tetrabenazine (Rx)

Brand and Other Names:Xenazine
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 12.5mg
  • 25mg

Huntington Disease

Indicated for treatment of chorea associated with Huntington’s disease

Individualize and slowly titrate dosage over several weeks to identify a dose that reduces chorea and is well tolerated

Total daily dose up to 50 mg/day

  • 12.5 mg PO qDay initially; after 1 week, the dose should be increased to 12.5 mg q12hr
  • Maintenance: Titrate slowly by weekly intervals of 12.5 mg/day to identify dose that reduces chorea and is tolerated
  • If daily dose is 37.5 to 50 mg/day, administer in divided doses q8hr
  • Not to exceed 25 mg per single dose for total daily dosage between 37.5-50 mg/day

Total Daily dose >50 mg/day

  • If >50 mg/day is required, test and genotype to determine if poor or extensive metabolizers of CYP2D6; not to exceed 100 mg/day or 37.5 mg/dose
  • Dose maintenance requirements are dependent on CYP2D6 genotype (see Dosage Modifications)

Dosage Modifications

CYP2D6 extensive/intermediate metabolizers

  • Extensive metabolizers may require dose >50 mg/day
  • If total daily dose >50 mg/day, administer in divided doses q8hr
  • Titrate slowly by 12.5 mg/day qWeek to identify dose that reduces chorea and is tolerated
  • If >50 mg/day is required, do not to exceed 37.5 mg per single dose or a total daily dose of 100 mg/day

CYP2D6 poor metabolizers

  • Not to exceed 25 mg per single dose or a total daily dose of 50 mg/day

Hepatic impairment

  • Contraindicated; it is not possible to adjust the dose to ensure safe use

Dosing Considerations

May take with or without food

Dosage interruption >5 days: Retitrate dose when treatment resumed

Dosage interruption <5 days: May resume at previous maintenance dose without titration

Suspend upward dosage titration and reduce dose; discontinue if adverse reaction (intolerable effects such as: akathisia, restlessness, parkinsonism, insomnia, depression, suicidality, anxiety, sedation) does not resolve (may stop without taper)

Treatment discontinuation

  • May discontinue without tapering
  • Chorea may re-emerge within 12-18 hr after last dose

Tardive Dyskinesia (Off-label)

Investigational (see www.clinicaltrials.gov)

Safety and efficacy not established

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Interactions

Interaction Checker

and tetrabenazine

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      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (12)

            • deutetrabenazine

              tetrabenazine, deutetrabenazine. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Do not use these drugs concomitantly. Deutetrabenazine may be initiated the day after discontinuing tetrabenazine.

            • goserelin

              goserelin increases toxicity of tetrabenazine by QTc interval. Contraindicated. Increases risk of torsades de pointes.

            • isocarboxazid

              tetrabenazine, isocarboxazid. Other (see comment). Contraindicated. Comment: Risk of acute hypertensive episode; separate by 14 d. Mechanism: MAOI causes accumulation of NE in neuron and tetrabenazine stimulates NE release.

            • leuprolide

              leuprolide increases toxicity of tetrabenazine by QTc interval. Contraindicated. Increases risk of torsades de pointes.

            • linezolid

              tetrabenazine, linezolid. Other (see comment). Contraindicated. Comment: Risk of acute hypertensive episode; separate by 14 d. Mechanism: MAOI causes accumulation of NE in neuron and tetrabenazine stimulates NE release.

            • phenelzine

              tetrabenazine, phenelzine. Other (see comment). Contraindicated. Comment: Risk of acute hypertensive episode; separate by 14 d. Mechanism: MAOI causes accumulation of NE in neuron and tetrabenazine stimulates NE release.

            • procarbazine

              tetrabenazine, procarbazine. Other (see comment). Contraindicated. Comment: Risk of acute hypertensive episode; separate by 14 d. Mechanism: MAOI causes accumulation of NE in neuron and tetrabenazine stimulates NE release.

            • rasagiline

              tetrabenazine, rasagiline. Other (see comment). Contraindicated. Comment: Risk of acute hypertensive episode; separate by 14 d. .

            • selegiline

              tetrabenazine, selegiline. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Risk of acute hypertensive episode; separate by 14 days. Mechanism: MAOI causes accumulation of norepinephrine in neuron and tetrabenazine stimulates norepinephrine release.

            • selegiline transdermal

              tetrabenazine increases effects of selegiline transdermal by pharmacodynamic synergism. Contraindicated. Risk of acute hypertensive episode; separate by 14 days. Mechanism: MAOI causes accumulation of NE in neuron and tetrabenazine stimulates NE release.

