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Deutetrabenazine: Drug information

Deutetrabenazine: Drug information
2024© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
For additional information see "Deutetrabenazine: Patient drug information"

For abbreviations, symbols, and age group definitions show table
ALERT: US Boxed Warning
Depression and suicidality in patients with Huntington disease:

Deutetrabenazine can increase the risk of depression and suicidal thoughts and behavior (suicidality) in patients with Huntington disease. Anyone considering the use of deutetrabenazine must balance the risks of depression and suicidality with the clinical need for treatment of chorea. Closely monitor patients for the emergence or worsening of depression, suicidality, or unusual changes in behavior. Patients, their caregivers, and families should be informed of the risk of depression and suicidality and should be instructed to report behaviors of concern promptly to the treating physician.

Particular caution should be exercised in treating patients with a history of depression or prior suicide attempts or ideation, which are increased in frequency in Huntington disease. Deutetrabenazine is contraindicated in patients who are suicidal, and in patients with untreated or inadequately treated depression.

Brand Names: US
  • Austedo;
  • Austedo Patient Titration Kit [DSC];
  • Austedo XR;
  • Austedo XR Patient Titration
Pharmacologic Category
  • Central Monoamine-Depleting Agent;
  • Vesicular Monoamine Transporter 2 (VMAT2) Inhibitor
Dosing: Adult

Note: Dose should be individualized. Maximum dose in CYP2D6 poor metabolizers is 36 mg/day.

Huntington disease–associated chorea

Huntington disease–associated chorea:

Immediate release: Oral: Initial: 6 mg twice daily; may increase dose weekly based on response and tolerability in increments of 6 mg/day; administer in 2 divided doses if total dose ≥12 mg/day; maximum recommended dose: 48 mg/day.

Extended release: Oral: Initial: 12 mg once daily; may increase dose weekly based on response and tolerability in increments of 6 mg/day, administered once daily; maximum recommended dose: 48 mg/day.

Tardive dyskinesia

Tardive dyskinesia:

Immediate release: Oral: Initial: 6 mg twice daily; may increase dose weekly based on response and tolerability in increments of 6 mg/day. Administer in 2 divided doses if total dose ≥12 mg/day; maximum recommended dose: 48 mg/day.

Extended release: Oral: Initial: 12 mg once daily; may increase dose weekly based on response and tolerability in increments of 6 mg/day, administered once daily; maximum recommended dose: 48 mg/day.

CYP2D6 poor metabolizers: Maximum dose: 36 mg/day.

Switching from immediate release to extended release : The same total daily dose of deutetrabenazine should be used.

Conversion from tetrabenazine: Discontinue tetrabenazine and initiate deutetrabenazine the following day, using the following conversion. May adjust dose weekly based on response and tolerability.

Deutetrabenazine Conversion From Tetrabenazine

Current tetrabenazine daily dose

Initial deutetrabenazine ER tablet dose

Initial deutetrabenazine IR tablet dose

12.5 mg

6 mg once daily

6 mg once daily

25 mg

12 mg once daily

6 mg twice daily

37.5 mg

18 mg once daily

9 mg twice daily

50 mg

24 mg once daily

12 mg twice daily

62.5 mg

30 mg once daily

15 mg twice daily

75 mg

36 mg once daily

18 mg twice daily

87.5 mg

42 mg once daily

21 mg twice daily

100 mg

48 mg once daily

24 mg twice daily

Reinitiation of therapy: If dosing is interrupted for <7 days, resume at previous maintenance dose. If dosing is interrupted for ≥7 days, retitrate when resuming.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Dosing: Hepatic Impairment: Adult

Use is contraindicated.

Dosing: Adjustment for Toxicity: Adult

Akathisia; parkinsonism: Reduce dose; therapy discontinuation may be necessary.

Depression or suicidality, unresolving: Consider discontinuation of therapy.

Hyperprolactinemia, symptomatic: Initiate appropriate laboratory assessment and consider discontinuation of therapy.

Neuroleptic malignant syndrome: Immediately discontinue deutetrabenazine; monitor and manage symptoms and concomitant complications. If deutetrabenazine therapy is reinitiated after recovery, monitor for signs of recurrence.

