Tetrabenazine: Spotlight on Drug Review

Kaur, Navneet; Kumar, Puneet; Jamwal, Sumit; Deshmukh, Rahul; Gauttam, Vinod

doi:10.1159/000449184

Cited by 66 publications

(61 citation statements)

References 51 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Tetrabenazine (TBZ) is the only US Food and Drug Administration‐approved drug for chorea in HD, and is usually taken 3 times daily. Although it was developed to treat psychosis, it was later found to ease hyperkinetic movement disorders, including chorea, tics, tardive dyskinesia, and dystonia, although, in the United States, it is licensed only for treating chorea 2. Unlike classical neuroleptics, this compound depletes presynaptic dopamine by blocking vesicular monoamine transporter type 2 (VMAT2) 3.…”

mentioning

confidence: 99%

Tetrabenazine Versus Deutetrabenazine for Huntington's Disease: Twins or Distant Cousins?

Rodrigues

Duarte

Costa

et al. 2017

Movement Disord Clin Pract

View full text Add to dashboard Cite

BackgroundTetrabenazine is the only US Food and Drug Administration‐approved drug for Huntington's disease, and deutetrabenazine was recently tested against placebo. A switching‐trial from tetrabenazine to deutetrabenazine is underway, but no head‐to‐head, blinded, randomized controlled trial is planned. Using meta‐analytical methodology, the authors compared these molecules.Methods RCTs comparing tetrabenazine or deutetrabenazine with placebo in Huntington's disease were searched. The authors assessed the Cochrane risk‐of‐bias tool, calculated indirect treatment comparisons, and applied the Grading of Recommendations Assessment, Development, and Evaluation (GRADE) framework.ResultsThe evidence network for this report comprised 1 tetrabenazine trial and 1 deutetrabenazine trial, both against placebo. Risk of bias was moderate in both. Participants in the tetrabenazine and deutetrabenazine trials did not differ significantly on motor scores or adverse events. Depression and somnolence scales significantly favored deutetrabenazine.ConclusionThere is low‐quality evidence that tetrabenazine and deutetrabenazine do not differ in efficacy or safety. It is important to note that these results are likely to remain the only head‐to‐head comparison between these 2 compounds in Huntington's disease.

show abstract

mentioning

confidence: 99%

Tetrabenazine Versus Deutetrabenazine for Huntington's Disease: Twins or Distant Cousins?

Rodrigues

Duarte

Costa

et al. 2017

Movement Disord Clin Pract

View full text Add to dashboard Cite

show abstract

“…Tetrabenazine has been used for clinical purposes in several countries decades. Tetrabenazine is a potent blocker of vesicular monoamine transporter [4][5]. There are few analytical methods published in the literature to detect the drug in biological fluids or to perform quality control of the medication [6].…”

Section: Introductionmentioning

confidence: 99%

An Applicable Method for the Estimation of Tetrabenazine by Simple RP-HPLC in Tablet Dosage Form

2017

View full text Add to dashboard Cite

The aim of this work was to develop and validate the assay test for Tetrabenazine in the pharmaceutical dosage forms by HPLC. The assay method by HPLC was found to be linear in the concentration range of 20 to 100 µg/mL. The mobile phase was composed of acetonitrile and buffer pH: 6.8 potassium dihydrogen phosphate (60:40 v/v) the flow rate of 1 mL/min using UV detection at 215 nm. The results of the analysis were validated by recovery studies. The percentage recovery method was found to be 99.33-100.87%. The LOD and LOQ were found to 0.04 μg/mL and 0.15 μg/mL. All the parameters of validation were in the acceptable range. This developed method was successfully applied to estimate the amount of Tetrabenazine in the tablets.

