Clinical pharmacology of the new beta-adrenergic blocking drugs. Part 6. A comparison of pindolol and propranolol in treatment of patients with angina pectoris. The role of intrinsic sympathomimetic activity

Frishman, William H.; Kostis, John B.; Strom, Joel A.; Hossler, Maryhelen; Elkayam, Uri; Goldner, Susan; Silverman, Ralph; Davis, Richard; Weinstein, Jerome; Eh, Sonnenblick

doi:10.1016/0002-8703(79)90261-8

Cited by 67 publications

(27 citation statements)

References 24 publications

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“…During exercise the reduction in heart rate is much greater than any positive chronotropic action arising from partial agonist activity and there will still be a marked reduction in heart rate after a ,8-adrenoceptor blocking drug with partial agonist activity. The present observations confirm these ideas as propranolol but not pindolol reduced supine heart rate following acute oral administration and are in agreement with previous studies (Aellig, 1976;Frishman et al, 1979;Svendsen etal., 1980;Svendsen & Hartling, 1981). Both drugs reduced exercise tachycardia.…”

Section: Discussionsupporting

confidence: 94%

Comparison of the effect of pindolol and propranolol on heart rate after acute and chronic administration.

Finch¹,

O'Connor²,

Harron³

et al. 1983

Brit J Clinical Pharma

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1 The present study compared the effects in healthy volunteers of the acute and chronic administration of placebo, pindolol and propranolol to see if the partial agonist activity of pindolol was reduced by the ,8-adrenoceptor blocking activity of pindolol on chronic administration.2 Five subjects received in random order for 8 days placebo, propranolol 160mg and pindolol 10mg; on days 1 and 8 treatments were given twice at 0 and 2 h. Heart rate in supine position and at end of exercise was recorded before dosing and at 2 and 4 h post-dosing on days 1 and 8. 3 Propranolol and pindolol reduced exercise heart rate to the same extent on days 1 and 8. 4 Propranolol reduced supine heart rate more than pindolol on days 1 and 8 but the difference was only significant on day 8.

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Section: Discussionsupporting

confidence: 94%

Comparison of the effect of pindolol and propranolol on heart rate after acute and chronic administration.

Finch¹,

O'Connor²,

Harron³

et al. 1983

Brit J Clinical Pharma

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“…Healthy individuals can sustain a heart rate of 40 to 50 without disability, unless there is clinical evidence of heart failure. 23 Drugs with intrinsic sympathomimetic activity do not lower the resting heart rate to the same degree as propranolol 24 ; however, all /3-blocking drugs are contraindicated (unless an artificial pacemaker is present) in patients with the "sick sinus syndrome." 25 If there is a partial or complete atrioventricular conduction defect, use of a /3-blocking drug may lead to a serious bradyarrhythmia.…”

Section: Sinus Node Dysfunction and Atrioventricular Conduction Delaymentioning

confidence: 99%

Beta-adrenergic receptor blockers. Adverse effects and drug interactions.

Frishman

1988

Hypertension

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Adverse effects of beta-adrenergic receptor blocking drugs can be divided into two categories: 1) those that result from known pharmacological consequences of beta-adrenergic receptor blockade; and 2) other reactions that do not appear to result from beta-adrenergic receptor blockade. Adverse effects of the first type include bronchospasm, heart failure, prolonged hypoglycemia, bradycardia, heart block, intermittent claudication, and Raynaud's phenomenon. Neurological reactions include depression, fatigue, and nightmares. It is not yet proven whether the beta 1-selective adrenergic blockers or those with partial agonist activity reduce the overall frequency of adverse reactions seen with propranolol. Patient age does not appear, in itself, to be associated with more beta-blocker side effects. Side effects of the second category are rare. They include an unusual oculomucocutaneous reaction and the possibility of oncogenesis. There are also many drugs that interact with beta-blockers, which may increase toxicity. Finally, there are specific patient characteristics where one beta-blocker may be more effective and safer than another.

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“…Reduced incidence of bradycardia, and negligible changes in cardiac output and peripheral vascular resistance and bronchoconstriction during pindolol treatment when compared to the incidence during propranolol treatment is generally attributed to the intrinsic sympathomimetic activity of pindolol (Dubach, 1975;Frishman et al, 1979). We presumed that the intrinsic sympathomimetic activity would be reflected in a different pattern of plasma catecholamines during treatment than that found during treatment with a P-adrenoceptor blocker devoid of intrinsic sympathomimetic activity.…”

Section: Discussionmentioning

confidence: 94%

Relationship of plasma catecholamines to blood pressure in hypertensive patients during beta‐adrenoceptor blockade with and without intrinsic sympathomimetic activity.

Kirsten¹,

Heintz²,

Böhmer³

et al. 1982

Brit J Clinical Pharma

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1 This study was designed to follow changes in plasma catecholamine concentrations during ,B-adrenoceptor blockade using doses of antagonists which decreased the mean arterial pressure (MAP) by about 15 mm Hg. Noradrenaline, adrenaline and dopamine were radioenzymatically determined in 34 patients with moderate essential hypertension during an 8 week course of treatment with either pindolol (with intrinsic sympathomimetic activity, ISA) or propranolol (without ISA). Plasma catecholamines were determined before and 1, 7, 28 and 56 days after commencement of treatment and 1 week after discontinuation of treatment. 2 After one day of pindolol therapy plasma catecholamine concentrations were decreased, but no decrease in MAP was observed. After one day of propranolol therapy, however, MAP was decreased, but except for increased levels of adrenaline, plasma catecholamines showed no changes. 3 On the 56th day of therapy both 0-adrenoceptor blockers had decreased the MAP. Pindolol therapy had caused a decrease in all three catecholamines whereas propranolol had caused no change except for decreased dopamine levels. 4 One week after cessation of propranolol therapy catecholamines were decreased but the MAP had begun to return to initial values; after cessation of pindolol therapy however, the MAP remained decreased. 5 The dissimilar relationships between blood pressure and catecholamine concentration during pindolol and propranolol therapy are evidence for multiple and different modes of action for P-adrenoceptor blockers with and without ISA. This study demonstrates that catecholamine concentrations were generally decreased during low-dose P-adrenoceptor blocker therapy, with lower catecholamine levels during pindolol treatment than during propranolol treatment.

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Clinical pharmacology of the new beta-adrenergic blocking drugs. Part 6. A comparison of pindolol and propranolol in treatment of patients with angina pectoris. The role of intrinsic sympathomimetic activity

Cited by 67 publications

References 24 publications

Comparison of the effect of pindolol and propranolol on heart rate after acute and chronic administration.

Comparison of the effect of pindolol and propranolol on heart rate after acute and chronic administration.

Beta-adrenergic receptor blockers. Adverse effects and drug interactions.

Relationship of plasma catecholamines to blood pressure in hypertensive patients during beta‐adrenoceptor blockade with and without intrinsic sympathomimetic activity.

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