a Department of Neurology , St. Joseph Hospital Berlin-Weissensee , Berlin , Germany.
Expert Rev Neurother. 2017 Dec;17(12):1135-1144. doi: 10.1080/14737175.2017.1386556. Epub 2017 Oct 12.
Chronic intake of typical neuroleptics or centrally acting dopamine receptor blocking antiemetics may cause onset of tardive syndromes. Various types exist. One of them is tardive dyskinesia, characterised by often stigmatising, purposeless, rapid, repetitive, stereotypic, involuntary movements of face, limbs or trunk. Effective symptomatic drug treatment options beyond application of tetrabenazine are rare. Tetrabenazine is usually administered three times daily due to the short half life of this agent. Areas covered: This narrative review discusses the value of valbenazine for the treatment of tardive dyskinesia as a therapeutic alternative to tetrabenazine. Expert commentary: Valbenazine is a selective inhibitor of vesicular monoamine transporter 2, which is metabolized to (+)-alpha-dihydrotetrabenazine. Valbenazine and particularly its metabolite inhibit vesicular monoamine transporter 2 function. Once daily intake of valbenazine ameliorated the severity of tardive dyskinesia. The chiral purity of valbenazine circumvents generation of the (-)alpha and (+) and (-)beta dihydrotetrabenazine metabolites of tetrabenazine or deutetrabenazine. Valbenazine and its metabolite do not antagonize postsynaptic monoamine receptors in contrast to the tetrabenazine formulations. Therefore one may hypothesize that fewer and less severe motor and psychopathological side effects will occur during valbenazine long term application compared with tetrabenazine or deutretrabenazine.
慢性摄入典型的神经安定药或中枢作用的多巴胺受体阻断止吐药可能导致迟发性综合征的发作。存在各种类型。其中之一是迟发性运动障碍,其特征是经常带有污名、无目的、快速、重复、刻板、不自主的面部、四肢或躯干运动。除了应用四苯嗪之外,有效的对症药物治疗选择很少。由于该药物的半衰期短,四苯嗪通常每天给药三次。
本叙述性评论讨论了 valbenazine 作为 tetrabenazine 的治疗替代物治疗迟发性运动障碍的价值。
valbenazine 是囊泡单胺转运蛋白 2 的选择性抑制剂,可代谢为(+)-α-二氢四苯嗪。valbenazine 及其代谢物抑制囊泡单胺转运蛋白 2 的功能。每日一次服用 valbenazine 可改善迟发性运动障碍的严重程度。valbenazine 的手性纯度避免了四苯嗪或去四苯嗪生成(-)α和(+)和(-)β二氢四苯嗪代谢物。与四苯嗪制剂不同,valbenazine 及其代谢物不拮抗突触后单胺受体。因此,人们可以假设与四苯嗪或去四苯嗪相比,valbenazine 长期应用期间发生的运动和精神病理副作用更少且更轻。