title: Pharmacokinetics of detomidine following intravenous or oral-transmucosal administration and sedative effects of the oral-transmucosal treatment in dogs.
abstract: OBJECTIVE
  To determine the pharmacokinetics of detomidine hydrochloride administered IV (as an injectable formulation) or by the oral-transmucosal (OTM) route (as a gel) and assess sedative effects of the OTM treatment in healthy dogs.
  
  
  METHODS
  12 healthy adult dogs.
  
  
  METHODS
  In phase 1, detomidine was administered by IV (0.5 mg/m(2)) or OTM (1 mg/m(2)) routes to 6 dogs. After a 24-hour washout period, each dog received the alternate treatment. Blood samples were collected for quantification via liquid chromatography with mass spectrometry and pharmacokinetic analysis. In phase 2, 6 dogs received dexmedetomidine IV (0.125 mg/m(2)) or detomidine gel by OTM administration (0.5 mg/m(2)), and sedation was measured by a blinded observer using 2 standardized sedation scales while dogs underwent jugular catheter placement. After a l-week washout period, each dog received the alternate treatment.
  
  
  RESULTS
  Median maximum concentration, time to maximum concentration, and bioavailability for detomidine gel following OTM administration were 7.03 ng/mL, 1.00 hour, and 34.52%, respectively; harmonic mean elimination half-life was 0.63 hours. All dogs were sedated and became laterally recumbent with phase 1 treatments. In phase 2, median global sedation score following OTM administration of detomidine gel was significantly lower (indicating a lesser degree of sedation) than that following IV dexmedetomidine treatment; however, total sedation score during jugular vein catheterization did not differ between treatments. The gel was subjectively easy to administer, and systemic absorption was sufficient for sedation.
  
  
  CONCLUSIONS
  Detomidine gel administered by the OTM route provided sedation suitable for a short, minimally invasive procedure in healthy dogs.
authors.forename: Kristen M
authors.initials: KM
authors.lastname: Messenger
authors.forename: Marie
authors.initials: M
authors.lastname: Hopfensperger
authors.forename: Heather K
authors.initials: HK
authors.lastname: Knych
authors.forename: Mark G
authors.initials: MG
authors.lastname: Papich
mesh_terms: D058956:Administration, Mucosal; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002853:Chromatography, Liquid; D020927:Dexmedetomidine / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D004285:Dogs / Q000378:metabolism*; D005260:Female; D005782:Gels; D006207:Half-Life; D006993:Hypnotics and Sedatives / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D007093:Imidazoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D007262:Infusions, Intravenous / Q000662:veterinary; D008297:Male; D013058:Mass Spectrometry
chemical_list: D005782:Gels; D006993:Hypnotics and Sedatives; D007093:Imidazoles; D020927:Dexmedetomidine; C041255:detomidine