Comparison of the efficacy and pharmacokinetics of conventional propranolol and a long acting preparation of propranolol.

Leahey, William J.; Neill, JD; Varma, M. P. S.; Shanks, R. G.

doi:10.1111/j.1365-2125.1980.tb04793.x

Cited by 57 publications

(39 citation statements)

References 15 publications

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“…Studies with LA prppranolol have clearly shown that after 160 mg of this formulation there is a significantly greater reduction in an exercise tachycardia at 24 h than with the conventional formulation (Leahey et al, 1980a). Similar studies have shown that there is no significant difference in the effects of 160 mg oxprenolol and 160 mg SR oxprenolol on an exercise tachycardia 24 h after administration and neither produces a significant reduction in the exercise tachycardia at this time (Leahey et al, 1980b;Bobik, Jennings, Korner, Ashley & Jackman, 1979).…”

Section: Discussionsupporting

confidence: 51%

“…Attention has been paid recently to the administration of the total daily dose of f3-adrenoceptor blocking drugs as a single dose. The administration of propranolol as a single dose each 24 h has been shown to control arterial pressure throughout this period (Wilson, Morgan & Morgan, 1976;Douglas-Jones, Baber & Lee, 1978) but at the end of the dose interval, the degree of cardiac /8-adrenergic receptor blockade will probably be small (Leahey et al, 1980a).…”

Section: Discussionmentioning

confidence: 99%

“…metoprolol have a short elimination half-life of 2-3 h and consequently should be taken every 6 to 8 h. Even drugs with a long elimination half-life (8-12 h) such as atenolol and sotalol may still be better taken 12 hourly. As increasing attention has been given in recent years to the problem of drug compliance in diseases such as hypertension and angina, slow release preparations of S-adrenoceptor blocking 0306-5251/81/020171-10 $01.00 drugs have become available to facilitate once-a-day administration (Leahey, Neill, Varma and Shanks, 1980a).…”

mentioning

confidence: 99%

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Observation on the efficacy and pharmacokinetics of betaxolol (SL 75212), a cardioselective beta‐adrenoceptor blocking drug.

Balnave¹,

Neill²,

Russell³

et al. 1981

Brit J Clinical Pharma

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1 Observations were made in five subjects who exercised before and at 2, 3, 6, 8, 24, 33 and 48 h after the oral administration of placebo and 5, 10,20 and 40 mg betaxolol. 2 The exercise heart rate remained constant at all times after the placebo. All doses of betaxolol significantly reduced the exercise tachycardia at all times. The maximum effect (34.4 + 2.2%) occurred after 40 mg.3 There was a small decline in effect from the peak to 24 h when 40 mg produced a 23.3+2.7% reduction and a further decline to 48 h when there was a 14.6 + 1.8% reduction. 4 Plasma levels of betaxolol were measured in these studies. The peak plasma concentration occurred between 3 and 8 h with different doses. The plasma elimination half-lives after 10, 20 and 40 mg were 11.4 + 2.5, 15.9 + 4.9 and 15.1 + 3.1 h. 5 The effects of 40 mg betaxolol, 200 mg atenolol, 160 mg propranolol, 160 mg oxprenolol, 400 mg sotalol and placebo on an exercise tachycardia were compared in five subjects who received all treatments in random order. 6 There was no significant difference in the maximum reduction produced in an exercise tachycardia by the different drugs. 7 The effect of all drugs decreased with time. The effect of oxprenolol had worn off at 24 h but at 48 h only atenolol and betaxolol produced significant reductions in the exercise tachycardia. 8 Plasma concentrations of the different drugs were measured and plasma elimination half-lives determined. The half-life for betaxolol was 24.5 h which was longer than that for any of the other drugs. 9 These observations show that betaxolol is a potent f-adrenoceptor antagonist with a long duration of effect on an exercise tachycardia and a long plasma elimination half-life.

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Section: Discussionsupporting

confidence: 51%

Section: Discussionmentioning

confidence: 99%

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confidence: 99%

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Observation on the efficacy and pharmacokinetics of betaxolol (SL 75212), a cardioselective beta‐adrenoceptor blocking drug.

