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  • Title: [Dose-response relationship and duration of action of acebutolol / investigations on heart rate behaviour and ischemic ST-segment depression].
    Author: Kober G, Mikludy R, Veidt J, Kaltenbach M.
    Journal: Arzneimittelforschung; 1982; 32(8):835-9. PubMed ID: 6890361.
    Abstract:
    1. The dose-response relationship and duration of action of 3'-acetyl-4'-(2-hydroxy-3-isopropylaminopropyl)-butyranilide (acebutolol, Prent) were determined under double-blind conditions in 9 volunteers using heart rate at rest and during exercise as a test parameter. 2. The effect of 200 mg of acebutolol on ischemic ST-segment depression, heart rate, and blood pressure was investigated in 10 patients with coronary heart disease. 3. Heart rate at rest and while standing was most markedly reduced in the volunteers 3 h following ingestion of acebutolol 300 mg. 100 and 300 mg lowered heart rate during exercise by 9.9 and 18.9%, respectively. No significant additional effect was achieved by increasing the dosage to 500 mg. 4. 24 h after single oral doses of 300 and 500 mg of acebutolol, nearly 50% of the substance's activity was still evident. 5. In patients with coronary heart disease, maximum heart rate during exercise 3 h after oral intake of 200 mg declined by 13%. The heart rate sum during ergometry fell by 11.2%. Systolic blood pressure at rest and during exercise also was lower. 6. A single oral dose of 100-300 mg of acebutolol consistently reduces heart rate during exercise as well as exercise-induced myocardial ischemia. Since the drug remains active over a 24-h period, administration once daily should provide an adequate therapeutic effect in many patients.
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