Precedex (dexmedetomidine HCl in 0.9 % sodium chloride)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Dexmedetomidine hydrochloride, a relatively selective alpha2-adrenergic agonist, is a sedative.
Dexmedetomidine hydrochloride is a relatively selective, centrally acting alpha2-adrenergic agonist.
alpha2-Adrenergic agonists such as dexmedetomidine and clonidine have dose-related sedative, anxiolytic, analgesic, and anesthetic-sparing effects and help maintain intraoperative hemodynamic stability by blunting the sympathetic response to surgery. In addition, alpha2-adrenergic agonists act through some of the same mechanisms as opiates in the brain (e.g., activation of G-proteins and potassium coupling), resulting in potentiation of opiate analgesia and allowing for a reduction in opiate dosage and accompanying respiratory depression during concomitant use. Dexmedetomidine does not appear to reduce dosage requirements of skeletal muscle relaxants.
Dexmedetomidine does not cause respiratory depression in healthy individuals when given by IV infusion in recommended dosages. The mechanism of action of transmucosal dexmedetomidine in the acute treatment of agitation associated with schizophrenia or bipolar I or II disorder is thought to be due to activation of presynaptic alpha2-adrenergic receptors.
Dexmedetomidine has a shorter half-life than clonidine (about 2 versus 8-12 hours, respectively), giving it a more favorable pharmacokinetic profile for perioperative use. Dexmedetomidine also has greater alpha2-selectivity than clonidine, thereby potentially reducing the incidence of undesirable alpha1-adrenergic effects such as hypotension and bradycardia. While dexmedetomidine exhibits alpha2-selectivity when given by slow IV infusion in low to moderate doses (10-300 mcg/kg), selectivity diminishes with administration of high doses (e.g., 1000 mcg/kg) or rapid IV administration.
The mean time for dexmedetomidine to dissolve in the mouth is approximately 6-8 or 18 minutes following sublingual or buccal administration, respectively. Dexmedetomidine is generally quantifiable in plasma within 5-20 minutes after transmucosal administration. Absolute bioavailability is approximately 72 or 82% following sublingual or buccal administration, respectively.
Early water intake (as early as 15 minutes postdose) has minimal effects on the rate or extent of sublingual absorption; effects of early water intake (<2 hours postdose) on absorption following buccal administration has not been evaluated The mean maximal plasma concentrations of dexmedetomidine were reached approximately 2 hours after sublingual or buccal administration.
Dexmedetomidine is rapidly distributed and crosses the blood-brain barrier. It has a plasma protein binding of approximately 94%. Dexmedetomidine undergoes almost complete biotransformation in the liver and is excreted in urine (95%) and feces (4%) with very little unchanged drug.
Biotransformation involves both direct glucuronidation and metabolism by the hepatic microsomal cytochrome P-450 (CYP) enzyme system. The major metabolic pathways of dexmedetomidine are direct N-glucuronidation, aliphatic hydroxylation mediated principally by CYP2A6, and N-methylation. Approximately 28% of dexmedetomidine metabolites excreted in urine have not been identified.
The terminal elimination half-life of dexmedetomidine following IV infusion is approximately 2 hours and approximately 2.8 hours following sublingual or buccal administration.
Dexmedetomidine is not subject to control under the Federal Controlled Substances Act of 1970. However, because the drug exhibits pharmacologic effects similar to clonidine in animals, it is possible that dexmedetomidine could produce a withdrawal-like syndrome upon abrupt discontinuance.
Generic name: dexmedetomidine HCl in 0.9 % sodium chloride
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
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Indications
The following indications are listed for Precedex:
- Sedation As Adjunct To Anesthesia
- Sedation In Intubated Patient
Also known as: Adjunct Sedation.
Dosing
Dosage of dexmedetomidine hydrochloride is expressed in terms of dexmedetomidine. Dosage of the drug for IV infusion should be individualized and titrated to the desired level of sedation.
