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The pharmacokinetics of acebvutolol in man, following the oral administration of acebutolol hcl as a single dose (400 mg), and during and after repeated oral dosing (400 mg, b.d.)
Author(s) -
Gulaid A. A.,
James I. M.,
Kaye C. M.,
Lewellen O. R. W.,
Roberts E.,
Sankey M.,
Smith J.,
Templeton R.,
Thomas R. J.
Publication year - 1981
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510020202
Subject(s) - acebutolol , pharmacokinetics , dosing , oral administration , pharmacology , metabolite , antiarrhythmic agent , excretion , chemistry , medicine , endocrinology , blood pressure , heart disease
The pharmacokinetics of acebutolol have been studied in eight healthy male volunteers following the oral administration of acebutolol hydrochloride (‘Sectral’, May & Baker) as a single dose (400 mg), and during and after repeated oral dosing (400 mg, b.d. for 56 days). Following single dose administration, considerable inter‐subject variation in plasma levels of parent drug and the major metabolite, diacetolol. was evident. Acebutolol appeared to be eliminated from plasma in a bi‐phasic manner, and this was confirmed from urinary excretion rate data. Mean initial and terminal half‐lives of about 2 and 11 h, respectively, were determined. Plasma levels of diacetolol were greater than those of parent drug from 3 to 4 h following dose administration. Total urinary excretion of diacetolol was generally greater than that of acebutolol. During repeated dosing, steady‐state plasma levels of acebutolol and diacetolol were achieved in 6 volunteers. Acebutolol did not appear to stimulate or inhibit its metabolism.