beta‐Adrenoceptor blocking activity and duration of action of pindolol and propranolol in healthy volunteers.

Aellig, W. H.

doi:10.1111/j.1365-2125.1976.tb00600.x

Cited by 68 publications

(44 citation statements)

References 11 publications

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“…Higher starting doses were used after administration of the ,-adrenoceptor blocking drugs. From the isoprenaline dose-response curves the dose of isoprenaline required to increase heart rate to 120 beats/min was determined, as described previously (Aellig, 1976). Dose-response relationship of oral doses from 0.5 to 10 mg in comparison with 5 and 15 mg pindolol on exercise-induced tachycardia Six volunteers with a mean age of 27 + 1 years and a mean body weight of 75 ± 4 kg received oral doses of 0.5 and 2 mg of bopindolol and 5 and 15 mg of pindolol in randomised order.…”

Section: Methodsmentioning

confidence: 99%

Pharmacological experiments in healthy volunteers with bopindolol, a long‐acting beta‐adrenoceptor blocking drug with partial agonist activity.

Aellig¹

1985

Brit J Clinical Pharma

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1 Bopindolol is a potent and specific ,3-adrenoceptor antagonist with partial agonist activity. In animal experiments it blocks both ,Bl-and P2-adrenoceptors and possesses a long duration of action. In the present study in healthy volunteers bopindolol was about ten times more potent than pindolol in reducing isoprenaline-induced and exerciseinduced tachycardia.2 In experiments on exercise-induced tachycardia an oral dose of 2 mg produced a near maximum reduction of exercise heart rate, occurring within 2 to 3 h of administration. With higher doses (up to 12 mg) the maximum effect was reached earlier (between 1 and 2 h). The long duration of action of bopindolol observed in animal studies was confirmed in man. Twenty-four hours after 4 and 10 mg bopindolol more than 2/3 of the maximum effect was still present. After 48 h 38% of the maximum effect of 4 mg and 50% of that of 12 mg remained. Even at 72 and 96 h exercise-induced tachycardia was still significantly lowered after both doses of the drug. 3 When bopindolol was administered once daily for 5 days there was a slight increase in the maximum reduction of exercise-induced tachycardia during treatment with 1 mg/day but not with 4 mg/day, which produced a near maximum effect.

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Section: Methodsmentioning

confidence: 99%

Pharmacological experiments in healthy volunteers with bopindolol, a long‐acting beta‐adrenoceptor blocking drug with partial agonist activity.

Aellig¹

1985

Brit J Clinical Pharma

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“…This formula can be applied when intravenous data are not available and when the drug is eliminated mainly by metabolism as in the case of oxprenolol (Riess et al, 1975). Since pindolol (LB 46, Viskeng), a P-adrenoceptor blocking agent (Aellig, 1976a), is metabolized in man to only a moderate extent and is mainly excreted unchanged in the urine (Gugler, Herold & Dengler, 1974), it was of interest to review published and unpublished pharmacokinetic data on this compound in order to ascertain whether or not it is subject to an appreciable first-pass effect.…”

Section: Pindolol Ap-adrenoceptor Blocking Agent With a Negligible Fmentioning

confidence: 99%

Pindolol, a beta‐adrenoceptor blocking agent with a negligible first‐ pass effect.

Meier¹,

Nüesch²

1977

Brit J Clinical Pharma

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“…Although observations in patients with hypertension have shown that satisfactory control of arterial pressure can be obtained throughout a 24 h period with twice daily administration (Berglund, Anderson, Habssen & Olander, 1973) and even once daily administration of propranolol (Wilson, Morgan & Morgan, 1976;Douglas-Jones, Baber & Lee, 1978), this may not be an effective regime for other 0306-5251/80/010033-08 $01.00 conditions such as angina or cardiac arrhythmias where the therapeutic effect may be more directly related to cardiac JJ-adrenoceptor blockade which is not maintained over 24 h after single dose of 100 mg propranolol (Aellig, 1976). Although a therapeutic effect with propranolol may be obtained in hypertension by giving the total daily amount as a single dose once per day, high plasma levels will occur shortly after administration which may produce adverse effects.…”

Section: Introductionmentioning

confidence: 99%

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

Leahey¹,

Neill²,

Varma³

et al. 1980

Brit J Clinical Pharma

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1 Plasma levels of propranolol were measured at intervals after the oral administration of 160 mg propranolol and 160 mg L.A. propranolol in ten subjects who received both drugs on separate occasions.2 Mean peak plasma concentration of propranolol occurred 2 h after propranolol and 10 h after the L.A. formulation; the peak concentration with the former was four times that with the latter. At 24 h the plasma level was significantly higher after L.A. propranolol. 3 Observations were made in nine healthy volunteers who exercised before and at intervals after the oral administration of 160 mg propranolol and 160 mg L.A. propranolol.4 Propranolol produced a maximum reduction (27.84 + 2.4%) in the exercise tachycardia at 3 h and L.A. propranolol a maximum reduction (22.00 + 1.73%) at 6 h. The effects at 24 h were 9.24 + 1.55 and 16.79 + 2.16% respectively.5 Five subjects were given 160 mg propranolol as a single dose daily for 8 days and on a separate occasion similar treatment with L.A. propranolol. Subjects were exercised and blood samples were taken before and 3 h after each dose on days 1 to 5 and on day 8. propranolol were 12.5 to 17.5 (trough values) and 18.4 to 50.0 (peak values) ng/ml. 8 These observations show that the new long acting formulation of propranolol produces a significant reduction of an exercise tachycardia throughout a 24 h period without a very high initial effect during single and multiple dosing. This formulation should be suitable for once a day administration.

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beta‐Adrenoceptor blocking activity and duration of action of pindolol and propranolol in healthy volunteers.

Cited by 68 publications

References 11 publications

Pharmacological experiments in healthy volunteers with bopindolol, a long‐acting beta‐adrenoceptor blocking drug with partial agonist activity.

Pharmacological experiments in healthy volunteers with bopindolol, a long‐acting beta‐adrenoceptor blocking drug with partial agonist activity.

Pindolol, a beta‐adrenoceptor blocking agent with a negligible first‐ pass effect.

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

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