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VMAT2 Inhibitor — Hyperkinetic Movement Disorders Pregnancy: Not recommended during pregnancy or in women of childbearing potential not using contraception — there are no adequate and well-controlled studies in pregnant women, animal studies have shown reproductive toxicity and the potential risk for humans is unknown; the effects on labour and delivery are unknown. Contraindicated during breastfeeding (§4.3/§4.6).

Tetrabenazine

Brand names: Nitoman

Tetrabenazine is a monoamine-depleting agent used to control hyperkinetic movement disorders, notably the chorea of Huntington's disease and some forms of hemiballismus and severe tardive dyskinesia.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: Hyperkinetic movement disorders in Huntington's chorea: initial dose 25 mg three times a day, increased by 25 mg per day every three or four days until either satisfactory efficacy is achieved or undesirable side effects occur (tolerance limit)
Route: Oral — tablets taken with sufficient liquid (water or other non-alcoholic beverages) and not chewed
Frequency: Three times a day
Max: 200 mg daily — in general the maximum daily dose of 200 mg tetrabenazine should not be exceeded
Dosing and administration times are variable and must be individually adjusted according to the severity of disease and response to treatment; the dose recommendation serves only as a guideline. If no improvement is seen after seven days of taking the maximum dose, the medicine is unlikely to benefit the patient even if the dose is further increased or treatment prolonged, and withdrawal should be considered. Once a stable maintenance dose is achieved, review treatment at regular intervals. Tardive dyskinesia: the recommended initial dose is 12.5 mg per day, then increased depending on the patient's response; discontinue if there is no clear improvement or if adverse reactions cannot be tolerated; the maximum daily dose of 200 mg should not be exceeded. Resumption of treatment after an interruption of more than 5 days (or an interruption due to a change in medical condition or concomitant medicines): retitrate — initiate at 12.5 mg twice a day, wait 7 days, then titrate up by 12.5 mg per day; if akathisia, restlessness, parkinsonism, depression, insomnia, anxiety or intolerable sedation occur, stop titration and reduce the dose. Discontinuation is associated with the return of chorea (without significant worsening compared with baseline). Elderly: no specific studies in patients over 65 years; tetrabenazine 25 mg has been given to elderly patients at the recommended adult dose without discernible adverse effects. Paediatric population: no adequately controlled clinical studies have been performed in children and a dosage recommendation cannot be given — limited clinical experience suggests that treatment be started at approximately half the daily dose for an adult and then slowly and carefully adjusted depending on tolerance and individual reaction. Patients taking CYP2D6 inhibitors: determine the appropriate dose for each patient by titration — the dose required may be influenced by CYP2D6 metaboliser status and by co-administered potent CYP2D6 inhibitors.

Dose adjustments

Renal

In patients with impaired liver or kidney function, dose titration should be done slowly and lower daily doses may be required. Impaired hepatic function (Child-Pugh score 5 to 9) is a contraindication.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

  • Hypersensitivity to the active substance or to any of the excipients
  • Acute risk of suicide
  • Untreated or insufficiently treated depression
  • Existing prolactin-dependent tumours, such as prolactin-dependent pituitary tumours or breast cancer
  • Presence of a phaeochromocytoma
  • Breastfeeding
  • Intake of monoamine oxidase inhibitors (MAOIs) concomitantly or less than 14 days previously
  • Impaired hepatic function (Child-Pugh score 5 to 9)
  • Concomitant intake of reserpine
  • Parkinson's syndrome and hypokinetic-rigid syndrome

Side effects

  • Drowsiness (very common) — the most common dose-dependent adverse reaction
  • Depression (very common), associated with suicidal ideation and suicidal behaviour in individual cases
  • Parkinsonism, which may include impaired balance, tremor and increased salivation (very common)
  • Agitation, anxiety, insomnia and confusion (common)
  • Dysphagia, nausea, vomiting, epigastralgia, diarrhoea, constipation and dry mouth (common)

Interactions

  • Monoamine oxidase inhibitors — contraindicated; at least 14 days must elapse between stopping tetrabenazine and starting an MAOI, and between stopping an MAOI and starting tetrabenazine (§4.3/§4.4)
  • Reserpine — concomitant intake is contraindicated (§4.3). US labelling states at least 20 days should elapse after stopping reserpine before starting tetrabenazine (US label §7.2)
  • Potent/strong CYP2D6 inhibitors (e.g. quinidine, fluoxetine, paroxetine) — the tetrabenazine metabolites alpha-HTBZ and beta-HTBZ are CYP2D6 substrates, so the dose required may be influenced by CYP2D6 metaboliser status and by concomitant strong inhibitors; determine dose by titration (§4.2/§4.4). US labelling caps the total dose at 50 mg/day with a maximum single dose of 25 mg in patients taking strong CYP2D6 inhibitors (US label §2.3/§7.1)
  • Deutetrabenazine or valbenazine — contraindicated in the US labelling (US label §4)
  • Other medicinal products that prolong QTc — not recommended in combination (US label §5.8)

Clinical monograph

How it works

It reversibly inhibits vesicular monoamine transporter 2 (VMAT2), depleting presynaptic stores of dopamine and other monoamines and so reducing involuntary movements.

Prescribing in practice

  • It can cause or worsen depression and suicidal ideation, so patients should be assessed for low mood and monitored, and it is contraindicated in those with untreated or inadequately treated depression.
  • Parkinsonism, sedation, akathisia and, rarely, a neuroleptic malignant syndrome-like reaction can occur.
  • It should be avoided alongside monoamine oxidase inhibitors and used cautiously with other dopamine-blocking or QT-prolonging drugs.

Monitoring

Monitor mood and for emerging suicidal thoughts, alongside parkinsonian features, swallowing and signs of QT prolongation.

Counselling the patient

  • Report any worsening mood, hopelessness or thoughts of self-harm promptly.
  • Tell your clinician if you become stiff, slow, very drowsy or develop restlessness.

Evidence & guidelines

Benefit on chorea in Huntington's disease is supported by randomised controlled trial data and reflected in its licensed indication.

Reference: NICE NG42 (Huntington's Disease); TETRA-HD Trial; MHRA SPC Nitoman; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.