Esketamine
Class: Antidepressants, Miscellaneous
- NMDA Receptor Antagonists
- N-Methyl-d-aspartate Receptor Antagonists
Chemical Name: (2S)-2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one
Molecular Formula: C13H16ClNOC13H16ClNO•HCl
CAS Number: 33643-46-8
Brands: Spravato
Warning
- Sedation
May cause sedation following administration. Administer only in a registered healthcare setting. (See Restricted Distribution Program under Dosage and Administration.)
Monitor patients for ≥2 hours after administration, then assess whether patient is considered clinically stable and ready to leave the healthcare setting. (See Sedation under Cautions.)
- Dissociation
May cause dissociative or perceptual changes following administration. Administer only in a registered healthcare setting. (See Restricted Distribution Program under Dosage and Administration.)
Monitor patients for ≥2 hours after administration, then assess whether patient is considered clinically stable and ready to leave the healthcare setting. (See Dissociation under Cautions.)
- Abuse and Misuse
Potential for abuse and misuse.
Consider risks and benefits of prescribing esketamine prior to use in patients at higher risk of abuse. Monitor patients for signs and symptoms of abuse and misuse. (See Abuse and Misuse under Cautions.)
- Suicidality
Antidepressants increased risk of suicidal thinking and behavior (suicidality) compared with placebo in pediatric and young adult patients in short-term studies. Esketamine is not labeled for use in pediatric patients. (See Pediatric Use under Cautions.)
Closely monitor all patients receiving antidepressants for clinical worsening and for emergence of suicidality. (See Suicidality under Cautions.)
Risk Evaluation and Mitigation Strategy (REMS):
FDA approved a REMS for esketamine to ensure that the benefits outweigh the risks. The REMS may apply to one or more preparations of esketamine and consists of the following: elements to assure safe use and implementation system. See https://www.accessdata.fda.gov/scripts/cder/rems/.
Introduction
Antidepressant; N-methyl-d-aspartate (NMDA) receptor antagonist and S-enantiomer of racemic ketamine.
Uses for Esketamine
Treatment-resistant Depression
Used intranasally for treatment (in combination with an oral antidepressant) of treatment-resistant depression. Although there are various definitions of treatment-resistant depression, the condition is often defined as the failure of ≥2 trials of first-line antidepressants given in an adequate dosage for an adequate duration of therapy.
Intranasal esketamine substantially improved depressive symptoms as measured by the Montgomery-Asberg Depression Rating Scale (MADRS) within 24 hours of administration in a short-term clinica