deutetrabenazine

Contraindicated in:

Hepatic impairment;
Concurrent use of MAO inhibitors, tetrabenazine, or valbenazine;
Patients who are suicidal or have untreated or inadequately treated depression;
Congenital long QT syndrome or cardiac arrhythmias.

Use Cautiously in:

History of/propensity for depression, psychiatric illness, or suicidality;
Poor CYP2D6 metabolizers; initial dose ↓ required;
Concurrent use of strong CYP2D6 inhibitors (initial dose ↓ required);
Bradycardia, hypokalemia, hypomagnesemia, or concurrent use of QT-interval prolonging drugs;
History of breast cancer;
OB: Use during pregnancy only when potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only when potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: QTc interval prolongation

Endo: hyperprolactinemia

GI: constipation, diarrhea, dry mouth

GU: urinary tract infection

MS: bradykinesia

Neuro: akathisia, sedation/somnolence, agitation, anxiety, depression, dizziness, fatigue, gait disturbances, insomnia, NEUROLEPTIC MALIGNANT SYNDROME, parkinsonism, restlessness, SUICIDAL THOUGHTS/IDEATION, tremor

Interactions ⬆ ⬇

Drug-drug:

Concurrent use of MAO inhibitors↑ risk of serious adverse reactions and are contraindicated; wait ≥14 days after discontinuing to initiate deutetrabenazine.
Concurrent use of tetrabenazine or valbenazine is contraindicated.
Strong CYP2D6 inhibitors, including bupropion, fluoxetine, paroxetine, and quinidine, may ↑ levels; ↓ dose of deutetrabenazine.
QTc interval prolonging drugs may ↑ risk of QTc interval prolongation.
Concurrent use with dopamine antagonists or antipsychotics may ↑ risk of neuroleptic malignant syndrome and extrapyramidal disorders.
Concurrent use of alcohol or other CNS depressants may ↑ risk of CNS depression.

Availability ⬆ ⬇

Immediate-release tablets: 6 mg; 9 mg; 12 mg
Extended-release tablets: 6 mg; 12 mg; 18 mg; 24 mg; 30 mg; 36 mg; 42 mg; 48 mg

Route/Dosage ⬆ ⬇

When switching between immediate-release and extended-release formulations, use same total daily dose.

Huntington's Disease

PO (Adults ): Immediate-release tablets (Austedo): 6 mg twice daily; may ↑ dose by 6 mg/day at weekly intervals (max dose = 48 mg/day) based on tolerability to reduce chorea. Extended-release tablets (Austedo XR): 12 mg once daily; may ↑ dose by 6 mg/day at weekly intervals (max dose = 48 mg/day) based on tolerability to reduce chorea.Concurrent use of strong CYP2D6 inhibitors or poor CYP2D6 metabolizers: Do not exceed dose of 36 mg/day.

Tardive Dyskinesia

PO (Adults ): Immediate-release tablets (Austedo): 6 mg twice daily; may ↑ dose by 6 mg/day at weekly intervals (max dose = 48 mg/day) based on tolerability to reduce tardive dyskinesia. Extended-release tablets (Austedo XR): 12 mg once daily; may ↑ dose by 6 mg/day at weekly intervals (max dose = 48 mg/day) based on tolerability to reduce tardive dyskinesia.Concurrent use of strong CYP2D6 inhibitors or poor CYP2D6 metabolizers: Do not exceed dose of 36 mg/day.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Its major metabolites act as reversible inhibitors of the vesicle monoamine transporter type 2 (VMAT-2), resulting in decreased reuptake of monoamines (including serotonin, norepinephrine, and dopamine) into vesicles in presynaptic neurons and depletion of monoamine stores.

Therapeutic effects:

Decreased chorea due to Huntington's Disease.
Reduced severity of tardive dyskinesia.

Classifications ⬆ ⬇

Therapeutic Classification: antichoreas

Pharmacologic Classification: reversible monoamine depleters

Pharmacokinetics ⬆ ⬇

Absorption: ≥80% absorbed following oral administration.

Distribution: Extensively distributed to tissues.

Metabolism/Excretion: Metabolized in liver to two active metabolites (α-dihydrotetrabenazine (α-HTBZ) and β-HTBZ), which are subsequently metabolized primarily via CYP2D6 (and to lesser extent by CYP1A2 and CYP3A4/5) to several minor metabolites (the CYP2D6 enzyme system exhibits genetic polymorphism; 7% of population may be poor metabolizers and may have significantly ↑ concentrations and an ↑ risk of adverse effects). Primarily excreted in the urine as metabolites.

Half-Life: 9–10 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	3–4 hr	12 hr
PO-XR	unknown	3 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take deutetrabenazine as directed. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
Advise patient and family to monitor for changes, especially sudden changes in mood, behaviors, thoughts, or feelings. If new or worse feelings of sadness; crying spells; lack of interest in friends or activities; sleeping a lot more or less; feelings of unimportance, guilt, hopelessness, or helplessness; irritability or aggression; more or less hunger; difficulty paying attention; or thoughts of self-harm or suicide occur, notify health care professional promptly.
Advise patient to notify health care professional if signs and symptoms of neuroleptic malignant syndrome, akathisia, or irregular heartbeat occurs.
Advise patient to avoid driving and other activities requiring alertness until response to medication is known.
Inform patient of potential side effects and instruct patient to notify health care professional if side effects occur.
Advise patient to avoid alcohol or sedating drugs; may increase drowsiness.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

Pronunciation ⬆ ⬇

du-tet-ra-BEN-a-zeen

Code ⬆

NDC Code

68546- Teva Neuroscience, Inc.
- 68546-170- Austedo
  - 68546-170-60- 60 TABLET, COATED in 1 BOTTLE (68546-170-60)

68546- Teva Neuroscience, Inc.
- 68546-170- Austedo
  - 68546-170-66- 60 TABLET, COATED in 1 BOTTLE (68546-170-66)

68546- Teva Neuroscience, Inc.
- 68546-171- Austedo
  - 68546-171-60- 60 TABLET, COATED in 1 BOTTLE (68546-171-60)

68546- Teva Neuroscience, Inc.
- 68546-171- Austedo
  - 68546-171-66- 60 TABLET, COATED in 1 BOTTLE (68546-171-66)

68546- Teva Neuroscience, Inc.
- 68546-172- Austedo
  - 68546-172-60- 60 TABLET, COATED in 1 BOTTLE (68546-172-60)

68546- Teva Neuroscience, Inc.
- 68546-172- Austedo
  - 68546-172-66- 60 TABLET, COATED in 1 BOTTLE (68546-172-66)

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