Dosing: Older Adult

Refer to adult dosing; use with caution.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%: Central nervous system: Drowsiness (11%)

1% to 10%:

Central nervous system: Fatigue (9%), insomnia (4% to 7%), anxiety (4%), depression (≤4%), agitation (≤4%), akathisia (≤4%), restlessness (≤4%), suicidal ideation (2%)

Gastrointestinal: Diarrhea (9%), xerostomia (9%), constipation (4%)

Genitourinary: Urinary tract infection (7%)

Hematologic & oncologic: Bruise (4%)

Respiratory: Nasopharyngitis (4%)

Frequency not defined:

Central nervous system: Sedation

Contraindications

Hepatic impairment; patients with Huntington disease who are suicidal or have untreated or inadequately treated depression; coadministration with tetrabenazine or valbenazine; coadministration with or within 14 days of discontinuing monoamine oxidase inhibitors (MAOIs); coadministration with or within 20 days of discontinuing reserpine.

Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Warnings/Precautions

Concerns related to adverse effects:

• Akathisia: Use has been associated with akathisia; monitor for signs and symptoms of restlessness and agitation. Dosage reduction or discontinuation may be necessary.

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery, driving).

• Hyperprolactinemia: May increase prolactin levels; clinical significance of hyperprolactinemia in patients with breast cancer or other prolactin-dependent tumors is unknown.

• Neuroleptic malignant syndrome: Use may be associated with neuroleptic malignant syndrome (NMS); monitor for mental status changes, fever, muscle rigidity and/or autonomic instability. Discontinue with confirmed NMS; may recur with reintroduction of treatment; monitor carefully.

• Ophthalmic effects: Binds to melanin-containing tissues in animal studies; may result in accumulation and toxicity with extended use and long-term ophthalmic effects. Clinical relevance and monitoring recommendations are unknown.

• Parkinsonism: Parkinsonism, including bradykinesia and gait disturbances (leading to falls or the emergence/worsening of tremor in some cases), has been reported in patients with Huntington disease. Most cases occurred within 2 weeks of initiation or dose escalation and resolved following discontinuation. Development of these symptoms may be difficult to differentiate from progression of the underlying disease; dose reduction or discontinuation of therapy may be necessary.

• QTc prolongation: QTc prolongation may occur but is found to be clinically insignificant when deutetrabenazine is administered within the recommended dosage range. Avoid use in patients with congenital QT prolongation or a history of cardiac arrhythmias. Risk may be increased in patients with bradycardia, hypokalemia, hypomagnesemia, concomitant use of drugs known to cause QT prolongation, or presence of congenital QTc prolongation.

Special populations:

• CYP2D6 poor metabolizers: CYP2D6 poor metabolizers have increased levels of primary drug metabolites; maximum dosage should not exceed 36 mg/day in poor metabolizers.

• Huntington disease: May worsen mood, cognition, rigidity, and functional capacity in patients with Huntington disease, which can be difficult to differentiate from progression of the underlying disease. Underlying chorea may improve over time in some patients, thereby decreasing the need for therapy. Reevaluate patients' need for treatment by periodically assessing the effect on chorea and possible adverse effects. Dose reduction or discontinuation of therapy may be necessary.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral:

Austedo: 6 mg [contains fd&c blue #2 (indigo carm) aluminum lake, fd&c red #40(allura red ac)aluminum lake]

Austedo: 9 mg [contains fd&c blue #2 (indigo carm) aluminum lake]

Austedo: 12 mg [contains fd&c blue #2 (indigo carm) aluminum lake, fd&c yellow #6(sunset yellow)alumin lake]

Tablet Extended Release 24 Hour, Oral:

Austedo XR: 6 mg, 12 mg [contains fd&c blue #2 (indigo carm) aluminum lake, fd&c red #40(allura red ac)aluminum lake, fd&c yellow #6(sunset yellow)alumin lake]

Austedo XR: 24 mg [contains fd&c blue #2 (indigo carm) aluminum lake, fd&c red #40(allura red ac)aluminum lake]

Tablet Extended Release Therapy Pack, Oral:

Austedo XR Patient Titration: 6 & 12 & 24 MG (42 ea) [contains fd&c blue #2 (indigo carm) aluminum lake, fd&c red #40(allura red ac)aluminum lake, fd&c yellow #6(sunset yellow)alumin lake]

