A Pharmacokinetic and Pharmacodynamic Study of Oral Dexmedetomidine

ConclusionsOral administration of dexmedetomidine in doses between 300 and 700 mcg was associated with decreases in heart rate and mean arterial pressure. Despite low oral absorption, the 700-mcg dose scheme reached clinically relevant concentrations for possible use as a sleep-enhancing medication.Editor ’s PerspectiveWhat We Already Know about This TopicDexmedetomidine is an alpha-2 adrenergic agonist sedative that is approved for intravenous usePlasma dexmedetomidine concentrations between 0.2 ng/mg and 0.3 ng/ml result in rousable sedationLow plasma dexmedetomidine concentrations are associated with decreased mean arterial pressure and heart rateWhat This Article Tells Us That Is NewThe hypotheses that oral dexmedetomidine would be associated with hemodynamic stability and plasma concentrations consistent with rousable sedation were tested in a phase I dose-escalation study in 15 normal volunteersOral dexmedetomidine bioavailability was low (7.2% [95% CI, 4.7 to 14%])Oral dexmedetomidine (300 µg, 500 µg, and 700 µg) was associated with plasma concentration–dependent decreases in mean arterial pressure and heart rateOnly the 700- µg oral dose produced plasma concentrations associated with sedation
Source: Anesthesiology - Category: Anesthesiology Source Type: research