Dexmedetomidine: Effects, dosage

How does dexmedetomidine work?

Dexmedetomidine inhibits the release of the nerve messenger noradrenaline in a specific brain region: the locus caeruleus. This structure of the brain is particularly rich in nerve cells that communicate via norepinephrine and are involved in controlling orientation as well as attention.

Less norepinephrine due to dexmedetomidine subsequently means less messenger substance to activate these nerve cells. For this reason, dexmedetomidine has a primarily sedative effect. In addition, it mediates analgesic and muscle relaxant effects.

How quickly does dexmedetomidine work?

Physicians administer the active ingredient as an infusion. The effect is almost instantaneous and can be very well controlled.

What is dexmedetomidine approved for?

Second, physicians may administer dexmedetomidine to adult, non-intubated patients for sedation before and/or during diagnostic or surgical procedures.

Even though dexmedetomidine belongs to the group of sedatives (tranquilizers), it is not used for sleep or anxiety disorders.

How dexmedetomidine is used

Dexmedetomidine is given in the form of the water-soluble dexmedetomidine hydrochloride as an infusion. The dosage is based on body weight. It is usually between 0.2 and 1.4 micrograms per kilogram of body weight per hour (= 1.4 micrograms kg/h). The maximum dose is 1.4 micrograms kg/h.

During dexmedetomidine administration, medical personnel monitor the individual’s heart rate and blood pressure, among other things.

The most common side effects of dexmedetomidine can be attributed to inhibition of norepinephrine release. These include blood pressure drop, blood pressure rise, and low heart rate (bradycardia).

Much less common are restlessness and blood sugar fluctuations.

If you suspect or develop side effects, please contact a doctor or health care professional.

When should you not use dexmedetomidine?

In general, do not administer dexmedetomidine in the following cases:

  • if you are hypersensitive or allergic to the active substance or to any of the components of the medication
  • in advanced heart block (grade 2 or 3) in patients without a pacemaker (heart block = disturbance of the conduction of excitation in the heart)
  • in uncontrolled high blood pressure
  • during pregnancy
  • in children and adolescents under 18 years of age

These drug interactions may occur with dexmedetomidine.

Dexmedetomidine enhances the depressant properties of other drugs with sedative and/or sleep-inducing effects. These include, but are not limited to:

  • Anesthetics (such as isoflurane, propofol, midazolam).
  • sleeping pills (such as benzodiazepines, Z-drugs)
  • strong painkillers from the opioid group (such as morphine and alfentanil)

Dexmedetomidine blocks the enzyme cytochrome P450 2B6 (CYP2B6). Thus, in principle, interactions with drugs that are degraded via CYP2B6 are conceivable. Whether this is clinically relevant is not known.

Dexmedetomidine possibly enhances the blood pressure and heart rate lowering effect of other drugs (e.g. beta blockers).

Dexmedetomidine during breastfeeding.

Dexmedetomidine passes into breast milk. However, its level is below the detection limit 24 hours after treatment ends.

Medical professionals work with the mother to decide whether to stop breastfeeding and, if so, for how long.

How to get medicines with dexmedetomidine

Dexmedetomidine is available by prescription in Germany, Austria, and Switzerland. The medication is administered exclusively by personnel trained to do so.