Dexmedetomidine Hydrochloride

Trade Names:
Precedex
- Injection, solution 100 mcg/mL

Pharmacology

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Relatively selective alpha-2 adrenergic agonist with sedative properties.

Pharmacokinetics

Absorption

Following IV administration, distribution half-life is approximately 6 min. Pharmacokinetics are linear in the dose range of 0.2 to 0.7 mcg/kg/h. Average plasma protein binding is 94%.

Distribution

Steady-state Vd is approximately 118 L.

Metabolism

Undergoes almost complete biotransformation via direct glucuronidation as well as CYP2A6.

Elimination

Terminal elimination half-life is approximately 2 h. Cl is approximately 39 L/h. No unchanged drug is detected in the urine.

Special Populations

Pharmacokinetics not different in patients with severe renal function impairment (CrCl less than 30 mL/min) compared with healthy individuals.

Cl and plasma protein binding are decreased in patients with hepatic function impairment. Dosage adjustment may be necessary in patients with hepatic function impairment.

Pharmacokinetics not altered by age.

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.

Unlabeled Uses

Treatment of shivering; adjunct to regional anesthesia; bridge to intensive care unit sedation and analgesia; supplement to regional block in patients undergoing carotid endarterectomy or during awake craniotomy; in selected patients with CHF; 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.

Contraindications

Standard considerations.

Dosage and Administration

IV

1 mcg/kg over 10 min, including awake fiberoptic intubation patients. For patients older than 65 yr of age and for less invasive procedures (eg, ophthalmic surgery), a loading dose of 0.5 mcg/kg over 10 min may be suitable. Consider a dose reduction in patients with impaired hepatic or renal function.

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. Adjust rate of infusion to achieve desired level of sedation. For awake fiberoptic intubation, a maintenance infusion of 0.7 mcg/kg/h is recommended until the endotracheal tube is secured. Consider dose reduction in patients older than 65 yr of age or for patients with impaired hepatic or renal function.

IV

1 mcg/kg over 10 min. Consider a dose reduction in patients older than 65 yr of age or for patients with impaired hepatic or renal function.

0.2 to 0.7 mcg/kg/h. Adjust rate of infusion to achieve desired level of sedation. Consider a dose reduction in patients older than 65 yr of age or for patients with impaired hepatic or renal function.

General Advice

• 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.
• 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.

Storage/Stability

Store at 59° to 86°F.

Drug Interactions

Additive effects are anticipated.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension (54%); bradycardia (14%); hypertension (13%); atrial fibrillation, tachycardia (5%); sinus tachycardia, ventricular tachycardia (1%); arrhythmia, AV block, BP fluctuations, cardiac arrest, extrasystoles, heart block, heart disorder, hemorrhage, hypertension, hypoxia, MI, supraventricular tachycardia, tachycardia, T-wave inversion, ventricular arrhythmia (postmarketing).

CNS

Agitation (2%); confusion, convulsion, delirium, dizziness, hallucination, headache, illusion, neuralgia, neuritis, seizures, speech disorder (postmarketing).

Dermatologic

Increased sweating (postmarketing).

EENT

Abnormal vision, photopsia (postmarketing).

GI

Nausea (9%); dry mouth (4%); abdominal pain, diarrhea, vomiting (3%).

Genitourinary

Decreased urine output (1%); increased BUN, oliguria (postmarketing).

Hematologic

Anemia (2%).

Hepatic

Abnormal hepatic function, increased ALT, increased AST, hyperbilirubinemia, increased gamma-glutamyl transpepsidase (postmarketing).

Metabolic-Nutritional

Hypovolemia (3%); hyperglycemia (2%); hypocalcemia (1%); acidosis, hyperkalemia, hypoglycemia, increased alkaline phosphatase, respiratory acidosis, thirst (postmarketing).

Respiratory

Respiratory depression (37%); atelectasis (3%); hypoxia, pleural effusion (2%); pulmonary edema, wheezing (1%); apnea, bronchospasm, dyspnea, hypercapnia, hypoventilation, hypoxia, pulmonary congestion (postmarketing).

Miscellaneous

Pyrexia (4%); chills, postprocedural hemorrhage (2%); hemorrhage, hyperpyrexia, light anesthesia, pain, rigors (postmarketing).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Select dose with caution because elderly patients are more likely to have decreased renal function.

Renal Function

Consider dosage reduction in patients with impaired renal function.

Hepatic Function

Consider dosage reduction in patients with impaired hepatic function.

Arousability

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.

Transient hypertension

May occur in association with peripheral vasoconstriction, primarily during the loading dose.

Withdrawal symptoms

If administered for more than 24 h and stopped abruptly, withdrawal symptoms, including agitation, headache, and nervousness, accompanied or followed by rapid increase in BP and elevated catecholamine concentrations, may occur.

Overdosage

Symptoms

Bradycardia, cardiac arrest, first-degree AV block, hypotension, second-degree heart block.

Patient Information

• 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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