Article date: December 2003
By: Markku Anttila, Jani Penttilä, Antti Helminen, Lauri Vuorilehto, Harry Scheinin, in Volume 56, Issue 6, pages 691-693
Aim To determine the absolute bioavailability of extravascularly administered dexmedetomidine, a novel a2‐adrenoceptor agonist, in healthy subjects.
Methods Single 2 µg kg−1 doses of dexmedetomidine were given intravenously, intramuscularly, perorally and buccally (where the solution is not swallowed) to 12 healthy male subjects. The drug concentration‐time data were analysed using linear one‐compartment (buccal and peroral data), or two‐compartment modelling (intravenous data), or noncompartmental methods (intramuscular data).
Results Mean (95% CI) absolute bioavailability after peroral, buccal and intramuscular administration was 16% (12–20%), 82% (73–92%) and 104% (96–112%), respectively.
Conclusion Dexmedetomidine is well absorbed systemically through the oral mucosa, and therefore buccal dosing may provide an effective, noninvasive route to administer the drug.
DOI: 10.1046/j.1365-2125.2003.01944.x
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