QuickView for Tetrabenazine (compound)

Summary
General Info

PubChem

PubChem Compound 11634155

Name:	Tetrabenazine
PubChem Compound ID:	11634155
Description:	A drug formerly used as an antipsychotic and treatment of various movement disorders. Tetrabenazine blocks neurotransmitter uptake into adrenergic storage vesicles and has been used as a high affinity label for the vesicle transport system.
Molecular formula:	C₁₉H₂₇NO₃
Molecular weight:	317.423 g/mol

DrugBank

Identification

Name:	Tetrabenazine
Name (isomeric):	DB04844
Drug Type:	small molecule
Description:	A drug formerly used as an antipsychotic and treatment of various movement disorders. Tetrabenazine blocks neurotransmitter uptake into adrenergic storage vesicles and has been used as a high affinity label for the vesicle transport system.
Synonyms:	Tetrabenzine; Tetrabenazina [inn-spanish]; Tetrabenzaine; Tetra benazin; Tetrabenazinum [inn-latin]
Brand:	Regulin, Nitoman, Xenazine, Rubigen
Category:	Adrenergic Uptake Inhibitors
CAS number:	58-46-8

Pharmacology

Indication:	For the symptomatical treatment of hyperkinetic movement disorder.
Mechanism of Action:	Tetrabenazine works mainly as a VMAT-inhibitor and as such promotes the early metabolic degradation of the neurotransmitter dopamine. Dopamine is required for fine motor movement, so the inhibition of its transmission can lessen the effects of any hyperkinetic movement.
Protein binding:	82-85%
Biotransformation:	CYP2D6 mediated hepatic metabolism.
Route of elimination:	After oral administration, tetrabenazine is extensively hepatically metabolized, and the metabolites are primarily renally eliminated. In a mass balance study in 6 healthy volunteers, approximately 75% of the dose was excreted in the urine and fecal recovery accounted for approximately 7-16% of the dose. Urinary excretion of α-HTBZ or β-HTBZ (the major metabolites)accounted for less than 10% of the administered dose.
Clearance:	Tetrabenazine is cleared renally and fecally.
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

Haloperidol	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Droperidol	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Furazolidone	Tetrabenazine may increase the adverse/toxic effects of Furazolidine. Concomitant therapy is contraindicated.
Cocaine	CYP2D6 Inhibitors (Strong) such as cocaine may increase the serum concentration of tetrabenazine. Specifically, concentrations of the active alpha- and beta-dihydrotetrabenazine metabolites may be increased. Patients receiving a strong inhibitor of CYP2D6 together with tetrabenazine should not exceed 50mg of tetrabenazine. Also, patients already taking tetrabenazine prior to starting a strong CYP2D6 inhibitor should have their tetrabenazine dose reduced by 50% upon initiation of the strong CYP2D6 inhibitor.
Phenelzine	Tetrabenazine may increase the adverse/toxic effects of Phenelzine. Concomitant therapy is contraindicated.

Haloperidol	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Droperidol	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Furazolidone	Tetrabenazine may increase the adverse/toxic effects of Furazolidine. Concomitant therapy is contraindicated.
Cocaine	CYP2D6 Inhibitors (Strong) such as cocaine may increase the serum concentration of tetrabenazine. Specifically, concentrations of the active alpha- and beta-dihydrotetrabenazine metabolites may be increased. Patients receiving a strong inhibitor of CYP2D6 together with tetrabenazine should not exceed 50mg of tetrabenazine. Also, patients already taking tetrabenazine prior to starting a strong CYP2D6 inhibitor should have their tetrabenazine dose reduced by 50% upon initiation of the strong CYP2D6 inhibitor.
Phenelzine	Tetrabenazine may increase the adverse/toxic effects of Phenelzine. Concomitant therapy is contraindicated.
Telithromycin	Telithromycin may increase the QTc-prolonging effect of Tetrabenazine. Concomitant therapy should be avoided.
Prochlorperazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Rasagiline	Tetrabenazine may increase the adverse/toxic effects of Rasagiline. Concomitant therapy is contraindicated.
Flupenthixol	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Linezolid	Tetrabenazine may increase the adverse/toxic effects of Linezolid. Concomitant therapy is contraindicated.
Toremifene	May cause additive QTc-prolonging effects. Concomitant therapy is contraindicated.
Lumefantrine	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Trimipramine	May cause additive QTc-prolonging effects. Concomitant therapy should be avoided.
Chlorpromazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Procarbazine	Tetrabenazine may increase the adverse/toxic effects of Procarbazine. Concomitant therapy is contraindicated.
Pimozide	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Selegiline	Tetrabenazine may increase the adverse/toxic effects of Selegiline. Concomitant therapy is contraindicated.
Molindone	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Clozapine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Mesoridazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Zuclopenthixol	Additive QTc prolongation may occur. QTc prolongation can lead to Torsade de Pointes (TdP). Concomitant therapy should be avoided.
Ziprasidone	Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
Quetiapine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Olanzapine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Thiothixene	Additive QTc prolongation may occur. QTc prolongation can lead to Torsade de Pointes (TdP). Concomitant therapy should be avoided.
Moclobemide	Tetrabenazine may increase the adverse/toxic effects of Moclobemide. Concomitant therapy is contraindicated.
Acetophenazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Paliperidone	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Aripiprazole	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Reserpine	Reserpine may increase the adverse/toxic effects of Tetrabenazine. Concomitant therapy is contraindicated.
Tranylcypromine	Tetrabenazine may increase the adverse/toxic effects of Tranylcypromine. Concomitant therapy is contraindicated.
Thioridazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Trifluoperazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Tacrolimus	May cause additive QTc-prolonging effects. Concomitant therapy should be avoided.
Vorinostat	Additive QTc prolongation may occur. Concomitant therapy should be avoided.
Loxapine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Triprolidine	The CNS depressants, Triprolidine and Tetrabenazine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Isocarboxazid	Tetrabenazine may increase the adverse/toxic effects of Isocarboxazid. Concomitant therapy is contraindicated.
Fluphenazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Artemether	Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Levodopa	Tetrabenazine may cause Parkinsonian symptoms and neutralize the effect of Levodopa.
Risperidone	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Perphenazine	May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
Terbinafine	Terbinafine may reduce the metabolism and clearance of Tetrabenazine. Consider alternate therapy or monitor for therapeutic/adverse effects of Tetrabenazine if Terbinafine is initiated, discontinued or dose changed.
Voriconazole	Additive QTc prolongation may occur. Concomitant therapy should be avoided.

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Targets

Synaptic vesicular amine transporter

Enzymes

Cytochrome P450 2D6