title: The pharmacokinetics of the beta 2-adrenoceptor agonist, tulobuterol, given transdermally and by inhalation.
abstract: We have studied the pharmacokinetics of tulobuterol given transdermally or by aerosol inhalation in healthy male volunteers. Tulobuterol was rapidly absorbed after inhalation, with a tmax of 0.8-1.5 h. The Cmax and the AUC increased linearly with dose. Tulobuterol was well absorbed after transdermal administration, with an absorption lag-time of about 4 h. The Cmax and AUC increased linearly with dose and the tmax was about 9-12 h. The mean percentage of drug absorbed during the application of a patch for 24 h was 82-90% after a single dose and 82-85% during repeated dosing. The mean urinary recoveries as unchanged drug after a single inhalation and patch application were 3-4% and 5-6% respectively. Tulobuterol did not accumulate during repeated inhalation or transdermal application. It was well tolerated, except for an increase in heart rate of 10-20 beats.min-1 after five repeated applications of a 4 mg patch.
authors.affiliation: Department of Pharmacology, Hamamatsu University School of Medicine, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Uematsu
authors.forename: M
authors.initials: M
authors.lastname: Nakano
authors.forename: K
authors.initials: K
authors.lastname: Kosuge
authors.forename: M
authors.initials: M
authors.lastname: Kanamaru
authors.forename: M
authors.initials: M
authors.lastname: Nakashima
mesh_terms: D000279:Administration, Cutaneous; D000280:Administration, Inhalation; D000284:Administration, Oral; D000318:Adrenergic beta-Agonists / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000328:Adult; D001993:Bronchodilator Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D012016:Reference Values; D013726:Terbutaline / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics
chemical_list: D000318:Adrenergic beta-Agonists; D001993:Bronchodilator Agents; C010809:tulobuterol; D013726:Terbutaline