The mode of action of theophylline

doi:10.1185/03007997909115905

Paper

The mode of action of theophylline

Published 1979 · R. Pauweis

Current Medical Research and Opinion

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Abstract

SummaryThe different pharmacological actions of theophylline are reviewed. Apart from its bronchodilating effect, theophylline acts on the respiratory centre and has valuable cardiovascular and renal effects. Side-effects are gastro-intestinal intolerance, central nervous stimulation and cardiovascular disturbances. The main hypotheses concerning the molecular basis of theophylline's activity are discussed. Although phosphodiesterase inhibition has been generally accepted, until recently, as the mechanism probably involved in the bronchodilating activity, other mechanisms such as inhibition of beta-adrenoceptor subsensitivity, inhibition of the adenosine receptor and intracellular translocation of calcium may also be involved and more relevant to the anti-allergic activity.

Study Snapshot

Theophylline has bronchodilating, respiratory, cardiovascular, and renal effects, with potential mechanisms including phosphodiesterase inhibition, beta-adrenoceptor subsensitivity, adenosine receptor inhibition, and intracellular calcium translocation.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

The mode of action of theophylline

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References

Effects of aminophylline upon right and left ventricular performance in chronic obstructive pulmonary disease: noninvasive assessment by radionuclide angiocardiography.

Aminophylline acutely enhances biventricular performance in COPD patients, with similar effects observed in normal subjects without pulmonary compromise.

Adenosine analogs inhibit adipocyte adenylate cyclase by a GTP-dependent process: basis for actions of adenosine and methylxanthines on cyclic AMP production and lipolysis.

Adenosine and methylxanthines effectively inhibit fat cell metabolism by affecting adipocyte adenylate cyclase through a GTP-dependent process.

Regulation of beta-adrenergic response in human lymphocytes: agonist induced subsensitivity.

Preincubation with isoproterenol leads to loss of beta-adrenergic response in lymphocytes, while PGE1 affects both isoproterenol and PGE1 sensitivities, with some abnormalities restored by theophylline treatment.

INHIBITION OF HUMAN PULMONARY PHOSPHODIESTERASE ACTIVITY BY THERAPEUTIC LEVELS OF THEOPHYLLINE

Theophylline's bronchodilator action in reversible airways disease is primarily due to inhibition of cyclic nucleotide phosphodiesterase, with therapeutic levels effectively decreasing this enzyme's activity.

Rat mast cell high affinity cyclic nucleotide phosphodiesterases: separation and inhibitory effects of two antiallergic agents.

Rat mast cells have two major phosphodiesterase fractions, with cyclic GMP being the preferred substrate, and both antiallergic agents inhibit their activity.

Citations

Changes in etilefrine-induced CNS effects when associated with theophylline.

Theophylline antagonizes the depressive effects of high doses of etilefrine, but the LD 50 of both drugs remains unchanged when administered simultaneously.

Bronchodilator drugs in childhood asthma.

Bronchodilator drugs in childhood asthma are categorized into age-related groups, with a focus on bronchodilators for children over 7 years, between ages 3 and 7 years, and those under 3 years.