Bioavailability of dexmedetomidine after extravascular doses in healthy subjects.
OBJECTIVE
To determine the absolute bioavailability of extravascularly administered dexmedetomidine, a novel a2-adrenoceptor agonist, in healthy subjects.


METHODS
Single 2 microg x 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.


CONCLUSIONS
Dexmedetomidine is well absorbed systemically through the oral mucosa, and therefore buccal dosing may provide an effective, noninvasive route to administer the drug.
Anttila
Markku
M
Orion Corporation, Orion Pharma, Turku, Finland.
Penttilä
Jani
J
Helminen
Antti
A
Vuorilehto
Lauri
L
Scheinin
Harry
H
D000316:Adrenergic alpha-Agonists / Q000493:pharmacokinetics*; D000328:Adult; D001682:Biological Availability; D018592:Cross-Over Studies; D020927:Dexmedetomidine / Q000493:pharmacokinetics*; D006207:Half-Life; D006801:Humans; D007262:Infusions, Intravenous; D007273:Injections, Intramuscular; D008297:Male
D000316:Adrenergic alpha-Agonists; D020927:Dexmedetomidine