Valbenazine Tosylate is indicated for the treatment of adults with Tardive Dyskinesia.

Valbenazine and its active metabolite selectively inhibit vesicular monoamine transporter 2 (VMAT2) with high affinity and minimal activity on VMAT1. This reduces the uptake and storage of monoamine neurotransmitters such as dopamine, serotonin, and norepinephrine in synaptic vesicles, making them more susceptible to breakdown by cytosolic enzymes. As a result, presynaptic release of these neurotransmitters is decreased due to reduced vesicular availability. Neither valbenazine nor its metabolite shows significant off-target binding to dopamine, serotonin, or adrenergic receptors.

The initial dose is 40 mg once daily. After one week, increase the dose to the recommended dose of 80 mg once daily. Continuation of 40 mg once daily may be considered for some patients. Administer it orally with or without food.

Concomitant use of Valbenazine with MAO inhibitors (MAOIs) may increase monoamine neurotransmitter levels in synapses, which may increase the risk of adverse reactions such as serotonin syndrome or may reduce the therapeutic effect of Valbenazine. Therefore, concurrent use of Valbenazine with MAOIs should be avoided. Co-administration of Valbenazine with strong CYP3A4 inhibitors increases the exposure (Cmax and AUC) of Valbenazine and its active metabolite compared to Valbenazine alone. Dose reduction is recommended when used with strong CYP3A4 inhibitors. Dose adjustment based on tolerability may be considered when used with strong CYP2D6 inhibitors. Concomitant use with strong CYP3A4 inducers is not recommended. Digoxin levels should be monitored when used together, as increased exposure may raise the risk of digoxin-related adverse effects.

Somnolence, QT prolongation.

Limited data in pregnant women are insufficient to determine drug-associated risk. Breastfeeding is not recommended during treatment and for 5 days after the final dose of Valbenazine.

Valbenazine may cause somnolence and can impair the ability to drive or operate machinery. It may prolong the QT interval. Dose adjustment may be required in CYP2D6 poor metabolizers or when used with strong CYP2D6 inhibitors. Avoid use in patients with congenital long QT syndrome or arrhythmia associated with QT prolongation. No dose adjustment is needed in mild to moderate renal impairment, but it is not recommended in severe renal impairment.

No specific information on overdose symptoms is available from clinical trials. No known antidote exists. Treatment should include supportive care with close monitoring and consideration of multiple drug involvement.

Store below 25°C in a cool and dry place. Protect from light. Keep all medicines out of the reach of children.