dexmedetomidine (Rx)

>10%

Hypotension (28%)

1-10%

AFib

Anemia

Bradycardia

Fever

Pleural effusion

Leukocytosis

Pulmonary edema

Postmarketing Reports

Electrocardiogram QT prolonged

Hypernatremia

Polyuria

Acute renal failure

Respiratory distress syndrome

Respiratory failure

Contraindications

Hypersensitivity

Cautions

Continuously monitor patients while on therapy; therapy should be administered only by persons skilled in the management of patients in the intensive care or operating room setting

Bradycardia and sinus arrest have occurred in young healthy volunteers with high vagal tone or with different routes of administration, including rapid intravenous or bolus administration

Transient hypertension reported primarily during loading dose; consider reduction in loading infusion rate

Patients can become aroused/alert with stimulation; this alone should not be considered as lack of efficacy

Prolonged exposure to dexmedetomidine beyond 24 hours may be associated with tolerance and tachyphylaxis and a dose-related increase in adverse events (eg, ARDS, respiratory failure, agitation)

Use with caution in hepatic impairment; consider dose reduction

Hypotension and bradycardia may necessitate medical intervention; may be more pronounced in patients with hypovolemia, diabetes mellitus, or chronic hypertension, and in the elderly; use with caution in patients with advanced heart block or severe ventricular dysfunction

Use with caution with concomitant administration of other vasodilators or negative chronotropic agents; use with caution due to additive pharmacodynamic effects

Withdrawal symptoms after discontinuation reported when administered for longer than 6 hr; most common events reported include nausea, vomiting, and agitation

In adult subjects, tachycardia and hypertension reported, requiring intervention 48 hr following study drug discontinuation; if tachycardia and/or hypertension occurs after discontinuation, supportive therapy is indicated

Mechanism of Action

Centrally acting alpha2-adrenoceptor agonist that has sedative and anesthetic properties possibly by activating G-proteins in the brainstem, which results in the inhibition of norepinephrine release

Pharmacokinetics

Half-life, elimination: 6 min; 2 hr (terminal)

Peak plasma: 0.3-1.5 ng/mL

Protein bound: 94%

Vd: 118 L

Metabolism: Liver, including glucuronidation and CYP2A6

Metabolites: 3-hydroxy, 3-carboxy, 3-hydroxy N-methyl, 3-carboxy N-methyl, and N-methyl O-glucuronide dexmedetomidine

Total body clearance: 39 L/hr

Excretion: Urine (95%); feces (4%)

IV Incompatibilities

Y-site: ampho B, diazepam

IV Compatibilities

Solution: D5W, LR, NS, mannitol 20%

Y-site (partial list): amiodarone, cefepime, cefoperazone, ceftriaxone, chlorpromazine, ciprofloxacin, clindamycin, digoxin, diphenhydramine, dobutamine, dopamine, epinephrine, fluconazole, furosemide, heparin, hydroxyzine, labetalol, lidocaine, linezolid, lorazepam, meperidine, metoclopramide, MgSO4, metronidazole, KCl, nitroglycein, prochlorperazine, promethazine, NaHCO3, Na-nitroprusside, TMP-SMX, vancomycin, verapamil

Not Spec: atracurium, atropine, etomidate, fentanyl, glycopyrrolate, midazolam, mivacurium, morphine, pancuronium, phenylephrine, succinylcholine, thiopental, vecuronium

IV Preparation

Dilute in NS

IV Administration

Use controlled infusion device; use components made with synthetic or coated natural rubber gaskets

Infuse loading dose over 10 min