Вилазодон

Описание

In January 2011, the U.S. FDA approved vilazodone for the treatment of major depressive disorder (MDD). Vilazodone is a novel antidepressant agent that combines potent serotonin reuptake inhibition (IC₅₀=0.2 nM) with high affinity for 5-HT1A receptors (IC₅₀=0.5 nM)and partial 5-HT1A receptor agonist functional activity. Vilazodone has good selectivity over other monoamine receptors and is efficacious in preclinical models of depression in rats and mice. Vilazodone is an indolylbutylpiperazine derivative that has been prepared by coupling of an indolylbutyl chloride or tosylate with 5-(piperazin-1-yl)benzofuran-2- carboxamide or the corresponding ester. The cyanoindole portion of vilazodone is important for conferring high affinity for both the serotonin transporter and the 5-HT1A receptor. Para-substitution on the phenyl group attached to the piperidine moiety reduces affinity for dopamine receptors, while the carboxamide group provides improved pharmacokinetic properties.

Химические свойства

Light Yellow Solid

Использование

Labelled analogue of Vilazodone

Определение

ChEBI: A 1-benzofuran that is 5-(piperazin-1-yl}-1-benzofuran-2-carboxamide having a (5-cyanoindol-3-yl)butyl group attached at position N-4 on the piperazine ring. Used for the treatment of major depressive disorder.

Механизм действия

The mechanism of action of Vilazodone antidepressant is to enhance the release of serotonin from the serotonergic pathway in the brain by inhibiting the serotonin transporter (similar to a selective serotonin reuptake inhibitor (SSRI)) while stimulating the serotonin-1a receptor through partial agonism. Its agonistic effects are similar to those of the anxiolytic drug buspirone.

Побочные эффекты

The most common side effects of Vilazodone administered orally include: diarrhoea, dizziness, headache, dry mouth, nausea, vomiting, and sleep disturbances. These symptoms are mild and may disappear within a few days or weeks. Other serious side effects that may occur include: bleeding, hyponatraemia (low levels of sodium in the blood, manifested by dizziness, light-headedness, difficulty concentrating and fainting), mania, seizures (loss of consciousness, twitching of limbs), closed-angle glaucoma (sudden eye pain or loss of vision) and allergic reactions. Seek medical attention if any of these serious adverse symptoms occur.