β‐Adrenoceptor blocking properties and cardioselectivity of M &amp; B 17,803A

Basil, B.; Jordan, Roy; Loveless, A.; Maxwell, D. R.

doi:10.1111/j.1476-5381.1973.tb06906.x

Cited by 98 publications

(51 citation statements)

References 15 publications

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“…The observed cardio-selectivity of acebutolol was comparable with that of practolol as in other studies using anaesthetized dogs (Briant, Dollery, Fenyvesi & George, 1971;Basil et al, 1973) but Baird & Linnell (1972) found this drug to be much less cardioselective in guinea-pigs and there is doubt about its selectivity in man (see Basil et al, 1973;Briant, Dollery, Fenyvesi & George, 1973).…”

Section: Discussionmentioning

confidence: 48%

“…Some of these drugs, notably propranolol, frequently induce respiratory distress in asthmatic subjects, an effect thought to result from block of ,¢adrenoceptors in airways smooth muscle (McNeill, 1964;Richardson & Sterling, 1969 practolol . In clinical trials with asthmatic subjects practolol caused a much lower incidence of respiratory side effects than propranolol (MacDonald & McNeill, 1968;Bernecker & Roetscher, 1970 (Basil, Jordan, Loveless & Maxwell, 1973). The cardioselectivity of practolol and similar agents probably results from differences in the nature of the 3-adrenoceptors in cardiac and airways smooth muscle.…”

mentioning

confidence: 99%

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The SELECTIVITY OF Β‐ADRENOCEPTOR ANTAGONISTS ON CARDIOVASCULAR AND BRONCHODILATOR RESPONSES TO ISOPRENALINE IN THE ANAESTHETIZED DOG

Daly¹,

Flook²,

Levy³

1975

British J Pharmacology

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1The actions of five 1-adrenoceptor antagonists, chosen because of reported differences in their selectivities, were compared using the positive chronotropic, vasodepressor and bronchodilator responses to isoprenaline in anaesthetized dogs. 2 Propranolol was a potent antagonist of the isoprenaline responses in all three systems. 3 Practolol and acebutolol (M & B 17,803) blocked the positive chronotropic responses to isoprenaline to a greater extent than the vasodepressor or bronchodilator responses. 4 Butoxamine and a-methyl dichloroisoprenaline showed the opposite selectivity, blocking the vasodepressor and bronchodilator responses to isoprenaline to a greater extent than positive chronotropic responses. However, both drugs were considerably less potent than the other antagonists studied and their selectivities were less clear-cut than those of practolol or acebutolol. 5 All the antagonists lowered the resting heart rate and to a lesser extent the diastolic blood pressure. The effects of propranolol, practolol and acebutolol on heart rate probably result from cardiac f-adrenoceptor blockade. With butoxamine and a-methyl dichloroisoprenaline, however, the effects on heart rate probably result from a direct cardiodepressant action. 6 The relevance of the results to the problem of the sub-classification of ,B-adrenoceptors is discussed.

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Section: Discussionmentioning

confidence: 48%

mentioning

confidence: 99%

The SELECTIVITY OF Β‐ADRENOCEPTOR ANTAGONISTS ON CARDIOVASCULAR AND BRONCHODILATOR RESPONSES TO ISOPRENALINE IN THE ANAESTHETIZED DOG

Daly¹,

Flook²,

Levy³

1975

British J Pharmacology

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“…The oral doses of propranolol and acebutolol required to halve the potency of intravenous isoprenaline in producing tachycardia were 0.15 and 0.9 mg/kg respectively at 40-80 min, confirming that with the conditions of this experiment the two compounds have ,B-adrenoceptor blocking potency comparable with that seen in other species (Basil et al, 1973b). …”

Section: Introductionsupporting

confidence: 66%

“…Propranolol was the most potent of the drugs tested in reducing the frequency of ectopic beats following methylchloroform and adrenaline administration in the anaesthetized cat and the order of potency (propranolol, acebutolol, prac-tolol) of the 3-adrenoreceptor blocking agents in this test follows their order of potency in inhibiting cardiac 3-receptors (Basil et al, 1973b). Furthermore the doses used, 0.01-2 mg/kg, are low compared to the doses required to revert an established ouabain-induced arrhythmia.…”

