The pharmacokinetics of the β2-adrenoceptor agonist, tulobuterol, in Beagle dogs following transdermal and intravenous administration

• Published in: The veterinary journal (1997) Vol. 208; pp. 90 - 92
• Main Authors: Kim, J.H., Kim, T.H., Park, H.J., Choi, Y.J., Kang, J.H., Song, K.H., Koo, T.S., Seo, K.W.
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01-02-2016
• Subjects: Administration, Cutaneous; Administration, Intravenous - veterinary; Adrenergic beta-2 Receptor Agonists - blood; Adrenergic beta-2 Receptor Agonists - pharmacokinetics; Animals; Bronchodilator Agents - blood; Bronchodilator Agents - pharmacokinetics; Canine; Dogs - metabolism; Pharmacokinetics; Random Allocation; Terbutaline - analogs & derivatives; Terbutaline - blood; Terbutaline - pharmacokinetics; Transdermal patch; Tulobuterol; β2-adrenoceptor agonist; Pharmacokinetics; Transdermal patch; β2-adrenoceptor agonist; Canine; Tulobuterol; β-adrenoceptor agonist
• DOI: 10.1016/j.tvjl.2015.10.012
• EISSN: 1532-2971
• ISSN: 1090-0233

•A tulobuterol patch containing a β2-adrenergic agonist at two different doses was investigated.•The pharmacokinetics of tulobuterol was evaluated in dogs after intravenous and transdermal administration.•A therapeutic blood concentration was reached with both transdermal doses.•The tulobuterol patch can be safely and effectively used in dogs.
Tulobuterol is a β2-adrenergic agonist that was the first bronchodilator approved as a transdermal patch for humans. Previous studies have examined the pharmacokinetics of tulobuterol in humans but not in the veterinary species. In this study, the pharmacokinetics of tulobuterol was examined in healthy Beagle dogs after transdermal and intravenous administration. The Cmax was 2.09 ng/mL at 16.0 h for a 0.2 mg/kg patch and 4.85 ng/mL at 13.6 h for a 0.4 mg/kg patch. The effective blood level in humans is 1–3 ng/mL, a concentration achieved using the 0.2 mg/kg patch in dogs. In conclusion, application of a 0.2 mg/kg tulobuterol patch to healthy dogs led to an apparently effective blood concentration for 24 h.