A multicentre study of twice daily acebutolol (‘Sectral’) in the treatment of hypertension in general practice
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An open multicentre study was carried out under uncontrolled conditions in general practice to investigate the efficacy and acceptability of twice daily acebutolol in patients with mild to severe hypertension. Data from 1007 patients were analyzed. Most (901) had been treated previously with other hypertensive agents before starting on acebutolol. Oral dosages of acebutolol ranged from 200 mg to 1200 mg/day, according to individual requirements, and 331 patients received concomitant therapy, usually with a diuretic, either from the start of therapy or after 4 to 8 weeks. A significant reduction (p less than 0.001) was observed in mean diastolic blood pressure over the 12-week assessment period, and response increased with treatment duration. There were 280 reports of side-effects and 63 patients were withdrawn from the study for this reason.Keywords:
Acebutolol
Dose
Concomitant
Clinical Practice
Acebutolol
Essential hypertension
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Acebutolol
Essential hypertension
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Summary— Pharmacokinetics and the degree of β‐blockade of sustained release (SR) acebutolol (500 mg/day) and conventional acebutolol (200 mg tid) were examined after the first oral dose and after 10 days of treatment in ten healthy volunteers. After the first dose, acebutolol C max did not significantly differ between the two formulations; however, on day 10 acebutolol C max was significantly higher after SR formulation. C max of diacetolol, the major metabolite, did not differ between SR and conventional acebutolol neither on day 1 nor on day 10. The dose‐corrected relative bio‐availability of acebutolol was not different from 100% on day 1 and day 10; however the dose‐corrected diacetolol AUC, SR/conventional ratio, was significantly lower than 100% on days 1 and 10. Both acebutolol preparations exerted a significant reduction in exercise tachycardia over 24 h on day 1 and day 10; however, conventional acebutolol exhibited a greater reduction 24 h after the first dose. Exercise‐induced increase in systolic blood pressure was similarly inhibited by both treatments except for 24 h after the first dose when systolic blood pressure was significantly higher with SR than with conventional acebutolol. The percent reduction in heart rate during exercise was linearly correlated with log acebutolol plasma concentrations for each treatment regimen. These results suggest that β‐blockade exerted by SR acebutolol in healthy volunteers is equivalent to that of conventional acebutolol.
Acebutolol
Pharmacodynamics
Antiarrhythmic agent
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Acebutolol
Essential hypertension
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Acebutolol whose hypotensive properties are well established, appears as a most interesting beta-adrenergic blocking agent for simplification of treatment of moderate hypertension in man. Hypertensive patients likely to benefit from treatment with acebutolol can be identified within 5 days after administration of a single initial dose of the product. Long-term treatment with acebutolol can be considered in those patients identified as receptive. In non-responders, acebutolol can be used in combination with a diuretic agent. Such simplification of the therapeutic schedule in hypertension will certainly be helpfull both to the physician and his patient.
Acebutolol
Seniority
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Acebutololのβ遮断作用およびβ1選択性を検討するため，ラットの糖，脂質代謝系ならびにイヌの心筋および肝臓のadenylate cyclase活性におよぼす影響をpropranolo1と比較した．Acebutololはadrenalineによるラット血清中乳酸の上昇を抑制し，β遮断作用を示したが，propranololと比較すると約1/6の強さであった．Adrenalineによるラット血清中グルコースおよび遊離脂肪酸の上昇に対し，accbutololは遊離脂肪酸上昇をより選択的に抑制する傾向を示し，また1-isoproterenolによるイヌ心筋および肝臓のadenylate cyclase活性の上昇に対するacebutololの抑制作用は心筋adenylate cyclase活性により顕著であった．一方，propranololは心筋および肝臓のadenylate cyclase活性の上昇をいずれもacebutololより強く抑制したが，両臓器間に抑制作用の明らかな差は見出せなかった．以上の成績から，acebutololのβ遮断作用はpropranololに比較して弱いが，強い心臓選択性を持つことが示唆された．
Acebutolol
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Effects of acebutolol on carbohydrate and lipid metabolism in rats and on adenylate cyclase of heart and liver in dogs were investigated to determine the beta receptor blocking properties of the compound. Acebutolol exhibited the beta blocking activity and inhibited the increase of serum lactate concentration induced by adrenaline. This inhibition was about one-sixth as potent as that of propranolol. In hyperglycemic and free fatty acid effects of adrenaline, acebutolol inhibited the adrenaline-induced free fatty acid increase more effectively than hyperglycemia induced by adrenaline. In the inhibition of stimulated adenylate cyclase activity in the heart and liver, acebutolol was more active on the heart than on liver. Relative beta1 specificity of acebutolol was 93.2. Inhibition of propranolol on adenylate cyclase activity was more potent than that of acebutolol on both tissues, but showed no specificity. These results suggest that acebutolol is beta1 selective, although its beta blocking potency is less than that of propranolol.
Acebutolol
BETA (programming language)
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This double-blind clinical study was carried out in order to compare the therapeutic activity of propranolol, and a new beta-adrenergic blocker, acebutolol, in essential hypertension. The hypotensive activity of acebutolol was confirmed when a dosage of 600 mg/day was used, with en absence of side effects.
Acebutolol
Beta blocker
Essential hypertension
Adrenergic beta-Antagonists
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Acebutolol, a cardioselective beta-blocker, was studied at doses of 600 to 800 mg in a double-blind trial against placebo in 33 patients with essential hypertension. A moderate reduction in the arterial pressure was seen with placebo, but the pressure was greatly reduced by treatment with acebutolol (p less than 0,01). The heart rate was unchanged after placebo and was reduced by about 10 p.cent by acebutolol. Similarly plasma renin activity, in both lying and standing subjects, was not changed by the placebo, but it was greatly reduced by acebutolol. In the 33 patients studied, the arterial pressure returned to normal in 13 cases (39 p.cent), an improvement was obtained in 12 cases (36 p.cent) but in 8 cases (24 p.cent) the hypertension was not modified by acebutolol. The tolerance to acebutolol was excellent in all cases. No relationship was found between the hypotensive effect of acebutolol and the heart rate or its augmentation induced by orthostatism nor with the levels of plasma renin activity.
Acebutolol
Plasma renin activity
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Fifty hypertensive patients were given a beta-blocker, acebutolol, alone or in association with other hypotensive drugs, in an open therapeutic trial lasting for a year. The results of treatment were considered to be good or moderate in 74 p.cent of the patients. Treatment failures were recorded in 26 p.cent. The mean dosage of acebutolol was 10 mg/kg (maximum 22 mg/kg) and the drug was very well tolerated. Hypertension with an increased cardiac index and reno-vascular hypertension with increased plasma renin activity are good indications for acebutolol.
Acebutolol
Plasma renin activity
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