AIM: 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. CONCLUSION:Dexmedetomidine is well absorbed systemically through the oral mucosa, and therefore buccal dosing may provide an effective, noninvasive route to administer the drug.
RCT Entities:
AIM: 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. CONCLUSION:Dexmedetomidine is well absorbed systemically through the oral mucosa, and therefore buccal dosing may provide an effective, noninvasive route to administer the drug.
Authors: V P Shah; K K Midha; S Dighe; I J McGilveray; J P Skelly; A Yacobi; T Layloff; C T Viswanathan; C E Cook; R D McDowall Journal: Eur J Drug Metab Pharmacokinet Date: 1991 Oct-Dec Impact factor: 2.441
Authors: H Scheinin; S Karhuvaara; K T Olkkola; A Kallio; M Anttila; L Vuorilehto; M Scheinin Journal: Clin Pharmacol Ther Date: 1992-11 Impact factor: 6.875
Authors: Shubham Chamadia; Juan C Pedemonte; Lauren E Hobbs; Hao Deng; Sarah Nguyen; Luis I Cortinez; Oluwaseun Akeju Journal: Anesthesiology Date: 2020-12-01 Impact factor: 7.892