            • tranylcypromine

              tetrabenazine, tranylcypromine. Other (see comment). Contraindicated. Comment: Risk of acute hypertensive episode; separate by 14 d. Mechanism: MAOI causes accumulation of NE in neuron and tetrabenazine stimulates NE release.

            • valbenazine

              tetrabenazine, valbenazine. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Do not use these drugs concomitantly.

            Serious - Use Alternative (39)

            • alfuzosin

              alfuzosin and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • apomorphine

              apomorphine and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • aripiprazole

              aripiprazole and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • artemether

              artemether and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • atomoxetine

              atomoxetine and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • bedaquiline

              bedaquiline and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • ceritinib

              ceritinib and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • citalopram

              citalopram and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • clarithromycin

              clarithromycin and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • clozapine

              clozapine and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • crizotinib

              crizotinib and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • dasatinib

              dasatinib and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • degarelix

              degarelix and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • desflurane

              desflurane and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • dofetilide

              dofetilide increases toxicity of tetrabenazine by QTc interval. Avoid or Use Alternate Drug.

            • dolasetron

              dolasetron and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • donepezil

              donepezil and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • efavirenz

              efavirenz and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • encorafenib

              encorafenib and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug. Encorafenib is associated with dose-dependent QTc interval prolongation. Avoid with drugs known to prolong QT interval.

            • entrectinib

              tetrabenazine and entrectinib both increase QTc interval. Avoid or Use Alternate Drug.

            • eribulin

              eribulin and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug. Potential for enhanced QTc-prolonging effects; if concurrent use is necessary then ECG monitoring is recommended.

            • escitalopram

              escitalopram increases toxicity of tetrabenazine by QTc interval. Avoid or Use Alternate Drug.

            • fexinidazole

              fexinidazole and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug. Avoid coadministration of fexinidazole with drugs known to block potassium channels and/or prolong QT interval.

            • fingolimod

              fingolimod and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • glasdegib

              tetrabenazine and glasdegib both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, monitor for increased risk of QTc interval prolongation.

            • histrelin

              histrelin increases toxicity of tetrabenazine by QTc interval. Avoid or Use Alternate Drug. Increases risk of torsades de pointes.

            • hydroxychloroquine sulfate

              hydroxychloroquine sulfate and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • inotuzumab

              inotuzumab and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug. If unable to avoid concomitant use, obtain ECGs and electrolytes before and after initiation of any drug known to prolong QTc, and periodically monitor as clinically indicated during treatment.

            • iobenguane I 131

              tetrabenazine will decrease the level or effect of iobenguane I 131 by Other (see comment). Avoid or Use Alternate Drug. Based on the mechanism of action of iobenguane, drugs that reduce catecholamine uptake or that deplete catecholamine stores may interfere with iobenguane uptake into cells, and thus, reduce iobenguane efficacy. Discontinue interfering drugs for at least 5 half-lives before administration of either the dosimetry or an iobenguane dose. Do not administer these drugs until at least 7 days after each iobenguane dose.

            • lefamulin

              lefamulin and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • mefloquine

              mefloquine increases toxicity of tetrabenazine by QTc interval. Avoid or Use Alternate Drug. Mefloquine may enhance the QTc prolonging effect of high risk QTc prolonging agents.

            • metoclopramide intranasal

              tetrabenazine, metoclopramide intranasal. Either increases effects of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Avoid use of metoclopramide intranasal or interacting drug, depending on importance of drug to patient.

            • mobocertinib

              mobocertinib and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug. If coadministration unavoidable, reduce mobocertinib dose and monitor QTc interval more frequently.

            • panobinostat

              tetrabenazine and panobinostat both increase QTc interval. Avoid or Use Alternate Drug. Panobinostat is known to significantly prolong QT interval. Panobinostat prescribing information states use with drugs known to prolong QTc is not recommended.

            • pimavanserin

              pimavanserin and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug. Coadministration may increase the risk of QT prolongation and cardiac arrhythmia.

            • pitolisant

              tetrabenazine and pitolisant both increase QTc interval. Avoid or Use Alternate Drug.

            • ribociclib

              ribociclib and tetrabenazine both increase QTc interval. Avoid or Use Alternate Drug.

            • safinamide

              tetrabenazine decreases effects of safinamide by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Dopamine antagonists may decrease safinamide effects and exacerbate Parkinson disease symptoms.

