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.

journal_name

Eur J Clin Pharmacol

authors

Uematsu T,Nakano M,Kosuge K,Kanamaru M,Nakashima M

doi

10.1007/BF00316473

subject

Has Abstract

pub_date

1993-01-01 00:00:00

pages

361-4

issue

4

eissn

0031-6970

issn

1432-1041

journal_volume

44

pub_type

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