Balnave¹,

Neill²,

Russell³

et al. 1981

Brit J Clinical Pharma

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“…Arthur et al (1985) examined propranolol levels in 10 cirrhotic patients who were given 160 mg daily of a long acting preparation for 7 days. A steady state was established after 3 days and levels in most patients were must higher than control data obtained from the literature (Leahey et al, 1980). In the present study detailed information on the pharmacokinetics of propranolol have been obtained by using an acute intravenous dose and two different oral doses to produce steady state.…”

Section: Discussionmentioning

confidence: 92%

“…In normal subjects a long acting preparation of propranolol that is taken once daily, has been shown to produce plasma concentrations which maintain significant 3-adrenoceptor blockade throughout the dose interval (Leahey et al, 1980 …”

Section: Introductionmentioning

confidence: 99%

A comparative pharmacokinetic study of conventional propranolol and long acting preparation of propranolol in patients with cirrhosis and normal controls.

Watson

Bastain

Larkin

et al. 1987

Brit J Clinical Pharma

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1 Six male patients with alcoholic cirrhosis and seven normal control subjects were each given 80 mg twice daily of conventional propranolol for 1 week and 160 mg once daily of a long acting preparation (LA) of propranolol for 1 week. 2 Plasma propranolol levels were measured at regular intervals on the first and seventh days of both weeks and also following an acute intravenous infusion of 10 mg propranolol on a separate occasion. 3 After the single intravenous dose the elimination half‐life tended to be prolonged in the cirrhotic group (median 7.15 h) compared with controls (median 2.92 h) (P = 0.055). 4 After multiple oral dosing with 80 mg twice daily of conventional propranolol the steady‐state plasma concentration (Css), area under the curve (AUC tau), peak concentration (Cmax) and trough concentration (Cmin) were significantly higher in cirrhotic patients and the peak: trough ratio (Cmax/Cmin) was significantly lower than controls. 5 After multiple oral dosing with 160 mg LA once daily Cmin was significantly higher than Cmax/min significantly lower in cirrhotic patients; Css, AUC and Cmax were higher than controls but not statistically different. 6 Within both subject groups the bioavailability of 80 mg twice daily of conventional propranolol tended to be greater than 160 mg LA once daily. Cmax was significantly higher in both groups and Css higher in the cirrhotic group with conventional propranolol. 7 In the cirrhotic group the mean reduction in supine heart rate in the steady state was 31.8% with conventional 80 mg twice daily propranolol and 23.75% with 160 mg LA once daily.(ABSTRACT TRUNCATED AT 250 WORDS)

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Propranolol has direct antithyroid activity: Inhibition of iodide transport in cultured thyroid follicles

Murakami

Nasu

Fukayama

et al. 1993

Cell Biochemistry & Function

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The effect of propranolol on the process of thyroid hormone formation was studied in a physiological culture system. Porcine thyroid follicles were preincubated with propranolol for 24 h. Iodide transport, iodine organification, and de novo thyroid hormone formation were measured by incubating these follicles with the mixture of carrier-free 0.1 microCi Na125I and 50 nM NaI for 2 to 6 h at 37 degrees C. A concentration of propranolol greater than 100 microM inhibited iodide transport in a dose-dependent manner; this inhibition was non-competitive with iodide and independent of thyrotropin (TSH). Reduced iodine organification and thyroid hormone formation was seen with 150 microM propranolol or greater. The inhibitory action of propranolol was not caused by beta-blocking activity, since D-propranolol (devoid of beta-blocking activity) inhibited iodide transport, and other beta-blockers (metoprolol, atenolol, and labetalol) did not inhibit iodide transport. The inhibition of iodide transport was most likely caused by membrane stabilizing activity since quinidine, which possesses the same membrane stabilizing activity as propranolol, also inhibited iodide transport. TSH-mediated cAMP generation and Na+K+ ATPase activity, membrane functions for iodide transport, were unaffected by propranolol. Our study has shown, for the first time, that propranolol has a direct antithyroid action, namely inhibition of iodide transport in the intact thyroid follicle.

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Comparison of the efficacy and pharmacokinetics of conventional propranolol and a long acting preparation of propranolol.

Cited by 57 publications

References 15 publications

Observation on the efficacy and pharmacokinetics of betaxolol (SL 75212), a cardioselective beta‐adrenoceptor blocking drug.

Observation on the efficacy and pharmacokinetics of betaxolol (SL 75212), a cardioselective beta‐adrenoceptor blocking drug.

A comparative pharmacokinetic study of conventional propranolol and long acting preparation of propranolol in patients with cirrhosis and normal controls.

Propranolol has direct antithyroid activity: Inhibition of iodide transport in cultured thyroid follicles

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