Dexmedetomidine

Products

Dexmedetomidine is commercially available as a concentrate for the preparation of an infusion solution (Dexdor). It was approved in many countries in 2012.

Structure and properties

Dexmedetomidine (C13H16N2, Mr = 200.3 g/mol) is an imidazole derivative and the -enantiomer of medetomidine. It is structurally closely related to detomidine and is present in drugs as dexmedetomidine hydrochloride, a white crystalline powder that is soluble in water.

Effects

Dexmedetomidine (ATC N05CM18) has sedative, analgesic, sympatholytic, and muscle relaxant properties. The effects are due to agonism at α2 receptors.

Indications

  • For sedation of adult patients receiving intensive care who require a depth of sedation that still permits arousal by verbal stimulation (this corresponds to a classification of 0 to -3 according to the Richmond Agitation-Sedation Scale RASS).
  • For sedation of adult, non-intubated patients before and/or during diagnostic or surgical procedures requiring sedation, i.e., procedural sedation/awake sedation.

Dosage

According to the SmPC. The drug is administered as a diluted intravenous infusion using a controlled infusion pump.

Contraindications

Dexmedetomidine is contraindicated in hypersensitivity, advanced heart block in patients without pacemakers, uncontrolled hypotension, and acute cerebrovascular events. For complete precautions, see the drug label.

Interactions

Anesthetics, sedatives, hypnotics, antihypertensives, and opioids may cause potentiation. Dexmedetomidine is an inhibitor of CYP2B6 and may cause interactions with CYP2D6 substrates. It may also be a CYP inducer.

Adverse effects

The most common possible adverse effects include low or high blood pressure, slow pulse, low or high blood glucose, agitation, myocardial ischemia, nausea, vomiting, and dry mouth.