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NERVOUS SYSTEM › PSYCHOLEPTICS › HYPNOTICS AND SEDATIVES › Other hypnotics and sedatives
dexmedetomidine
N05CM18
Forms & Strengths
- Intravenous injection: 100 mcg/mL in 2 mL, 50 mL, and 100 mL vials
- Intravenous premix: 200 mcg in 50 mL (4 mcg/mL) and 400 mcg in 100 mL (4 mcg/mL) 0.9% NaCl
- Sublingual film: 100 mcg, 180 mcg
Adult Dosing
- Procedural sedation: Loading infusion 1 mcg/kg over 10 minutes, followed by maintenance infusion titrated to 0.6 mcg/kg/hour (range 0.2-1 mcg/kg/hour)
- Intensive care unit sedation: Loading infusion 1 mcg/kg over 10 minutes (optional), followed by maintenance infusion 0.2 to 1.4 mcg/kg/hour
- Sublingual film (Agitation in schizophrenia/bipolar): 180 mcg sublingually, may repeat 90 mcg after 2 hours if needed
Pediatric Dosing
- ICU sedation (Off-label): Loading infusion 0.5-1 mcg/kg over 10-20 minutes, followed by maintenance 0.2-1 mcg/kg/hour
- Safety and efficacy in pediatric patients under 18 years have not been established for FDA-approved indications
Indications
- Sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care setting
- Sedation of non-intubated patients prior to and/or during surgical and other procedures
- Treatment of acute agitation associated with schizophrenia or bipolar disorder (sublingual film)
Mechanism of Action
- Selective alpha-2 adrenergic receptor agonist with sympatholytic and sedative properties
- Stimulation of alpha-2 receptors in the brainstem (locus coeruleus) inhibits neuronal firing, inducing a state resembling natural sleep
- Provides analgesia and reduces anesthetic and opioid requirements via spinal and supraspinal alpha-2 receptor activity
Contraindications
- Hypersensitivity to dexmedetomidine or any component of the formulation
- Severe hepatic impairment (for sublingual film formulations)
Adverse Reactions
- Hypotension
- Bradycardia
- Dry mouth
- Hypertension (typically during initial loading dose)
- Nausea
- Tachycardia
- Respiratory depression (mild to moderate)
Drug Interactions
- Anesthetics, sedatives, hypnotics, and opioids: Potentiation of central nervous system depression, hypotension, and bradycardia
- Inhibitors and inducers of CYP2A6: Potential for altered clearance of dexmedetomidine
- Drugs that decrease heart rate (e.g., beta-blockers, non-dihydropyridine calcium channel blockers): Risk of additive bradycardia and heart block
Curated Content: Needs Vetting Before Put to Clinical Use