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Pharmacokinetics and beta-blocking effects of transdermal timolol.

Abstract：

:The pharmacokinetic profiles of transdermal timolol 6 and 24 mg (as 5 and 20% w/v patches) was studied in four healthy young volunteers. To assess its bioavailability, the pharmacokinetics of an IV infusion of timolol maleate 5 mg was also determined in the same subjects. When the 20% (w/v) timolol patch was applied, the mean bioavailability was 74.4%. Plasma timolol concentrations were below the detection limit when a 5% patch was applied to the same skin area in all four subjects, except for one in whom the bioavailability was 23.6%. Weak erythema developed at the application site in all of the volunteers after application of the 20% (w/v) patch. However, erythema did not develop in any volunteer when the 5% patch was applied. The beta-blocking effect was determined by exercise testing. Similar plasma levels generated similar changes in exercise-induced heart rate after the transdermal and intravenous administration of timolol.

journal_name

Eur J Clin Pharmacol

journal_title

European journal of clinical pharmacology

authors

Kubota K,Yamada T,Kikuchi K,Koyama E,Ishizaki T

doi

10.1007/BF00315551

subject

Has Abstract

pub_date

1993-01-01 00:00:00

pages

493-5

issue

5

eissn

0031-6970

issn

1432-1041

journal_volume

44

pub_type

杂志文章

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