Influence of intrinsic sympathomimetic activity (ISA) during beta‐ adrenoceptor blockade in asthmatics.

Dorow, P

doi:10.1111/j.1365-2125.1982.tb01936.x

Cited by 15 publications

(12 citation statements)

References 2 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…However, Dorrow also showed that, when administered in equipotent doses, propranolol increased bronchial sensitivity to histamine while pindolol and metoprolol did not. 31 Other studies produced similar resultswhen pindolol was administeredintravenously. [32][33][34][35] However, Benson et al, in a study with five asthmatic patients, found that pindolol 5 mg po led to a significant reduction in the FEV compared with placebo."…”

Section: Pulmonary Functionsupporting

confidence: 53%

Intrinsic Sympathomimetic Activity: Physiological Reality or Marketing Phenomenon

Black¹,

Mann²

1984

Drug Intelligence & Clinical Pharmacy

View full text Add to dashboard Cite

Intrinsic sympathomimetic activity (ISA) describes the partial beta-adrenergic agonist responses elicited by a series of beta-adrenergic antagonists. The dual effect on the beta-adrenergic receptor appears to be related to structural specificity of the drugs allowing competitive binding to the receptor (antagonist activity) and partial interaction at the receptor's activation site (agonist activity). The clinical effects of a beta-adrenergic antagonist with ISA depend on the relative balance of the drug's inherent antagonist and agonist activity and on the degree of underlying sympathetic tone in the patient. Theoretically, the agonist activity may be beneficial in the patient in whom beta-adrenergic antagonists are indicated, but who has concomitant bradycardia and/or mild to moderate congestive heart failure or compromised pulmonary function, or in the patient being withdrawn from beta-adrenergic antagonist therapy. There is positive evidence from clinical trials that in select patient populations a few of these benefits of ISA are afforded without compromise to beta-adrenergic antagonist activity. However, predisposing factors such as acute illness and individual idiosyncrasies may interfere with the manifestations of the agonist effects. Further, maximal response to full beta-adrenergic agonists will be diminished by concurrent therapy with beta-adrenergic antagonists regardless of ISA presence. In summary, ISA does have a physiological basis and increased experience in larger patient populations will help to place it in proper clinical perspective.

show abstract

Section: Pulmonary Functionsupporting

confidence: 53%

Intrinsic Sympathomimetic Activity: Physiological Reality or Marketing Phenomenon

Black¹,

Mann²

1984

Drug Intelligence & Clinical Pharmacy

View full text Add to dashboard Cite

show abstract

“…We have previously reported a nega tive influence on different lung function parameters and on the bronchial reactivity of patients with symptom-free bronchial asthma [7], There is evidence that in these patients bronchoconstriction might not be solely induced by mere /3-adrenoceptor blockade [14]. The decrease in mucociliary clearance in coronary patients with a nor mal lung function observed in this study offers an additional factor for the bron chopulmonary risks of propranolol and other propranolol-like drugs.…”

Section: Discussionmentioning

confidence: 68%

“…Pindolol, which blocks //-and //¡-adrenoceptors, exhibits a neutral influ ence on lung function and mucociliary clearance due to its partial agonist activity [7]. Pharmacological studies suggest that the stimulant effects of pindolol are exert ed principally on //¡-adrenoceptors [16].…”

Section: Discussionmentioning

confidence: 99%

“…De fects in mucociliary transport are common in patients with chronic obstructive lung disease [2,3], This type of lung dysfunc tion is often found in patients with coro nary heart disease (CHD), especially when they are smokers [4][5][6]. In these patients, therapy of CHD with /I-adrenoceptorblocking drugs may lead to further deteri oration of mucociliary transport, with in creased deterioration of pulmonary and cardiac function [7].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Influence of Propranolol, Metoprolol, and Pindolol on Mucociliary Clearance in Patients with Coronary Heart Disease

Dorow¹,

Weiss²,

Félix³

et al. 1984

Respiration

View full text Add to dashboard Cite

The effects of the β-adrenoceptor-blocking drugs propranolol, metoprolol, pindolol, and placebo, on mucociliary clearance were studied in three groups of 6 subjects with coronary heart disease and normal lung function. Clearance rates of inhaled ^99mTc-labeled human serum albumin minimicrospheres were determined over the apical right region of the lung with a gamma camera. A 3-day medication of propranolol 40 mg b.i.d., when compared with placebo, led to a significant decrease (p ≤ 0.05) in mucociliary clearance. Metoprolol 50 mg b.i.d. or pindolol 5 mg b.i.d. did not show any influence on mucociliary clearance. Implications for the use of different types of β-adrenoceptor-blocking drugs in the treatment of coronary heart disease are discussed.

show abstract

“…The subject of partial agonist activity and lung function is discussed separately in the same issue of the journal (Louis, 1982;Dorow, 1982;Ruffin etal., 1982).…”

Section: Whithdrawal Symptomsmentioning

confidence: 99%

Pindolol‐a beta‐adrenoceptor blocking drug with partial agonist activity: clinical pharmacological considerations.

Aellig¹

1982

Brit J Clinical Pharma

View full text Add to dashboard Cite

1 Pindolol is a beta‐adrenoceptor antagonist equally effective on beta 1‐ and beta 2‐adrenoceptors which has a relatively long duration of action. It is practically completely absorbed and, unlike most other beta‐adrenoceptor blockers, is only metabolized to a small extent during the first passage through the liver. 2 Pindolol possesses partial agonist activity (intrinsic sympathomimetic activity, ISA). This means that apart from blocking beta‐adrenoceptors it produces some stimulation. Pindolol therefore only slightly influences normal sympathetic drive at rest but effectively reduces the effects of elevated sympathetic activity. 3 Various therapeutic advantages have been attributed to the partial agonist activity of pindolol: no or only slight alterations in normal cardiac output, heart rate and peripheral blood flow occur. Peripheral resistance is reduced during chronic oral therapy. No alteration of HDL/LDL cholesterol ratio has been observed. Rebound phenomena on sudden withdrawal of therapy and bronchoconstriction in susceptible patients are less likely than with drugs devoid of ISA.

show abstract

Influence of intrinsic sympathomimetic activity (ISA) during beta‐ adrenoceptor blockade in asthmatics.

Cited by 15 publications

References 2 publications

Intrinsic Sympathomimetic Activity: Physiological Reality or Marketing Phenomenon

Intrinsic Sympathomimetic Activity: Physiological Reality or Marketing Phenomenon

Influence of Propranolol, Metoprolol, and Pindolol on Mucociliary Clearance in Patients with Coronary Heart Disease

Pindolol‐a beta‐adrenoceptor blocking drug with partial agonist activity: clinical pharmacological considerations.

Contact Info

Product

Resources

About