Trade Names:Precedex- Injection, solution 100 mcg/mL
Relatively selective alpha-2 adrenergic agonist with sedative properties.
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%.
Steady-state Vd is approximately 118 L.
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. No unchanged drug is detected in the urine.
Pharmacokinetics not different in patients with severe renal function 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 function impairment. Dosage adjustment may be necessary in patients with hepatic function impairment.Elderly
Pharmacokinetics not altered by age.Gender
No difference in pharmacokinetics based on gender.
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.
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.
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.Maintenance dose
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.Intensive Care Unit SedationAdults
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.Maintenance dose
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.
Store at 59° to 86°F.
Additive effects are anticipated.
None well documented.
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).
Agitation (2%); confusion, convulsion, delirium, dizziness, hallucination, headache, illusion, neuralgia, neuritis, seizures, speech disorder (postmarketing).
Increased sweating (postmarketing).
Abnormal vision, photopsia (postmarketing).
Nausea (9%); dry mouth (4%); abdominal pain, diarrhea, vomiting (3%).
Decreased urine output (1%); increased BUN, oliguria (postmarketing).
Abnormal hepatic function, increased ALT, increased AST, hyperbilirubinemia, increased gamma-glutamyl transpepsidase (postmarketing).
Hypovolemia (3%); hyperglycemia (2%); hypocalcemia (1%); acidosis, hyperkalemia, hypoglycemia, increased alkaline phosphatase, respiratory acidosis, thirst (postmarketing).
Respiratory depression (37%); atelectasis (3%); hypoxia, pleural effusion (2%); pulmonary edema, wheezing (1%); apnea, bronchospasm, dyspnea, hypercapnia, hypoventilation, hypoxia, pulmonary congestion (postmarketing).
Pyrexia (4%); chills, postprocedural hemorrhage (2%); hemorrhage, hyperpyrexia, light anesthesia, pain, rigors (postmarketing).
Continuously monitor patients because of known pharmacologic effects.
Category C .
Safety and efficacy not established.
Select dose with caution because elderly patients are more likely to have decreased renal function.
Consider dosage reduction in patients with impaired renal function.
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.
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.
May occur in association with peripheral vasoconstriction, primarily during the loading dose.
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.
Bradycardia, cardiac arrest, first-degree AV block, hypotension, second-degree heart block.
Copyright © 2009 Wolters Kluwer Health.