Hypertensive and Renin-Suppressing Activities of Propranolol in Hypertensive Patients

Leonetti, Gastone; G, Mayer; Morganti, Alberto; Terzoli, L.; Zanchetti, Alberto; Bianchetti, G.; Salle, E. Di; Morselli, P. L.; Chidsey, Charles A.

doi:10.1042/cs0480491

Cited by 83 publications

(38 citation statements)

References 24 publications

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“…Contrary to previous reports (Koch-Weser, 1975) The second objection is that the dose-response and the timing of the response is different for suppression of renin and for control of hypertension (Morgan, Roberts, Carney, Louis & Doyle, 1975). Suppression of plasma renin activity is achieved by relatively small doses, similar to those controlling exercise tachycardia but very large doses are often required for the effective control of hypertension (Leonetti, Mayer, Terzoli, Zanchetti, Bianchetti, Morsalli, Di Salle & Chidsey, 1975). Even the modest hypotensive effect of small doses of propranolol does not follow the plasma renin activity which falls within an hour.…”

Section: Renin and P-adrenoceptor Blockade-the Mechanism Of The Hypotcontrasting

confidence: 41%

Renin and beta‐adenoceptor blockade‐the mechanism of the hypotensive effect?

Hamer¹

1976

Brit J Clinical Pharma

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Section: Renin and P-adrenoceptor Blockade-the Mechanism Of The Hypotcontrasting

confidence: 41%

Renin and beta‐adenoceptor blockade‐the mechanism of the hypotensive effect?

Hamer¹

1976

Brit J Clinical Pharma

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“…Other work suggests that the further reduction in blood pressure after chronic treatment with 8-adrenoceptor antagonists occurs within a few days (Haglund & Collste, 1980;Leonetti et al, 1975).…”

Section: Discussionmentioning

confidence: 99%

The effects of acute or chronic ingestion of propranolol or metoprolol on the physiological responses to prolonged, submaximal exercise in hypertensive men.

Wilcox¹,

Bennett²,

Macdonald³

et al. 1984

Brit J Clinical Pharma

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1 We have studied the physiological responses to 50 min of intermittent, moderate exercise in hypertensive men after the ingestion of a single dose of placebo, propranolol or metoprolol, and also after 28 days treatment. In addition, subjective assessments of mood were made during the last 7 days of each period of chronic treatment. 2 Heart rate and blood pressure, both at rest and during exercise, were significantly reduced by a single dose of propranolol or metoprolol; more marked effects were observed after chronic treatment. 3 Ventilation and gas exchange during exercise were only slightly disturbed by single doses of propranolol or metoprolol, whereas chronic treatment had no effect. 4 Perceived exertion scores were increased after a single dose of either drug, compared to placebo, and the effect of propranolol was greater than that of metoprolol. With chronic treatment there were fewer differences between the perceived exertion scores during exercise, although 'leg' fatigue remained greater after propranolol than after placebo. 5 Sweating from the forehead during exercise was enhanced by a single dose of either f3-adrenoceptor antagonist, with propranolol having the greater effect. After chronic treatment the effect of propranolol was diminished, whereas the effect of metoprolol was maintained. 6 Very few disturbances of mood were found after chronic ingestion of the f8-adrenoceptor antagonists.

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“…The new Oros preparation of metoprolol may prolong the delivery of the drug sufficiently to enable once-daily dosing in some patients (Kendall et al, 1982 matic (Cruickshank, 1983) and important doserelated changes in resting heart rate have not been observed. This is illustrated by the observation that a four-fold increase in propranolol or metoprolol dose was associated with only an additional 5-6 beats/min reduction in resting heart rate (Collste et al, 1980;Leonetti et al, 1975;Serlin et al, 1980). When symptomatic bradycardia follows therapeutic doses of a fadrenoceptor blocker this must in part be due to high vagal tone (Shand, 1975) or to associated cardiac disease.…”

Section: Propranololmentioning

confidence: 99%

Polymorphic metabolism of beta‐adrenoceptor antagonists.

Silas¹,

Lennard²,

Tucker³

et al. 1984

Brit J Clinical Pharma

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Most beta‐adrenoceptor blockers undergo extensive oxidative metabolism. The evidence for polymorphism of the debrisoquine type is reviewed. The AUC and half‐life of metoprolol were considerably greater in poor metabolisers (PM) of debrisoquine than in extensive metabolisers (EM). Metoprolol alpha‐hydroxylation is impaired and O‐dealkylation must also be affected. Polymorphism in the former route has been demonstrated in a population of 143 patients to be directly related to debrisoquine phenotype. Bufuralol AUC and half‐life are much higher in PM than EM subjects. Hydroxylation at the 1 and 4 positions are affected. Genetic polymorphism for 1‐hydroxylation has been shown in family and population studies. Propranolol 4‐hydroxylation is defective in PM subjects of debrisoquine but propranolol AUC is not related to phenotype, presumably because other major pathways are unaffected. Oxidation phenotype correlates well with intensity and duration of beta‐ adrenoceptor blockade after metoprolol, PM subjects requiring only once‐ daily dosing. However, in EM subjects twice‐daily dosing is required even if slow release preparations are used, since plasma metoprolol concentrations may remain negligible 24 h after dosing. The beta‐ adrenoceptor blocking effects of propranolol and bufuralol are unlikely to be influenced by oxidation status. Anecdotal reports of toxicity arising in PM subjects taking metoprolol or propranolol need to be substantiated. However, vomiting after the administration of bufuralol often occurs in poor metabolisers. Metabolic interactions with drugs sharing the same enzyme system are discussed. Debrisoquine and bufuralol competitively inhibit each other's metabolism in vitro. (ABSTRACT TRUNCATED AT 250 WORDS)

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Hypertensive and Renin-Suppressing Activities of Propranolol in Hypertensive Patients

Cited by 83 publications

References 24 publications

Renin and beta‐adenoceptor blockade‐the mechanism of the hypotensive effect?

Renin and beta‐adenoceptor blockade‐the mechanism of the hypotensive effect?

The effects of acute or chronic ingestion of propranolol or metoprolol on the physiological responses to prolonged, submaximal exercise in hypertensive men.

Polymorphic metabolism of beta‐adrenoceptor antagonists.

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