            • triptorelin

              triptorelin increases toxicity of tetrabenazine by QTc interval. Avoid or Use Alternate Drug. Increases risk of torsades de pointes.

            Monitor Closely (53)

            • abiraterone

              abiraterone increases levels of tetrabenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Avoid coadministration of abiraterone with substrates of CYP2D6. If alternative therapy cannot be used, exercise caution and consider a dose reduction of the CYP2D6 substrate.

            • albuterol

              albuterol and tetrabenazine both increase QTc interval. Use Caution/Monitor.

            • alfuzosin

              tetrabenazine and alfuzosin both increase QTc interval. Use Caution/Monitor.

            • amoxapine

              amoxapine and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • arformoterol

              arformoterol and tetrabenazine both increase QTc interval. Use Caution/Monitor.

            • aripiprazole

              aripiprazole and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • brexanolone

              brexanolone, tetrabenazine. Either increases toxicity of the other by sedation. Use Caution/Monitor.

            • cenobamate

              cenobamate, tetrabenazine. Either increases effects of the other by sedation. Use Caution/Monitor.

            • chlorpromazine

              chlorpromazine and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • ciprofloxacin

              ciprofloxacin and tetrabenazine both increase QTc interval. Use Caution/Monitor. Ciprofloxacin elicits minimal effects on QT interval. Caution if used in combination with other drugs known to affect QT interval or in patients with other risk factors.

            • clobazam

              tetrabenazine, clobazam. Other (see comment). Use Caution/Monitor. Comment: Concomitant administration can increase the potential for CNS effects (e.g., increased sedation or respiratory depression).

            • clozapine

              clozapine and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • droperidol

              droperidol and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • esketamine intranasal

              esketamine intranasal, tetrabenazine. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely.

            • fluoxetine

              fluoxetine increases effects of tetrabenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Decrease tetrabenazine dose by 50% when coadministered with strong CYP2D6 inhibitors.

            • fluphenazine

              fluphenazine and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • fostemsavir

              tetrabenazine and fostemsavir both increase QTc interval. Use Caution/Monitor. QTc prolongation reported with higher than recommended doses of fostemsavir.

            • haloperidol

              haloperidol and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • iloperidone

              iloperidone and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • lasmiditan

              lasmiditan, tetrabenazine. Either increases effects of the other by sedation. Use Caution/Monitor. Coadministration of lasmiditan and other CNS depressant drugs, including alcohol have not been evaluated in clinical studies. Lasmiditan may cause sedation, as well as other cognitive and/or neuropsychiatric adverse reactions.

            • lemborexant

              lemborexant will increase the level or effect of tetrabenazine by sedation. Modify Therapy/Monitor Closely. Dosage adjustment may be necessary if lemborexant is coadministered with other CNS depressants because of potentially additive effects.

            • lenvatinib

              tetrabenazine and lenvatinib both increase QTc interval. Use Caution/Monitor. Lenvatinib prescribing information recommends monitoring ECG closely when coadministered with QT prolonging drugs.

            • lofexidine

              tetrabenazine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.

            • loxapine

              loxapine and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • loxapine inhaled

              loxapine inhaled and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • lurasidone

              lurasidone, tetrabenazine. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Potential for increased CNS depressant effects when used concurrently; monitor for increased adverse effects and toxicity.

            • metoclopramide

              metoclopramide and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • midazolam intranasal

              midazolam intranasal, tetrabenazine. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Concomitant use of barbiturates, alcohol, or other CNS depressants may increase the risk of hypoventilation, airway obstruction, desaturation, or apnea and may contribute to profound and/or prolonged drug effect.

            • olanzapine

              olanzapine and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • osilodrostat

              osilodrostat and tetrabenazine both increase QTc interval. Use Caution/Monitor.

            • oxaliplatin

              oxaliplatin will increase the level or effect of tetrabenazine by Other (see comment). Use Caution/Monitor. Monitor for ECG changes if therapy is initiated in patients with drugs known to prolong QT interval.

            • ozanimod

              ozanimod and tetrabenazine both increase QTc interval. Modify Therapy/Monitor Closely. The potential additive effects on heart rate, treatment with ozanimod should generally not be initiated in patients who are concurrently treated with QT prolonging drugs with known arrhythmogenic properties.

            • paliperidone

              paliperidone and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • paroxetine

              paroxetine increases effects of tetrabenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Decrease tetrabenazine dose by 50% when coadministered with strong CYP2D6 inhibitors.