show abstract

“…Developed in the 1950s [18], tetrabenazine is currently approved for the treatment of moderate to severe TD in some countries, and has been used and studied off-label for TD in the USA [19,20]. Tetrabenazine undergoes rapid absorption and metabolism with a half-life of approximately 10 h [21], and requires multiple daily dosing [20].…”

mentioning

confidence: 99%

“…Tetrabenazine undergoes rapid absorption and metabolism with a half-life of approximately 10 h [21], and requires multiple daily dosing [20]. As a consequence of this rapid metabolism, chorea has been shown to recur within 12-18 h after the last dose of tetrabenazine [20].…”

mentioning

confidence: 99%

“…Tetrabenazine binds selectively to VMAT2, but it is the dihydrotetrabenazine (HTBZ) metabolites that have the main pharmacologic effects. However, some of these metabolites (i.e., different HTBZ stereoisomers) have affinity for other off-target receptors [22], possibly contributing to unwanted side effects that can be dose-limiting and possibly confound treatment efforts [20,23,24]. In addition, due to its tolerability and pharmacokinetic profile, use of tetrabenazine for Huntington's disease includes recommendations for CYP2D6 genotyping to screen for poor metabolizer status when exceeding doses of 50 mg/day [15].…”

mentioning

confidence: 99%

See 1 more Smart Citation

Treatment of tardive dyskinesia with tetrabenazine or valbenazine: a systematic review

2018

View full text Add to dashboard Cite

Up to 30% of patients taking antipsychotics may develop tardive dyskinesia (TD). Recent evidence-based recommendations demonstrate an unmet need for effective TD management. This systematic review was designed to update the evidence for TD treatment, comparing two vesicular monoamine transporter 2 (VMAT2) inhibitors, tetrabenazine and valbenazine. Of 487 PubMed/Embase search results, 11 studies met the review criteria. Valbenazine efficacy was demonstrated in rigorously designed clinical trials that meet the guidelines for AAN Class I evidence. Due to differences in study designs and a lack of standardized and controlled trials with tetrabenazine, a formal meta-analysis comparing the agents was not possible. However, valbenazine appears to have fewer side effects and a more favorable once-daily dosing regimen for the treatment of TD. Tardive dyskinesia (TD) is an involuntary movement disorder induced by prolonged exposure to dopamine receptor blocking agents (DRBAs), including antipsychotics and antiemetics [1,2]. Research shows that the prescription of antipsychotics alone increased more than threefold over 10 years; conservative estimates thus indicate that approximately 5 million patients have been exposed to antipsychotics in the United States (US) [3]. Given that the estimated global mean prevalence of TD is 30% in studies of patients currently treated with a first-generation antipsychotic and 21% in those currently treated with a second-generation antipsychotic, this disorder remains a significant problem for psychiatric patients who may experience stigma, embarrassment, and impairment in social functioning (and sometimes physical functioning) as a consequence of developing TD [4]. While the prevalence of TD has been extensively studied, the associated healthcare burden is the subject of continuing investigation [3][4][5]. Previous studies have shown that the presence of TD in patients with schizophrenia may correlate with impaired cognition, poor response to treatment, greater risk of relapse, longer hospital stays, lower quality of life and functioning, a progressive course, and increased mortality [6].Through the mechanism of blocking dopamine receptors, antipsychotics have proven to be highly effective and essential drugs for controlling psychotic symptoms in patients with conditions such as schizophrenia and bipolar disorder [7][8][9][10]. However, dopamine is also involved as a key neurotransmitter in other neural pathways, notably the motor circuit [7,11]. Blockade in the motor circuit may lead to upregulation and hypersensitivity of post-synaptic dopamine receptors, resulting in an increase of dopaminergic signaling and the emergence of abnormal movements associated with TD [10,12].Vesicular monoamine transporters (VMATs) are presynaptic intracellular transmembrane proteins that have a critical role in the packaging, storage and release of dopamine and other monoamines [13]. Inhibition of VMAT2, which is the predominant isoform in the brain, interferes with dopamine uptake and storage in presynapti...

show abstract

Tetrabenazine: Spotlight on Drug Review

Cited by 66 publications

References 51 publications

Tetrabenazine Versus Deutetrabenazine for Huntington's Disease: Twins or Distant Cousins?

Tetrabenazine Versus Deutetrabenazine for Huntington's Disease: Twins or Distant Cousins?

An Applicable Method for the Estimation of Tetrabenazine by Simple RP-HPLC in Tablet Dosage Form

Treatment of tardive dyskinesia with tetrabenazine or valbenazine: a systematic review

Contact Info

Product

Resources

About