Tetrabenazine
- Atc Codes:N07XX06
- CAS Codes:58-46-8
- PHARMGKB ID:58-46-8
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Denmark: Nitoman; France: Xenazine; Germany: Nitoman, Xenazine; Greece: Xenazine; Ireland: Nitoman; Italy: Xenazina; Malta: Xenazine; Netherlands: Xenazine; Portugal: Nitoman, Revocon; Spain: Nitoman; Sweden: Xenazine; UK: Xenazine.
North America
Canada: Nitoman; USA: Xenazine.
Drug combinations
Chemistry
Tetrabenazine: C~19~H~27~NO~3~. Mw: 317.42. 1,3,4,6,7,11b-Hexahydro-3-isobutyl-9,10-dimethoxy-2H-benzo[a]quinolizin-2-one. CAS-58-46-8.
Pharmacologic Category
Central Nervous System Agents, Miscellaneous. Central Monoamine-Depleting Agent. (ATC-Code: N07XX06).
Mechanism of action
Within basal ganglia, interferes with and depletes monoamine neurotransmitters (including dopamine, serotonin, and norepinephrine) in presynaptic vesicles (probably through actions on vesicle monoamine transporter). Tetrabenazine inhibits presynaptic dopamine release and also blocks CNS dopamine receptors. Effects resemble reserpine but with less peripheral activity and shorter duration of action. Treatment results in symptomatic improvement of hyperkinetic movement disorders, including Huntington’s chorea, hemiballismus, senile chorea, tic, Gilles de la Tourette’s syndrome, and tardive dyskinesia.
Therapeutic use
Treatment of chorea associated with Huntington’s disease. Treatment of hyperkinetic movement disorders, including Huntington’s chorea, hemiballismus, senile chorea, Tourette syndrome, and tardive dyskinesia.
Pregnancy and lactiation implications
Adverse events observed in some animal studies. There are no adequate, well-controlled studies in pregnant women. Avoid use in pregnant women unless potential benefit justifies potential risk to fetus. Not recommended in nursing women.
Unlabeled use
Contraindications
Actively suicidal patients, or with untreated or inadequately treated depression. Hepatic impairment. Use with or within 14 days of MAOIs. Use with or within 20 days of reserpine. Hypersensitivity to tetrabenazine or any component of the formulation. History or current episode of clinical depression.
Warnings and precautions
Use associated with akathisia. May cause CNS depression. May increase risk for depression and suicidal ideation. Use with caution in history of depression. Use associated with esophageal dysmotility, dysphagia, and aspiration. Use with caution in risk of aspiration pneumonia. Use may be associated with NMS. May cause orthostatic hypotension. Has been shown to prolong QT interval alone (minimal) and with other drugs with comparable effects on QT interval (additive). Avoid use in congenital QT prolongation, history of cardiac arrhythmias, or concomitant drugs known to cause QT prolongation. Use with caution in Parkinson’s disease (may induce/exacerbate symptoms of parkinsonism (more common in elderly patients)), and in breast cancer or other prolactin-dependent tumors (elevates prolactin levels). Possible comorbid psychiatric disorders and potential psychiatric adverse effects. Not studied with concomitant use of neuroleptic drugs (e.g. haloperidol, olanzapine), adverse effects may be additive. Patients should be tested for CYP2D6 gene. Should not be used to treat levodopa-induced dyskinesia.