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NERVOUS SYSTEM › PSYCHOLEPTICS › HYPNOTICS AND SEDATIVES › Benzodiazepine derivatives
remimazolam
N05CD14
Forms & Strengths
- IV solution 1 mg/mL in single‑use vial
- Powder for reconstitution to 5 mg/mL
Adult Dosing
- Procedural sedation: 5 mg IV bolus over ≤60 s, then 1 mg/min infusion titrated to effect
- Induction of GA: 0.2 mg/kg IV bolus (max 12 mg), followed by 0.1–0.2 mg/kg/h infusion
- Maintenance GA: 0.05–0.1 mg/kg/h infusion as needed
- ICU sedation: start 0.025–0.05 mg/kg/h, titrate to RASS −2 to 0
Pediatric Dosing
- Not FDA‑approved; limited data: 0.1–0.2 mg/kg IV bolus for sedation, then 0.05–0.2 mg/kg/h infusion
- Maximum single dose 0.3 mg/kg recommended in studies up to 40 kg
Indications
- Procedural sedation for endoscopy, bronchoscopy, interventional radiology
- Induction and maintenance of general anesthesia for short‑duration surgery
- Sedation of mechanically ventilated adults in ICU
Mechanism of Action
- Positive allosteric modulator at the benzodiazepine site of the GABA_A receptor
- Enhances GABA‑mediated chloride influx → neuronal hyperpolarisation
- Rapid hydrolysis by tissue carboxylesterases to inactive metabolite CNS7054
Contraindications
- Known hypersensitivity to remimazolam or other benzodiazepines
- Severe acute narrow‑angle glaucoma (relative)
- Patients with significant respiratory depression without airway support
Adverse Reactions
- Dose‑related hypotension
- Respiratory depression, apnea
- Bradycardia
- Nausea/vomiting
- Injection‑site pain
- Paradoxical agitation
- Dizziness, headache
Drug Interactions
- Additive CNS depression with opioids, alcohol, barbiturates, other GABAergic agents
- Flumazenil reverses sedation; may precipitate withdrawal
- CYP3A4 inhibitors (ketoconazole, clarithromycin) can increase exposure
- CYP3A4 inducers (rifampin, carbamazepine) may reduce effect
Curated Content: Needs Vetting Before Put to Clinical Use