Tetrabenazine

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Generic Name of Tetrabenazine - Learn More

Tetrabenazine

Tetrabenazine Precaution - What You Need to Know

Before starting Tetrabenazine, it is essential to consult with a healthcare provider, especially in the presence of the following conditions:

- Neuropsychiatric Disorders: Tetrabenazine can exacerbate symptoms of depression, anxiety, or suicidal thoughts. Patients with a history of depression, mood disorders, or suicidal behavior should be closely monitored. Tetrabenazine may increase the risk of depression and suicidal ideation, particularly in those with pre-existing psychiatric conditions.
- Hepatic Impairment: Caution is needed in patients with liver disease, as Tetrabenazine is metabolized by the liver. Dose adjustments may be necessary for patients with mild to moderate hepatic impairment. Severe liver dysfunction is a contraindication for using the drug.
- Cardiovascular Conditions: Tetrabenazine can cause orthostatic hypotension, QT prolongation, and other cardiovascular side effects. Patients with a history of heart disease, arrhythmias, or low blood pressure should use this medication with caution.
- Parkinson’s Disease: Caution is needed when using Tetrabenazine in patients with Parkinson’s disease due to the risk of worsening motor symptoms.
- Pregnancy and Breastfeeding: Tetrabenazine is classified as Category C during pregnancy, meaning its use should only be considered if the benefits outweigh the risks. It is unknown whether Tetrabenazine is excreted in breast milk, so breastfeeding mothers should consult their healthcare provider before using this medication.

Tetrabenazine Indication - Uses and Benefits

Tetrabenazine is primarily indicated for the treatment of hyperkinetic movement disorders, particularly:

- Huntington’s Disease: Tetrabenazine is approved for the treatment of chorea (involuntary movements) associated with Huntington’s disease. It helps reduce the severity and frequency of these uncontrolled movements, improving the quality of life.
- Tardive Dyskinesia: Tetrabenazine is used to manage tardive dyskinesia, a condition characterized by involuntary, repetitive movements, often caused by prolonged use of antipsychotic medications.
- Tourette Syndrome: Tetrabenazine may be prescribed off-label for Tourette syndrome to help manage motor and vocal tics that are severe and impair the patient’s functioning.

Tetrabenazine Contraindications - Important Warnings

Tetrabenazine should not be used in the following situations:

- Hypersensitivity: Tetrabenazine is contraindicated in patients with a known hypersensitivity to the drug or any of its components.
- Severe Hepatic Impairment: Patients with severe liver dysfunction should not use Tetrabenazine, as it is metabolized by the liver and can cause toxicity in such individuals.
- Concurrent Use with Monoamine Oxidase Inhibitors (MAOIs): Tetrabenazine should not be used concurrently with MAOIs, as this combination increases the risk of serotonin syndrome, a potentially life-threatening condition.
- QT Prolongation: Tetrabenazine is contraindicated in patients with a prolonged QT interval or those who are taking drugs that prolong the QT interval, as this can lead to serious cardiac arrhythmias.
- Pregnancy: Tetrabenazine should not be used during pregnancy unless absolutely necessary, as it has the potential to harm the fetus.

Tetrabenazine Side Effects - What to Expect

Common and severe side effects of Tetrabenazine include:

- Sedation and Drowsiness: One of the most common side effects is sedation and drowsiness, which can impair the patient’s ability to perform daily activities, such as driving or operating heavy machinery.
- Extrapyramidal Symptoms: Tetrabenazine can cause movement disorders, including parkinsonism, akathisia (restlessness), and dystonia (muscle spasms).
- Depression: Tetrabenazine can cause or worsen depression, and may lead to suicidal ideation or behavior in some patients, particularly those with a history of mood disorders.
- Fatigue: Patients often report feeling unusually tired or fatigued while taking Tetrabenazine.
- Parkinsonism: Long-term use may increase the risk of Parkinsonian symptoms such as bradykinesia, rigidity, and tremors.
- Weight Gain or Loss: Some patients may experience weight changes, either weight gain or loss, while using Tetrabenazine.
- QT Prolongation: Tetrabenazine can cause QT interval prolongation, increasing the risk of serious arrhythmias and requiring monitoring of cardiac function.
- Somnolence: Some patients may experience excessive sleepiness or an overwhelming desire to sleep during the day.

