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Pronunciation: dex-ME-de-TOE-mi-deen HYE-droe-KLOR-ide
Class: Sedative and hypnotic, nonbarbiturate
- Injection, solution, concentrate 100 mcg/mL
Relatively selective alpha-2 adrenergic agonist with sedative properties.
Pharmacokinetics are linear in the dose range of 0.2 to 0.7 mcg/kg/h.
Steady-state Vd is approximately 118 L. Following IV administration, distribution half-life is approximately 6 min. Average plasma protein binding is 94%.
Undergoes almost complete biotransformation via direct glucuronidation as well as CYP2A6.
Terminal elimination half-life is approximately 2 h. Cl is approximately 39 L/h. Excreted in the urine (95%) and feces (4%). No unchanged drug is detected in the urine.
Special PopulationsRenal Function Impairment
Pharmacokinetics not different in patients with severe renal impairment (CrCl less than 30 mL/min) compared with healthy individuals.Hepatic Function Impairment
Cl and plasma protein binding are decreased in patients with hepatic impairment. Dosage adjustment may be necessary in patients with hepatic impairment.Elderly
Pharmacokinetics are not altered by age.Children
Pharmacokinetics have not been studied in children.Gender
No difference in pharmacokinetics based on gender.
Indications and Usage
Sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care setting; sedation of nonintubated patients prior to and/or during surgical and other procedures.
Adjunct to regional anesthesia; bridge to intensive care unit (ICU) sedation and analgesia; in selected patients with CHF; supplement to regional block in patients undergoing carotid endarterectomy or during awake craniotomy; to control agitation while receiving noninvasive ventilatory support, such as mask continuous or bilevel positive airway pressure; to minimize withdrawal phenomena in critically ill patients who have received long-term benzodiazepines and opioids during their hospitalization; to reduce nausea and vomiting in children with cyclic vomiting syndrome; treatment of shivering.
None well documented.
Dosage and AdministrationInitiation of Procedural Sedation
Adults Loading dose
IV 1 mcg/kg over 10 min, including awake fiberoptic intubation patients. For less invasive procedures (eg, ophthalmic surgery), a loading dose of 0.5 mcg/kg over 10 min may be suitable.Maintenance dose
IV Start with 0.6 mcg/kg/h and titrate to achieve desired clinical effect with doses ranging from 0.2 to 1 mcg/kg/h. For awake fiberoptic intubation, a maintenance infusion of 0.7 mcg/kg/h is recommended until the endotracheal tube is secured.ICU Sedation
Adults Loading dose
IV Up to 1 mcg/kg over 10 min. For patients being converted from alternate sedative therapy, a loading dose may not be required.Maintenance dose
IV 0.2 to 0.7 mcg/kg/h. Adjust rate of infusion to achieve desired level of sedation.Elderly Initiation of procedural sedation
IV Use a loading dose of 0.5 mcg/kg over 10 min. Consider a dose reduction for the maintenance dose.ICU sedation
IV Consider a dose reduction.Hepatic function impairment
IV Consider a dose reduction.
- Administer by continuous IV infusion not exceeding 24 h.
- Administer using a controlled infusion devise.
- Preparation of solution is the same for loading and maintenance doses. Dilute with sodium chloride 0.9% to achieve required concentration (4 mcg/mL) prior to administration.
- Withdraw 2 mL of dexmedetomidine and add to 48 mL of sodium chloride 0.9% injection to achieve a total volume of 50 mL. Shake gently to mix.
- Do not administer through the same IV catheter with blood or plasma.
- Incompatible with amphotericin B and diazepam.
- Use administration components made with synthetic or coated natural rubber gaskets.
Store between 59° and 86°F.
Drug InteractionsAnesthetics, hypnotics, opioids, sedatives
Additive effects are anticipated. When coadministered with dexmedetomidine, a reduction in dosage of dexmedetomidine or the concomitant anesthetic, sedative, hypnotic, or opioid may be required.
Hypotension (56%); bradycardia (42%); hypotension requiring intervention, systolic hypertension (28%); tachycardia (25%); hypertension requiring intervention (19%); hypertension (16%); diastolic hypertension (12%); tachycardia requiring intervention (10%); bradycardia requiring intervention (5%); atrial fibrillation (4%); arrhythmia, AV block, BP fluctuations, cardiac arrest, extrasystoles, heart block, heart disorder, MI, supraventricular tachycardia, T-wave inversion, ventricular arrhythmia, ventricular tachycardia (postmarketing).
Agitation (8%); anxiety (5%); confusion, convulsion, delirium, dizziness, hallucination, headache, illusion, neuralgia, neuritis, speech disorder (postmarketing).
Increased sweating (postmarketing).
Abnormal vision, photopsia (postmarketing).
Nausea (11%); constipation (6%); dry mouth (4%); abdominal pain, diarrhea (postmarketing).
Acute renal failure, oliguria (2%); decreased urine output (1%); increased BUN (postmarketing).
Abnormal hepatic function, hyperbilirubinemia, increased ALT, increased AST, increased GGT (postmarketing).
Hypokalemia (9%); hyperglycemia (7%); hypoglycemia, peripheral edema (5%); hypovolemia (3%); thirst (2%); hypocalcemia, hypomagnesemia (1%); acidosis, hyperkalemia, increased alkaline phosphatase (postmarketing).
Respiratory depression (37%); respiratory failure (6%); acute respiratory distress syndrome (3%); pleural effusion (2%); wheezing (1%); apnea, bronchospasm, dyspnea, hypercapnia, hypoventilation, hypoxia, pulmonary congestion, respiratory acidosis (postmarketing).
Pyrexia (7%); generalized edema (2%); hemorrhage, hyperpyrexia, light anesthesia, pain, rigors (postmarketing).
Continuously monitor patients because of known pharmacologic effects.
Category C .
Safety and efficacy have not been established.
Increased incidence of bradycardia and hypotension in elderly patients. Consider a dosage reduction.
Consider dosage reduction in patients with impaired hepatic function.
Some patients may be arousable and alert when stimulated. Do not consider this alone to be evidence of lack of efficacy.
Bradycardia, hypotension, sinus arrest
Have been reported in patients with high vagal tone or with different routes of administration, including rapid IV or bolus administration. Bradycardia and/or hypotension may be more pronounced in elderly patients or in patients with chronic hypertension, diabetes mellitus, or hypovolemia. Administer with caution to patients with advanced heart block and/or severe ventricular dysfunction.
Has been associated with use beyond 24 h.
May occur in association with peripheral vasoconstriction, primarily during the loading dose.
Withdrawal symptoms, including agitation, hypertension, nausea, tachycardia, and vomiting, may occur up to 48 h after discontinuation of dexmedetomidine.
Bradycardia, cardiac arrest, first-degree AV block, hypotension, second-degree heart block.
- Instruct patients who receive an infusion for more than 6 h to report agitation, headache, and nervousness to health care provider. These symptoms may occur for up to 48 h after infusion.
- Instruct patients to report the following symptoms to health care provider, which may occur within 48 h of administration: abdominal pain, confusion, constipation, diarrhea, dizziness or light-headedness, excessive sweating, salt cravings, weakness, or weight loss.
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