Tablet Therapy Pack, Oral:

Austedo Patient Titration Kit: 6 & 9 & 12 MG (70 ea [DSC]) [contains fd&c blue #2 (indigo carm) aluminum lake, fd&c red #40(allura red ac)aluminum lake, fd&c yellow #6(sunset yellow)alumin lake]

Generic Equivalent Available: US

No

Pricing: US

Tablet Extended Release Therapy Pack (Austedo XR Patient Titration Oral)

6 & 12 & 24 mg (per each): $195.24

Tablet, 24-hour (Austedo XR Oral)

6 mg (per each): $97.62

12 mg (per each): $195.24

24 mg (per each): $292.86

Tablets (Austedo Oral)

6 mg (per each): $97.62

9 mg (per each): $109.82

12 mg (per each): $146.43

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Oral:

Immediate release: Administer with food. Manufacturer labeling recommends that tablets should be swallowed whole, not chewed, crushed, or broken; however, a case report describes crushing deutetrabenazine 6 mg tablets and dissolving in 10 to 20 mL of sterile water for PEG tube administration, flushing the PEG tube before and after administration with 15 mL sterile water, with no reported adverse effects (Ref).

Extended release: Administer with or without food. Swallow whole; do not break, chew, or crush.

Medication Guide and/or Vaccine Information Statement (VIS)

An FDA-approved patient medication guide, which is available with the product information and as follows, must be dispensed with this medication:

Austedo: https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/216354s000lbl.pdf#page=29

Use: Labeled Indications

Chorea associated with Huntington disease: Treatment of chorea associated with Huntington disease in adults.

Tardive dyskinesia: Treatment of tardive dyskinesia in adults.

Metabolism/Transport Effects

Substrate of CYP1A2 (minor), CYP2D6 (major), CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Ajmaline: May increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy

Alizapride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Antipsychotic Agents: Deutetrabenazine may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, the risk for akathisia, parkinsonism, or neuroleptic malignant syndrome may be increased. Risk C: Monitor therapy

Artemether and Lumefantrine: May increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Azelastine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider therapy modification

Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Risk C: Monitor therapy

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Bromopride: May enhance the adverse/toxic effect of Deutetrabenazine. Specifically, the risk for akathisia, parkinsonism, or neuroleptic malignant syndrome may be increased. Risk C: Monitor therapy

Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Risk D: Consider therapy modification

Cannabinoid-Containing Products: CNS Depressants may enhance the CNS depressant effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider therapy modification

Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy

CYP2D6 Inhibitors (Moderate): May increase serum concentrations of the active metabolite(s) of Deutetrabenazine. Risk C: Monitor therapy

CYP2D6 Inhibitors (Strong): May increase serum concentrations of the active metabolite(s) of Deutetrabenazine. Management: The total daily dose of deutetrabenazine should not exceed 36 mg with concurrent use of a strong CYP2D6 inhibitor. Risk D: Consider therapy modification

Daridorexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification

DexmedeTOMIDine: CNS Depressants may enhance the CNS depressant effect of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider therapy modification

Difelikefalin: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Doxylamine: CNS Depressants may enhance the CNS depressant effect of Doxylamine. Risk C: Monitor therapy

DroPERidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification

Esketamine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Flunarizine: CNS Depressants may enhance the CNS depressant effect of Flunarizine. Risk X: Avoid combination

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider therapy modification

Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of Haloperidol. Risk C: Monitor therapy

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider therapy modification

Ixabepilone: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Kava Kava: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Kratom: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider therapy modification

Levodopa-Foslevodopa: Vesicular Monoamine Transporter 2 (VMAT2) Inhibitors may diminish the therapeutic effect of Levodopa-Foslevodopa. Management: Consider alternatives to the coadministration of levodopa and vesicular monoamine transporter 2 (VMAT2) inhibitors. If combined, monitor for reduced levodopa efficacy. Risk D: Consider therapy modification

Lisuride: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Loxapine: CNS Depressants may enhance the CNS depressant effect of Loxapine. Risk D: Consider therapy modification

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Mavorixafor: May increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider therapy modification

