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dexmedetomidine (Precedex)

 

Classes: Sedatives

Dosing and uses of Precedex (dexmedetomidine)

 

Adult dosage forms and strengths

injectable solution

  • 100mcg/mL

 

ICU Sedation

Load: 1 mcg/kg IV over 10 minutes

Maintenance 0.2-1.4 mcg/kg/hr IV

Titrate less frequently than q30min to prevent hypotension

 

Fiberoptic Intubation

Load: 1 mcg/kg IV over 10 minutes

Maintenance 0.7 mcg/kg/hr IV

 

Procedural Sedation

Load: 1 mcg/kg IV over 10 minutes

Maintenance 0.6 mcg/kg/hr IV titrate to effect (usually 0.2-1 mcg/kg/hr)

Titrate less frequently than q30min to prevent hypotension

 

Renal Impairment

Dose reduction may be required

 

Hepatic Impairment

Dose reduction may be required

 

Pediatric dosage forms and strengths

Safety and efficacy not established

 

Geriatric dosage forms and strengths

Load: 0.5 mcg/kg IV over 10 minutes

 

Precedex (dexmedetomidine) adverse (side) effects

>10%

Hypotension (28%)

 

1-10%

AFiB

Anemia

Bradycardia

Fever

Pleural effusion

Leukocytosis

Pulmonary edema

 

Postmarketing Reports

Electrocardiogram QT prolonged

Hypernatremia

Polyuria

 

Warnings

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

Potential withdrawal symptoms if abruptly withdrawn after >24 hr use

 

Pregnancy and lactation

Pregnancy category: C

Lactation: Excretion in milk unknown; use with caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Precedex (dexmedetomidine)

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%)

 

Administration

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