эпилепсией без терапии и беременные с эпилепсией, принимающие противоэпилептические препараты. Описаны случаи применения препаратов этой группы по другим показаниям. Эти данные помогают адекватно оценить тератогенность противоэпилептических препаратов в современном мире и объяснить причины врожденных синдромов, которые связывали с применением этих лекарственных средств во второй половине прошлого века. При соблюдении определенных условий наиболее безопасным препаратом является ламотриджин. Наряду с этим, со временем взгляды изменились и в отношении одного из первых противосудорожных препаратов фенитоина, разработаны рекомендации по его применению у беременных женщин

This review presents information on pharmaceuticals that have the properties of inverse agonists. The article describes the features of the interaction of the ligand - receptor with constitutive conformational changes. Many of ligands, assumed to be neutral antagonists, behave as inverse agonists displaying negative efficacy in experimental systems. This suggests that their therapeutic actions may involve not only receptor blockade, but also the decrease of spontaneous receptor activity. Examples of inverse agonists that influence the processes of excitation of adrenergic, histaminergic, opioid and benzodiazepine receptors are presented. The existence of constitutive activity in vivo and its pathophysiological relevance are also discussed

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The authors declare that there are no conflicts of interest present.