Metoclopramide: Deutetrabenazine may enhance the adverse/toxic effect of Metoclopramide. Specifically, the risk for akathisia, parkinsonism, or neuroleptic malignant syndrome may be increased. Risk C: Monitor therapy

MetyroSINE: May enhance the adverse/toxic effect of Vesicular Monoamine Transporter 2 (VMAT2) Inhibitors. Specifically, the risk for extrapyramidal symptoms and excessive sedation may be increased. Risk C: Monitor therapy

Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Monoamine Oxidase Inhibitors: May enhance the adverse/toxic effect of Deutetrabenazine. Risk X: Avoid combination

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Olopatadine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination

Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Oxybate Salt Products: CNS Depressants may enhance the CNS depressant effect of Oxybate Salt Products. Management: Consider alternatives to this combination when possible. If combined, dose reduction or discontinuation of one or more CNS depressants (including the oxybate salt product) should be considered. Interrupt oxybate salt treatment during short-term opioid use Risk D: Consider therapy modification

OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination

Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Peginterferon Alfa-2b may increase the serum concentration of CYP2D6 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy

Procarbazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy

Reserpine: May enhance the adverse/toxic effect of Deutetrabenazine. Risk X: Avoid combination

Ropeginterferon Alfa-2b: CNS Depressants may enhance the adverse/toxic effect of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider therapy modification

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk C: Monitor therapy

Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification

Tetrabenazine: Deutetrabenazine may enhance the adverse/toxic effect of Tetrabenazine. Risk X: Avoid combination

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination

Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Valbenazine: Deutetrabenazine may enhance the adverse/toxic effect of Valbenazine. Risk X: Avoid combination

Valerian: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider therapy modification

Zuranolone: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider therapy modification

Reproductive Considerations

Although not evaluated in preclinical studies, deutetrabenazine may increase serum prolactin concentrations which may lead to amenorrhea or impotence.

Pregnancy Considerations

Adverse events were not observed in available animal reproduction studies.

Breastfeeding Considerations

It is not known if deutetrabenazine or its metabolites are present in breast milk. According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.

Dietary Considerations

Administer IR tablets with food.

Monitoring Parameters

Electrolytes; EKG; signs/symptoms of depression or suicidal ideation; signs and/or symptoms of NMS, restlessness and agitation.

Mechanism of Action

The precise mechanism by which deutetrabenazine exerts its effects is unknown. Its major metabolites (alpha-dihydrotetrabenazine [HTBZ] and beta-HTBZ) act as reversible inhibitors of the human vesicular monoamine transporter type 2 (VMAT-2) and thereby decrease the uptake of monoamines (including dopamine, serotonin, norepinephrine, and histamine) into synaptic vesicles and deplete the monoamine stores.

Pharmacokinetics (Adult Data Unless Noted)

Distribution: alpha-HTBZ: ~500 L; beta-HTBZ: 730 L.

Protein binding: alpha-HTBZ: 60% to 68%; beta-HTBZ: 59% to 63%.

Metabolism: Extensive hepatic metabolism via carbonyl reductase to alpha-dihydrotetrabenazine (HTBZ) and beta-HTBZ (active major metabolites), which are subsequently metabolized via CYP2D6 (minor contributions of CYP1A2 and CYP3A4/5) to form several minor metabolites.

Bioavailability: 80%.

Half-life elimination: 9 to 10 hours.

Time to peak, plasma: 3 to 4 hours.

Excretion: Urine (75% to 86%; <10% as active major metabolites); feces (8% to 11%).

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Poor CYP2D6 metabolizers: It is likely that the exposure to alpha-HTBZ and beta-HTBZ would be increased ~3-fold.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (BD) Bangladesh: Ajuben;
  • (BR) Brazil: Austedo;
  • (KR) Korea, Republic of: Austedo;
  • (PR) Puerto Rico: Austedo
  1. Austedo (deutetrabenazine) tablets [prescribing information]. Parsippany, NJ: Teva Pharmaceuticals USA Inc; February 2023.
  2. Wietholter JP, Sizemore J, Piechowski K. Crushing deutetrabenazine for treatment of tardive dyskinesia in a patient with severe orofacial symptoms: a case report. Am J Health Syst Pharm. 2020;77(18):1477-1481. doi:10.1093/ajhp/zxaa205 [PubMed 32761113]
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