Valbenazine (US Brand name Ingrezza®) is a vesicular monoamine transporter 2 (VMAT2) inhibitor. Here is basic information about this medication. Other articles on this website with more advanced information and tips related to this medication are linked to under Related Pages below.
Treatment of adults with tardive dyskinesia
The initial dose is 40 mg once a day.
After one week, the dose should usually be increased to 80 mg once daily.
But, there are some exceptions.
If the person cannot tolerate 80 mg/day, the dose can be reduced to either 60 mg/day or 40 mg/day. Note: Valbenazine is available not only in 40 mg and 80 mg capsules but now also in 60 mg strength.
Also, the maximum recommended dose is 40 mg once daily in the following persons:
1. Those who are CYP2D6 poor metabolizers.
2. Those who are also taking a medication that is a strong CYP2D6 inhibitor. This is not a farfetched scenario; the use of such medications is not rare. Examples of medications that are strong 2D6 inhibitors include (alphabetically):
– Cinacalcet (used to reduce serum calcium, for example, in patients with chronic renal disease who are on dialysis)
3. Those who are also taking a medication that is a strong CYP3A4 inhibitor. Examples of medications that are strong 3A4 inhibitors are (alphabetically) clarithromycin, itraconazole, ketoconazole.
4. Those with moderate or severe impairment of liver function.
Administration and instructions
Valbenazine can be taken with or without food.
Dosage forms and strengths
Capsules: 40 mg, 60 mg, 80 mg
Valbenazine carries a warning about somnolence and about the risk of QT prolongation.
Potential side effects
Please see THIS PAGE for a handout listing both the common and less common side effects of this medication along with the percentages of patients who report them.
Valbenazine is metabolized by two pathways:
1. By hydrolysis to its active metabolite [+]-α-HTBZ. This active metabolite is then metabolized by CYP450 2D6
2. By oxidative metabolism (mainly by CYP450 3A4/5).
This is why dose reduction is recommended in both:
– Those who are CYP450 2D6 poor metabolizers or taking a strong 2D6 inhibitor
– Those taking a strong 3A4 inhibitor.
Important! Please refer to the full Prescribing Information (see link below) before prescribing this medication.
Caroff SN, Aggarwal S, Yonan C. Treatment of tardive dyskinesia with tetrabenazine or valbenazine: a systematic review. J Comp Eff Res. 2018 Feb;7(2):135-148. doi: 10.2217/cer-2017-0065. Epub 2017 Oct 2. PMID: 28965423.
Short-term clinical trials
Longer-term clinical trials
Factor SA, Remington G, Comella CL, Correll CU, Burke J, Jimenez R, Liang GS, O’Brien CF. The Effects of Valbenazine in Participants with Tardive Dyskinesia: Results of the 1-Year KINECT 3 Extension Study. J Clin Psychiatry. 2017 Nov/Dec;78(9):1344-1350. doi: 10.4088/JCP.17m11777. PMID: 29141124.
Lindenmayer JP, Verghese C, Marder SR, Burke J, Jimenez R, Siegert S, Liang GS, O’Brien CF. A long-term, open-label study of valbenazine for tardive dyskinesia. CNS Spectr. 2021 Aug;26(4):345-353. doi: 10.1017/S109285292000108X. Epub 2020 May 18. PMID: 32419679.
Marder SR, Singer C, Lindenmayer JP, Tanner CM, Comella CL, Verghese C, Jimenez R, Liang GS, Burke J, OʼBrien CF. A Phase 3, 1-Year, Open-Label Trial of Valbenazine in Adults With Tardive Dyskinesia. J Clin Psychopharmacol. 2019 Nov/Dec;39(6):620-627. doi: 10.1097/JCP.0000000000001111. PMID: 31688452.
Marder SR, Lindenmayer JP, Shah C, Carmack T, Angelov AS, Lundt L. Onset and Resolution of Key Adverse Events in Valbenazine-Treated Patients with Tardive Dyskinesia: Pooled Analyses from Two Long-Term Clinical Trials. CNS Spectr. 2021 Apr;26(2):151. doi: 10.1017/S1092852920002394. PMID: 34127126.
Thai-Cuarto D, O’Brien CF, Jimenez R, Liang GS, Burke J. Cardiovascular Profile of Valbenazine: Analysis of Pooled Data from Three Randomized, Double-Blind, Placebo-Controlled Trials. Drug Saf. 2018 Apr;41(4):429-440. doi: 10.1007/s40264-017-0623-1. PMID: 29218680; PMCID: PMC5878201.
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