            • perphenazine

              perphenazine and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • pimozide

              pimozide and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • prochlorperazine

              prochlorperazine and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • promethazine

              promethazine and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • quetiapine

              quetiapine and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • quinidine

              quinidine increases effects of tetrabenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Decrease tetrabenazine dose by 50% when coadministered with strong CYP2D6 inhibitors.

            • remimazolam

              remimazolam, tetrabenazine. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely. Coadministration may result in profound sedation, respiratory depression, coma, and/or death. Continuously monitor vital signs during sedation and recovery period if coadministered. Carefully titrate remimazolam dose if administered with opioid analgesics and/or sedative/hypnotics.

            • risperidone

              risperidone and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • ritonavir

              ritonavir increases effects of tetrabenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Decrease tetrabenazine dose by 50% when coadministered with strong CYP2D6 inhibitors.

            • selpercatinib

              selpercatinib increases toxicity of tetrabenazine by QTc interval. Use Caution/Monitor.

            • sodium sulfate/?magnesium sulfate/potassium chloride

              sodium sulfate/?magnesium sulfate/potassium chloride increases toxicity of tetrabenazine by QTc interval. Use Caution/Monitor. Consider predose and post-colonoscopy ECGs in patients at increased risk of serious cardiac arrhythmias. .

            • sodium sulfate/potassium sulfate/magnesium sulfate

              sodium sulfate/potassium sulfate/magnesium sulfate increases toxicity of tetrabenazine by QTc interval. Use Caution/Monitor. Consider predose and post-colonoscopy ECGs in patients at increased risk of serious cardiac arrhythmias. .

            • stiripentol

              stiripentol, tetrabenazine. Either increases effects of the other by sedation. Use Caution/Monitor. Concomitant use stiripentol with other CNS depressants, including alcohol, may increase the risk of sedation and somnolence.

            • thioridazine

              thioridazine and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • thiothixene

              thiothixene and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • triclabendazole

              triclabendazole and tetrabenazine both increase QTc interval. Use Caution/Monitor.

            • trifluoperazine

              trifluoperazine and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            • voclosporin

              voclosporin, tetrabenazine. Either increases effects of the other by QTc interval. Use Caution/Monitor.

            • ziprasidone

              ziprasidone and tetrabenazine both increase antidopaminergic effects, including extrapyramidal symptoms and neuroleptic malignant syndrome. Modify Therapy/Monitor Closely.

            Minor (2)

            • azithromycin

              azithromycin increases toxicity of tetrabenazine by QTc interval. Minor/Significance Unknown.

            • chloroquine

              chloroquine increases toxicity of tetrabenazine by QTc interval. Minor/Significance Unknown.

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            Adverse Effects

            >10%

            Sedation/somnolence (31%)

            Fatigue (22%)

            Insomnia (22%)

            Depression (19%)

            Akathisia (19%)

            Extrapyramidal event (15%)

            Anxiety (15%)

            Nausea (13%)

            1-10%

            Irritability (9%)

            Bruising (6%)

            Vomiting (6%)

            Decreased appetite (4%)

            Dysuria (4%)

            Obsessive reaction (4%)

            Imbalance (9%)

            Parkinsonism/bradykinesia (9%)

            Dizziness (4%)

            Dysarthria (4%)

            Unsteady gait (4%)

            Headache (4%)

            Frequency Not Defined

            QTc prolongation

            Neuroleptic malignant syndrome

            Orthostatic Hypotension

            Restlessness and agitation

            Dysphagia

            Depression and suicidality

            Postmarketing Reports

            Nervous system disorders: Tremor

            Psychiatric disorders: Confusion, worsening aggression, depression/suicidality

            Respiratory, thoracic and mediastinal disorders: Pneumonia

            Skin and subcutaneous tissue disorders: Hyperhidrosis, skin rash

            Endocrine system: Hyperprolactinemia

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            Warnings

            Black Box Warnings

            Increased risk of depression and suicidal thoughts and behavior (suicidality) in patients with Huntington’s disease

            Balance risks of depression and suicidality with the clinical need for control of choreiform movements when considering the use of tetrabenazine

            Monitor for emergence or worsening of depression, suicidality, or unusual changes in behavior

            Inform patients, caregivers and families of the risk of depression and suicidality and instruct to report behaviors of concern promptly to the treating physician

            Caution in patients with a history of depression or prior suicide attempts or ideation

            Contraindicated in patients who are actively suicidal, and in patients with untreated or inadequately treated depression

            Contraindications

            Hypersensitivity

            Hepatic impairment

            Patients who are actively suicidal, or who have untreated or inadequately treated depression (see Black Box Warnings)

