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Nature 452 , 633637 (2008)

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Indications: Huntington's Chorea (a hyperkinetic movement disorder) A drug of first choice for this condition Side Effects: Sedation Depression (suicidal tendencies) Parkinsonism symptoms Lacks the hypotensive & GI side effects of reserpine due to its selectivity for central VMAT2 Pharmacokinetics: * undergoes rapid hepatic metabolism involving carbonyl reductase and CYP2D6 to 2 active metabolites -dihydrotetrabenazine (-HTBZ) and -dihydrotetrabenazine (-HTBZ), with eventual renal elimination of metabolites the -HTBZ and -HTBZ metabolites are primarily responsible for the pharmacological & therapeutic effects produced by the parent prodrug Readily crosses the blood brain barrier & depletes cerebral monoamine stores