Speed of onset of pharmacodynamic activity of propranolol, practolol, oxprenolol and metoprolol after intravenous infection in man.

Lochan, Rajiv; Silke, Bernard; Taylor, S. H.

doi:10.1111/j.1365-2125.1981.tb01295.x

Cited by 10 publications

(1 citation statement)

References 16 publications

(9 reference statements)

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“…We have previously demonstrated that attenuation of catecholamine stimulation of cardiac,8-adrenoceptors is substantial, although not necessarily maximal, by 4-5 min following i.v. bolus of four,-adrenoceptor antagonists (Lochan et al, 1981). Thus changes induced in haemodynamic variables at the times of the haemodynamic measurements in the present study are likely to reflect the pharmacodynamic activity of the drug.…”

Section: Discussionmentioning

confidence: 64%

Haemodynamic dose‐response effects of i.v. penbutolol in angina pectoris.

Silke¹,

Verma²,

Hussain³

et al. 1983

Brit J Clinical Pharma

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1 The haemodynamic dose-response effects of intravenous penbutolol, a newer ,3-adrenoceptor antagonist with intrinsic sympathomimetic activity but without cardioselectivity, were evaluated in 10 patients with angiographically documented coronary artery disease.2 Following four logarithmetically cumulative i.v. boluses (0.5-4 mg dosage range) there was a log linear increase in plasma penbutolol concentration; the levels achieved (51 + 8 to 219 + 19 ng/ml) were in the therapeutic range (12 to 250 ng/ml). 3 Penbutolol resulted in a linear decrease in heart rate (maximum AHR -4 beats/min; P < 0.01); there was a small increase in pulmonary artery occluded pressure which reached its maximum at the lower doses (maximum APAOP + lmm Hg; P < 0.01). The resting cardiac output, blood pressure and calculated systemic vascular resistance were unchanged. 4 During 4 min steady-state supine bicycle exercise there was attenuation of exercise cardiac output (AC.I. -0.6 1 min-' m-2; P < 0.01) and systolic pressor response (ASBP -13 mm Hg; P < 0.01) compared with control observations without change in other measured or derived variables.5 The haemodynamic profile of penbutolol compared favourably with other ,8-adrenoceptor antagonists previously evaluated under similar conditions in patients with ischaemic heart disease. Over the i.v. dose-range evaluated penbutolol attenuated exercise-induced angina with a relatively modest depression of cardiac performance; the small change induced in resting haemodynamic variables may, in part, have been contributed to by the intrinsic sympathomimetic activity of penbutolol.

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Section: Discussionmentioning

confidence: 64%

Haemodynamic dose‐response effects of i.v. penbutolol in angina pectoris.

Silke¹,

Verma²,

Hussain³

et al. 1983

Brit J Clinical Pharma

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Controlled Beta‐Receptor Blockade with Esmolol and Flestolol

Murthy

Frishman

1988

Pharmacotherapy

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Beta-receptor-blocking agents are commonly used in the management of various cardiovascular diseases. Recently, esmolol, a pharmacokinetically novel cardioselective beta-receptor-blocking agent, has been introduced for use in the treatment of critically ill patients. It is devoid of intrinsic sympathomimetic activity and in doses used clinically, it has no direct depressant effect on the heart. Esmolol is an ester and is metabolized by choline-esterase to ASL 8123, an inactive molecule. Esmolol has an elimination half-life of nine minutes which accounts for its ultrashort duration of action. This unique pharmacokinetic property provides two advantages over other longer-acting beta-receptor-blocking agents. First, the magnitude of beta-receptor blockade can be titrated to a desired level. Second, if adverse effects are experienced, reducing the dosage or terminating the infusion results in rapid reversal of its pharmacological effects. Another ultrashort-acting, non-cardioselective beta-receptor blocking agent, flestolol is undergoing clinical evaluation. Esmolol has been approved for the management of supraventricular tachycardia. The clinical safety of these novel drugs will expand the use of beta-receptor-blocking agents in the management of cardiovascular diseases in critically ill patients.

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Comparison of the acute haemodynamic effects of bopindolol and propranolol at rest and during supine exercise

Fitscha¹,

Meisner²,

Tiso³

1988

Eur J Clin Pharmacol

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The acute cardiovascular effects of two beta-adrenoceptor blocking agents, bopindolol and propranolol, were compared in a randomized study in 16 male patients with coronary heart disease. All patients had had an uncomplicated acute myocardial infarction at least 8 weeks earlier. The two drugs reduced the arterial blood pressure to the same extent, both at rest and during exercise. As heart rate and stroke volume were also decreased, cardiac output was reduced, whereas systemic vascular resistance was increased at rest and during exercise. Left ventricular filling pressure was increased. No statistically significant differences in these variables were seen between the two groups.

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Speed of onset of pharmacodynamic activity of propranolol, practolol, oxprenolol and metoprolol after intravenous infection in man.

Cited by 10 publications

References 16 publications

Haemodynamic dose‐response effects of i.v. penbutolol in angina pectoris.

Haemodynamic dose‐response effects of i.v. penbutolol in angina pectoris.

Controlled Beta‐Receptor Blockade with Esmolol and Flestolol

Comparison of the acute haemodynamic effects of bopindolol and propranolol at rest and during supine exercise

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