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Influence of short- and long-term inhalation of salbutamol on lung function and β2-andrenoceptors of mononuclear blood cells in asthmatic children

  • Pneumology
  • Published:
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Abstract

Clinical observations have shown that some asthma patients develop tachyphylaxis to β-sympathomimetic drugs. As down-regulation of the number of β-adrenoceptors in different human tissues after exposure to catecholamines and β-adrenergic drugs is well known, we investigated whether a interrelation exists between β-adrenoceptor down-regulation and clinically detectable β-adrenergic subsensitivity during β-sympathomimetic treatment. The following results were obtained: 1. β2-Sympathomimetic inhalation treatment with salbutamol in therapeutic doses led to a significant downregulation of β2-adrenoceptors and consecutive cyclic adenosine monophosphate response to isoprenaline. This effect was already detectable after short-term treatment of 3–7 days in 9 asthmatic children. 2. In the long-term study over 6 months, salbutamol inhalation in 12 asthmatic children led to a significant down-regulation of β-adrenoceptor binding sites on mononuclear blood cells (MNC) from 1539±91 to 1115±99 after 14 days, remaining in this range thereafter. 3. The mean airway resistance (Raw) of these 12 patients decreased significantly within 14 days from 8.1±0.8 to 5.7±0.5 cm H2O/l/s to remain stable throughout the 6 months of salbutamol treatment. The differences in Raw before and immediately after inhalation of 0.2 mg salbutamol (2 puffs) were unchanged during the study period. It is concluded, that long-term inhalative treatment with salbutamol over a period of 6 months does not result in refractoriness to β-adrenergic drugs in the airways of asthmatic children, even though a significant down-regulation of β2-receptors on peripheral MNC occurs.

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Abbreviations

cAMP:

cyclic adenosine monophosphate

ICYP:

iodo-cyano-pindolo

MNC:

mononuclear blood cells

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Author notes

  1. A. Schuster

    Present address: Cardiovascular Research Institute, University of California, Box 0130, 94143, San Francisco, CA, USA

Authors and Affiliations

  1. Kinderklinik der Heinrich-Heine-Universität, Moorenstrasse 5, W-4000, Düsseldorf, Federal Republic of Germany

    A. Schuster & R. Kozlik

  2. Kinderpoliklinik der Ludwig-Maximilians-Universität, Pettenkoferstrasse 8a, W-8000, München, Federal Republic of Germany

    D. Reinhardt

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  2. R. Kozlik
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  3. D. Reinhardt
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Schuster, A., Kozlik, R. & Reinhardt, D. Influence of short- and long-term inhalation of salbutamol on lung function and β2-andrenoceptors of mononuclear blood cells in asthmatic children. Eur J Pediatr 150, 209–213 (1991). https://doi.org/10.1007/BF01963569

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