Pharmacy Practice, Loma Linda University School of Pharmacy, Shryock Hall, 24745 Stewart St, Loma Linda, CA 92350, United States of America; Department of Neurology, Loma Linda University School of Medicine, Faculty Medical Offices, 11370 Anderson, Suite B-100, Loma Linda, CA 92350, United States of America.
Pharmaceutical, Administrative and Basic Sciences, Loma Linda University Schools of Pharmacy and Medicine, 11175 Campus St, CSP21020, Loma Linda, CA 92350, United States of America.
Pharmacol Ther. 2020 Aug;212:107580. doi: 10.1016/j.pharmthera.2020.107580. Epub 2020 May 23.
Hyperkinetic movement disorders comprise a variety of conditions characterized by involuntary movements, which include but are not limited to tardive dyskinesia, chorea associated with Huntington's Disease, and tic disorders. The class of medications that have been used to treat these conditions includes Vesicular Monoamine Transporter-2 (VMAT2) inhibitors. In 2008, the FDA approved tetrabenazine as a treatment for chorea associated with Huntington's Disease. Optimization of the pharmacology of tetrabenazine has since led to the approval of two new VMAT2 inhibitors, deutetrabenazine and valbenazine. The objective of this review is to provide background on the role of VMAT in monoamine neurotransmission, the mechanism of VMAT2 inhibition on the treatment of hyperkinetic disorders (specifically tardive dyskinesia and chorea associated with Huntington's Disease), the pharmacology and pharmacokinetics of the commercially available VMAT2 inhibitors, and a summary of the clinical data to support application of these medications.
多动性运动障碍包括多种以不自主运动为特征的病症，其中包括但不限于迟发性运动障碍、亨廷顿舞蹈病相关的舞蹈症和抽动障碍。用于治疗这些病症的药物类别包括囊泡单胺转运蛋白 2（VMAT2）抑制剂。2008 年，FDA 批准了四苯嗪作为亨廷顿舞蹈病相关舞蹈症的治疗药物。对四苯嗪药理学的优化导致了两种新的 VMAT2 抑制剂——右苯丙胺和丙戊茶碱的批准。本综述的目的是提供囊泡单胺转运蛋白在单胺神经递质传递中的作用、VMAT2 抑制治疗多动性障碍（特别是迟发性运动障碍和亨廷顿舞蹈病相关的舞蹈症）的机制、市售 VMAT2 抑制剂的药理学和药代动力学以及支持这些药物应用的临床数据摘要。
