Last reviewed 2026-04-22 · How we verify

CI-581a

CI-581a is a dissociative anesthetic that acts as an NMDA receptor antagonist to produce rapid-onset anesthesia and analgesia.

CI-581a is a dissociative anesthetic that acts as an NMDA receptor antagonist to produce rapid-onset anesthesia and analgesia. Used for Induction and maintenance of anesthesia, Analgesia and sedation.

At a glance

Mechanism of action

CI-581a (ketamine) blocks N-methyl-D-aspartate (NMDA) glutamate receptors, leading to dissociative anesthesia characterized by analgesia, amnesia, and unconsciousness while preserving airway reflexes and respiratory drive. The drug produces its effects through non-competitive antagonism at the phencyclidine binding site within the NMDA receptor ion channel.

Approved indications

• Induction and maintenance of anesthesia
• Analgesia and sedation

Common side effects

• Dissociative/psychotomimetic effects
• Emergence reactions
• Hypertension
• Tachycardia
• Nausea/vomiting

Key clinical trials

• Glutamatergic Modulation as a Treatment for Depressive Symptoms Among Patients With Post-acute Sequelae of COVID (PASC): A Pilot Trial (PHASE2)
• Glutamatergic Modulation to Facilitate the Behavioral Treatment of Cocaine Use Disorders (PHASE3)
• Facilitating Rapid Naltrexone Initiation (PHASE3)
• The Role of Brief Potent Glutamatergic Modulation in Addressing Problem Drinking (PHASE2)
• Facilitating the Behavioral Treatment of Cannabis Use Disorder (PHASE1)
• Glutamatergic Modulation of Disordered Alcohol Use (PHASE2, PHASE3)
• The Effect of Glutamatergic Modulation on Cocaine Self-administration (PHASE2)

Primary sources

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