valbenazine INGREZZA

Class: VMAT2 Antagonist
FDA Indications: Tardive Dyskinesia
Off-Label Use: Tourette's Disorder
Prescribing
Forms: 40, 80mg capsule
Dose Range: 40-80 mg/day
Starting: 40 mg qd x1 week then ↑ dose to 80 mg qd

NAMI drug fact sheet

Precautions
Contraindications: Avoid use in patients with congenital long QT syndrome or with arrhythmias associated with a prolonged QT interval
Serious Side Effects: QT ↑
Side Effects: headache, sedation/somnolence, akathisia
Pharmacodynamics
1° MOA: Reversibly ↓'s DA release by selectively inhibiting pre-synaptic VMAT2, thereby reducing the postsynaptic stimulation of D2 receptors and the severity of dyskinetic movements
Target: VMAT2
Pharmacokinetics
t½: 20 (15-22)° TMAX: 0.5-1°
Substrate of: 3A4, 2D6
Inhibits: ∅ ; Induces:
Active Metabolites: DTBZ
DDIs
Misc
  • - the only agent that has demonstrated significant efficacy and tolerability for TD management
  • - valbenazine is a prodrug that is hydrolyzed to the active metabolite DTBZ
  • - during initial studies valbenazine appeared to have no effect on depression, suicidality, and there were no clinically significant changes in measures of schizophrenia symptoms
Special Populations

Category Undefined.—The limited available data on use in pregnancy are insufficient to inform a drug-associated risk

There is no information regarding the presence of valbenazine or its metabolites in human milk, the effects on the breastfed infant, or the effects on milk production

No dosage adjustment is necessary for patients with mild to moderate renal impairment. Use is not recommended in patients with severe renal impairment

Recommended dose for patients with moderate or severe hepatic impairment is 40 mg daily

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Last updated August 27 2018 18:45:06. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.