Alpha-Adrenergic Blockers - Central-Acting (Alpha₂-Agonists); Sedative, Miscellaneous

Sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care setting; duration of infusion should not exceed 24 hours

C

Caution should be exercised when administered to a nursing woman

Hypersensitivity to dexmedetomidine or any component; use outside of an intensive care setting

Should be administered only by persons skilled in management of patients in intensive care setting. Patients should be continuously monitored. Episodes of bradycardia and sinus arrest have been associated with dexmedetomidine. Reports of hypotension and bradycardia have been associated with dexmedetomidine infusion. If medical intervention is required, treatment may include stopping or decreasing the infusion; increasing the rate of I.V. fluid administration, use of pressor agents, and elevation of the lower extremities. Transient hypertension has been primarily observed during the dose in association with the initial peripheral vasoconstrictive effects of dexmedetomidine. Treatment of this is not generally necessary; however, reduction of infusion rate may be desirable.

>10%:

Cardiovascular: Hypotension (30%)

Gastrointestinal: Nausea (11%)

1% to 10%:

Cardiovascular: Bradycardia (8%), atrial fibrillation (7%)

Central nervous system: Pain (3%)

Hematologic: Anemia (3%), leukocytosis (2%)

Renal: Oliguria (2%)

Respiratory: Hypoxia (6%), pulmonary edema (2%), pleural effusion (3%)

Miscellaneous: Infection (2%), thirst (2%)

In reports of overdosages where the blood concentration was 13 times the upper boundary of the therapeutic range, first degree A-V block and second degree heart block occurred. No hemodynamic compromise was noted with the A-V block and the heart block resolved spontaneously within one minute. Two patients who received a 2 mcg/kg loading dose over 10 minutes experienced bradycardia and/or hypotension. One patient who received a loading dose of undiluted dexmedetomidine (19.4 mcg/kg) had cardiac arrest and was successfully resuscitated.

CYP2A6 enzyme substrate

Compatible with lactated Ringer's, 5% dextrose in water, 0.9% sodium chloride in water, 20% mannitol, thiopental, etomidate, vecuronium, pancuronium, succinylcholine, atracurium, mivacurium, glycopyrrolate, phenylephrine, atropine, midazolam, morphine, fentanyl, and a plasma substitute

Selective alpha₂-adrenoceptor agonist with sedative properties; alpha₁ activity was observed at high doses or after rapid infusions

Onset of action: Rapid

Distribution: V_ss: Approximately 118 L; rapid

Protein binding: 94%

Metabolism: Undergoes complete biotransformation which involves both direct glucuronidation, as well as cytochrome P-450-mediated metabolism

Half-life: 6 minutes; terminal: 2 hours

Elimination: 95% in urine and 4% in feces

Individualized and titrated to desired clinical effect

Dosage adjustment in renal/hepatic impairment: Dosage reduction may need to be considered

Administer using a controlled infusion device

Level of sedation, heart rate, respiration, rhythm

No information available to require special precautions

No effects or complications reported

Must be diluted in 0.9% sodium chloride solution to achieve the required concentration prior to administration. Advisable to use administration components made with synthetic or coated natural rubber gaskets. Parenteral products should be inspected visually for particulate matter and discoloration prior to administration.

Injection, 100 mcg/mL (2 mL vial, 2 mL ampul)