Dexmedetomidine

Uses

Dexmedetomidine Hydrochloride Injection is a central alpha-2 adrenergic agonist used for sedation of non-intubated patients prior to and/or during surgical and other procedures.

Dexmedetomidine is also used to associated treatment for these conditions: Benzodiazepine Withdrawal, Cyclic Vomiting Syndrome, Shivering caused by Anesthesia, Sedative therapy

How Dexmedetomidine works

Dexmedetomidine is a specific and selective alpha-2 adrenoceptor agonist. By binding to the presynaptic alpha-2 adrenoceptors, it inhibits the release if norepinephrine, therefore, terminate the propagation of pain signals. Activation of the postsynaptic alpha-2 adrenoceptors inhibits the sympathetic activity decreases blood pressure and heart rate.

Dosage

Dexmedetomidine dosage

Dilute in 0.9% Sodium Chloride Injection to concentration of 4 mcg/mL prior to administration.

To be administered only by health care providers skilled in the management of patients in the operating room setting.

Administer intravenously using a controlled infusion device. Administration duration should not exceed 24 hours.

Continuously monitor blood pressure, heart rate, and oxygen levels during administration and as clinically appropriate after discontinuation.

Initiation of Procedural Sedation:

• More invasive procedures or awake fiberoptic intubation:1 mcg/kg over 10 minutes
• Less invasive procedures such as ophthalmic surgery:0.5 mcg/kg over 10 minutes

Maintenance of Procedural Sedation

• All procedures except awake fiberoptic intubation:Generally, initiate at 0.6 mcg/kg/hour and titrate to achieve desired clinical effect with dosages ranging from 0.2 to 1 mcg/kg/hour.
• Awake fiberoptic intubation:Administer 0.7 mcg/kg/hour until the endotracheal tube is secured

Side Effects

Pregnancy: There are no studies conducted with dexmedetomidine hydrochloride in pregnant women to inform any drug-associated risks.

Lactation: There is no information regarding the presence of dexmedetomidine hydrochloride in human milk, the effects of the drug on the breastfed infant, or the effects of the drug on milk production.

Precaution

Bradycardia and Sinus Arrest: Consider decreasing or stopping dexmedetomidine HCl infusion; decreasing or stopping other medications that depress sinus node function; administering anticholinergic agents (e.g., glycopyrrolate, atropine); and/or administering pressor agents.

Hypotension: Consider decreasing or stopping dexmedetomidine HCl infusion; increasing rate of intravenous fluid administration; elevating lower extremities, and/or administering pressor agents.

Transient Hypertension: Observed primarily during administration of loading dose. Consider reducing loading infusion rate.

Arousability: 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.

Interaction

Anesthetics, sedatives/hypnotics, opioids: Can potentiate sedating effects. Consider reducing dosage of dexmedetomidine HCl or co-administered drug.

Food Interaction

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Dexmedetomidine Drug Interaction

Moderate: diltiazem, diltiazem, metoprolol, metoprolol, metoprolol, metoprolol, valproic acid, valproic acidUnknown: aspirin, aspirin, epinephrine, epinephrine, glucose, glucose, heparin, heparin, lvp solution, lvp solution, acetaminophen, acetaminophen

Dexmedetomidine Disease Interaction

Major: depressionModerate: glaucoma, liver disease, cardiovascular dysfunction

Volume of Distribution

• 118 L

Half Life

2 hours

Clearance

• 39 L/h [Healthy volunteers receiving IV infusion (0.2-0.7 mcg/kg/hr)]

Elimination Route

A mass balance study demonstrated that after nine days an average of 95% of the radioactivity, following intravenous administration of radiolabeled dexmedetomidine, was recovered in the urine and 4% in the feces. Fractionation of the radioactivity excreted in urine demonstrated that products of N-glucuronidation accounted for approximately 34% of the cumulative urinary excretion. The majority of metabolites are excreted in the urine.

Pregnancy & Breastfeeding use

Pregnancy: There are no studies conducted with dexmedetomidine hydrochloride in pregnant women to inform any drug-associated risks.

Lactation: There is no information regarding the presence of dexmedetomidine hydrochloride in human milk, the effects of the drug on the breastfed infant, or the effects of the drug on milk production.

Contraindication

None

Special Warning

Geriatric patients (age greater than 65 years): Recommended loading infusion dosage for initiation of procedural sedation is 0.5 mcg/kg over 10 minutes. Consider dosage reduction for maintenance

Hepatic impairment: Consider dosage reduction for initiation and maintenance of procedural sedation.

Innovators Monograph

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