Last reviewed 2026-04-23 · How we verify

Midazolam Nasal Spray

Midazolam is a benzodiazepine that enhances inhibitory GABA neurotransmission in the central nervous system to produce sedation and anxiolysis.

Midazolam is a benzodiazepine that enhances inhibitory GABA neurotransmission in the central nervous system to produce sedation and anxiolysis. Used for Acute seizure management or seizure cluster treatment, Pre-procedural sedation and anxiolysis.

At a glance

Mechanism of action

Midazolam binds to GABA-A receptors on neurons, potentiating the effect of the inhibitory neurotransmitter GABA. This increases chloride ion influx, hyperpolarizes neurons, and reduces neuronal excitability. The nasal spray formulation provides rapid onset of action suitable for acute sedation or anxiety management in clinical settings.

Approved indications

• Acute seizure management or seizure cluster treatment
• Pre-procedural sedation and anxiolysis

Common side effects

• Sedation / drowsiness
• Headache
• Nasal irritation
• Dizziness
• Respiratory depression

Key clinical trials

• Administration of Intranasal Midazolam for Anxiety in Palliative Care (PHASE2)
• Anxiolysis for Laceration Repair in Children (PHASE3)
• Non-anesthesiologist-administered Propofol During the Flexible Bronchoscopy (NA)
• A Single-centre Study of Entonox Versus Midazolam Sedation in Gastroscopy (PHASE4)
• Intranasal vs Buccal vs Intramuscular Midazolam for the Home and Emergency Treatment of Acute Seizures (PHASE4)
• Microbial Colonization in Lung Cancer Patients
• Buccal Versus Intranasal Route of Administration of Midazolam Spray in Behavior Management of Pre-School Patients (PHASE2)
• Study to Evaluate the Safety and Efficacy of USL261 (Intranasal Midazolam) in Patients With Seizure Clusters (PHASE3)

Primary sources

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