Circulation, Vol 61, 555-560, Copyright © 1980 by American Heart Association
G Jackson, J Schwartz, RE Kates, M Winchester and DC Harrison
The physiology, pharmacokinetics and efficacy of atenolol, a
cardioselective beta-adrenergic blocking agent, were evaluated in 10
patients with stable angina pectoris in a single-blind, dose-ranging study.
After a 1-month control placebo period, atenolol was administered once
daily at dosages of 25, 50, 100 and 200 mg for 2-week periods. All patients
had fewer anginal attacks and consumed fewer nitroglycerin tablets than mg
for 2-week periods. All patients had fewer anginal attacks and consumed
fewer nitroglycerin tablets than during the placebo period.
Twenty-four-hour ambulatory ECG recordings showed a decrease in mean hourly
heart rate throughout the dosing period, with preservation of diurnal
variation. Maximal, symptom- limited, treadmill exercise tests performed 3
hours after drug ingestion showed significantly increased exercise time and
decreased double products for all doses, but especially with 100-mg and
200-mg doses. Exercise time 24 hours after drug ingestion continued to show
a decrease in maximum heart rate and double product, with 100-mg and 200-
mg doses again being most effective. Atenolol serum levels correlated with
percent reduction in exercise heart rate and increased exercise time. Serum
levels rose linearly, with an average elimination half-life of about 10
hours after chronic oral dosing. Thus, atenolol was an effective
antianginal agent and suppressed resting and exercise- stressed heart rate
for 24 hours after ingestion when given in a 100-mg or 200-mg dose once
daily.
ARTICLES
Atenolol: once-daily cardioselective beta blockade for angina pectoris