Dexmedetomidine hydrochloride for buccal or sublingual administration is available as strips containing 120 or 180 mcg of dexmedetomidine; the 120 or 180 mcg strips may be cut in half to obtain doses of 60 or 90 mcg, respectively.
Dosage reductions may be needed in patients concomitantly receiving other anesthetics, sedatives, hypnotics, or opiates.
Administer by IV infusion or by sublingual or buccal administration depending on the dosage form.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*None.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects occurring in >2% of adults receiving IV dexmedetomidine include hypotension, bradycardia, and dry mouth.
The most common adverse effects occurring in >5% of pediatric patients 1 month to <17 years of age receiving IV dexmedetomidine include bradypnea, bradycardia, hypertension, and hypotension.
The most common adverse effects occurring in >=5% of adults receiving sublingual/buccal dexmedetomidine include somnolence, oral paresthesia or oral hypoesthesia, dizziness, dry mouth, hypotension, and orthostatic hypotension.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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The manufacturer states that safety and efficacy of dexmedetomidine for ICU sedation have not been established in pediatric patients. However, the drug has been used in pediatric patients undergoing sedation in the ICU or other settings to facilitate mechanical ventilation or other procedures (e.g., radiologic imaging). A wide range of dosage regimens has been used. Although there are some data suggesting a possible role of dexmedetomidine for sedation in pediatric patients, additional study is needed to evaluate the drug's safety in this population.
The safety and efficacy of IV dexmedetomidine have been established in pediatric patients 1 month to <18 years of age for sedation during noninvasive procedures. Use in this age group is based on a randomized, double-blind, dose-ranging, safety and efficacy trial in nonintubated pediatric patients 1 month to <17 years of age who required sedation prior to undergoing MRI scans. An increase in frequency of bradypnea, bradycardia, hypertension, and hypotension was observed in pediatric patients treated with dexmedetomidine. The overall safety profile of the drug in pediatric patients was consistent with the known safety profile in adults. The safety and efficacy of dexmedetomidine for sedation during noninvasive procedures have not been established in pediatric patients <1 month of age.
The safety and efficacy of sublingual/buccal dexmedetomidine have not been established in pediatric patients.
Data from randomized controlled trials and case reports have not identified a drug-associated risk of major birth defects and miscarriage associated with use of IV dexmedetomidine during pregnancy; however, the reported exposures occurred after the first trimester. Most of the exposures occurred at the time of caesarean section delivery, and adverse effects on maternal outcomes or infant Apgar scores were not observed. Available data indicate that dexmedetomidine crosses the placenta.
In animal reproduction studies, fetal toxicity (lower fetal viability and reduced live fetuses) occurred with subcutaneous administration of dexmedetomidine to pregnant rats during organogenesis at doses 1.8 times the maximum recommended human dose of 17.8 mcg/kg per day. Developmental toxicity (low pup weights and adult offspring weights, decreased grip strength, increased early implantation loss, and decreased viability of second-generation offspring) occurred when pregnant rats received subcutaneous dexmedetomidine at doses less than the clinical dose from late pregnancy through lactation and weaning.
There are no available data on the use of dexmedetomidine strips for sublingual or buccal administration in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal effects.
Dexmedetomidine is distributed into human milk following IV infusion. The potential effects of IV or transmucosal dexmedetomidine on the breast-fed infant or on milk production are not known.
Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for dexmedetomidine and any potential adverse effects on the breast-fed infant from the drug or from the underlying condition. Advise nursing women receiving the drug to monitor the breast-fed infant for irritability.
A higher incidence of bradycardia and hypotension has been reported in geriatric patients >65 years of age receiving IV dexmedetomidine. Consider reducing the dosage of IV dexmedetomidine in geriatric patients. A reduced loading dose of IV dexmedetomidine is recommended in geriatric patients receiving the drug for procedural sedation.
Dosage reduction of sublingual/buccal dexmedetomidine is recommended in geriatric patients. Clinical studies did not include sufficient numbers of patients >=65 years of age to determine whether efficacy of transmucosal dexmedetomidine in these patients differs from younger adults.
ICD codes
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Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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