            Coadministration with deutetrabenazine or valbenazine

            Concomitant MAO inhibitor or within 14 days of discontinuing MAO inhibitor

            Reserpine

            • Do not use tetrabenazine and reserpine concomitantly
            • Reserpine binds irreversibly to VMAT2 and the duration of its effect is several days
            • Caution when switching from reserpine to tetrabenazine; wait for chorea to re-emerge before administering tetrabenazine to avoid overdosage and major CNS depletion of serotonin and norepinephrine
            • At least 20 days should elapse after stopping reserpine before starting tetrabenazine

            Cautions

            Not indicated for treatment of levodopa-induced dyskinetic movements

            Should only be used by physicians experienced with treatment of hyperkinetic disorders

            May cause depression; consider risk of suicidality; should be balanced against need for treatment of chorea; discontinue at first sign

            May induce symptoms of Parkinsonism, including symptoms of tardive dyskinesia; akathisia, restlessness, and agitation may occur; reduce dose or discontinue

            Dysphagia, a component of Huntington chorea, may also be caused by dopamine antagonists such as tetrabenazine

            Neuroleptic malignant syndrome (NMS) reported; clinical manifestations include hyperpyrexia, muscle rigidity, altered mental status and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmia); additional signs include elevated creatinine phosphokinase, myoglobinuria, rhabdomyolysis, and acute renal failure

            May cause sedation/somnolence; avoid alcohol and other sedative drugs

            May prolong QTc interval

            May cause orthostatic hypotension

            Concomitant use of neuroleptics (eg, haloperidol, chlorpromazine, risperidone, olanzapine) may cause additive effects of QTc prolongation, NMS, and extrapyramidal disorders

            Caution with poor CYP2D6 metabolizers or drugs that inhibit CYP2D6 (eg, fluoxetine, paroxetine, quinidine); may markedly increase exposure to tetrabenazine active metabolites (alpha- and beta-HTBZ)

            Hyperprolactinemia has resulted from dopaminergic antagonists

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            Pregnancy & Lactation

            Pregnancy

            There are no adequate data on the developmental risk associated with therapy in pregnant women; administration of tetrabenazine to rats throughout pregnancy and lactation resulted in an increase in stillbirths and postnatal offspring mortality

            Lactation

            There are no data on presence of tetrabenazine or metabolites in human milk, effects on breastfed infant, or on milk production; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and potential adverse effects on breastfed infant or underlying maternal condition

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Reversibly inhibits human vesicular monoamine transporter type 2 (VMAT2), resulting in decreased uptake of monoamines (eg, dopamine, serotonin, norepinephrine, histamine) into synaptic vesicles and depletion of monoamine stores from nerve terminals

            This effect is similar to reserpine, but with less peripheral activity and is shorter-acting

            Absorption

            Extent of absorption is at least 75%

            Distribution

            Protein Bound: 82-85%; 59-68% (metabolites)

            Parent drug and metabolites bind to melanin-containing tissues (ie, eye, skin)

            Rapidly distributed in brain (highest binding in striatum, lowest binding in cortex)

            Metabolism

            Rapid and extensively metabolized in liver by carbonyl reductase to active metabolites

            Metabolites (active): alpha-hydroxytetrabenazine, beta-hydroxytetrabenazine

            Active metabolites are predominantly metabolized by CYP2D6

            Elimination

            Half-Life: 7 hr (alpha-hydroxytetrabenazine); 5 hr (beta-hydroxytetrabenazine)

            Excretion: 75% urine; 7-16% feces; excreted mostly as metabolites

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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            Xenazine oral
            -
            25 mg tablet
            Xenazine oral
            -
            12.5 mg tablet
            tetrabenazine oral
            -
            25 mg tablet
            tetrabenazine oral
            -
            25 mg tablet
            tetrabenazine oral
            -
            25 mg tablet
            tetrabenazine oral
            -
            12.5 mg tablet
            tetrabenazine oral
            -
            25 mg tablet
            tetrabenazine oral
            -
            12.5 mg tablet
            tetrabenazine oral
            -
            12.5 mg tablet
            tetrabenazine oral
            -
            25 mg tablet
            tetrabenazine oral
            -
            12.5 mg tablet
            tetrabenazine oral
            -
            25 mg tablet
            tetrabenazine oral
            -
            12.5 mg tablet

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Patient Education
            tetrabenazine oral

            TETRABENAZINE - ORAL

            (TE-tra-BEN-a-zeen)

