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Kinetics of pamatolol, a cardioselective beta adrenoreceptor blocker
Author(s) -
Carruthers S. George,
Pentikainen Pertti,
Hosier James P.,
Azarnoff Daniel L.
Publication year - 1979
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt1979266682
Subject(s) - beta (programming language) , kinetics , beta blocker , pharmacology , chemistry , medicine , computer science , physics , heart failure , programming language , quantum mechanics
The systemic bioavailability, elimination half‐life (t½), and plasma concentration‐response relationships of pamatolol, a relatively cardioselective beta adrenoceptor blocker, have been measured in healthy subjects. Pamatolol is rapidly and completely absorbed after ora! dosing. Elimination t½ ranged from 2.9 to 4.6 hr after oral doses and from 2.2 to 5.6 hr after intravenous doses. There was a clear relationship between log plasma pamatolol concentration and sympathetic blockade assessed by reduction of exercise heart rate. Concentration‐response curves were essentially identical after oral and intravenous doses. There is no evidence of a first‐pass effect, nor is there any evidence of metabolite activity.