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What is the classification of deutetrabenazine?

2 min read

Deutetrabenazine, first approved by the FDA in 2017, is primarily classified as a vesicular monoamine transporter 2 (VMAT2) inhibitor. This medication, known by the brand names Austedo and Austedo XR, is a specifically modified version of the older drug tetrabenazine, designed for improved pharmacokinetics.

Quick Summary

Deutetrabenazine is a VMAT2 inhibitor, a class of drugs that depletes monoamine neurotransmitters to treat involuntary movements, including chorea associated with Huntington's disease and tardive dyskinesia.

Key Points

  • VMAT2 Inhibitor: Deutetrabenazine is classified as a vesicular monoamine transporter 2 (VMAT2) inhibitor.

  • Deuterated Compound: It is a modified, deuterated form of tetrabenazine.

  • Monoamine Depletion: It blocks VMAT2, depleting monoamines like dopamine to control movements.

  • Extended Half-Life: Deuteration gives it a longer half-life, allowing less frequent dosing.

  • Improved Tolerability: It has a potentially better tolerability profile with fewer neuropsychiatric side effects compared to tetrabenazine.

  • Indicated Conditions: It treats chorea associated with Huntington's disease and tardive dyskinesia.

  • Symptomatic Relief: It provides symptomatic relief but does not cure the underlying diseases.

In This Article

The Pharmacological Classification of Deutetrabenazine

Deutetrabenazine is a prescription medication used for the symptomatic treatment of specific movement disorders. Its primary pharmacological classification is as a vesicular monoamine transporter 2 (VMAT2) inhibitor. It is also known as a central monoamine-depleting agent. This classification is key to understanding its action in the central nervous system to manage involuntary movements.

VMAT2 is responsible for transporting monoamine neurotransmitters into synaptic vesicles. By reversibly inhibiting VMAT2, deutetrabenazine prevents this transport, leading to degradation of monoamines and a reduction in neurotransmission. This reduction helps lessen abnormal involuntary movements in conditions with hyperactive dopaminergic signaling.

Mechanism of Action: How Deutetrabenazine Controls Movement

Deutetrabenazine's mechanism as a VMAT2 inhibitor involves several steps:

  • Deutetrabenazine binds to the VMAT2 protein.
  • This blocks the transport of monoamines into vesicles.
  • Blocked monoamines are degraded in the cytoplasm.
  • This depletes monoamine stores and reduces neurotransmission.
  • Reduced signaling helps decrease involuntary movements.

Key Differences: Deutetrabenazine vs. Tetrabenazine

Deutetrabenazine (Austedo) is a deuterated version of tetrabenazine (Xenazine). Deuteration, replacing hydrogen with deuterium, alters the drug's metabolism and pharmacokinetics.

Comparison of VMAT2 Inhibitors: Deutetrabenazine vs. Tetrabenazine

Feature Deutetrabenazine (Austedo) Tetrabenazine (Xenazine)
Molecular Modification Deuterated form. Non-deuterated form.
Half-Life Longer due to slower metabolism. Shorter.
Dosing Frequency Less frequent, typically twice daily or once daily for extended-release. More frequent, typically three times daily.
Metabolism Slower by CYP2D6. Faster by CYP2D6.
Peak Concentration Reduced peak plasma concentrations. Higher peak plasma concentrations.
Tolerability Profile Potentially more favorable, lower risk of neuropsychiatric adverse effects. Higher incidence of neuropsychiatric side effects.

Clinical Applications and Side Effects

Deutetrabenazine treats two conditions with involuntary movements:

  • Chorea associated with Huntington's disease: Manages the jerky movements.
  • Tardive dyskinesia (TD): Reduces repetitive involuntary movements.

Common side effects include sleepiness, tiredness, diarrhea, and dry mouth. Serious, less common effects can include:

  • Depression and Suicidal Thoughts: Requires close monitoring, especially in Huntington's patients.
  • Parkinsonism: Can cause Parkinson's-like symptoms.
  • Neuroleptic Malignant Syndrome (NMS): A rare, serious condition with fever, stiff muscles, confusion, etc..
  • Akathisia: Inner restlessness.

Conclusion

Deutetrabenazine is classified as a VMAT2 inhibitor. It depletes monoamines to control involuntary movements in Huntington's disease chorea and tardive dyskinesia. Deuteration provides a longer duration of action, less frequent dosing, and a better tolerability profile than tetrabenazine. This makes it an important treatment for hyperkinetic movement disorders.

For more information, consult the MedlinePlus drug information page on deutetrabenazine.

Frequently Asked Questions

The primary drug class of deutetrabenazine is a vesicular monoamine transporter 2 (VMAT2) inhibitor.

It works by inhibiting VMAT2, which transports monoamine neurotransmitters (like dopamine) into storage vesicles. This depletion of monoamines helps reduce abnormal involuntary movements.

Deutetrabenazine is a deuterated version of tetrabenazine, leading to slower metabolism, a longer duration of action, less frequent dosing, and potentially fewer side effects.

Deutetrabenazine is used to treat chorea associated with Huntington's disease and involuntary movements from tardive dyskinesia.

Yes, serious side effects can include an increased risk of depression and suicidal ideation, parkinsonism, and neuroleptic malignant syndrome.

The brand names for deutetrabenazine are Austedo and Austedo XR.

Deutetrabenazine can have serious interactions with other drugs and should not be taken with MAOIs or reserpine. Caution is needed with strong CYP2D6 inhibitors or other medications causing drowsiness.

No, deutetrabenazine only treats the chorea associated with Huntington's disease. It does not cure or halt the disease progression.

References

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Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.