Assessment of selective β‐adrenoceptor blockade in man

Briant, Robin; Dollery, C. T.; Fenyvesi, T; George, Charles F.

doi:10.1111/j.1476-5381.1973.tb08272.x

Cited by 55 publications

(22 citation statements)

References 26 publications

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“…Surprisingly, the lower dose of acebutolol showed a considerable blockade of isoprenaline tachycardia but only very weak antagonism of the drop in diastolic blood pressure, whereas the higher dose produced approximately the same effects as propranolol, 0.01 mg/kg, on both heart rate and diastolic blood pressure. This apparent non-cardioselectivity of the higher dose of acebutolol is in accordance with the report of Briant, Dollery & George (1974) who also found no cardioselectivity of acebutolol, comparing its effects against isoprenaline tachycardia and vasodilation. On the other hand, acebutolol has been shown to possess cardioselectivity in vitro on human cardiac vs. bronchial 3-adrenoceptors (Harms, 1976a).…”

Section: Plasma Renin Activitysupporting

confidence: 79%

Blockade of isoprenaline‐induced changes in plasma free fatty acids, immunoreactive insulin levels and plasma renin activity in healthy human subjects, by propranolol, pindolol, practolol, atenolol, metoprolol and acebutolol.

Harms¹,

Gooren²,

Spoelstra³

et al. 1978

Brit J Clinical Pharma

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I The effects of intravenously administered propranolol 0.01 and 0.03, pindolol 0.001 and 0.003, practolol 0.12 and 0.36, atenolol 0.03 and 0.09, metoprolol 0.045 and 0.135 and acebutolol 0.12 and 0.36 mg/kg, on isoprenaline-induced changes in heart rate, blood pressure, plasma free fatty acids, immunoreactive insulin plasma levels and plasma renin activity were determined in six healthy human subjects. 2 Propranolol, atenolol and metoprolol had a stronger effect on resting heart rate than practolol, acebutolol and pindolol, probably reflecting differences in intrinsic f,-sympathomimetic activity.Antagonist potencies against isoprenaline-induced changes in heart rate and blood pressure suggested cardioselectivity for practolol, atenolol, metoprolol and the lower dose of acebutolol and noncardioselectivity for propranolol, pindolol and the higher dose of acebutolol. 3 All six f-adrenoceptor blocking agents were able, to a varying extent, to antagonize the isoprenaline-induced increases in plasma free fatty acids and plasma immunoreactive insulin levels. In general, the cardioselective agents were relatively less effective antagonists than the non-cardioselective agents.4 Resting plasma renin activity was reduced by all six fJ-adrenoceptor blocking agents, suggestive of the presence of fJ1-adrenoceptors mediating renin release, but the non-cardioselective agents propranolol and pindolol seemed relatively more effective in antagonizing isoprenaline-induced increases in plasma renin activity than the cardioselective agents, which indicates that 62-adrenoceptors might also be involved.5 The results are compatible with the hypothesis that both #,-and fJ2-adrenoceptors are involved in the regulation oflipolysis, insulin release and renin release.

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Section: Plasma Renin Activitysupporting

confidence: 79%

Blockade of isoprenaline‐induced changes in plasma free fatty acids, immunoreactive insulin levels and plasma renin activity in healthy human subjects, by propranolol, pindolol, practolol, atenolol, metoprolol and acebutolol.

Harms¹,

Gooren²,

Spoelstra³

et al. 1978

Brit J Clinical Pharma

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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%

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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“…Atenolol, the PI-selective adrenoceptor antagonist, had a smaller but nevertheless significant effect on both of these parameters even at a dose of 25 mg; such an effect on diastolic pressure has been reported previously (Conway et al, 1976). Forearm blood flow has been used previously in the assessment of Padrenoceptor antagonists, with either intraarterial isoprenaline (Brick et al, 1968;Briant et al, 1973), or intravenous bolus injections (Mougeot et al, 1981;. During intravenous administration, changes in forearm blood flow may be influenced by proximal cardiovascular changes, for example, in perfusion pressure.…”

Section: Studymentioning

confidence: 99%

Effects of the beta 2‐adrenoceptor antagonist ICI 118,551 on exercise tachycardia and isoprenaline‐induced beta‐adrenoceptor responses in man.

Arnold¹,

O'Connor²,

Riddell³

et al. 1985

Brit J Clinical Pharma

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ICI 118,551, 5 to 80 mg orally, did not significantly alter resting heart rate or blood pressure. In doses less than 40 mg the reduction in exercise tachycardia was under 10 beats/min. ICI 118,551, 10 to 40 mg, did not appear to reduce the maximum rise in systolic pressure with isoprenaline but did attenuate the changes in diastolic pressure, forearm blood flow and finger tremor. It also attenuated the isoprenaline‐induced changes in serum glucose, insulin and potassium. On these observed changes, the effect of ICI 118,551 20 mg was similar to that of 40 mg and of propranolol 10 mg, but greater than that of atenolol 25 mg. An isoprenaline tachycardia was attenuated by all doses of ICI 118,551 studied. After atropine (0.04 mg/kg) ICI 118,551 20 mg still significantly reduced the effects of isoprenaline suggesting that functional beta 2‐adrenoceptors may be present in the human heart. In doses less than 40 mg, ICI 118,551 appears to be a selective and competitive antagonist of beta 2‐adrenoceptors in man.

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Assessment of selective β‐adrenoceptor blockade in man

Cited by 55 publications

References 26 publications

Blockade of isoprenaline‐induced changes in plasma free fatty acids, immunoreactive insulin levels and plasma renin activity in healthy human subjects, by propranolol, pindolol, practolol, atenolol, metoprolol and acebutolol.

Blockade of isoprenaline‐induced changes in plasma free fatty acids, immunoreactive insulin levels and plasma renin activity in healthy human subjects, by propranolol, pindolol, practolol, atenolol, metoprolol and acebutolol.

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

Effects of the beta 2‐adrenoceptor antagonist ICI 118,551 on exercise tachycardia and isoprenaline‐induced beta‐adrenoceptor responses in man.

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