Comparison of Adrenergic Beta-blocking Drugs in Angina Pectoris

Sharma, B; Meeran, M K; Galvin, Margaret; Tulpule, Anil; Whitaker, William; Taylor, Stanley H.

doi:10.1136/bmj.3.5767.152

Cited by 18 publications

(10 citation statements)

References 17 publications

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“…Sharma et al (16) have shown that the duration of relief from exerciseinduced anginal pain can be closely correlated with the magnitude and duration of beta blockade. In hypertension the relationship between therapeutic response and beta blockade is less clear but it is likely that the antihypertensive property of beta-receptor antagonists is related, at least in part, to the blockade of beta-adrenergic receptors in the heart.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetic and pharmacodynamic studies of single oral doses of metoprolol in normal volunteers

Kendall¹,

Brown²,

Grieve

et al. 1977

European Journal of Drug Metabolism and Pharmacokinetics

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The effects of three orally administered doses of metoprolol, a beta 1 adrenoceptor antagonist, on resting blood pressures, resting pulse rates and heart rates during maximum exercise have been compared with those of placebo in six healthy male volunteers.The differences in blood pressures and pulse rates at rest were small and only statistically significant at isolated time points during the 24 hours study period. The reduction in exercise heart rates reached maximum values at 1.5 to 2 hours after drug administration and thereafter increased linearly with time. The zero-order rate constants for this process were similar for each of the three doses investigated.The mean durations of beta blockade after oral administration of 50,100 and 200 mg. were 13.2,16.9 and 19.2 hours, respectively. An apparent linear relationship between exercise heart rate and logarithm of the drug concentration in plasma was observed for each dose studied.The relationship between area under the plasma concentration curve and dose is statistically compatible with a linear function in the range 50 to 200 mg. The actual areas, however, suggest the possibility of an increased bioavailability for the higher dose.The significance of these results is discussed in relation to the possible use of a single daily dosage regimen in the treatment of angina pectoris and hypertension. IntraductionMetoprolol (Lopresor®, Ciba-Geigy) is a selective beta-adrenergic receptor blocking drug which has been shown to be effectivein the treatment of angina pectoris (1) and hypertension (2). One of the main problems in the management of these conditions is lack of compliance by patients with long-term oral therapy. Compliance is influenced by a number of factors, including the nature and duration of the illness, the treatment administered, the incidence and severity of drug related side-effects,and the frequency of daily dosage.The incidence of side-effectswith beta-receptor blocking drugs is low and unlikely to reduce compliance. Frequency of dosing, however, appears to be an important determinant (3) and simplification of the dosage Send reprint requests to: regimen could lead to a significantimprovement in overall compliance. Most beta-blocking drugs are recommended to be taken two, three or four times a day depending on the elimination half-life of the drug in plasma. Recent studies (4) (5) with other beta-blocking drugs have shown that effective control of blood pressure can be achieved with once daily dosage regimens. Before recommending a similar regimen for metoprolol it would be desirable to have data comparing the efficacy of different dosage regimens in the treatment of angina and hypertension.In the present study the effects of single oral doses of 50, 100 and 200 mg. metoprolol on resting blood pressures, pulse rate and heart rate during maximum dynamic exercise, were compared with those of placebo in healthy volunteers. The plasma concentration and urinary excretion profiles for the three oral doses of metoprolol were also compared to determine whethe...

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetic and pharmacodynamic studies of single oral doses of metoprolol in normal volunteers

Kendall¹,

Brown²,

Grieve

et al. 1977

European Journal of Drug Metabolism and Pharmacokinetics

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“…This has been done for oxprenolol against other 5-blocking agents (e.g. Sharma et al, 1971). It is as effective in angina pectoris as other drugs of its class.…”

Section: Discussionmentioning

confidence: 99%

Comparative trial of perhexiline maleate and oxprenolol in patients with angina pectoris

Pilcher¹

1978

Postgraduate Medical Journal

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Summary A random single-blind study of oxprenolol against perhexiline has been undertaken in angina pectoris. Both drugs were effective in treatment (P<0·01) but perhexiline was better than oxprenolol (P<0·05), 12 of the 14 patients preferring perhexiline. Offset against this was the greater incidence of side effects with perhexiline, including one patient who later developed peripheral neuropathy. Despite the greater efficacy of perhexiline, it is suggested that side effects should preclude its routine prescription as a drug of first choice in angina pectoris. It should remain of value in the special situations of resistant angina and angina with heart failure or bronchospasm, when its use should be carefully monitored for these side effects.

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“…Approximately a century later chemotherapeutic measures were introduced by two English physicians. Lauder Brunton, in 1867, used amyl nitrite to relieve (Sharma et al, 1971;Aronow, 1976;Conolly et al, 1976;Prichard, 1976;Short, 1977). A number of P-adrenoceptor antagonists have been developed.…”

Section: Discussionmentioning

confidence: 99%

Improved physical performance as a therapeutic objective in patients with angina.

Ling¹,

Groel²

1979

Brit J Clinical Pharma

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1 Improvement in physical performance, based on exercise tolerance, self-assessed work and physician-rated functional capacities, is proposed as a measure of efficacy of anti-anginal therapy in the rehabilitation of the cardiac patient. 2 Improved physical performance parallels changes in frequency of anginal attacks and a nitroglycerin requirements following P-blocker therapy. 3 Nadolol (a P-blocker), given once daily is as effective as propranolol, given four times daily as an anti-anginal agent.

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Comparison of Adrenergic Beta-blocking Drugs in Angina Pectoris

Cited by 18 publications

References 17 publications

Pharmacokinetic and pharmacodynamic studies of single oral doses of metoprolol in normal volunteers

Pharmacokinetic and pharmacodynamic studies of single oral doses of metoprolol in normal volunteers

Comparative trial of perhexiline maleate and oxprenolol in patients with angina pectoris

Improved physical performance as a therapeutic objective in patients with angina.

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