Esketamine: Difference between revisions
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Expand Esketamine with Stahl-sourced detail (with skepticism) |
Terminology sweep: drug/medication → medicine |
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| pregnancy = Avoid; may cause fetal harm | | pregnancy = Avoid; may cause fetal harm | ||
| legal = Rx, Schedule III (US). REMS program required. | | legal = Rx, Schedule III (US). REMS program required. | ||
| intro = '''Esketamine''' (brand name Spravato) is the S-enantiomer of ketamine, FDA-approved as an intranasal | | intro = '''Esketamine''' (brand name Spravato) is the S-enantiomer of ketamine, FDA-approved as an intranasal medicine for treatment-resistant depression (March 2019) and for major depression with acute suicidal ideation or behavior (August 2020). The S-enantiomer has approximately 4-fold higher NMDA receptor affinity than the R-enantiomer; Spravato delivers it via a nasal spray under direct medical supervision in a REMS-certified setting due to risks of dissociation, sedation, and abuse. | ||
Mechanism: uncompetitive NMDA receptor antagonism on GABA interneurons disinhibits glutamatergic output, leading to AMPA receptor activation, BDNF/VEGF release, and rapid synaptogenesis through mTOR pathway activation. Antidepressant onset within hours is striking compared to monoaminergic antidepressants (4-6 weeks). Patients must be monitored ≥2 hours after dose due to dissociation, sedation, and blood pressure elevation. | Mechanism: uncompetitive NMDA receptor antagonism on GABA interneurons disinhibits glutamatergic output, leading to AMPA receptor activation, BDNF/VEGF release, and rapid synaptogenesis through mTOR pathway activation. Antidepressant onset within hours is striking compared to monoaminergic antidepressants (4-6 weeks). Patients must be monitored ≥2 hours after dose due to dissociation, sedation, and blood pressure elevation. | ||