Esketamine

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Medication used for treatment-resistant depression

Esketamine
INN
Drug class
Routes of administration	Nasal spray
Pregnancy category
Bioavailability
Metabolism	Liver (CYP2B6, CYP3A4)
Elimination half-life	7-12 hours
Excretion	Urine
Legal status
CAS Number	33643-46-8
PubChem	123631
DrugBank	DB01221
ChemSpider	110146
KEGG	D09373

Esketamine, sold under the brand name Spravato, is a medication used for the treatment of treatment-resistant depression (TRD). It is a stereoisomer of ketamine, specifically the S(+) enantiomer. Esketamine is administered as a nasal spray and works as a NMDA receptor antagonist.

Medical uses

Esketamine is primarily used for treatment-resistant depression in adults who have not responded adequately to at least two different antidepressant treatments. It is often used in conjunction with an oral antidepressant.

Mechanism of action

Esketamine acts as a NMDA receptor antagonist, which is believed to contribute to its rapid antidepressant effects. By blocking the NMDA receptor, esketamine increases the levels of glutamate in the brain, which in turn activates AMPA receptors and leads to the release of brain-derived neurotrophic factor (BDNF). This cascade of events is thought to contribute to the synaptic plasticity and antidepressant effects observed with esketamine.

Side effects

Common side effects of esketamine include dissociation, dizziness, nausea, sedation, vertigo, and increased blood pressure. Due to its potential for abuse and dissociative effects, esketamine is classified as a Schedule III controlled substance in the United States.

History

Esketamine was approved by the U.S. Food and Drug Administration (FDA) in March 2019 for the treatment of treatment-resistant depression. It was developed by Janssen Pharmaceuticals, a subsidiary of Johnson & Johnson.

Related pages

• Ketamine
• Antidepressant
• NMDA receptor antagonist
• Treatment-resistant depression
• Brain-derived neurotrophic factor