How intrinsic sympathomimetic activity modulates the haemodynamic responses to beta‐adrenoceptor antagonists. A clue to the nature of their antihypertensive mechanism.

Veld, A. J. Man In 'T; Schalekamp, M. A. D. H.

doi:10.1111/j.1365-2125.1982.tb01922.x

Cited by 93 publications

(27 citation statements)

References 107 publications

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“…Pindolol, the ,-adrenoceptor antagonist with the most prominent ISA, limits the bradycardia seen with non-ISA 3-adrenoceptor blockers (Carruthers & Twum-Barima, 1981 Veld & Schalekamp, 1982;Gibson, 1974;Atterhog et al, 1976), rises in resting pulmonary capillary wedge pressure are attenuated (Majid et al, 1970) and systemic vascular resistance is reduced rather than increased (Svensson et al, 1981).…”

Section: Introductionmentioning

confidence: 99%

Cardiac effects of beta‐adrenoceptor blockade with intrinsic sympathomimetic activity during submaximal exercise.

Ades

1987

Brit J Clinical Pharma

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1. beta‐adrenoceptor blocking agents with intrinsic sympathomimetic activity (ISA) are characterized by lesser depression of cardiac performance during low levels of sympathetic stimulation than beta‐ adrenoceptor blocking agents lacking ISA. Studies of the effects of ISA on cardiac output and on the determinants of myocardial oxygen demand during submaximal exercise are described and distinct differences between beta‐adrenoceptor antagonists with and without ISA emerge. 2. At doses which produce similar effects on maximal exercise heart rate, and resting and exercise systolic blood pressure, pindolol, a beta‐ adrenoceptor blocking agent with substantial ISA, allows a higher submaximal exercise cardiac output and submaximal heart rate X systolic blood pressure product than does propranolol, a beta‐adrenoceptor antagonist without ISA. 3. These findings may have clinical relevance in specific groups of patients such as those with arterial hypertension, where the preservation of cardiac function may allow for a more physiologic exercise response. Implications in patients with coronary artery disease and chronic heart failure await further study.

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Section: Introductionmentioning

confidence: 99%

Cardiac effects of beta‐adrenoceptor blockade with intrinsic sympathomimetic activity during submaximal exercise.

Ades

1987

Brit J Clinical Pharma

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“…[1][2][3][4][5][6][7][8][9][10][11][12][13] The introduction of p3-adrenoceptor antagonists with different so-called "ancillary" pharmacological properties has challenged some of these theories. For example, cardiac output and renin are suppressed to a lesser extent by ,3-adrenoceptor antagonists with a relatively high degree of partial agonist activity as compared with f-adrenoceptor antagonists lacking this property, yet the antihypertensive efficacy of these drugs is the same.2'4'15 Furthermore, for a central mode of action, the drug's penetration of the blood-brain barrier is a prerequisite.…”

mentioning

confidence: 99%

Hemodynamic and hormonal adaptations to beta-adrenoceptor blockade. A 24-hour study of acebutolol, atenolol, pindolol, and propranolol in hypertensive patients.

et al. 1988

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“…The finding of an apparent reduction in plasma noradrenaline following chronic treatment with pindolol (Kirsten etal., 1982) was used as evidence in support of the hypothesis that blockade of prejunctional 3-adrenoceptors is responsible for the hypotensive action of 3-adrenoceptor blockers (Man in' T Veld & Schalekamp, 1982). However, studies claiming to show a fall in plasma noradrenaline with pindolol were either inadequately controlled or based on comparisons with 1-adrenoceptor blockers without ISA (Franz et al, 1980;Kirsten et al, 1982).…”

Section: Introductionmentioning

confidence: 99%

Plasma catecholamines following exercise in hypertensives treated with pindolol: comparison with placebo and metoprolol.

Vandongen¹,

Margetts²,

DeKlerk³

et al. 1986

Brit J Clinical Pharma

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1 This study re-examines the proposal that 3-adrenoceptor blockers with intrinsic sympathomimetic activity decrease plasma noradrenaline levels. 2 Thirteen patients (aged 29-65 years) with uncomplicated essential hypertension were randomly allocated to a three period, double-blind cross-over trial. The treatment periods, each of 3 weeks duration, were composed of placebo, pindolol (5 mg twice daily) and metoprolol (100 mg twice daily), dispensed in identical capsules. At the end of each treatment period, patients were exercised on a bicycle ergometer to a predetermined workload. Blood pressure and heart rate were measured before, immediately on completion of exercise and after 10 min post-exercise rest. Blood samples for plasma noradrenaline and adrenaline determination were also collected at these times. 3 Blood pressures were similar during treatment with pindolol and metoprolol. As expected, heart rate was consistently lower during metoprolol treatment. 4 Basal, pre-exercise plasma noradrenaline and adrenaline were similar at the end of each treatment period. However, the increase following exercise was significantly greater during metoprolol treatment. The post-exercise increase during pindolol treatment was indistinguishable from that in the placebo period. 5 These findings, in a randomised placebo-controlled study, therefore demonstrate that pindolol does not influence basal or exercise-stimulated plasma noradrenaline and adrenaline concentrations. This is best explained by a lack of effect of pindolol on the plasma clearance of catecholamines, which is impaired by ,-adrenoceptor blockers devoid of intrinsic sympathomimetic activity.

show abstract

How intrinsic sympathomimetic activity modulates the haemodynamic responses to beta‐adrenoceptor antagonists. A clue to the nature of their antihypertensive mechanism.

Cited by 93 publications

References 107 publications

Cardiac effects of beta‐adrenoceptor blockade with intrinsic sympathomimetic activity during submaximal exercise.

Cardiac effects of beta‐adrenoceptor blockade with intrinsic sympathomimetic activity during submaximal exercise.

Hemodynamic and hormonal adaptations to beta-adrenoceptor blockade. A 24-hour study of acebutolol, atenolol, pindolol, and propranolol in hypertensive patients.

Plasma catecholamines following exercise in hypertensives treated with pindolol: comparison with placebo and metoprolol.

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