DEXMEDETOMIDINE

brands

Class

• Highly selective agonist at alpha 2 receptors

DEXMEDETOMIDINE commonly prescribed for

(Bold for FDA approved)

How DEXMEDETOMIDINE works

• For agitation, the mechanism is thought to be due to activation of presynaptic alpha 2 receptors</br>

• Induces sedation by decreasing activity of noradrenergic neurons in the locus coeruleus, which in turn increases downstream activity of GABA neurons in the hypothalamic sleep center (ventrolateral preoptic area [VLPO])

How long until DEXMEDETOMIDINE works

• Can reduce agitation in 20–30 minutes

Notable Side Effects

• Somnolence, oral paresthesia, oral hypoesthesia, dizziness, dry mouth

Life Threatening Side Effects

• Hypotension, orthostatic hypotension, bradycardia

weight gain

unusual

sedation

problematic

What to do about DEXMEDETOMIDINE side effects

• Patients should be adequately hydrated and should sit or lie down until vital signs are within normal range

• If patient is unable to remain seated or lying down, precautions should be taken to reduce the risk of falls

• Patients should be alert and not experiencing orthostatic hypotension or symptomatic hypotension prior to allowing them to resume ambulation

usual dosage range

• Mild or moderate agitation: 120 μg

• Severe agitation: 180 μg

Dosage Forms

• Sublingual film 120 μg, 180 μg

long term use

• Dexmedetomidine sublingual was not studied for longer than 24 hours after the first dose

habit forming

• Dexmedetomidine sublingual was not studied for longer than 24 hours after the first dose; there may be a risk of physical dependence and withdrawal syndrome and/ or tolerance and tachyphylaxis if it is used in a manner other than indicated

Renal Impairment

• Dose adjustment not necessary

Hepatic Impairment

• Vital signs, including orthostatic measurements, should be assessed prior to the administration of subsequent doses

Cardiac Impairment

• Avoid use in patients with hypotension, orthostatic hypotension, advanced heart block, severe ventricular dysfunction, or history of syncope

• Avoid use in patients with risk factors for a prolonged QTc interval

Elderly

• For patients ages 65 and older, the maximum recommended initial dose is 120 μg; optional second and third doses of 60 μg can be administered at least 2 hours apart; the maximum recommended total daily dosage is 240 μg

• Vital signs, including orthostatic measurements, should be assessed prior to the administration of subsequent doses

Children and Adolescents

• Safety and efficacy have not been established

• Sublingual dexmedetomidine is currently being studied as a treatment for agitation associated with pediatric schizophrenia (ages 13–17) and bipolar disorder (ages 10–17)

Pregnancy

• Controlled studies have not been conducted in pregnant women

• Available data from published randomized controlled trials and case reports of use with intravenously administered dexmedetomidine during pregnancy indicate that dexmedetomidine crosses the placenta

• There are no available data for the use of intravenous dexmedetomidine during the first trimester of pregnancy; most data are based on studies of exposure during cesarean-section delivery; those studies did not identify an adverse effect on maternal outcomes or infant Apgar scores

• When administered to pregnant rats subcutaneously during organogenesis, fetal toxicity (increased post-implantation loss and reduced live pups) occurred in the presence of maternal toxicity (decreased body weight) at doses 5 times the maximum recommended human dose (MRHD)

• When administered to rats during late pregnancy through lactation and weaning, adverse developmental effects, including early implantation loss and decreased viability of second-generation offspring, occurred at doses less than or equal to the MRHD

Breast Feeding

• Some drug is found in mother’s breast milk