Effects of pindolol and propranolol on beta‐adrenergic receptors on human lymphocytes.

Molinoff, P B; Aarons, R D; Nies, Alan S.; Gerber, J G; Wolfe, B B; Goens, MB

doi:10.1111/j.1365-2125.1982.tb01942.x

Cited by 25 publications

(4 citation statements)

References 1 publication

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“…Absence of f-adrenoceptor antagonist withdrawal hypersensitivity following slow-release oxprenolol was recently reported (Bolli et al, 1981), leading to the suggestion that the phenomenon does not occur after /8-adrenoceptor antagonists possessing partial agonist activity. A similar lack of withdrawal hypersensitivity has been reported in some studies with pindolol (Rangno & Langlois, 1982;Szecsi etal., 1982) and in particular a down regulation of human lymphocyte f-adrenoceptor density has been noted with this drug and attributed to its partial agonist activity (Molinoff et al, 1982). In contrast we have previously reported that the phenomenon does occur after stopping oxprenolol (Ross et al, 1981).…”

Section: Introductionmentioning

confidence: 86%

beta‐Adrenoceptor hypersensitivity after stopping oxprenolol: discrepant findings not attributable to methodology.

Singh¹,

Rimmer²,

Mj³

et al. 1983

Brit J Clinical Pharma

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Using isoprenaline and glyceryl trinitrate (GTN) induced tachycardia we have compared the rebound ,8-adrenoceptor hypersensitivity on stopping slow-release and conventional oxprenolol in young normotensive subjects. Heart rate on standing with GTN rose after stopping slow-release and conventional oxprenolol to peak levels on day 2 or 3 significantly greater than corresponding control levels off treatment on day 5. The isoprenaline CD25 (the dose required to increase heart rate by 25 beats/min) fell after stopping conventional oxprenolol to a significantly lower level on day 3 than the control level off treatment on day 5. Contrary to a recent report describing no rebound 83-adrenoceptor hypersensitivity on stopping slow-release oxprenolol we have demonstrated it after stopping slow release as well as conventional oxprenolol.

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Section: Introductionmentioning

confidence: 86%

beta‐Adrenoceptor hypersensitivity after stopping oxprenolol: discrepant findings not attributable to methodology.

Singh¹,

Rimmer²,

Mj³

et al. 1983

Brit J Clinical Pharma

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“…Chronic ,B-adrenoceptor antagonism usually results in an increase in ,B-adrenoceptors by the process of receptor upregulation (Aarons et al, 1980;Molinoff & Aarons, 1983). In contrast, a reduction in 1adrenoceptor number and down regulation has been reported for 1-adrenoceptor antagonists with marked partial agonist activity (Molinoff et al, 1982;Giudicelli et al, 1984). However, for adimolol there is no previous report of significant partial agonist activity and, from the clinical study, the reduction in resting heart rate also suggests that adimolol does not possess this property.…”

Section: Lmentioning

confidence: 96%

Adimolol, a long acting beta‐adrenoceptor blocker in man.

Elliott

Jones

Deighton

et al. 1987

Brit J Clinical Pharma

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A comparative study in eight healthy normotensive males of the effects on blood pressure, heart rate and beta‐adrenoceptor function following single oral doses of adimolol (600 mg), propranolol (240 mg) and placebo. Both active treatments produced small but significant reductions in blood pressure and heart rate, supine and erect. These effects persisted for up to 7 days after adimolol. The heart rate increases following both dynamic exercise and intravenous isoprenaline were attenuated by both propranolol and adimolol. With adimolol evidence of functional beta‐adrenoceptor antagonism was sustained for up to 7 days. Lymphocyte beta‐adrenoceptor binding studies showed that both adimolol and propranolol significantly reduced affinity for beta‐ adrenoceptors. In addition, adimolol significantly reduced receptor number and even by 3 days after dosing Bmax had only returned to half the control value. In a small sub‐group of subjects there was no evidence to suggest that adimolol had additional alpha‐adrenoceptor antagonist properties. Adimolol was detected in plasma for up to 3 days after dosing. The mean terminal elimination half‐life was 14 h, compared to 3 h for propranolol. This study confirms that adimolol has prolonged beta‐adrenoceptor antagonist activity with effects persisting for up to 7 days after a single dose. The reduction in beta‐ adrenoceptor number following adimolol suggests that this prolonged effect may not be solely due to competitive antagonism but may additionally depend upon non‐competitive antagonism at beta‐ adrenoceptors.

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“…The validity of using peripheral blood lymphocytes as an index of b2-adrenoreceptors in other organs has been established in man and in experimental animals (1,2). The authors have made the assumption that the density of &receptors on peripheral blood mononuclear cells correlates with that found in the splanchnic bed.…”

Section: Commentsmentioning

confidence: 99%

“…The approach is feasible. Indeed, clinical examples have already been published (1)(2)(3)(4). Growing a decision tree and meticulously pruning its branches, probabilities and utilities is hard and timeconsuming work.…”

mentioning

confidence: 99%

β2-Adrenergic receptors in propranolol therapy: Does down-regulation do it?

Burroughs

1987

Hepatology

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The density and affinity of beta‐2‐adrenoceptors on mononuclear cells from peripheral blood were studied in fifteen patients with cirrhosis of different severity and in thirteen controls. There was no significant difference between cirrhotic patients and controls in density or affinity of beta‐2 binding sites. Within the cirrhotic group, however, the number of binding sites per cell was significantly lower in patients with severe ascites than in patients with mild to moderate or no ascites. This down‐regulation of beta‐adrenoceptors could influence the haemodynamic response to beta‐blockers.

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Effects of pindolol and propranolol on beta‐adrenergic receptors on human lymphocytes.

Cited by 25 publications

References 1 publication

beta‐Adrenoceptor hypersensitivity after stopping oxprenolol: discrepant findings not attributable to methodology.

beta‐Adrenoceptor hypersensitivity after stopping oxprenolol: discrepant findings not attributable to methodology.

Adimolol, a long acting beta‐adrenoceptor blocker in man.

β2-Adrenergic receptors in propranolol therapy: Does down-regulation do it?

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