Tetrabenazine Pregnancy Category ID - Safety Information

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Tetrabenazine Mode of Action - How It Works

Tetrabenazine is a dopamine depletor that works by inhibiting the vesicular monoamine transporter 2 (VMAT2). By blocking VMAT2, it prevents the storage of dopamine, serotonin, norepinephrine, and histamine in nerve terminals. This leads to a depletion of dopamine in the brain, which reduces excessive dopamine activity, particularly in areas of the brain involved in movement control.

In conditions like Huntington’s disease and tardive dyskinesia, where there is overactivity of dopamine in the brain's movement control centers, Tetrabenazine helps reduce chorea (involuntary movements) and other hyperkinetic symptoms by lowering dopamine levels. It is also thought to help restore the balance of neurotransmitters involved in motor function and mood regulation.

Tetrabenazine Drug Interactions - What to Avoid

Tetrabenazine can interact with several medications and substances, potentially altering its effectiveness or increasing the risk of side effects:

- CNS Depressants: Concomitant use with CNS depressants, such as alcohol, benzodiazepines, or opioids, can increase the sedative effects of Tetrabenazine and increase the risk of sedation or respiratory depression.
- MAO Inhibitors: Tetrabenazine should not be used with monoamine oxidase inhibitors (MAOIs) due to an increased risk of serotonin syndrome. A washout period of at least 14 days should be observed between the use of Tetrabenazine and MAOIs.
- Dopamine Agonists: Caution should be exercised when using dopamine agonists such as pramipexole or ropinirole in combination with Tetrabenazine, as both drugs affect dopamine levels and may lead to motor dysfunction or other unwanted effects.
- Antipsychotics: Antipsychotic medications, especially those that block dopamine receptors, can have an additive effect with Tetrabenazine in terms of movement disorders and should be used cautiously when taken together.
- Antidepressants: Tetrabenazine may interact with antidepressants that increase serotonin (SSRIs, SNRIs) or dopamine levels, leading to serotonin syndrome or mood swings.
- Cytochrome P450 Enzyme Interactions: Tetrabenazine is metabolized by CYP2D6, and drugs that inhibit or induce this enzyme (e.g., fluoxetine, paroxetine, carbamazepine) may alter the drug’s metabolism, requiring dose adjustments.

Tetrabenazine Adult Dose - Recommended Dosage

The typical adult dosing for Tetrabenazine is as follows:

- Huntington's Disease (Chorea): The recommended starting dose is 12.5 mg daily for the first week. The dose is gradually increased by 12.5 mg per week to a maximum of 50 mg per day, depending on the patient's tolerance and clinical response.
- Tardive Dyskinesia: The starting dose is typically 12.5 mg daily, with gradual dose escalation up to 50 mg daily, as needed, based on the patient’s condition.
- Tourette Syndrome: For Tourette syndrome, the starting dose is usually 12.5 mg daily, with gradual dose adjustments up to a maximum of 50 mg daily.

Tetrabenazine Child Dose - Dosage for Children

Tetrabenazine is not typically recommended for use in children under the age of 18 years due to limited safety and efficacy data in pediatric populations. If prescribed for Tourette syndrome in children, the dosage is generally similar to adults but should be tailored based on the child’s weight and response to therapy. Always consult a pediatrician before initiating treatment for younger patients.

Tetrabenazine Renal Dose - Dosage for Kidney Conditions

Since Tetrabenazine is primarily metabolized by the liver, renal impairment does not significantly affect its clearance. However, Tetrabenazine should be used cautiously in patients with severe renal dysfunction. It is important to monitor the patient’s condition closely for any signs of excessive sedation or motor dysfunction.