Methods for treating hyperkinetic diseases and disorders, such as tardive dyskinesia, are provided. In a certain embodiment, the potent VMAT2 inhibitor (+)a-3-isobutyl-9,10-dimethoxy- 1,3,4,6,7,1 lb-hexahydro-2H-pyrido[2,l-a]isoquinolin-2-ol ((+)a-HTBZ) is used in the methods described herein for treating a subject in need thereof.