Valbenazine

Valbenazine is used to treat tardive dyskinesia.

Valbenazine is available under the following different brand names: Ingrezza.

Dosages of Valbenazine:

Dosage Forms and Strengths

Capsule

• 40mg
• 80mg

Dosage Considerations – Should be Given as Follows:

Tardive Dyskinesia

• 40 mg orally once daily for 1 week, then increase to the recommended dose of 80 mg orally once daily
• Continuation of 40 mg once daily may be considered for some patients
• Safety and efficacy not established in pediatric patients

Dosage Modifications

• Strong CYP3A4 inducers: Coadministration not recommended
• Strong CYP3A4 inhibitors: If co-administered, reduce valbenazine dose to 40 mg/day
• Strong CYP2D6 inhibitors or known CYP2D6 poor metabolizers: If co-administered, consider reducing the dose

Hepatic impairment

• Mild: No dose adjustment required
• Moderate-to-severe (Child-Pugh 7-15): Not to exceed 40 mg/day

Renal impairment

• Mild-to-moderate (CrCl 30-90 mL/minute): No dose adjustment required
• Severe (CrCl less than 30 mL/minute): Use not recommended

Common side effects of Valbenazine include:

• Drowsiness/sleepiness
• Anticholinergic effects (dry mouth/nose/throat, constipation, flushing, confusion, blurred vision)
• Balance disorders/fall
• Headache
• Restlessness
• Vomiting
• Nausea
• Joint pain

Postmarketing side effects of valbenazine reported include:

• Hypersensitivity
• QT prolongation
• Rash

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

• Severe interactions of valbenazine include:
  • deutetrabenazine
  • tetrabenazine
• Valbenazine has serious interactions with at least 35 different drugs.
• Valbenazine has severe or moderate interactions with at least 42 different drugs.
• Valbenazine has no listed mild interactions with other drugs.

Warnings

• This medication contains valbenazine. Do not take Ingrezza if you are allergic to valbenazine or any ingredients contained in this drug.
• Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Patients with a history of hypersensitivity to drugs or components of the formulation

Effects of Drug Abuse

• No information available

Short-Term Effects

• See "What Are Side Effects Associated with Using Valbenazine?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Valbenazine?"

Cautions

• Can cause somnolence; warn patients not to perform activities requiring mental alertness (e.g., driving or operating hazardous machinery) until they know how they will be affected

QT prolongation

• May prolong the QT interval, although the degree of QT prolongation is not clinically significant at concentrations expected with recommended dosing
• If co-administered with a strong CYP2D6 or CYP3A4 inhibitor, or patients who are CYP2D6 poor metabolizers, valbenazine concentrations may increase and cause clinically significant QT prolongation
• Avoid in patients with congenital long QT syndrome or with arrhythmias associated with a prolonged QT interval
• For patients at increased risk of a prolonged QT interval, assess the QT interval before increasing the dosage

Drug interaction overview

• MAOIs
  • Avoid coadministration
  • Concomitant use may increase the concentration of monoamine neurotransmitters in synapses, potentially leading to increased risk of adverse reactions (e.g., serotonin syndrome) or attenuated treatment effect of valbenazine

• Strong CYP3A4 inhibitors
  • Reduce valbenazine dose
  • Coadministration increases exposure (Cmax and AUC) to valbenazine and its active metabolite compared with the use of valbenazine alone

• Strong CYP2D6 inhibitors
  • Consider reducing valbenazine dose based on tolerability
  • Coadministration increases exposure (Cmax and AUC) to valbenazine's active metabolite compared with the use of valbenazine alone

• Strong CYP3A4 inducers
  • Concomitant use is not recommended
  • Coadministration decreases systemic exposure of valbenazine and its active metabolite, thereby decreasing the efficacy

• Digoxin
  • Coadministration increases digoxin levels owing to P-gp inhibition
  • Monitor digoxin levels if co-administered; dosage adjustment of digoxin may be necessary

Pregnancy and Lactation

• Data are limited on the use of valbenazine in pregnant women. Based on animal studies, valbenazine may cause fetal harm. Pregnant women should be advised of the potential risk.
• It is unknown if valbenazine is distributed in human breast milk. Based on animal findings of increased perinatal mortality in exposed fetuses and pups, women are advised not to breastfeed during treatment with valbenazine and for 5 days after the final dose.