Premium
Bioavailability of dexmedetomidine after extravascular doses in healthy subjects
Author(s) -
Anttila Markku,
Penttilä Jani,
Helminen Antti,
Vuorilehto Lauri,
Scheinin Harry
Publication year - 2003
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1046/j.1365-2125.2003.01944.x
Subject(s) - bioavailability , dexmedetomidine , buccal administration , medicine , anesthesia , pharmacology , dosing , pharmacokinetics , agonist , oral administration , drug , receptor , sedation
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.