title: Bioavailability of detomidine administered sublingually to horses as an oromucosal gel.
abstract: The objective of the study was to determine the absorption, bioavailability and sedative effect of detomidine administered to horses as an oromucosal gel compared to intravenous and intramuscular administration of detomidine injectable solution. The study was open and randomized, with three sequences crossover design. Nine healthy horses were given 40 μg/kg detomidine intravenously, intramuscularly or administered under the tongue with a 7-day wash-out period between treatments. Blood samples were collected before and after drug administration for the measurement of detomidine concentrations in serum. The effects of the route of administration on heart rate and rhythm were evaluated and the depth of sedation assessed. Mean (±SD) bioavailability of detomidine was 22% (±5.3%) after sublingual administration and 38.2% (±7.9%) after intramuscular administration. The sedative effects correlated with detomidine concentrations regardless of the route of administration. We conclude that less detomidine is absorbed when given sublingually than when given intramuscularly, because part of it does not reach the circulation. Sublingual administration of detomidine oromucosal gel at 40 μg/kg produces safe sedation in horses. Slow absorption leads to fewer and less pronounced adverse effects than the more rapid absorption after intramuscular injection.
authors.affiliation: Orion Corporation, Orion Pharma, Turku, Finland Agrifood Research Finland, Ypäjä, Finland. helena.kaukinen@orionpharma.com
authors.forename: H
authors.initials: H
authors.lastname: Kaukinen
authors.forename: J
authors.initials: J
authors.lastname: Aspegrén
authors.forename: S
authors.initials: S
authors.lastname: Hyyppä
authors.forename: L
authors.initials: L
authors.lastname: Tamm
authors.forename: J S
authors.initials: JS
authors.lastname: Salonen
mesh_terms: D000286:Administration, Sublingual; D000818:Animals; D001682:Biological Availability; D018592:Cross-Over Studies; D004333:Drug Administration Routes; D005260:Female; D005782:Gels; D006736:Horses / Q000097:blood*; D006993:Hypnotics and Sedatives / Q000097:blood / Q000493:pharmacokinetics*; D007093:Imidazoles / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male
chemical_list: D005782:Gels; D006993:Hypnotics and Sedatives; D007093:Imidazoles; C041255:detomidine