            COMMON BRAND NAME(S): Xenazine

            WARNING: Tetrabenazine can sometimes increase the risk of depression and suicidal thoughts/attempts. People with Huntington's disease are more likely to have depression and suicidal thoughts/attempts. Discuss the risks and benefits of this medication with your doctor. People who are not being treated for their depression and suicidal thoughts/attempts, or people who have persistent symptoms of these conditions (even with medication/treatment) must not use tetrabenazine. Tell your doctor right away if you or your family/caregivers notice that you have new/worsening symptoms of depression, sadness, loss of interest in activities you used to enjoy, suicidal thoughts/attempts, or other mental/mood/behavior changes (such as new/worsening anxiety, panic attacks, trouble sleeping, irritability, hostile/angry feelings, strong/abnormal urges, severe restlessness, very rapid speech).

            USES: Tetrabenazine is used to decrease the uncontrollable movements (chorea) caused by Huntington's disease. However, it is not a cure for the disease. Reducing the chorea will help you take part in more of your normal daily activities. This medication is thought to work by decreasing the amount of certain natural substances in the brain (monoamines such as dopamine, serotonin, and norepinephrine), which are involved with nerve and muscle function. Tetrabenazine belongs to a class of drugs called monoamine depletors.

            HOW TO USE: Read the Medication Guide provided by your pharmacist before you start using tetrabenazine and each time you get a refill. If you have any questions, consult your doctor or pharmacist.Take this medication by mouth with or without food, usually once a day in the morning when you first start treatment or as directed by your doctor. Your doctor may gradually increase your dose to 2 or 3 times a day over several weeks. A slow increase in your dose will help your doctor find the best dose for you while keeping side effects as low as possible.The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time(s) each day.If you stop taking this drug for several days, then start taking it again, you may need to slowly increase your dose until you reach the regular dose you had been taking. Follow your doctor's directions on how to restart treatment.Tell your doctor if your uncontrolled movements do not improve or if they worsen.

            SIDE EFFECTS: See also Warning section.Drowsiness, trouble sleeping, tiredness, dizziness, nausea, and vomiting may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly. Your doctor may need to adjust your dose to reduce these side effects.To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Sometimes tetrabenazine can cause side effects that are similar to the symptoms of worsening Huntington's disease. Your doctor may need to adjust your dose to see if these side effects are due to the drug or to the disease. Tell your doctor right away if any of these serious side effects occur: mental/mood changes (such as new/worsening depression, suicidal thoughts/attempts, problems with thinking), Parkinson's disease symptoms (such as shaking/tremors, slowed movement, loss of balance), trouble swallowing, restlessness.Tell your doctor right away if any of these unlikely but serious side effects occur: signs of increased prolactin hormone (such as enlarged breasts, abnormal breast milk production, decreased sexual ability, a change in menstrual cycle).This medication may rarely cause a very serious condition called neuroleptic malignant syndrome (NMS). Get medical help right away if you have any of the following symptoms: fever, muscle stiffness/pain/tenderness/weakness, severe tiredness, severe confusion, sweating, fast/irregular heartbeat, dark urine, signs of kidney problems (such as change in the amount of urine).A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: See also Warning section.Before taking tetrabenazine, tell your doctor or pharmacist if you are allergic to it; or to deutetrabenazine; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: breast cancer, liver problems, certain heart problems (fast/slow/irregular heartbeat, QT prolongation in the EKG).This drug may make you dizzy or drowsy. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

            DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug are: valbenazine.Taking MAO inhibitors with this medication may cause a serious (possibly fatal) drug interaction. Do not take any MAO inhibitors (isocarboxazid, linezolid, metaxalone, methylene blue, moclobemide, phenelzine, procarbazine, rasagiline, safinamide, selegiline, tranylcypromine) during treatment with this medication. Most MAO inhibitors should also not be taken for two weeks before and after treatment with this medication. Ask your doctor when to start or stop taking this medication.Tetrabenazine is very similar to deutetrabenazine. Do not use medications containing deutetrabenazine while using tetrabenazine.

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: muscle stiffness/pain, fixed upward position of the eyeballs, sweating, dizziness, severe drowsiness.

            NOTES: Do not share this medication with others.Laboratory and/or medical tests may be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

            MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store at room temperature at 77 degrees F (25 degrees C) away from light and moisture. Brief storage between 59-86 degrees F (15-30 degrees C) is permitted. Do not store in the bathroom. Keep all medicines away from children and pets.

            Information last revised September 2021. Copyright(c) 2021 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.