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Dexmedetomidine

Dexmedetomidine is a selective a2 agonist with a 1,600:1 preference for a2 receptors. It is intravenously


administered as an infusion from 0.1 to 1.5 g/kg/minute with a terminal elimination half-life of 2 hours.
Most often, this a2 agonist is used in the intensive care and operating room settings as a sedative and
analgesic due to its central sympatholytic effects. Dexmedetomidine undergoes extensive
biotransformation in the liver and is excreted mostly in the urine; liver impairment can dramatically
increase plasma levels and duration of action due to signifiantly decreased metabolism during infusion.
It’s potent binding and short half-life can induce physiologic dependence and result in the aforementioned
withdrawal phenomenon after only days of administration resulting in tachycardia, hypertension, and
anxiety. Interestingly, large intravenous boluses (0.25 to 1 g/kg over 3 to 5 minutes) result in a
paradoxical hypertension with a decrease in heart rate and resembles phenylephrine and is the resultant
effect of crossover a1 stimulation.

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