Section: Discussionmentioning

confidence: 99%

“…In view of the somewhat surprising difference between acebutolol and propranolol in these experiments, the,-blocking activities of the two compounds were compared following oral administration to the conscious rabbit (Basil et al, 1973b). The oral doses of propranolol and acebutolol required to halve the potency of intravenous isoprenaline in producing tachycardia were 0.15 and 0.9 mg/kg respectively at 40-80 min, confirming that with the conditions of this experiment the two compounds have ,B-adrenoceptor blocking potency comparable with that seen in other species (Basil et al, 1973b).…”

Section: Introductionmentioning

confidence: 99%

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A COMPARISON OF THE EXPERIMENTAL ANTI‐ARRHYTHMIC PROPERTIES OF ACEBUTOLOL: (M & B 17,803), PROPRANOLOL AND PRACTOLOL

Basil

Jordan

Loveless

et al. 1974

British J Pharmacology

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The β‐adrenoceptor blocking agent, acebutolol (M & B 17,803), has been compared with propranolol, practolol, lignocaine and quinidine for its ability to revert or prevent various types of experimental arrhythmias. By intravenous infusion, acebutolol had one half the potency of propranolol in reverting an established ouabain‐induced ventricular arrhythmia in the anaesthetized dog. Practolol was ineffective in the conditions used. High oral doses of acebutolol or propranolol significantly increased the arrhythmic dose of ouabain in the conscious rabbit. Similar doses of practolol produced a significant decrease (i.e. potentiation) in the dose of ouabain required to produce arrhythmia. Lignocaine and quinidine showed no or little activity in this test. Propranolol, acebutolol and practolol were all effective in decreasing the frequency of ectopic beats induced by adrenaline and methylchloroform in the anaesthetized cat. Lignocaine and quinidine were only weakly effective. Acebutolol and propranolol were equally effective either intravenously or orally in reducing the incidence of ventricular fibrillation produced by chloroform in mice. It is suggested that the wide spectrum of experimental anti‐arrhythmic activity of acebutolol coupled with its cardioselectivity may make it an interesting compound in the treatment of cardiac arrhythmias in man.

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Acebutolol in supraventricular arrhythmias

Aronow

Camp

Turbow

et al. 1979

Clin Pharma and Therapeutics

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The effect of intravenous acebutolol on supraventricular arrhythmias was evaluated in 20 patients, 5 with chronic obstructive pulmonary disease. A rapid ventricular rate in atrial fibrillation was slowed greater than 15% in all of 10 patients by acebutolol and in none of 5 patients by saline. A rapid ventricular rate in atrial flutter was slowed greater than 15% in all of 6 patients by acebutolol and in none of 3 patients by saline. Frequent premature atrial beats were abolished or reduced by greater than 75% in each of 2 patients by acebutolol and not in a patient by saline. Acebutolol converted multifocal atrial tachycardia to sinus rhythm in a patient. Digitalis-induced nonparoxysmal atrioventricular junctional tachycardia was not affected by saline but was abolished by acebutolol in a patient. Acebutolol was well tolerated in each of 5 patients with chronic obstructive pulmonary disease. Acebutolol is useful in the treatment of supraventricular arrhythmias.

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β‐Adrenoceptor blocking properties and cardioselectivity of M & B 17,803A

Cited by 98 publications

References 15 publications

The SELECTIVITY OF Β‐ADRENOCEPTOR ANTAGONISTS ON CARDIOVASCULAR AND BRONCHODILATOR RESPONSES TO ISOPRENALINE IN THE ANAESTHETIZED DOG

The SELECTIVITY OF Β‐ADRENOCEPTOR ANTAGONISTS ON CARDIOVASCULAR AND BRONCHODILATOR RESPONSES TO ISOPRENALINE IN THE ANAESTHETIZED DOG

A COMPARISON OF THE EXPERIMENTAL ANTI‐ARRHYTHMIC PROPERTIES OF ACEBUTOLOL: (M & B 17,803), PROPRANOLOL AND PRACTOLOL

Acebutolol in supraventricular arrhythmias

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